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Title:
SUBSTITUTED ARYLALKANOIC ACID DERIVATIVE AND USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2005/016862
Kind Code:
A1
Abstract:
A compound represented by the formula (I)[In the formula, Link represents a saturated or unsaturated straight hydrocarbon chain having 1 to 3 carbon atoms, C2 to C6 in the aromatic ring (E) independently represent a ring-constituting carbon atom, one of the ring-constituting carbon atoms may be replaced with V, V represents nitrogen atom, or carbon atom substituted with Zx, Zx represents a saturated alkyl group having 1 to 4 carbon atoms and the like, Rs represents -D-Rx etc., D represents a single bond, oxygen atom and the like, Rx represents a saturated alkyl group having 3 to 8 carbon atoms and the like, AR represents a partially unsaturated or completely unsaturated condensed bicyclic carbon ring or a heterocyclic ring, and Y represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms and the like] or a salt thereof. A compound having prostaglandin production-suppressing action and leukotriene production-suppressing action is provided.

Inventors:
Shoda, Motoshi (2-37-1005, Minami-cho Mishima-shi, Shizuoka, 411-0842, JP)
Kuriyama, Hiroshi (205-8, Obuchi Fuji-shi, Shizuoka 01, 41708, JP)
Application Number:
PCT/JP2004/011952
Publication Date:
February 24, 2005
Filing Date:
August 13, 2004
Export Citation:
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Assignee:
ASAHI KASEI PHARMA CORPORATION (9-1 Kanda Mitoshiro-cho, Chiyoda-ku, Tokyo 81, 10184, JP)
Shoda, Motoshi (2-37-1005, Minami-cho Mishima-shi, Shizuoka, 411-0842, JP)
Kuriyama, Hiroshi (205-8, Obuchi Fuji-shi, Shizuoka 01, 41708, JP)
International Classes:
C07C45/68; C07C45/71; C07C47/575; C07C59/64; C07C59/66; C07C59/68; C07C59/72; C07C69/616; C07C69/734; C07C205/44; C07C205/56; C07C217/18; C07C217/76; C07C229/42; C07C307/10; C07C309/65; C07C311/29; C07C317/44; C07C317/46; C07C323/12; C07C323/62; C07C335/16; C07C335/22; C07D207/323; C07D209/08; C07D209/12; C07D209/46; C07D213/64; C07D213/68; C07D213/74; C07D215/04; C07D215/14; C07D215/227; C07D217/02; C07D217/24; C07D231/56; C07D233/02; C07D233/54; C07D235/06; C07D235/08; C07D235/26; C07D235/28; C07D235/30; C07D239/74; C07D241/42; C07D249/04; C07D249/18; C07D261/08; C07D263/56; C07D263/58; C07D275/04; C07D277/24; C07D277/62; C07D277/68; C07D277/70; C07D277/82; C07D285/14; C07D295/155; C07D307/68; C07D307/79; C07D307/80; C07D317/54; C07D319/18; C07D333/32; C07D333/54; C07D333/56; C07D401/04; C07D401/12; C07D403/12; C07D405/12; C07D409/12; C07D413/12; C07D417/12; C07D417/14; C07D471/04; C07D487/04; C07D495/04; C07D207/32; C07D215/22; (IPC1-7): C07C59/64; C07C59/68; C07C59/72; C07C69/734; C07C205/44; C07C205/56; C07C217/18; C07C217/76; C07C229/42
Attorney, Agent or Firm:
SIKs & Co. (8th Floor, Kyobashi-Nisshoku Bldg. 8-7, Kyobashi 1-chom, Chuo-ku Tokyo 31, 10400, JP)
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Claims:
CLAIMS
1. A compound represented by the formula (I): [In the formula, Link represents a saturated or unsaturated straight hydrocarbon chain having 1 to 3 carbon atoms. C2, C3, C4, C5, and C6 in the aromatic ring (E) independently represent a ringconstituting carbon atom. One of the ringconstituting carbon atoms to which Rs and AR do not bind may be replaced with V. V represents nitrogen atom, or carbon atom substituted with Zx. Zx represents a linear or branched saturated alkyl group having 1 to 4 carbon atoms, fluorine atom, chlorine atom, bromine atom, nitro group, OR9, orN (Rnl) (Rn2). R9 represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, orAs Qp, wherein A6 represents a single bond or methylene, Qp represents phenyl group, and the phenyl group may be substituted with one of T'or two or more of the same or different Tl. T'represents a linear or branched saturated alkyl group having 1 to 4 carbon atoms, hydroxyl group, fluorine atom, chlorine atom, bromine atom, trifluoromethyl group, nitro group, an alkoxy group having 1 to 4 carbon atoms, or a monoor dialkylamino group having 1 to 4 carbon atoms. Rnl represents hydrogen atom or a linear or branched saturated alkyl group having 1 to 4 carbon atoms, Rn2 has the same meaning as Rnl, or representsCOR23 orSO2R24, or binds to Rnl to form a 3to 6membered ring together with the nitrogen atom to which they bind to form a saturated nitrogencontaining cycloalkyl group or morpholino group. R23 represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms,OA6Qp, orN (R25) (R26). R25 represents hydrogen atom, or a linear or branched saturated alkyl group having 1 to 4 carbon atoms. R26 has the same meaning as R25, or binds to R25 to form a 3 to 6membered ring together with the nitrogen atom to which they bind to form a saturated nitrogencontaining cycloalkyl group or morpholino group. R24 represents a lower alkyl group having 1 to 4 carbon atoms, amino group, or a mono or dialkylamino group having 1 to 4 carbon atoms. Rs representsDRx orN (Ry) (Rz). D represents a single bond, oxygen atom, sulfur atom,S (O),S (O) 2, or C (O). Rx represents a linear or branched saturated alkyl group having 3 to 8 carbon atoms, Ra represented by the following formula: Ri (CH2) k (Ra) Rb represented by the following formula : (Rb) or Rc represented by the following formula. Symbol k in Ra represents 0 or an integer of 1 to 3. R1 represents a saturated cyclic alkyl group having 3 to 7 carbon atoms, or a condensed saturated cyclic alkyl group having 6 to 8 carbon atoms, and Rl may be substituted with one of lower alkyl group having 1 to 4 carbon atoms or two or more of the same or different lower alkyl groups having 1 to 4 carbon atoms. Q in Rb represents a partially unsaturated or completely unsaturated monocyclic or condensed bicyclic carbon ring or a heterocyclic ring (q), and binds to A2 at an arbitrary position on the ring. The heterocyclic ring (q) contains the same or different 1 to 4 ringconstituting heteroatoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom. A1 represents a single bond or an alkylene (a) having 1 to 3 carbon atoms, and the alkylene (a) may be substituted with a lower alkyl group having 1 to 4 carbon atoms or phenyl group. A2 represents a single bond, oxygen atom, sulfur atom,S (O),S (0) 2, orN (R4) (provided that when A2 represents oxygen atom, sulfur atom,S (O),S (0) 2 orN (R4) , Al represents ethylene or trimethylene). R2 and R3 independently represent hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms, oxo group, thioxo group, fluorine atom, chlorine atom, bromine atom, trifluoromethyl group,OR5,N (R6) (R6'),NHCOR, NHSO2R3, orA6Qa, or they bind to each other to represent methylenedioxy group. Qa represents a partially unsaturated or completely unsaturated monocyclic or condensed bicyclic carbon ring or a heterocyclic ring (qa), binds to A6 at an arbitrary position on the ring, and may be substituted with one of T1 or two or more of the same or different T1. The heterocyclic ring (qa) contains the same or different 1 to 4 ringconstituting heteroatoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom. R4 and R6 independently represent hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms. R5 and R7 independently represent hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, orA6Qa. R3 represents a lower alkyl group having 1 to 4 carbon atoms. R6'has the same meaning as R6, or binds to R6 to form a 3to 6membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogencontaining cycloalkyl group or morpholino group. Symbol p in Rc represents an integer of 2 to 4. A4 represents a single bond, methylene, or ethylene. A5 representsC (O),C (S), orS (0) 2. Rd represents hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or Qa. Re represents an alkyl group having 1 to 8 carbon atoms,A6Qa, (CH2) iRl4,OR28,SR28, orN (R29) (R30). Symbol i represents an integer of 1 to 3, R14 represents hydroxyl group, an alkoxy group having 1 to 4 carbon atoms, carboxyl group, or an N, N dialkylcarbamoyl group having 1 to 4 carbon atoms. R28 represents an alkyl group having 1 to 8 carbon atoms, orA6Qa. R29 represents an alkyl group having 1 to 8 carbon atoms, an alkoxycarbonyl group having 1 to 4 carbon atoms, orAsQa. R30 represents hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, or binds to R29 to form a 3to 6membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogencontaining cycloalkyl group or morpholino group. Rz has the same meaning as Rx, or Rz represents methyl group, ethyl group, orA5Re. Ry represents hydrogen atom, an alkyl group having 1 to 8 carbon atoms, orA6Qp, or Ry may bind to Rz to form, together with a nitrogen atom to which they bind, a saturated or unsaturated 3 to 7membered nitrogencontaining cyclic group, wherein said nitrogencontaining cyclic group may optionally be substituted with one or two lower alkyl groups having 1 to 4 carbon atoms wherein said two alkyl groups may be the same or different. AR represents a partially unsaturated or completely unsaturated condensed bicyclic carbon ring or a heterocyclic ring (ar), and may be substituted with one of Xa or two or more of the same or different Xa. The heterocyclic ring (ar) contains the same or different 1 to 4 ringconstituting heteroatoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom. Xa represents a linear or branched saturated alkyl group having 1 to 4 carbon atoms, a saturated cyclic alkyl group having 3 to 7 carbon atoms, oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group,(CH2) iRl4,ORl°,N (Rll) (Rl2), SO2Rl3, orCOR27. Rio represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, or(CH2) iRJ4. Rll represents hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms. R12 represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a hydroxyalkyl group having 2 to 4 carbon atoms, CORl5, orSO2Rl6, or binds to R"to form a 3to 6membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogencontaining cycloalkyl group or morpholino group. R15 represents a lower alkyl group having 1 to 4 carbon atoms, a hydroxyalkyl group having 2 to 4 carbon atoms, amino group, a monoor dialkylamino group having 1 to 4 carbon atoms, orA6Qa. R13 and R16 independently represent a lower alkyl group having 1 to 4 carbon atoms, amino group, or a monoor dialkylamino group having 1 to 4 carbon atoms. R27 represents hydrogen atom, hydroxyl group, an alkoxy group having 1 to 4 carbon atoms, a lower alkyl group having 1 to 4 carbon atoms, amino group, or a monoor dialkylamino group having 1 to 4 carbon atoms. Y represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, (CH2) mN (R18) (Ri9) orC (R20) 20C (O) A3R21. Symbol m represents an integer of 2 or 3. R18 is the same as Rl9, or binds to Rl9 to form a 3to 6membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogencontaining cycloalkyl group or morpholino group. Rl9 represents methyl group, ethyl group, or propyl group. R20 represents hydrogen atom, methyl group, ethyl group, or propyl group. R2l represents a lower alkyl group having 1 to 4 carbon atoms, a cyclic saturated alkyl group having 3 to 6 carbon atoms, or phenyl group, and A3 represents a single bond, or oxygen atom. ] or a salt thereof.
2. The compound or salt thereof according to claim 1, wherein Link is (CH2) n, n is an integer of 1 to 3, Rz has the same meaning as that of Rx or representsA5Re when Rs isN (Ry) (Rz), and Ry is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or A6Qp, or Ry binds to Rz to form, together with a nitrogen atom to which they bind, a saturated or unsaturated 3 to 7membered nitrogencontaining cyclic group.
3. The compound or salt thereof according to claim 2, wherein AR is a residue of naphthalene, benzofuran, benzo [b] thiophene, indole, benzothiazole, dihydro3Hbenzothiazole, quinoline, dihydrolHquinoline, benzo [d] isothiazole, 1Hindazole, benzo [c] isothiazole, 2Hindazole, imidazo [1, 2a] pyridine, 1H pyrrolo [2, 3b] pyridine, isoquinoline, dihydro2Hisoquinoline, cinnoline, quinazoline, quinoxaline, lHbenzimidazole, benzoxazole, 1Hpyrrolo [3, 2b] pyridine, benzo [1, 2,5] thiadiazole, 1Hbenzotriazole, 1, 3dihydropyrrolo [2, 3b] pyridine, 1,3 dihydrobenzimidazole, dihydro3Hbenzoxazole, phthalazine, [1, 8] naphthalidine, [1, 5] naphthalidine, lHpyrrolo [3, 2c]pyridine, 1Hpyrrolo [2, 3e] pyridine, 1H pyrazolo [4, 3b]pyridine, 1Hpyrazolo [4, 3c] pyridine, lHpyrazolo [3, 4c] pyridine, 1H pyrazolo [3, 4b] pyridine, [1, 2,4] triazolo [4, 3a]pyridine, thieno [3, 2c] pyridine, thieno [3, 2b]pyridine, 1Hthieno [3, 2c] pyrazole, benzo [d] isoxazole, benzo [c] isoxazole, indolizine, 1,3dihydroindole, lHpyrazolo [3, 4d] thiazole, 2H isoindole, [1, 2,4] triazolo [1, 5a]pyrimidine, 1Hpyrazolo [3, 4b] pyrazine, 1H imidazo [4, 5b] pyrazine, 7Hpurine, or 4Hchromene (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa).
4. The compound or salt thereof according to claim 2, wherein AR is naphthalen2yl group, naphthalen1yl group, benzofuran5yl group, benzofuran 4yl group, benzofuran2yl group, benzo [b] thiophen5yl group, benzo [b] thiophen4 yl group, benzo [b] thiophen2yl group, indol5yl group, indol4yl group, indol6yl group, benzothiazol6yl group, benzothiazol7yl group, benzothiazol5yl group, benzothiazol4yl group, dihydro3Hbenzothiazol6yl group, dihydro3H benzothiazol7yl group, dihydro3Hbenzothiazol5yl group, dihydro3H benzothiazol4yl group, quinolin6yl group, quinolin3yl group, quinolin5yl group, quinolin7yl group, dihydrolHquinolin6yl group, dihydrolHquinolin5 yl group, benzo [d] isothiazol5yl group, benzo [d] isothiazol4yl group, benzo [d] isothiazol6yl group, benzo [d] isothiazol7yl group, lHindazol5yl group, lHindazol4ylgroup, lHindazol6yl group, benzo [c] isothiazol5yl group, benzo [c]isothiazol4yl group, benzo [c]isothiazol6yl group, benzo [c] isothiazol7yl group, 2Hindazol5yl group, 2Hindazol4yl group, 2Hindazol6yl group, imidazo [1, 2a]pyridin6yl group, imidazo [1, 2a]pyridin7yl group, lHpyrrolo [2,3 b]pyridin5yl group, 1Hpyrrolo [2, 3b] pyridin4yl group, isoquinolin6yl group, isoquinolin3yl group, isoquinolin5yl group, isoquinolin7yl group, dihydro2H isoquinolin6yl group, dihydro2Hisoquinolin5yl group, cinnolin6yl group, cinnolin5yl group, quinazolin6yl group, quinazolin7yl group, quinazolin5yl group, quinoxalin2yl group, quinoxalin6yl group, quinoxalin5yl group, 1H benzimidazol5yl group, lHbenzimidazol4ylgroup, benzoxazol5yl group, benzoxazol6yl group, benzoxazol4yl group, benzoxazol7yl group, 1H pyrrolo [3, 2b] pyridin5yl group, 1Hpyrrolo [3, 2b]pyridin6yl group, benzol, 2,5] thiadiazol5yl group, benzo [1, 2,5] thiadiazol4yl group, 1H benzotriazol5yl group, lHbenzotriazol4yl group, 1, 3dihydropyrrolo [2, 3 b]pyridin5yl group, 1, 3dihydropyrrolo [2, 3b] pyridin4yl group, 1, 3 dihydrobenzimidazol5yl group, 1, 3dihydrobenzimidazol4yl group, dihydro3H benzoxazol6yl group, dihydro3Hbenzoxazol7yl group, dihydro3Hbenzoxazol5 yl group, dihydro3Hbenzoxazol4yl group, phthalazin6yl group, phthalazin5yl group, [1, 8] naphthalidin3yl group, [1, 8] naphthalidin4yl group, [1, 5] naphthalidin3yl group, [1, 5] naphthalidin4yl group, lHpyrrolo [3,2 c] pyridin6yl group, lHpyrrolo [3, 2c] pyridin4yl group, 1Hpyrrolo [2, 3c] pyridin 5yl group, 1Hpyrrolo [2, 3c] pyridin4yl group, 1Hpyrazolo [4, 3b] pyridin5yl group, 1Hpyrazolo [4, 3b] pyridin6yl group, 1Hpyrazolo [4, 3c] pyridin6yl group, 1Hpyrazolo [4, 3c] pyridin4yl group, 1Hpyrazolo [3, 4c] pyridin5yl group, 1H pyrazolo [3, 4c] pyridin4yl group, 1Hpyrazolo [3, 4b]pyridin5yl group, 1H pyrazolo [3, 4b] pyridin4yl group, [1, 2,4] triazolo [4, 3a] pyridin6yl group, [1, 2,4] triazolo [4, 3a] pyridin7yl group, thieno [3, 2c] pyridin2yl group, thieno [3,2 c] pyridin3yl group, thieno [3, 2c] pyridin6yl group, thieno [3, 2b] pyridin2yl group, thieno [3, 2b] pyridin3yl group, thieno [3, 2b] pyridin5yl group, thieno [3,2 b] pyridin6yl group, 1Hthieno [3, 2c] pyrazol5yl group, 1Hthieno [3, 2c] pyrazol4 yl group, benzo [d] isoxazol5yl group, benzo [d] isoxazol4yl group, benzo [d] isoxazol 6yl group, benzo [d] isoxazol7yl group, benzo [c] isoxazol5yl group, benzo [c] isoxazol4yl group, benzo [c] isoxazol6yl group, benzo [c] isoxazol7yl group, indolizin7yl group, indolizin6yl group, indolizine8yl group, 1, 3dihydroindol5 yl group, 1, 3dihydroindol4yl group, 1, 3dihydroindol6yl group, 1Hpyrazolo [3,4 d] thiazol5yl group, 2Hisoindol5yl group, 2Hisoindol4yl group, [1, 2,4] triazolo [1, 5a] pyrimidin6yl group, 1Hpyrazolo [3, 4b] pyrazin5yl group, 1Himidazo [4, 5b] pyrazin5yl group, 7Hpurin2yl group, 4Hchromen6yl group, or 4Hchromen5yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa).
5. The compound or salt thereof according to any one of claims 2 to 4 mentioned above, wherein Rs isDRx orN (Ry) (Rz), D is a single bond, oxygen atom, sulfur atom,S (O),S (0) 2, orC (O), Rx is a linear or branched saturated alkyl group having 3 to 8 carbon atoms, or Ra, Rb, or Rc, k in Ra is 0 or an integer of 1 to 3, RI is a saturated cycloalkyl group having 3 to 7 carbon atoms or a condensed saturated cycloalkyl group having 6 to 8 carbon atoms, Rl may be substituted with one of lower alkyl group having 1 to 4 carbon atoms or two or more of the same or different lower alkyl groups having 1 to 4 carbon atoms, Q in Rb is phenyl group, thienyl group, furyl group, pyrrolyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, indazolyl group, 4Hchromenyl group, dihydrobenzodioxyl group, benzoisoxazolyl group, pyrrolopyridinyl group, pyrazolopyridinyl group, triazolopyridinyl group, thienopyridinyl group, thienopyrazolyl group, 1, 3dihydrobenzimidazole group, dihydro3Hbenzoxazole group, or dihydro3Hbenzothiazole group (the aforementioned groups bond to A2 at an arbitrary position on the rings), Al is a single bond or an alkylene (a) having 1 to 3 carbon atoms, the alkylene (a) may be substituted with a lower alkyl group having 1 to 4 carbon atoms or phenyl group, A2 is a single bond, oxygen atom, sulfur atom,S (O),S (0) 2, orN (R4) (provided that when A2 represents oxygen atom, sulfur atom,S (O) ,S (0) 2, orN (R4), Al represents ethylene or trimethylene), R2 and R3 independently represent hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms, oxo group, thioxo group, fluorine atom, chlorine atom, bromine atom, trifluoromethyl group,OR5,N (R6) (R6'),NHCOR7,NHSO2R8, orA6Qa, or they bind to each other to represent methylenedioxy group, Qa is phenyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, naphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, or indazolyl group (the aforementioned groups may be substituted with one of T1 or two or more of the same or different Tl, and bind to As at an arbitrary position on the rings), R4 and R6 independently represent hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R5 and R7 independently represent hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, orA6Qa, R8 is a lower alkyl group having 1 to 4 carbon atoms, R6' has the same meaning as R6, or binds to R6 to form a 3to 6membered ring together with the nitrogen atom to which they bind to form a saturated nitrogen containing cycloalkyl group or morpholino group, p in Rc is an integer of 2 to 4, A4 is a single bond or methylene or ethylene, A5 isC (O),C (S) , orS (0) 2, Rd is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or Qa, Re is an alkyl group having 1 to 8 carbon atoms,A6Qa, (CH2) iRl4,OR28,SR28, orN (R29) (R30), i is an integer of 1 to 3, R14 is hydroxyl group, an alkoxy group having 1 to 4 carbon atoms, carboxyl group, or an N, Ndialkylcarbamoyl group having 1 to 4 carbon atoms, R28 is an alkyl group having 1 to 8 carbon atoms orA6Qa, R29 is an alkyl group having 1 to 8 carbon atoms, an alkoxycarbonyl group having 1 to 4 carbon atoms, orA6Qa group, R30 is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, or binds to R29 to form a 3to 6membered ring together with the nitrogen atom to which they bind to form a saturated nitrogencontaining cycloalkyl group or morpholino group, Rz has the same meaning as Rx, or isA5Re, and Ry is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, orA6Qp, or binds to Rz to form a saturated or unsaturated nitrogencontaining cyclic substituent having 3 to 7 atoms together with nitrogen atom to which they binds.
6. The compound or salt thereof according to any one of claims 2 to 5, wherein Rs isORx.
7. The compound or salt thereof according to claim 2, wherein AR binds to C3 in the aromatic ring (E), and Rs binds to one of the ringconstituting carbon atoms C4, C5, and C6.
8. The compound or salt thereof according to claim 2, wherein AR binds to C2 in the aromatic ring (E), and Rs binds to one of the ringconstituting carbon atoms C3, C4, and C5.
9. The compound or salt thereof according to claim 7, wherein Rs is0Rx, and all of C2, C3, C4, C5, and C6 in the aromatic ring (E) are not replaced with V.
10. The compound or salt thereof according to claim 8, wherein n is an integer of 2, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.
11. The compound or salt thereof according to claim 7, wherein Rs binds to the ringconstituting carbon atom C5 or C6 in the aromatic ring (E).
12. The compound or salt thereof according to claim 11, wherein Rs isORx, and all of C2, C3, C4, C5, and C6 in the aromatic ring (E) are not replaced with V.
13. The compound or salt thereof according to claim 12, wherein n is an integer of 2, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.
14. The compound or salt thereof according to claim 7, wherein Rs binds to C4 in the aromatic ring (E), and C6 is replaced with V.
15. The compound or salt thereof according to claim 14, wherein n is an integer of 2, V is carbon atom substituted with Zx, D is oxygen atom, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.
16. The compound or salt thereof according to claim 7, wherein Rs binds to C4 in the aromatic ring (E), C5 is nitrogen atom, and C2 and C6 are unsubstituted ringconstituting carbon atoms.
17. The compound or salt thereof according to claim 16, wherein n is an integer of 2, Rs isORx, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.
18. The compound or salt thereof according to claim 7, wherein Rs binds to C4 in the aromatic ring (E), C5 is a ringconstituting carbon atom substituted with Zx, or an unsubstituted ringconstituting carbon atom, C2 and C6 are unsubstituted ringconstituting carbon atoms, and Rs isN (Ry) (Rz).
19. The compound or salt thereof according to claim 1, wherein Link is (CH2) n, n is an integer of 1 to 3, C2 and C6 in the aromatic ring (E) are unsubstituted ringconstituting carbon atoms, AR binds to C3 in the aromatic ring (E), and Rs isN (Ry) (Rz) and binds to C4 in the aromatic ring (E).
20. The compound or salt thereof according to claim 19, wherein n is 2, and C5 is carbon atom substituted with Zx or unsubstituted ringconstituting carbon atom.
21. The compound or salt thereof according to claim 19 or 20, wherein AR is naphthalen2yl group, naphthalen1yl group, benzofuran5yl group, benzofuran 4yl group, benzofuran2yl group, benzo [b] thiophen5yl group, benzo [b] thiophen4 yl group, benzo [b] thiophen2yl group, indol5yl group, indol4yl group, indol6yl group, benzothiazol6yl group, benzothiazol7yl group, benzothiazol5yl group, benzothiazol4yl group, dihydro3Hbenzothiazol6yl group, dihydro3H benzothiazol7yl group, dihydro3Hbenzothiazol5yl group, dihydro3H benzothiazol4yl group, quinolin6yl group, quinolin3yl group, quinolin5yl group, quinolin7yl group, dihydrolHquinolin6yl group, dihydrolHquinolin5 yl group, benzo [d] isothiazol5yl group, benzo [d] isothiazol4yl group, benzo [d] isothiazol6yl group, benzo [d] isothiazol7yl group, lHindazol5yl group, lHindazol4yl group, 1Hindazol6yl group, benzo [c] isothiazol5yl group, benzo [c] isothiazol4yl group, benzo [c] isothiazol6yl group, benzo [c] isothiazol7yl group, 2Hindazol5yl group, 2Hindazol4yl group, 2Hindazol6yl group, imidazo [1, 2a] pyridin6yl group, imidazo [1, 2a] pyridin7yl group, lHpyrrolo [2,3 b] pyridin5yl group, lHpyrrolo [2, 3bpyridin4yl group, isoquinolin6yl group, isoquinolin3yl group, isoquinolin5yl group, isoquinolin7yl group, dihydro2H isoquinolin6yl group, dihydro2Hisoquinolin5yl group, cinnolin6yl group, cinnolin5yl group, quinazolin6yl group, quinazolin7yl group, quinazolin5yl group, quinoxalin2yl group, quinoxalin6yl group, quinoxalin5yl group, 1H benzimidazol5yl group, lHbenzimidazol4yl group, benzoxazol5yl group, benzoxazol6yl group, benzoxazol4yl group, benzoxazol7yl group, 1H pyrrolo [3, 2b] pyridin5yl group, lHpyrrolo [3, 2b] pyridin6yl group, benzo [1, 2, 5] thiadiazol5yl group, benzo [1, 2,5] thiadiazol4yl group, 1H benzotriazol5yl group, lHbenzotriazol4yl group, 1, 3dihydropyrrolo [2,3 b] pyridin5yl group, 1, 3dihydropyrrolo [2, 3b] pyridin4yl group, 1,3 dihydrobenzimidazol5yl group, 1, 3dihydrobenzimidazol4yl group, dihydro3H benzoxazol6yl group, dihydro3Hbenzoxazol7yl group, dihydro3Hbenzoxazol5 yl group, dihydro3Hbenzoxazol4yl group, phthalazin6yl group, phthalazin5yl group, [1, 8] naphthalidin3yl group, [1, 8] naphthalidin4yl group, [1, 5] naphthalidin3yl group, [1, 5] naphthalidin4yl group, 1Hpyrrolo [3,2 c] pyridin6yl group, lHpyrrolo [3, 2c] pyridin4yl group, lHpyrrolo [2, 3c] pyridin 5yl group, 1Hpyrrolo [2, 3c]pyridin4yl group, 1Hpyrazolo [4, 3b] pyridin5yl group, 1Hpyrazolo [4, 3b] pyridin6yl group, lHpyrazolo [4, 3c] pyridin6yl group, 1Hpyrazolo [4, 3c] pyridin4yl group, 1Hpyrazolo [3, 4c] pyridin5yl group, 1H pyrazolo [3, 4c]pyridin4yl group, 1Hpyrazolo [3, 4b] pyridin5yl group, 1H pyrazolo [3, 4b] pyridin4yl group, [1, 2,4] triazolo [4, 3a] pyridin6yl group, [1, 2,4] triazolo [4, 3a]pyridin7yl group, thieno [3, 2c] pyridin2yl group, thieno [3, 2 c]pyridin3yl group, thieno [3, 2c] pyridin6yl group, thieno [3, 2b]pyridin2yl group, thieno [3, 2b] pyridin3yl group, thieno [3, 2b] pyridin5yl group, thieno [3,2 b] pyridin6yl group, lHthieno [3, 2c] pyrazol5yl group, lHthieno [3, 2c] pyrazol4 yl group, benzo [d]isoxazol5yl group, benzo [d]isoxazol4yl group, benzo [d] isoxazol 6yl group, benzo [d]isoxazol7yl group, benzo [clisoxazol5yl group, benzo [c]isoxazol4yl group, benzo [c]isoxazol6yl group, benzo [c] isoxazol7yl group, indolizin7yl group, indolizin6yl group, indolizine8yl group, 1, 3dihydroindol5 yl group, 1, 3dihydroindol4yl group, 1, 3dihydroindol6yl group, 1Hpyrazolo [3, 4 d] thiazol5yl group, 2Hisoindol5yl group, 2Hisoindol4yl group, [1, 2,4] triazolo [1, 5a] pyrimidin6yl group, 1Hpyrazolo [3, 4b] pyrazin5yl group, 1Himidazo [4, 5b]pyrazin5yl group, 7Hpurin2yl group, 4Hchromen6yl group, or 4Hchromen5yl group, wherein these groups may be substituted with one of Xa or two or more of the same or different Xa.
22. The compound or salt thereof according to any one of claim 19 to 21, wherein Rz is a linear or branched saturated alkyl group having 1 to 8 carbon atoms, or Rz is Ra, Rb, or Rc, k in Ra is 0 or an integer of 1 to 3, Rl is a saturated cyclic alkyl group having 3 to 7 carbon atoms or a condensed saturated cyclic alkyl group having 6 to 8 carbon atoms, R1 may be substituted with one of lower alkyl group having 1 to 4 carbon atoms or two or more of the same or different lower alkyl groups having 1 to 4 carbon atoms, Q in Rb is phenyl group, thienyl group, furyl group, pyrrolyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, indazolyl group, 4Hchromenyl group, dihydrobenzodioxyl group, benzoisoxazolyl group, pyrrolopyridinyl group, pyrazolopyridinyl group, triazolopyridinyl group, thienopyridinyl group, thienopyrazolyl group, 1, 3dihydrobenzimidazole group, dihydro3Hbenzoxazole group, or dihydro3Hbenzothiazole group (the aforementioned groups binds to A2 at an arbitrary position), Al is a single bond or an alkylene (a) having 1 to 3 carbon atoms, the alkylene (a) may be substituted with a lower alkyl group having 1 to 4 carbon atoms or phenyl group, A2 is a single bond, oxygen atom, sulfur atom,S (O),S (0) 2, orN (R4) (provided that when A2 represents oxygen atom, sulfur atom,S (O),S (0) 2, orN (R4), A1 represents ethylene or trimethylene), R2 and R3 independently represent hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms, oxo group, thioxo group, fluorine atom, chlorine atom, bromine atom, trifluoromethyl group, OR5,N (R6) (R6'),NHCOR7,NHS02Rs, orA6Qa, or they bind to each other to represent methylenedioxy group, Qa is phenyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, naphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, or indazolyl group (these groups may be substituted with one of T1 or two or more of the same or different T1, and bind to A6 at an arbitrary position on the ring), R4 and R6 independently represent hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R5 and R7 independently represent hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, orA6Qa, R8 is a lower alkyl group having 1 to 4 carbon atoms, R6'has the same meaning as R6, or binds to R6 to form a 3to 6membered ring together with the nitrogen atom to which they bind to form a saturated nitrogencontaining cycloalkyl group or morpholino group, p in Rc is an integer of 2 to 4, A4 is a single bond or methylene or ethylene, A5 isC (O),C (S), orS (0) 2, Rd is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or Qa, Re is an alkyl group having 1 to 8 carbon atoms,A6Qa, (CH2) iRl4,OR23,SR23, orN (R29) (R30), i is an integer of 1 to 3, R14 is hydroxyl group, an alkoxy group having 1 to 4 carbon atoms, carboxyl group, or an N, N dialkylcarbamoyl group having 1 to 4 carbon atoms, R23 is an alkyl group having 1 to 8 carbon atoms orA6Qa, R29 is an alkyl group having 1 to 8 carbon atoms, an alkoxycarbonyl group having 1 to 4 carbon atoms, orA6Qa group, R30 is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, or binds to R29 to form a 3 to 6membered ring together with the nitrogen atom to which they bind to form a saturated nitrogencontaining cycloalkyl group or morpholino group, and Ry is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or binds to Rz to form a saturated or unsaturated nitrogencontaining cyclic substituent having 3 to 7 atoms together with nitrogen atom to which they binds and said nitrogencontaining cyclic substituent may be substituted with one or two lower alkyl groups having 1 to 4 carbon atoms wherein said two alkyl groups may be the same or different.
23. The compound or salt thereof according to claim 7, wherein Rs binds to C4 in the aromatic ring (E), C5 is a ringconstituting carbon atom substituted with Zx, or an unsubstituted ringconstituting carbon atom, C2 and C6 are unsubstituted ringconstituting carbon atoms, Rs isDRx, and D is a single bond, sulfur atom, S (O),S (0) 2, orC (O).
24. The compound or salt thereof according to claim 7, wherein n is an integer of 2, Rs binds to C4 in the aromatic ring (E), C5 is carbon atom substituted withN (Rnl) (Rn2) (provided that one of Rnl and Rn2 is a substituent other than hydrogen atom), C2 and C6 are unsubstituted ringconstituting carbon atoms, Rs is ORx, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.
25. The compound or salt thereof according to claim 7, wherein n is an integer of 2, Rs binds to C4 in the aromatic ring (E), C5 is a ringconstituting carbon atom substituted with the substituent Zx, or an unsubstituted ringconstituting carbon atom, C2 and C6 are unsubstituted ringconstituting carbon atoms, Rs isO Rc, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.
26. A medicament containing the compound according to any one of claims 1 to 25 or a pharmacologically acceptable salt thereof as an active ingredient.
27. An agent for suppressing production of a prostaglandin and/or leukotriene, which comprises the compound according to any one of claims 1 to 25 or a pharmacologically acceptable salt thereof as an active ingredient.
28. The medicament according to claim 26, which is for prophylactic and/or therapeutic treatment of a disease caused by production of a prostaglandin and/or leukotriene.
29. A compound represented by the formula (II) : [In the formula, C2', C3', C4', C5', and C6'in the aromatic ring (E') independently represent a ringconstituting carbon atom, any one of them to which Rs'and G do not bind may be replaced with V, V'represents nitrogen atom, or carbon atom substituted with Zx', Zx'has the same meaning as Zx mentioned above, provided that when Zx contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx contains amino group, the amino group may be protected with Rp2, Rs'representsDRx'orN (Ry') (Rz'), DRx'andN (Ry') (Rz') have the same meanings asDRx andN (Ry) (Rz) mentioned above, respectively, provided that whenDRx orN (Ry) (Rz) contains hydroxyl group, the hydroxyl group may be protected with Rpl, and whenDRx or N (Ry) (Rz) contains amino group, the amino group may be protected with Rp2, G represents chlorine atom, bromine atom, iodine atom, mesylate group, triflate group, or an arenesulfonate group of which aromatic portion may be substituted with one of T1 or two or more of the same or different Tl, and Y'represents a lower alkyl group having 1 to 4 carbon atoms].
30. A compound represented by the formula (III) : [In the formula, C2', C3', C4', C5'and C6'in the aromatic ring (E') independently represent a ringconstituting carbon atom, any one of these ringconstituting carbon atoms to which Rs'and AR'do not bind may be replaced with V', and AR'has the same meaning as that of AR, provided that when AR contains hydroxyl group, the hydroxyl group may be protected with Rp, and whenAR contains amino group, the amino group may be protected with Rp2.].
Description:
DESCRIPTION Substituted Arylalkanoic Acid Derivative and Use Thereof Field of the Invention The present invention relates to a novel substituted arylalkanoic acid derivative. More specifically, the present invention relates to a substituted arylalkanoic acid derivative having an action as a medicament and a synthetic intermediate of said compound.

Background Art Various kinds of prostaglandins and various kinds of leukotrienes are produced in the bodies of mammals in response to variety of stimuli such as inflammatory stimuli and physical stimuli.

Both of prostaglandins and leukotrienes are metabolites of arachidonic acid, and they are physiologically active substances referred to as lipid mediators, and they cause various physiological responses of mammals by binding to receptors expressed on surfaces of various cells or in the cells.

Arachidonic acid is produced from a phospholipid as a substrate, such as phosphatidylcholine which is a cell membrane component, with the aid of an enzymatic activity of phospholipase A2 (PLA2).

Arachidonic acid produced by the action of PLA2 is converted into prostaglandin (PG) H2 with the aid of an enzymatic activity of constitutive type cyclooxygenase (COX) 1 or inducible type COX-2, and further converted into PGE2, PGD2, PGF2 a, PGI2, thromboxane (TX) A2 and the like with the aid of each synthetic enzyme. Further, arachidonic acid is also metabolized by the action of 5- lipoxygenase (5-LO) and thereby converted to leukotriene (LT) A4, and further converted to LTB4, LTC4, LTD4, LTE4 and the like by the enzymatic activities of LTA4 hydrolase, LTC4 synthase, glutathione S-transferase and the like [Goodman & Gilman, Pharmacological Basis of Therapeutics, 9th edition, p. 801, 1999 (Hirokawa Shoten); Funk, C. D. , SCIENCE, vol. 294, p. 1871, 2001].

Prostaglandins bind to each specific receptor to cause inflammatory reactions such as fervescence, enhancement of vascular permeability, vasodilation, swelling and pain, bronchial smooth muscle contraction, platelet aggregation, tumor cell proliferation, enhancement of bone resorption, nerve cell degeneration and the like, and thus play important roles in expression of symptoms or pathological formation for various diseases.

Leukotrienes are physiologically active substances which bind to each specific receptor to cause inflammatory reactions such as excessive accumulation of leucocytes and enhancement of vascular permeability, smooth muscle contraction, mucus secretion, proliferation of tumor cells and the like, and thus play important roles in expression of symptoms or pathological formation for various diseases.

Although inflammatory reactions themselves are essential reactions for living bodies to survive when they face pathogenic substances and affections, they are sometimes excessively caused or continue without any reason for providing evident benefit under certain situations or in certain diseases [Goodman & Gilman, Pharmacological Basis of Therapeutics, 9th edition, p. 827, 1999 (Hirokawa Shoten)].

The condition of living body referred to in this specification wherein an acute or chronic inflammatory reaction is observed means a condition that an excessive or unbeneficial acute or temporary inflammatory reaction or chronic and persistent inflammatory reaction is caused. Further, an inflammatory reaction refers to a series of events caused by stimuli, for example, physical hazards such as heat, infective substances, ischemia, antigen/antibody reaction and the like, and it is accompanied by flare, swelling, hyperalgesia, algesic onset and the like as well- known macroscopic clinical symptoms. It is known that, as histological mechanisms for these reactions, vasodilation, enhancement of vascular permeability, infiltration of leucocytes and phagocytes, histological decomposition and fibrosing and the like are caused [Goodman & Gilman, Pharmacological Basis of Therapeutics, 9th edition, p. 827, 1999 (Hirokawa Shoten) ]. It is known that many of these histological reactions are caused by prostaglandins and/or leukotrienes, and prostaglandins and/or leukotrienes plays important roles in inflammatory reactions.

For example, it was reported that, in a pathological tissue of rheumatoid arthritis, which is an autoimmune and chronic inflammatory disease, expression of COX-2 and production of PGE2 and TXA2 as well as expression of 5-LO and production of LTB4 were observed (Bonnet et al. , Prostaglandins, 1995, vol. 50, p. 127), and in a mouse deficient in FLAP, which is a protein required for activation of 5-LO, symptom of collagen-induced arthritis, which is a pathological model of chronic rheumatoid arthritis, was milder compared with that in a wild-type mouse (Griffiths et al. , J. Exp. Med. , 1997, vol. 185, p. 1123), and thus it has been suggested that prostaglandins and leukotrienes play important roles in the pathological formation of chronic rheumatoid arthritis.

It was reported that, in a pathological tissue of bronchial asthma, one of chronic allergic diseases, excessive production of PGD2 and TXA2 as well as excessive production of LTC4 and LTD4 were observed (Wenzel et al. , Am Rev.

Respir. Dis. , 1990, vol. 142, p. 112), and an airway hypersensitive reaction, which is a pathological model of bronchial asthma, was unlikely to occur in a PGD2 receptor- deficient mouse (Matsuoka et al. , SCIENCE, vol. 287, p. 2013,2000). Thus, it has been demonstrated that roles of prostaglandins and leukotrienes are important in bronchial asthma.

In a cerebral tissue after ischemic reperfusion, expression of COX-2 increased, and concentrations of PGL2 and TXAz increased, whereas activity of 5- LO increased, and production amount of LTC4 increased (Ohtsuki et al. , Am. J.

Physiol. , 1995, vol. 268, p. 1249). Thus, it is known that prostaglandins and leukotrienes play important roles in formation of infarct that is accepted as an ischemic reperfusion injury.

It has been revealed that, in a pathological tissue of Alzheimer's disease, one of the diseases with neurodegeneration, the COX activity and 5-LO activity increased, prostaglandins and leukotrienes cause formation of the ß-amyloid protein, one of the pathogenic substances of Alzheimer's disease, and further cause degeneration of nerve cells (Sugaya et al., Jpn. J. Pharmacol. , 2000, vol. 82, p. 85), and thus it is believed that prostaglandins and leukotrienes play important roles in the formation of neurodegenerative diseases such as Alzheimer's disease.

Furthermore, for example, it was reported that, in a pathological tissue of colon cancer, COX and 5-LO were expressed, and amounts of production of prostaglandins and leukotrienes were increased (Dreyling et al. , Biochim. Biophys.

Acta. , 1986, vol. 878, p. 184), and leukotriene caused increase in colon cancer cells (Qiao et al. , Biochim. Biophys. Acta, 1995, vol. 1258, p. 215 ; Hong et al. , Cancer Res., 1999, vol. 59, p. 2223). Thus, it is believed that prostaglandins and leukotrienes play important roles also in tissues of large bowel cancer.

Involvement of prostaglandins and/or leukotrienes in diseases and pathological conditions is not limited to those diseases exemplified above, and it has been demonstrated that prostaglandins and/or leukotrienes are involved in variety of conditions, various diseases, or various pathological conditions where acute or chronic inflammatory reactions are observed and their roles are important.

For the above reason, various prostaglandin production suppressors or leukotriene production suppressors are used as agents for prophylactic or therapeutic treatment of conditions, various diseases or pathological conditions where an acute or chronic inflammatory reaction is recognized. Various non- steroidal anti-inflammatory drugs (NSAIDS) as medicaments having a prostaglandin production-suppressing action are available and used as therapeutic agents for chronic rheumatoid arthritis and osteoarthritis, antiphlogistic-analgesic agents for injury and the like, prophylactic agents for cerebral infarction or myocardial infarction, prophylactic agents for colon polyposis and the like.

However, the class of NSAIDS suppress only production of prostaglandins, and as a result, they increase amounts of production of leukotrienes, and exhibit side effects such as asthmatic attack and gastrointestinal injury as well as renal disturbance.

Furthermore, a difference between an effective dose and a dose inducing the side effects is small in these NSAIDS, and no satisfactory agent is available from a viewpoint of therapeutic effect. A 5-LO inhibitor is available which is described in European Patent No. 279263 as a medicament having a leukotriene production- suppressing action, and the inhibitor is known as a prophylactic agent for asthma.

However, since the agent causes side effects such as hepatic disorder, its dosage is limited, and the agent is not satisfactory also from a viewpoint of therapeutic effect.

Since steroid agents suppress production of both of prostaglandins and leukotrienes, they are used as prophylactic agents or therapeutic agents for conditions of living bodies, various diseases and pathological conditions where various acute or chronic inflammatory reactions are observed. However, their actions are not limited to the lipid mediator production-suppressing action, and they exhibit severe side effects such as induction and exacerbation of infectious diseases due to the immunosuppression action, growth retardation due to normal cell antiproliferative activity, anetoderma and peptic ulcer. Therefore, their uses are limited.

Furthermore, for the above reasons, it is considered that compounds, that suppress the production of both of prostaglandins and leukotrienes and have reduced side effect, are effective as therapeutic agents or prophylactic agents for such conditions of living bodies, diseases or pathological conditions in mammals as described above, and methods of using such compounds together with medicaments available at present are more effective therapeutic or prophylactic methods.

Therefore, development of compounds suppressing the production of both of prostaglandins and leukotrienes, and manufacture of pharmaceutical preparations thereof are strongly desired.

As compounds structurally similar to the compounds of the present invention, for example, biphenyl-5-alkanoic acid derivatives and use thereof are described in W099/19291. However, the moiety of these compounds that corresponds to"AR"included in the formula (I) of the compounds of the present invention is phenyl group, and thus structural features of the above compounds are different. Further, biaryl phospholipase A2 inhibitors are described in U. S. Patent No. 5,391, 817 Japanese Patent Unexamined Publication (Kokai) No. 7-22399].

However, the moiety of these compounds that corresponds to"AR"included in the formula (I) of the compounds of the present invention is only defined to be phenyl group, and thus the structural features of the above compounds are different.

Bicyclic heterocyclic compounds are described in WO00/35886 as protease inhibitors.

However, the substituents of these compounds on the moiety that corresponds to "AR"included in the formula (I) of the compounds of the present invention are different, and further, the publication is completely silent about whether or not the compounds described in the above patent document have any prostaglandin production-suppressing action or leukotriene production-suppressing action.

[Patent document 1] W099/19291 [Patent document 2] U. S. Patent No. 5,391, 817 [Patent document 3] WO00/35886 Disclosure of the Invention An object of the present invention is to provide a novel compound having superior prostaglandin production-suppressing action and leukotriene production- suppressing action. Another object of the present invention is to provide a compound for prophylactic and/or therapeutic treatment of various inflammatory diseases, autoimmune diseases, allergic diseases, pain and fibrosis in mammals caused by lipid mediators. A further object of the present invention is to provide a pharmaceutical composition containing such a compound. A still further object of the present invention is to provide an intermediate for the production of the compound. These objects and other objects as well as advantages of the present invention will be apparent for those skilled in the art from the following descriptions.

In order to achieve the aforementioned objects, the inventors of the present invention conducted various researches. As a result, they found that the substituted arylalkanoic acid derivatives represented by the following general formula, which are novel compounds, had superior prostaglandin production- suppressing action and leukotriene production-suppressing action, and thus accomplished the present invention..

The present invention is embodied by, for example, those described in the following (1) to (191).

(1) A compound represented by the formula (I): [In the formula, Link represents a saturated or unsaturated straight hydrocarbon chain having 1 to 3 carbon atoms.

C2, C3, C4, C5, and C6 in the aromatic ring (E) independently represent a ring-constituting carbon atom. One of the ring-constituting carbon atoms to which Rs and AR do not bind may be replaced with V.

V represents nitrogen atom, or carbon atom substituted with Zx. Zx represents a linear or branched saturated alkyl group having 1 to 4 carbon atoms, fluorine atom, chlorine atom, bromine atom, nitro group, -OR9, or-N (Rnl) (Rn2). R9 represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, or-A6- Qp, wherein A6 represents a single bond or methylene, Qp represents phenyl group, and the phenyl group may be substituted with one of T1 or two or more of the same or different T1. T1 represents a linear or branched saturated alkyl group having 1 to 4 carbon atoms, hydroxyl group, fluorine atom, chlorine atom, bromine atom, trifluoromethyl group, nitro group, an alkoxy group having 1 to 4 carbon atoms, or a mono-or dialkylamino group having 1 to 4 carbon atoms. Rn'represents hydrogen atom or a linear or branched saturated alkyl group having 1 to 4 carbon atoms, Rn2 has the same meaning as Rnl, or represents-COR23 or-SO2R24, or binds to Rn1 to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to form a saturated nitrogen-containing cycloalkyl group or morpholino group. R23 represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms,-O-A6-Qp, or-N (R25) (R26).

R25 represents hydrogen atom, or a linear or branched saturated alkyl group having 1 to 4 carbon atoms. R26 has the same meaning as R25, or binds to R25 to form a 3- to 6-membered ring together with the nitrogen atom to which they bind to form a saturated nitrogen-containing cycloalkyl group or morpholino group. R24 represents a lower alkyl group having 1 to 4 carbon atoms, amino group, or a mono- or dialkylamino group having 1 to 4 carbon atoms.

Rs represents-D-Rx or-N (Ry) (Rz).

D represents a single bond, oxygen atom, sulfur atom,-S (O)-,-S (0) 2-, or C (0)-.

Rx represents a linear or branched saturated alkyl group having 3 to 8 carbon atoms, or represents Ra represented by the following formula: RI (CH2) k- (Ra) Rb represented by the following formula: or Rc represented by the following formula : k in Ra represents 0 or an integer of 1 to 3. RI represents a saturated cyclic alkyl group having 3 to 7 carbon atoms, or a condensed saturated cyclic alkyl group having 6 to 8 carbon atoms, and R1 may be substituted with one of lower alkyl group having 1 to 4 carbon atoms or two or more of the same or different lower alkyl groups having 1 to 4 carbon atoms. Q in Rb represents a partially unsaturated or completely unsaturated monocyclic or condensed bicyclic carbon ring or a heterocyclic ring (q), and binds to A2 at an arbitrary position. The heterocyclic ring (q) contains the same or different 1 to 4 ring-constituting heteroatoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom. A1 represents a single bond or an alkylene (a) having 1 to 3 carbon atoms, and the alkylene (a) may be substituted with a lower alkyl group having 1 to 4 carbon atoms or phenyl group. A2 represents a single bond, oxygen atom, sulfur atom,-S (O)-,-S (0) 2-, or-N (R4)- (provided that when A2 represents oxygen atom, sulfur atom,-S (O)-,-S (0) 2-or-N (R4)-, A1 represents ethylene or trimethylene). R2 and R3 independently represent hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms, oxo group, thioxo group, fluorine atom, chlorine atom, bromine atom, trifluoromethyl group,-OR5,-N (R6) (R6'),-NHCOR7,- NHS02R8, or-A6-Qa, or they bind to each other to represent methylenedioxy group.

Qa represents a partially unsaturated or completely unsaturated monocyclic or condensed bicyclic carbon ring or a heterocyclic ring (qa), binds to As at an arbitrary position on the ring, and may be substituted with one of T1 or two or more of the same or different T1. The heterocyclic ring (qa) contains the same or different 1 to 4 ring-constituting heteroatoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom. R4 and R6 independently represent hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms. R5 and R7 independently represent hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, or-A6-Qa. R8 represents a lower alkyl group having 1 to 4 carbon atoms.

Rs'has the same meaning as R6, or binds to R6 to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogen-containing cycloalkyl group or morpholino group. p in Rc represents an integer of 2 to 4. A4 represents a single bond, methylene, or ethylene. A5 represents-C (O)-,-C (S)-, or-S (0) 2-. Rd represents hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or Qa. Re represents an alkyl group having 1 to 8 carbon atoms,-A6-Qa,-(CH2) iR14,-OR23,-SR23, or-N (R29) (R30). i represents an integer of 1 to 3, R14 represents hydroxyl group, an alkoxy group having 1 to 4 carbon atoms, carboxyl group, or an N, N-dialkylcarbamoyl group having 1 to 4 carbon atoms. R28 represents an alkyl group having 1 to 8 carbon atoms, or-A6-Qa.

R29 represents an alkyl group having 1 to 8 carbon atoms, an alkoxycarbonyl group having 1 to 4 carbon atoms, or-A6-Qa. R30 represents hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, or binds to R29 to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogen-containing cycloalkyl group or morpholino group.

Rz has the same meaning as Rx, or Rz represents methyl group, ethyl group, or-A5-Re. Ry represents hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or-A6-Qp, or Ry may bind to Rz to form, together with a nitrogen atom to which they bind, a saturated or unsaturated 3 to 7-membered nitrogen-containing cyclic group, wherein said nitrogen-containing cyclic group may optionally be substituted with one or two lower alkyl groups having 1 to 4 carbon atoms wherein said two alkyl groups may be the same or different.

AR represents a partially unsaturated or completely unsaturated condensed bicyclic carbon ring or a heterocyclic ring (ar), and may be substituted with one of Xa or two or more of the same or different Xa. The heterocyclic ring (ar) contains the same or different 1 to 4 ring-constituting heteroatoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom. Xa represents a linear or branched saturated alkyl group having 1 to 4 carbon atoms, a saturated cyclic alkyl group having 3 to 7 carbon atoms, oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group,-(CH2) iRl4,-ORl°,-N (Rll) (Rl2), -SO2Rl3, or-COR27. Rlo represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, or- (CH2) iRl4. R"represents hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms. R12 represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a hydroxyalkyl group having 2 to 4 carbon atoms, -COR15, or-S02Rl6, or binds to Rll to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogen-containing cycloalkyl group or morpholino group. Rl5 represents a lower alkyl group having 1 to 4 carbon atoms, a hydroxyalkyl group having 2 to 4 carbon atoms, amino group, a mono-or dialkylamino group having 1 to 4 carbon atoms, or-A6-Qa. R13 and Rl6 independently represent a lower alkyl group having 1 to 4 carbon atoms, amino group, or a mono-or dialkylamino group having 1 to 4 carbon atoms. R27 represents hydrogen atom, hydroxyl group, an alkoxy group having 1 to 4 carbon atoms, a lower alkyl group having 1 to 4 carbon atoms, amino group, or a mono-or dialkylamino group having 1 to 4 carbon atoms.

Y represents hydrogen atoin, a lower alkyl group having 1 to 4 carbon atoms,- (CH2) mN (Ri8) (Ri9), or-C (R20) 2OC (O) A3R21. Symbol m represents an integer of 2 or 3. Rl8 is the same as Rl9, or binds to Rl9 to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogen-containing cycloalkyl group or morpholino group. R19 represents methyl group, ethyl group, or propyl group. R20 represents hydrogen atom, methyl group, ethyl group, or propyl group. R21 represents a lower alkyl group having 1 to 4 carbon atoms, a cyclic saturated alkyl group having 3 to 6 carbon atoms, or phenyl group, and A3 represents a single bond, or oxygen atom. This compound may sometimes be hereinafter referred to simply as"Compound (I)"of the present invention. "] or a salt thereof.

(1-2) The compound or salt thereof according to (1), wherein, in the formula (I), Link is- (CH2) n-, n is an integer of 1 to 3, Rz has the same meaning as that of Rx or represents-A5-Re when Rs is-N (Ry) (Rz), and Ry is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or A6-Qp, or Ry binds to Rz to form, together with a nitrogen atom to which they bind, a saturated or unsaturated 3 to 7-membered nitrogen-containing cyclic group.

(2) The compound or salt thereof according to (1) or (1-2) mentioned above, wherein, in the formula (I), AR binds to any atom among C2 and C3 in the aromatic ring (E).

(3) The compound or salt thereof according to any one of (1) to (2) mentioned above, wherein, in the formula (I), n is an integer of 2 (the description of"according to any one of (1) to (2) "includes (1-2) mentioned above, and the same or similar description should be construed in the same manner hereinafter in the specification).

(4) The compound or salt thereof according to any one of (1) to (3) mentioned above, wherein, in the formula (I), AR is a residue of naphthalene, benzofuran, benzo [b] thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-lH-quinoline, benzo [d] isothiazole, 1H-indazole, benzo [c]isothiazole, 2H- indazole, imidazo [1, 2-a]pyridine, 1H-pyrrolo [2, 3-b] pyridine, isoquinoline, dihydro- 2H-isoquinoline, cinnoline, quinazoline, quinoxaline, 1H-benzimidazole, benzoxazole, 1H-pyrrolo [3, 2-b] pyridine, benzo [1, 2,5] thiadiazole, 1H-benzotriazole, 1, 3-dihydropyrrolo [2, 3-b] pyridine, 1, 3-dihydrobenzimidazole, dihydro-3H- benzoxazole, phthalazine, [1, 8] naphthalidine, [1, 5] naphthalidine, lH-pyrrolo [3, 2- c] pyridine, lH-pyrrolo [2, 3-c]pyridine, 1H-pyrazolo [4, 3-b] pyridine, lH-pyrazolo [4,3- c] pyridine, lH-pyrazolo [3, 4-c]pyridine, 1H-pyrazolo [3, 4-b] pyridine, [1, 2, 4] triazolot4, 3-a] pyridine, thieno [3, 2-c] pyridine, thieno [3, 2-b]pyridine, 1H- thieno [3, 2-c] pyrazole, benzo [d] isoxazole, benzo [c] isoxazole, indolizine, 1, 3- dihydroindole, 1H-pyrazolo [3, 4-d] thiazole, 2H-isoindole, [1, 2,4] triazolo [1, 5- a] pyrimidine, lH-pyrazolo [3, 4-b]pyrazine, 1H-imidazo [4, 5-b]pyrazine, 7H-purine, or 4H-chromene (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa).

(5) The compound or salt thereof according to any one of (1) to (3) mentioned above, wherein, in the formula (I), AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [blthiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro- 3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H- benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin- 6-yl group, dihydro-lH-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo [c]isothiazol-5-yl group, benzo [c]isothiazol-4-yl group, benzo [clisothiazol-6-yl group, benzo [c] isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, 1H-pyrrolo [2, 3-b]pyridin-5-yl group, lH-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7- yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, lH-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7- yl group, lH-pyrrolo [3, 2-b] pyridin-5-yl group, lH-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2, 5] thiadiazol-4-yl group, 1H- benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2,3- b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1,3- dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H- benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5- yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3,2- c] pyridin-6-yl group, 1H-pyrrolo [3, 2-c] pyridin-4-yl group, 1H-pyrrolo [2, 3-c] pyridin- 5-yl group, 1H-pyrrolo[2,3-c]pyridin-4-yl group, lH-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazolo [4, 3-b]pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-4-yl group, lH-pyrazolo [3, 4-c] pyridin-5-yl group, 1H- pyrazolo [3, 4-c] pyridin-4-yl group, lH-pyrazolo [3, 4-b] pyridin-5-yl group, 1H- pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2, 4] triazolo [4, 3-a]pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a]pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3,2- e] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b] pyridin-3-yl group, thieno [3, 2-b]pyridin-5-yl group, thieno [3, 2- b] pyridin-6-yl group, 1H-thieno [3, 2-c] pyrazol-5-yl group, 1H-thieno [3, 2-c] pyrazol-4- yl group, benzo [d] isoxazol-5-yl group, benzo [d] isoxazol-4-yl group, benzo [d] isoxazol- 6-yl group, benzo [d] isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5- yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3,4- d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, lH-pyrazolo [3, 4-b] pyrazin-5-yl group, 1H-imidazo [4, 5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa).

(6) The compound or salt thereof according to any one of (1) to (3) mentioned above, wherein, in the formula (I), AR is a residue of naphthalene, benzofuran, benzo [b] thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-lH-quinoline, benzo [d]isothiazole, 1H-indazole, benzo[c]isothiazole, 2H- indazole, imidazo [1, 2-a]pyridine, 1H-pyrrolo [2, 3-b] pyridine, isoquinoline, or dihydro-2H-isoquinoline (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa).

(7) The compound or salt thereof according to any one of (1) to (3) mentioned above, wherein, in the formula (I), AR is a residue of cinnoline, quinazoline, quinoxaline, 1H-benzimidazole, benzoxazole, lH-pyrrolo [3, 2-b] pyridine, benzo [1, 2,5] thiadiazole, 1H-benzotriazole, 1, 3-dihydropyrrolo [2, 3-b] pyridine, 1,3-dihydrobenzimidazole, dihydro-3H-benzoxazole, phthalazine, [1, 8] naphthalidine, [1, 5] naphthalidine, 1H- pyrrolo [3, 2-c]pyridine, 1H-pyrrolo [2, 3-c]pyridine, 1H-pyrazolo [4, 3-b] pyridine, 1H- pyrazolo [4, 3-c]pyridine, 1H-pyrazolo [3, 4-c]pyridine, 1H-pyrazolo [3, 4-b] pyridine, [1, 2,4] triazolo [4, 3-a] pyridine, thieno [3, 2-c] pyridine, thieno [3, 2-b] pyridine, 1H- thieno [3, 2-c] pyrazole, benzo [d] isoxazole, benzo [c] isoxazole, indolizine, 1, 3- dihydroindole, lH-pyrazolo [3, 4-d] thiazole, lH-pyrazolo [3, 4-d] thiazole, 2H-isoindole, [1, 2,4] triazolo [1, 5-a] pyrimidine, lH-pyrazolo [3, 4-b] pyrazine, lH-imidazo [4, 5- b] pyrazine, 7H-purine, or 4H-chromene (the aforementioned residue may have one of Xa or two or more of the same or different Xa).

(8) The compound or salt thereof according to any one of (1) to (7) mentioned above, wherein, in the formula (I), Rs is-D-Rx or-N (Ry) (Rz), D is a single bond, oxygen atom, sulfur atom,-S (O)-,-S (0) 2-, or-C (O)-, Rx is a linear or branched saturated alkyl group having 3 to 8 carbon atoms, or Ra, Rb, or Rc, k in Ra is 0 or an integer of 1 to 3, Rl is a saturated cyclic alkyl group having 3 to 7 carbon atoms or a condensed saturated cyclic alkyl group having 6 to 8 carbon atoms, Rl may be substituted with one of lower alkyl group having 1 to 4 carbon atoms or two or more of the same or different lower alkyl groups having 1 to 4 carbon atoms, Q in Rb is phenyl group, thienyl group, furyl group, pyrrolyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, indazolyl group, 4H-chromenyl group, dihydrobenzodioxyl group, benzoisoxazolyl group, pyrrolopyridinyl group, pyrazolopyridinyl group, triazolopyridinyl group, thienopyridinyl group, thienopyrazolyl group, 1, 3-dihydrobenzimidazole group, dihydro-3H-benzoxazole group, or dihydro-3H-benzothiazole group (the aforementioned groups binds to A2 at an arbitrary position), Al is a single bond or an alkylene (a) having 1 to 3 carbon atoms, the alkylene (a) may be substituted with a lower alkyl group having 1 to 4 carbon atoms or phenyl group, A2 is a single bond, oxygen atom, sulfur atom,-S (O)-,-S (0) 2-, or-N (R4)- (provided that when A2 represents oxygen atom, sulfur atom,-S (O)-,-S (0) 2-, or-N (R4)-, A1 represents ethylene or trimethylene), R2 and R3 independently represent hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms, oxo group, thioxo group, fluorine atom, chlorine atom, bromine atom, trifluoromethyl group,- OR5,-N (R6) (R6'),-NHCOR7,-NHSO2R3, or-A6-Qa, or they bind to each other to represent methylenedioxy group, Qa is phenyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, naphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, or indazolyl group (these groups may be substituted with one of Tl or two or more of the same or different T1, and bind to As at an arbitrary position on the ring), R4 and R6 independently represent hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R5 and R7 independently represent hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, or-A6-Qa, R3 is a lower alkyl group having 1 to 4 carbon atoms, R6 has the same meaning as R6, or binds to R6 to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to form a saturated nitrogen-containing cycloalkyl group or morpholino group, p in Rc is an integer of 2 to 4, A4 is a single bond or methylene or ethylene, A5 is-C (0)-,-C (S) -, or-S (0) 2-, Rd is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or Qa, Re is an alkyl group having 1 to 8 carbon atoms,-A6-Qa, - (CH2) iRl4,-OR28,-SR28, or-N (R29) (R30), i is an integer of 1 to 3, R14 is hydroxyl group, an alkoxy group having 1 to 4 carbon atoms, carboxyl group, or an N, N- dialkylcarbamoyl group having 1 to 4 carbon atoms, R28 is an alkyl group having 1 to 8 carbon atoms or-As-Qa, R29 is an alkyl group having 1 to 8 carbon atoms, an alkoxycarbonyl group having 1 to 4 carbon atoms, or-A6-Qa group, R30 is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, or binds to R29 to form a 3- to 6-membered ring together with the nitrogen atom to which they bind to form a saturated nitrogen-containing cycloalkyl group or morpholino group, Rz has the same meaning as Rx, or is-A5-Re, and Ry is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or-A6-Qp, or binds to Rz to form a saturated or unsaturated nitrogen-containing cyclic substituent having 3 to 7 atoms together with nitrogen atom to which they binds.

(9) The compound or salt thereof according to any one of (1) to (8) mentioned above, wherein, in the formula (1), among C2, C3, C4, C5, and C6 in the aromatic ring (E), one ring-constituting atom to which Rs or AR does not bind is replaced with nitrogen atom.

(10) The compound or salt thereof according to any one of (1) to (8) mentioned above, wherein, in the formula (1), among C2, C3, C4, C5, or C6 in the aromatic ring (E), one ring-constituting atom to which Rs or AR does not bind is replaced with- N (Rnl) (Rn2) (provided that one of Rnl and Rn2 represents a substituent other than hydrogen atom).

(11) The compound or salt thereof according to (1) or (10) mentioned above, wherein, in the formula (1), Rs is-O-Rx.

(12) The compound or salt thereof according to any one of (1) to (11) mentioned above, wherein, in the formula (1), Rs is-O-Rc.

(13) The compound or salt thereof according to any one of (1) to (10) mentioned above, wherein, in the formula (I), Rs is-N (Ry) (Rz).

(14) The compound or salt thereof according to any one of (1) to (10) mentioned above, wherein, in the formula (1), Rs is-D-Rx, and D is a single bond, sulfur atom, -S (O)-,-S (0) 2-, or-C (O)-.

(15) The compound or salt thereof according to any one of (1) to (10) mentioned above, wherein, in the formula (I), Rs is-S-Rx.

(16) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (1), AR binds at the position of C2 in the aromatic ring (E), and Rs binds to one of the ring-constituting carbon atoms C3, C4, and C5.

(17) The compound or salt thereof according to (16) mentioned above, wherein, in the formula (I), Rs is-O-Rx, and no ring-constituting carbon atom in the aromatic ring (E) is replaced with V.

(18) The compound or salt thereof according to (16) or (17) mentioned above, wherein, in the formula (I), n is an integer of 2, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(19) The compound or salt thereof according to (4) mentioned above, wherein, in the formula (1), Link is- (CH2) n-, n is an integer of 2, AR binds at the position of C2 in the aromatic ring (E), Rs binds to one of ring-constituting carbon atoms C3, C4 and C5, Rs is-O-Rx, Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, and all of C2, C3, C4, C5, and C6 in the aromatic ring (E) are not replaced with V.

(20) The compound or salt thereof according to (5) mentioned above, wherein, in the formula (I), Link is- n-, n is an integer of 2, AR binds at the position of C2 in the aromatic ring (E), Rs binds to one of ring-constituting carbon atoms C3, C4 and C5, Rs is-O-Rx, Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, and all of C2, C3, C4, C5, and C6 in the aromatic ring (E) are not replaced with V.

(21) The compound or salt thereof according to any one of (16) to (20) mentioned above, wherein, in the formula (I), Xa which may substitute on AR is methyl group, ethyl group, propyl group, hydroxyethyl group, carboxymethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, methylamino group, dimethylamino group, carboxyl group, carbamoyl group, acetyl group, methanesulfonyl group, sulfamoyl group, or N, N-dimethylsulfamoyl group.

(22) The compound or salt thereof according to any one of (16) to (21) mentioned above, wherein, in the formula (I), Rs is-O-Rx, Rx is butyl group, isobutyl group, 2- ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, or cyclohexylmethyl group, or Rb (provided that Q in Rb is phenyl group or indan-2-yl group), Al is a single bond, a methylene group substituted with methyl group or ethyl group, or unsubstituted methylene group, or an ethylene group substituted with methyl group or ethyl group, or unsubstituted ethylene group, A2 is a single bond, oxygen atom, sulfur atom, -N (methyl) -, or- N (ethyl) - (provided that when A2 represents oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)-, A1 represents ethylene), and R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, or dimethylamino group (provided that when Q is phenyl group, is a single bond or unsubstituted methylene, and A2 is a single bond, one of R2 and R3 is a substituent other than hydrogen atom).

(23) The compound or salt thereof according to any one of (16) to (22) mentioned above, wherein, in the formula (1), Rx-D-binds at the position of C3 in the aromatic ring (E).

(24) The compound or salt thereof according to any one of (16) to (22) mentioned above, wherein, in the formula (I), Rx-D-binds at the position of C4 in the aromatic ring (E).

(25) The compound or salt thereof according to any one of (16) to (22) mentioned above, wherein, in the formula (1), Rx-D-binds at the position of C5 in the aromatic ring (E).

(26) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 1 to 3, AR binds to C2, Rs binds to one of the ring- constituting carbon atoms C3, C4, and C5, a ring-constituting atom among C3, C4, and C5 to which Rs does not bind may be replaced with V, V is nitrogen atom or carbon atom substituted with Zx, Zx is fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, or N, N-dimethylsulfamoylamino group, Rs is-D-Rx or-N (Ry) (Rz), D is oxygen atom or sulfur atom, Rx is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2- cyclopentylethyl group, or 2-cyclohexylethyl group, or Rb or Rc, Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group, and A2 is a single bond, oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl) - (provided that when A2 is oxygen atom, sulfur atom, -N (methyl) -, or-N (ethyl)-, Al represents ethylene). R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q is phenyl group, Al is a single bond or unsubstituted methylene, and A2 is a single bond, one of R2 and R3 is a substituent other than hydrogen atom).

Symbol p in Rc is an integer of 2 or 3, A4 is a single bond or methylene, A5 is-C (O)-, -C (S)-, or-S (0) 2-, Rd is hydrogen atom, or methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4- fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, or pyridin-4-yl group, Re is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4- methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen- 2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4- methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N- isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N' (4'methylphenyl) amino group, N- (4- chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2- yl) amino group, N- (furan-3-yl) amino group, N- (thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, or ethyloxycarbonylamino group, Rz is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3- fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5- methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan- 2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5, 6- dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, l- (3'chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2- methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2- fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4- chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4- difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2-13- (trifluoromethyl) phenyl] ethyl group, 2-14- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4- methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4- chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4- fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N- isobutylthiocarbamoyl group, t-butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N- cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N- cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N- cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N-phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4- methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4- chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4- fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4- fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-1- yl) carbonyl group, or (morpholino-4-yl) carbonyl group, Ry is hydrogen atom, methyl group, ethyl group, or isobutyl group, or binds to Rz to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol- 1-yl group, or pyrazol-1-yl group together with nitrogen atom to which they binds, AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4- yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro- lH-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, lH-indazol-5-yl group, lH-indazol-4-yl group, 1H-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [c] isothiazol-4-yl group, benzo [c] isothiazol-6-yl group, benzo [clisothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, lH-pyrrolo [2,3- blpyridin-5-yl group, lH-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H- isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H- benzimidazol-5-yl group, lH-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H- pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [l, 2, 5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, 1H- benzotriazol-5-yl group, lH-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2,3- b]pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1,3- dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H- benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5- yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, lH-pyrrolo [3, 2- c]pyridin-6-yl group, lH-pyrrolo [3, 2-c]pyridin-4-yl group, lH-pyrrolo [2, 3-c] pyridin- 5-yl group, lH-pyrrolo [2, 3-c] pyridin-4-yl group, 1H-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazolo [4, 3-b] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-4-yl group, lH-pyrazolo [3, 4-c] pyridin-5-yl group, 1H- pyrazolo [3, 4-c] pyridin-4-yl group, l H-pyrazolo [3, 4-b]pyridin-5-yl group, 1H- pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2- c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b] pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3, 2- b]pyridin-6-yl group, 1H-thieno [3, 2-c]pyrazol-5-yl group, lH-thieno [3, 2-c]pyrazol-4- yl group, benzo [d]isoxazol-5-yl group, benzo [d]isoxazol-4-yl group, benzo [d] isoxazol- 6-yl group, benzo [d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5- yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3,4- d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, 1H-pyrazolo [3, 4-b] pyrazin-5-yl group, 1H-imidazo [4, 5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa), Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2- hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N- dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2- aminoacetylamino group, methylsulfonylamino group, (N, N- dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N- methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N, N-dimethylcarbamoyl group, and Y is hydrogen atom, methyl group or ethyl group.

(27) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 2, C2 is carbon atom to which AR binds, C3 is carbon atom to which Rs binds, C4 may be replaced with V, C5 and C6 are unsubstituted ring-constituting carbon atoms, V is nitrogen atom, or carbon atom substituted with Zx, Zx is fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, or N, N- dimethylamino group, Rs is-O-Rx, Rx is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2-(4-fluorophenyl) ethyl group, 2-(2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, or 2- (N-ethyl-N-phenylamino) ethyl group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzolb] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3- dimethyl-lH-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1,2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-1H-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H- indol-5-yl group, 2-methyl-1-propyl-lH-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-lH- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol- 5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-lH-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

(28) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 2, C2 is carbon atom to which AR binds, C4 is carbon atom to which Rs binds, C5 may be replaced with V, C3 and C6 represents an unsubstituted ring-constituting carbon atom, V is nitrogen atom, or carbon atom substituted with Zx, Zx is fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, or N, N- dimethylamino group, Rs is-O-Rx, Rx is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3, 5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyllethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyll ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, or 2-(N-ethyl-N-phenylamino) ethyl group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-1H-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-1H- indol-5-yl group, 2-methyl-1-propyl-lH-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 1- methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol- 5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b]pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

(29) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), AR binds to C3 in the aromatic ring (E), and Rs binds to C5 or C6 in the aromatic ring (E).

(30) The compound or salt thereof according to (29) mentioned above, wherein, in the formula (I), Rs is-O-Rx, and all of C2, C3, C4, C5, and C6 in the aromatic ring (E) are not replaced with V.

(31) The compound or salt thereof according to (29) or (30) mentioned above, wherein, in the formula (I), n is an integer of 2, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(32) The compound or salt thereof according to (4) mentioned above, wherein, in the formula (1), Link is-(CH2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to the ring-constituting carbon atom C5 or C6 in the aromatic ring (E), Rs is-O-Rx, Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, and all of C2, C3, C4, C5, and C6 in the aromatic ring (E) are not replaced with V.

(33) The compound or salt thereof according to (5) mentioned above, wherein, in the formula (I), n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to the ring-constituting carbon atom C5 or C6 in the aromatic ring (E), Rs is-O-Rx, Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, and all of C2, C3, C4, C5, and C6 in the aromatic ring (E) are not replaced with V.

(34) The compound or salt thereof according to any one of (29) to (33) mentioned above, wherein, in the formula (I), Xa which may substitute on AR is methyl group, ethyl group, propyl group, hydroxyethyl group, carboxymethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, methylamino group, dimethylamino group, carboxyl group, carbamoyl group, acetyl group, methanesulfonyl group, sulfamoyl group, or N, N-dimethylsulfamoyl group.

(35) The compound or salt thereof according to any one of (29) to (34) mentioned above, wherein, in the formula (I), Rs is-O-Rx, Rx is butyl group, isobutyl group, 2- ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, or cyclohexylmethyl group, or Rb (provided that Q in Rb is phenyl group or indan-2-yl group), Al is a single bond, or methylene group substituted with methyl group or ethyl group or unsubstituted methylene group, or ethylene group substituted with methyl group or ethyl group or unsubstituted ethylene group, A2 is a single bond, oxygen atom, sulfur atom,-N (methyl)-, or- N (ethyl) - (provided that when A2 is oxygen atom, sulfur atom, -N (methyl) -, or- N (ethyl)-, Al is ethylene), and R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, or dimethylamino group (provided that when Q is phenyl group, Al is a single bond or unsubstituted methylene, and A2 is a single bond, one of R2 and R3 is a substituent other than hydrogen atom).

(36) The compound or salt thereof according to any one of (29) to (35) mentioned above, wherein, in the formula (I), Rs binds at the position of C5 in the aromatic ring (E).

(37) The compound or salt thereof according to any one of (29) to (35) mentioned above, wherein, in the formula (I), Rs binds at the position of C6 in the aromatic ring (E).

(38) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 2, C3 is carbon atom to which AR binds, C5 is carbon atom to which Rs binds, C2, C4 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-O-Rx, Rx is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2' (4'methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenylbxy) ethyl group, 2- (phenylthio) ethyl group, 2-(N-phenyl-N-methylamino) ethyl group, or 2-(N-ethyl-N-phenylamino) ethyl group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2, 3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, l-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-lH- indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-lH-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-methyl-3-hydroxy-1H-indazol-5- yl group, imidazo [1, 2-a]pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-1H- pyrrolol2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

(39) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), and C6 is replaced with V.

(40) The compound or salt thereof according to (39) mentioned above, wherein, in the formula (I), n is an integer of 2, V is carbon atom substituted with Zx, Rs is-O- Rx, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(41) The compound or salt thereof according to (4) mentioned above, wherein, in the formula (I), Link is- (CH2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), Cs is carbon atom substituted with Zx, Rs is-O-Rx, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(42) The compound or salt thereof according to (5) mentioned above, wherein, in the formula (I), Link is- (CH2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C6 is carbon atom substituted with Zx, Rs is-0-Rx, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(43) The compound or salt thereof according to any one of (39) to (42) mentioned above, wherein, in the formula (I), Xa which may substitute on AR is methyl group, ethyl group, propyl group, hydroxyethyl group, carboxymethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, methylamino group, dimethylamino group, carboxyl group, carbamoyl group, acetyl group, methanesulfonyl group, sulfamoyl group, or N, N-dimethylsulfamoyl group.

(44) The compound or salt thereof according to any one of (39) to (43) mentioned above, wherein, in the formula (I), Rs is-O-Rx, Rx is butyl group, isobutyl group, 2- ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, or cyclohexylmethyl group, or Rb (provided that Q in Rb is phenyl group or indan-2-yl group), Al is a single bond, or methylene group substituted with methyl group or ethyl group or unsubstituted methylene group, or ethylene group substituted with methyl group or ethyl group or unsubstituted ethylene group, A2 is a single bond, oxygen atom, sulfur atom, -N (methyl) -, or- N (ethyl)- (provided that when A2 is oxygen atom, sulfur atom,-N (methyl)-, or- N (ethyl)-, Al is ethylene), R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, or dimethylamino group (provided that when Q is phenyl group, Al is a single bond or unsubstituted methylene, and A2 is a single bond, one of R2 and R3 is a substituent other than hydrogen atom).

(45) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 2, C3 is carbon atom to which AR binds, C4 is carbon atom to which Rs binds, C6 is carbon atom substituted with Zx, C2 and C5 are unsubstituted ring- constituting carbon atoms, Zx is fluorine atom, methyl group, hydroxyl group, amino group, N- methylamino group, or N, N-dimethylamino group, Rs is-O-Rx, Rx is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2-(4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyll ethyl group, 2- [4- (trifluoromethyl) phenyl]ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, or 2-(N-ethyl-N-phenylamino) ethyl group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) nap hthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3- dimethyl-lH-indol-5-yl group, l-methyl-lH-indol-5-yl group, 1, 2-dimethyl-1H-indol- 5-yl group, 1, 3-dimethyl-1H-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-1H-indl-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H- indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-lH-indol-5-yl group, 1-(2-hydroxyethyl)-1H- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5- yl group, imidazo [l, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, l-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

(46) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is nitrogen atom, and C2 and C6 are unsubstituted ring- constituting carbon atoms.

(47) The compound or salt thereof according to (46) mentioned above, wherein, in the formula (I), n is an integer of 2, D is oxygen atom, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(48) The compound or salt thereof according to (4) mentioned above, wherein, in the formula (I), Link is- (CH2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is nitrogen atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is'O'Rx, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(49) The compound or salt thereof according to (5) mentioned above, wherein, in the formula (1), Link is- (CH2)"-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is nitrogen atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-O-Rx, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(50) The compound or salt thereof according to any one of (46) to (49) mentioned above, wherein, in the formula (I), Xa which may substitute on AR is methyl group, ethyl group, propyl group, hydroxyethyl group, carboxymethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, methylamino group, dimethylamino group, carboxyl group, carbamoyl group, acetyl group, methanesulfonyl group, sulfamoyl group, or N, N-dimethylsulfamoyl group.

(51) The compound or salt thereof according to any one of (46) to (50) mentioned above, wherein, in the formula (I), Rs is-O-Rx, Rx is butyl group, isobutyl group, 2- ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, or cyclohexylmethyl group, or Rb (provided that Q in Rb is phenyl group or indan-2-yl group), Al is a single bond, or methylene group substituted with methyl group or ethyl group or unsubstituted methylene group, or ethylene group substituted with methyl group or ethyl group or unsubstituted ethylene group, A2 is a single bond, oxygen atom, sulfur atom,-N (methyl)- or- N (ethyl)- (provided that when A2 is oxygen atom, sulfur atom,-N (methyl)-, or- N (ethyl)-, Al is ethylene), and R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, or dimethylamino group (provided that when Q is phenyl group, Al is a single bond or unsubstituted methylene, and A2 is a single bond, one of R2 and R3 is a substituent other than hydrogen atom).

(52) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 2, C3 is carbon atom to which AR binds, C4 is carbon atom to which Rs binds, C5 is nitrogen atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-O-Rx, Rx is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1-(3-fluorophenyl) ethyl group, 1-(4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4'fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2-(2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyll ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2-(N-phenyl-N-methylamino)ethyl group, or 2- (N-ethyl-N-phenylamino) ethyl group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino)naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3- dimethyl-lH-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1, 2-dimethyl-1H-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-lH-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-lH- indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-lH- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-1H- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-lH-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-lH-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

(53) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is a ring-constituting carbon atom substituted with Zx, or an unsubstituted ring-constituting carbon atom, C2 and C6 are unsubstituted ring- constituting carbon atoms, Rs is-D-Rx, and D is a single bond, sulfur atom,-S (O)-,- S (0) 2-, or-C (O)-.

(53-2) The compound of salt thereof according to (1-2) mentioned above, wherein, in the formula (I), AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is nitrogen atom, C2 and C6 are unsubstituted ring- constituting carbon atoms, Rs is-D-Rx, and D is a single bond, sulfur atom,-S (O)-,- S (0) 2-, or-C (O)-.

(53-3) The compound or salt thereof according to (53) or (53-2) mentioned above, wherein, in the formula (I), Rs is-D-Rx and D is single bond.

(54) The compound or salt thereof according to any one of (53) to (53-3) mentioned above, wherein, in the formula (I), n is an integer of 2, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(55) The compound or salt thereof according to (4) mentioned above, wherein, in the formula (I), Link is- (CH2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is a ring-constituting carbon atom substituted with Zx, or an unsubstituted ring-constituting carbon atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-D-Rx, D is a single bond, sulfur atom,-S (O)-,-S (0) 2-, or-C (O)-, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(55-2) The compound or a salt thereof according to (4) mentioned above, wherein, in the formula (1), Link is- (CH2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 may be replaced with V, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-D-Rx, D is a single bond, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(56) The compound or salt thereof according to (5) mentioned above, wherein, in the formula (I), Link is- (CH2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is a ring-constituting carbon atom substituted with Zx, or an unsubstituted ring-constituting carbon atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-D-Rx, D is a single bond, sulfur atom,-S (O)-,-S (0) 2-, or-C (O)-, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(56-2) The compound or a salt thereof according to (5) mentioned above, wherein, in the formula (I), Link is- (CH2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 may be replaced with V, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-D-Rx, D is a single bond, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(57) The compound or salt thereof according to any one of (53) to (56-2) mentioned above, wherein, in the formula (I), Xa which may substitute on AR is methyl group, ethyl group, propyl group, hydroxyethyl group, carboxymethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, methylamino group, dimethylamino group, carboxyl group, carbamoyl group, acetyl group, methanesulfonyl group, sulfamoyl group, or N, N-dimethylsulfamoyl group.

(58) The compound or salt thereof according to any one of (53) to (57) mentioned above, wherein, in the formula (I), Rs is-D-Rx, Rx is butyl group, isobutyl group, 2- ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, or cyclohexylmethyl group, or Rb (provided that Q in Rb is phenyl group or indan-2-yl group), Al is a single bond, or methylene group substituted with methyl group or ethyl group or unsubstituted methylene group, or ethylene group substituted with methyl group or ethyl group or unsubstituted ethylene group, A2 is a single bond, oxygen atom, sulfur atom, -N (methyl) -, or- N (ethyl)- (provided that when A2 represents oxygen atom, sulfur atom,-N (methyl)- or-N (ethyl)-, A1 represents ethylene), and R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, or dimethylamino group (provided that when Q is phenyl group, A is a single bond or unsubstituted methylene, and A2 is a single bond, one of R2 and R3 is a substituent other than hydrogen atom).

(58-2) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 1 to 3, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 may be replaced with V, C2 and C6 are unsubstituted ring-constituting carbon atoms, V is nitrogen atom or V is carbon atom substituted with Zx, Zx is any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, or N, N-dimethylamino group, Rs is-D-Rx, D is a single bond, Rx is butyl group, isobutyl group, 2- ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-cyclopentylethyl group, or 2- cyclohexylethyl group, or Rx is Rb or Rc (provided that Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group), A2 is a single bond, oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)- (provided that when A2 represents oxygen atom, sulfur atom,-N (methyl)- or- N (ethyl)-, Al represents ethylene), R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group, (provided that when Q is phenyl group, Al is a single bond or unsubstituted methylene, and A2 is a single bond, one of R2 and R3 is a substituent other than hydrogen atom). p in Rc is an integer of 2 or 3, A4 is a single bond or methylene, A5 is-C (O)-,-C (S)-, or'S (0) 2-, Rd is hydrogen atom, or methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4- chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, or pyridin-4-yl group, Re is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4- methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N- isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4- chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2- yl) amino group, N- (furan-3-yl) amino group, N- (thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, or ethyloxycarbonylamino group, AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4- yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro- lH-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzold] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, lH-indazol-5-yl group, lH-indazol-4-yl group, 1H-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [c] isothiazol-4-yl group, benzo [c] isothiazol-6-yl group, benzo [c] isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, 1H-pyrrolo [2,3- b] pyridin-5-yl group, lH-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H- isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H- benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H- pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [l, 2,5] thiadiazol-5-yl group, benzol, 2, 5] thiadiazol-4-yl group, 1H- benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2,3- b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1,3- dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H- benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5- yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3,2- cjpyridin-6-yl group, 1H-pyrrolo [3, 2-c] pyridin-4-yl group, 1H-pyrrolo [2, 3-c] pyridin- 5-yl group, 1H-pyrrolo [2, 3-c] pyridin-4-yl group, lH-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazolo [4, 3-b] pyridin-6-yl group, lH-pyrazolo [4, 3-c] pyridin-6-yl group, lH-pyrazolo [4, 3-c] pyridin-4-yl group, lH-pyrazolo [3, 4-c] pyridin-5-yl group, 1H- pyrazolo [3, 4-c]pyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H- pyrazolo [3, 4-b]pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a]pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a]pyridin-7-yl group, thieno [3, 2-c]pyridin-2-yl group, thieno [3,2- c]pyridin-3-yl group, thieno [3, 2-c]pyridin-6-yl group, thieno [3, 2-b\pyridin-2-yl group, thieno [3, 2-b]pyridin-3-yl group, thieno [3, 2-b]pyridin-5-yl group, thieno [3,2- b] pyridin-6-yl group, 1H-thieno [3, 2-c] pyrazol-5-yl group, 1H-thieno [3, 2-c] pyrazol-4- yl group, benzo [d] isoxazol-5-yl group, benzo [d] isoxazol-4-yl group, benzo [d] isoxazol- 6-yl group, benzo [d] isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c] isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5- yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, lH-pyrazolo [3,4- d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, lH-pyrazolo [3, 4-b] pyrazin-5-yl group, lH-imidazo [4, 5-b] pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa), Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2- hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N- dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2- aminoacetylamino group, methylsulfonylamino group, (N, N- dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N- methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N, N-dimethylcarbamoyl group, and Y is hydrogen atom, methyl group, or ethyl group.

(58-3) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (1), n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 may be replaced with V, C2 and C6 are unsubstituted ring-constituting carbon atoms, V is nitrogen atom or V is carbon atom substituted with Zx, Zx is any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, or N, N-dimethylamino group, Rs is-D-Rx, D is a single bond, Rx is butyl group, isobutyl group, 2- ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 2-methylphenyl group, 3-methylphenyl group, 4-methylphenyl group, 2, 3-dimethylphenyl group, 3,5-dimethylphenyl group, 2-methoxyphenyl group, 3-methoxyphenyl group, 4- methoxyphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2, 3- difluorophenyl group, 2,4-difluorophenyl group, 2, 5-difluorophenyl group, 3, 4- difluorophenyl group, 2, 3-dichlorophenyl group, 2,4-dichlorophenyl group, 2,5- dichlorophenyl group, 2,6-dichlorophenyl group, 3, 4-dichlorophenyl group, 3, 5- dichlorophenyl group, 2-trifluoromethylphenyl group, 3-trifluoromethylphenyl group, 4-trifluoromethylphenyl group, 4- (N, N-dimethylamino) phenyl group, indan- 2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan- 2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2- yl group, 4, 7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan- 2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5,6- dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, naphthalen-1-yl group, naphthalen-2-yl group, 1H-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1H-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, biphenyl-2-yl group, biphenyl 3-yl group, biphenyl-4- yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3- fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, l' (3'chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2- methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2- fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4- chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4- difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2, 6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2- methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2-(N-phenyl-N-methylamino) ethyl group, or 2-(N-ethyl-N-phenylamino) ethyl group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b]thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo[b]thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-1H-indol-5-yl group, l-propyl-1H- indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1-(2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5- yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-1H pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

(58-4) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (1), n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 may be replaced with V, C2 and C6 are unsubstituted ring-constituting carbon atoms, V is nitrogen atom or V is carbon atom substituted with Zx, Zx is any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, or N, N-dimethylamino group, Rs is-D-Rx, D is a single. bond, Rx is phenyl group, 2-methylphenyl group, 3-methylphenyl group, 4-methylphenyl group, 2,3-dimethylphenyl group, 3,5- dimethylphenyl group, 2-methoxyphenyl group, 3-methoxyphenyl group, 4- methoxyphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2,3- difluorophenyl group, 2, 4-difluorophenyl group, 2,5-difluorophenyl group, 3,4- difluorophenyl group, 2, 3-dichlorophenyl group, 2,4-dichlorophenyl group, 2,5- dichlorophenyl group, 2,6-dichlorophenyl group, 3,4-dichlorophenyl group, 3, 5- dichlorophenyl group, 2-trifluoromethylphenyl group, 3-trifluoromethylphenyl group, 4-trifluoromethylphenyl group, 4- (N, N-dimethylamino) phenyl group, indan- 2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan- 2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2- yl group, 4,7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan- 2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5,6- dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, naphthalen-1-yl group, naphthalen-2-yl group, 1H-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1H-indazol-5-yl group, or 1-methyl-lH-indazol-5-yl group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3- dimethyl-lH-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, l-ethyl-3- methyl-lH-indol-5-yl group, l-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-1H- indol-5-yl group, 2-methyl-1-propyl-lH-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, l-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

(58-5) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (1), n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C2, C5, and C6 are unsubstituted ring-constituting carbon atoms, Rs is-D-Rx, D is a single bond, Rx is phenyl group, 2-methylphenyl group, 3-methylphenyl group, 4-methylphenyl group, 2,3- dimethylphenyl group, 3,5-dimethylphenyl group, 2-methoxyphenyl group, 3- methoxyphenyl group, 4-methoxyphenyl group, 2-fluorophenyl group, 3- fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2,3-difluorophenyl group, 2, 4-difluorophenyl group, 2, 5-difluorophenyl group, 3, 4-difluorophenyl group, 2, 3-dichlorophenyl group, 2,4- dichlorophenyl group, 2,5-dichlorophenyl group, 2,6-dichlorophenyl group, 3,4- dichlorophenyl group, 3,5-dichlorophenyl group, 2-trifluoromethylphenyl group, 3- trifluoromethylphenyl group, 4-trifluoromethylphenyl group, 4- (N, N- dimethylamino) phenyl group, indan-2-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, naphthalen-1-yl group, naphthalen-2-yl group, lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, lH-indazol-5-yl group, or 1-methyl-lH- indazol-5-yl group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2,3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-1H-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, l-ethyl-3- methyl-lH-indol-5-yl group, l-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-lH- indol-5-yl group, 2-methyl-l-propyl-lH-indol-5-yl group, 3-methyl-l-propyl-lH- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-lH-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, l-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-lH- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

(59) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 1 to 3, C3 is carbon atom to which AR binds, C4 is carbon atom to which Rs binds, C5 may be replaced with V, C2 and C6 are unsubstituted ring-constituting carbon atoms, V is nitrogen atom, or carbon atom substituted with Zx, Zx is fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, or N, N-dimethylsulfamoylamino group, Rs is-S-Rx, Rx is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-cyclopentylethyl group, or 2-cyclohexylethyl group, or Rb or Rc, Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group, A2 is a single bond, oxygen atom, sulfur atom,- N (methyl) -, or-N (ethyl) - (provided that when A2 is oxygen atom, sulfur atom,- N (methyl) -, or-N (ethyl)-, Al is ethylene), R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q is phenyl group, Al is a single bond or unsubstituted methylene, and A2 is a single bond, one of R2 and R3 is a substituent other than hydrogen atom), p in Rc is an integer of 2 or 3, A4 is a single bond or methylene, A5 is-C (O)-,-C (S) -, or-S (0) 2-, Rd is hydrogen atom, or methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4- chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, or pyridin-4-yl group, Re is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4- methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N- isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4- chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2- yl) amino group, N- (furan-3-yl) amino group, N- (thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, or ethyloxycarbonylamino group, AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4- yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro- 1H-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, lH-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [c] isothiazol-4-yl group, benzo [clisothiazol-6-yl group, benzo [c] isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, 1H-pyrrolo [2, 3- b]pyridin-5-yl group, 1H-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H- isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H- benzimidazol-5-yl group, lH-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H- pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, 1H- benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2,3- b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b]pyridin-4-y] group, 1,3- dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H- benzoxazol-6-yl group, dihydro-3H-benzoxazol]-7-yl group, dihydro-3H-benzoxazol-5- yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, lH-pyrrolo [3,2- c] pyridin-6-yl group, lH-pyrrolo [3, 2-c] pyridin-4-yl group, lH-pyrrolo [2, 3-c] pyridin- 5-yl group, lH-pyrrolo [2, 3-c] pyridin-4-yl group, lH-pyrazolo [4, 3-b] pyridin-5-yl group, lH-pyrazolo [4, 3-b] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-e] pyridin-5-yl group, 1H- pyrazolo [3, 4-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H- pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2- c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b] pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3,2- b] pyridin-6-yl group, 1H-thieno [3, 2-c]pyrazol-5-yl group, lH-thieno [3, 2-c]pyrazol-4- yl group, benzo[d]isoxazol-5-yl group, benzo [d] isoxazol-4-yl group, benzo [d] isoxazol- 6-yl group, benzo [d] isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c] isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5- yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3, 4- d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, 1H-pyrazolo [3, 4-b]pyrazin-5-yl group, 1H-imidazo [4, 5-b] pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa), Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2- hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N- dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2- aminoacetylamino group, methylsulfonylamino group, (N, N- dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N- methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N, N-dimethylcarbamoyl group, and Y is hydrogen atom, methyl group, or ethyl group.

(59-2) The compound or salt thereof according to (1) mentioned above, wherein, in the formula (I), AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is a ring-constituting carbon atom substituted with Zx, or an unsubstituted ring-constituting carbon atom, C2 and C6 are unsubstituted ring- constituting carbon atoms, and Rs is-N (Ry) (Rz).

(59-3) The compound or salt thereof according to (1) mentioned above, wherein, in the formula (I), AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is nitrogen atom, C2 and C6 are unsubstituted ring- constituting carbon atoms, and Rs is-N (Ry) (Rz).

(60) The compound or salt thereof according to (59-2) or (59-3) mentioned above, wherein, in the formula (I), Link is- (CH2) n-, n is an integer of 2, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(61) The compound or salt thereof according to (4) mentioned above, wherein, in the formula (1), Link is- (CH2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is a ring-constituting carbon atom substituted with Zx, or an unsubstituted ring-constituting carbon atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-N (Ry) (Rz), and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(61-2) The compound or salt thereof according to (4) mentioned above, wherein, in the formula (I), Link is- (CH2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is nitrogen atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-N (Ry) (Rz), and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(62) The compound or salt thereof according to (5) mentioned above, wherein, in the formula (1), Link is- H2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is a ring-constituting carbon atom substituted with Zx, or an unsubstituted ring-constituting carbon atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-N (Ry) (Rz), and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(62-2) The compound or salt thereof according to (5) mentioned above, wherein, in the formula (1), Link is- H2) n, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is nitrogen atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-N (Ry) (Rz), and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(63) The compound or salt thereof according to any one of (59-2) to (62-2) mentioned above, wherein, in the formula (I), Xa which may substitute on AR is methyl group, ethyl group, propyl group, hydroxyethyl group, carboxymethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, methylamino group, dimethylamino group, carboxyl group, carbamoyl group, acetyl group, methanesulfonyl group, sulfamoyl group, or N, N-dimethylsulfamoyl group.

(64) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (1), n is an integer of 1 to 3, C3 is carbon atom to which AR binds, C4 is carbon atom to which Rs binds, C2, C5, and C6 are unsubstituted ring-constituting carbon atoms, Rs is-N (Ry) (Rz), Rz is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1-(4-fluorophenyl) ethyl group, 1-(2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyll ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4- methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4- chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4- fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N- isobutylthiocarbamoyl group, t'butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N- cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N- cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N- cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N'phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4- methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4- chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4- fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4- fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-1- yl) carbonyl group, or (morpholino-4-yl) carbonyl group, Ry is hydrogen atom, methyl group, ethyl group or isobutyl group, or binds to Rz to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol- 1-yl group, or pyrazol-1-yl group together with the nitrogen atom to which they bind, AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [blthiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4- yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro- lH-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, lH-indazol-5-yl group, 1H-indazol-4-yl group, lH-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [clisothiazol-4-yl group, benzo [clisothiazol-6-yl group, benzo [clisothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, lH-pyrrolo [2,3- blpyridin-5-yl group, 1H-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H- isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H- benzimidazol-5-yl group, l H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H- pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b]pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, 1H- benzotriazol-5-yl group, lH-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2,3- b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1,3- dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H- benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5- yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, lH-pyrrolo [3,2- c] pyridin-6-yl group, lH-pyrrolo [3, 2-c] pyridin-4-yl group, 1H-pyrrolo [2, 3-c] pyridin- 5-yl group, 1H-pyrrolo [2, 3-c]pyridin-4-yl group, lH-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazolo [4, 3-b] pyridin-6-yl group, lH-pyrazolo [4, 3-c]pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-4-yl group, lH-pyrazolo [3, 4-c] pyridin-5-yl group, 1H- pyrazolo [3, 4-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H- pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2- c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b]pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3,2- b] pyridin-6-yl group, 1H-thieno [3, 2-c]pyrazol-5-yl group, 1H-thieno [3, 2-c] pyrazol-4- yl group, benzo [d] isoxazol-5-yl group, benzo [d] isoxazol-4-yl group, benzo [d] isoxazol- 6-yl group, benzo [d] isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c]isoxazol-4-yl group, benzo [c]isoxazol-6-yl group, benzo [c] isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5- yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, lH-pyrazolo [3,4- d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, lH-pyrazolo [3, 4-b] pyrazin-5-yl group, lH-imidazo [4, 5-b] pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (these groups may be substituted with one of Xa or two or more of the same or different Xa), Xa represents oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2- hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N, N-dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N- methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N, N-dimethylcarbamoyl group, and Y is hydrogen atom, methyl group, or ethyl group.

(65) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 2, C3 is carbon atom to which AR binds, C4 is carbon atom to which Rs binds, C2, C5 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-N (Ry) (Rz), Rz is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, l' (3'chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2, 6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2-t3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2-(N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4- methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4- chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4- fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N- isobutylthiocarbamoyl group, t'butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N- cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N- cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N- cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N'phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4- methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4- chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4- fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4- fluorophenyl) thiocarbamoyl group, (pyrrolidino-l-yl) carbonyl group, (piperidino-1- yl) carbonyl group, or (morpholino-4-yl) carbonyl group, Ry is hydrogen atom, methyl group, ethyl group or isobutyl group, or binds to Rz to form pyrrolidino group, piperidino group, or morpholino group together with the nitrogen atom to which they bind, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2,3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, l-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-lH-indol-5-yl group, 1-ethyl-3- methyl-1H-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-lH- indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-1H- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-lH-indazol-5- yl group, imidazo [l, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, l-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

(65-2) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), Link is-(CH2) n-, n is an integer of 2, C3 is carbon atom to which AR binds, C4 is carbon atom to which Rs binds, C2, C5 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-N (Ry) (Rz), and the group represented by-N (Ry) (Rz) is N, N- dimethylamino group, N-ethyl-N-methylamino group, N, N-diethylamino group, N- methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N- methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N- butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N- (2- ethylbutyl) amino group, N- (2-ethylbutyl)-N-methylamino group, N- cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N- (cyclopentylmethyl) amino group, N- (cyclopentylmethyl)-N-methylamino group, N- (cyclohexylmethyl) amino group, N- (cyclohexylmethyl)-N-methylamino group, N- (2- methylphenyl) amino group, N- (4-methylphenyl) amino group, N- (2- fluorophenyl) amino group, N- (3-fluorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (2-chlorophenyl) amino group, N- (3-chlorophenyl) amino group, N- (4- chlorophenyl) amino group, N- (indan-2-yl) amino group, N- (l-phenylethyl) amino group, N- [1- (2-fluorophenyl) ethyl] amino group, N- [1- (3-fluorophenyl) ethyl] amino group, N- [1- (4-fluorophenyl) ethyl] amino group, N- [1- (2-chlorophenyl) ethyl] amino group, N- [1- (3-chlorophenyl) ethyl] amino group, N- [1- (4-chlorophenyl) ethyl] amino group, N- (2-methylphenylmethyl) amino group, N-methyl-N- (2- methylphenylmethyl) amino group, N- (3-methylphenylmethyl) amino group, N- methyl-N- (3-methylphenylmethyl) amino group, N- (4-methylphenylmethyl) amino group, N-methyl-N- (4-methylphenylmethyl) amino group, N- (2- fluorophenylmethyl) amino group, N- (2-fluorophenylmethyl)-N-methylamino group, N- (3-fluorophenylmethyl) amino group, N- (3-fluorophenylmethyl)-N-methylamino group, N- (4-fluorophenylmethyl) amino group, N- (4-fluorophenylmethyl)-N- methylamino group, N- (2-chlorophenylmethyl) amino group, N- (2- chlorophenylmethyl)-N-methylamino group, N- (3-chlorophenylmethyl) amino group, N- (3-chlorophenylmethyl)-N-methylamino group, N- (4-chlorophenylmethyl) amino group, N- (4-chlorophenylmethyl)-N-methylamino group, N- (2, 3- difluorophenylmethyl) amino group, N- (2, 3-difluorophenylmethyl)-N-methylamino group, N-(2, 4-difluorophenylmethyl) amino group, N- (2, 4-difluorophenylmethyl) -N- methylamino group, N- (2, 5-difluorophenylmethyl) amino group, N- (2, 5- difluorophenylmethyl)-N-methylamino group, N- (3, 4-difluorophenylmethyl) amino group, N- (3,4-difluorophenylmethyl)-N-methylamino group, N- (3,5- difluorophenylmethyl) amino group, N- (3, 5-difluorophenylmethyl)-N-methylamino group, N- (2, 3-dichlorophenylmethyl) amino group, N- (2, 3-dichlorophenylmethyl) -N- methylamino group, N-(2, 4-dichlorophenylmethyl) amino group, N- (2, 4- dichlorophenylmethyl)-N-methylamino group, N- (2,5-dichlorophenylmethyl) amino group, N- (2, 5-dichlorophenylmethyl)-N-methylamino group, N- (2,6- dichlorophenylmethyl) amino group, N- (2, 6-dichlorophenylmethyl) -N-methylamino group, N- (3, 4-dichlorophenylmethyl) amino group, N- (3,4-dichlorophenylmethyl)-N- methylamino group, N- (3, 5-dichlorophenylmethyl) amino group, N- (3, 5- dichlorophenylmethyl) -N-methylamino group, N-[2- (trifluoromethyl) phenylmethyl] amino group, N-methyl-N- [2- (trifluoromethyl) phenylmethyll amino group, N- [3- (trifluoromethyl) phenylmethyl] amino group, N-methyl-N- [3- (trifluoromethyl) p henylmethyfl amino group, N- [4- (trifluoromethyl) phenylmethyl] amino group, N-methyl-N- [4- (trifluoromethyl) phenylmethyl] amino group, 1-pyrrolidino group, 1- (4- methylpiperidino) group, 1-homopiperidino group, or 4-morpholino group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b]thiophen-5-yl group, 3- methylbenzo [b]thiophen-5-yl group, 2, 3-dimethylbenzo [b]thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-lH- indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-1H- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol]-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-lH-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-lH-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolot2, 3-b] pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

(65-3) The compound or salt thereof according to (1) mentioned above, wherein, in the formula (I), Link is- (CH2) n-, n is an integer of 2, C3 is carbon atom to which AR binds, C4 is carbon atom to which Rs binds, C5 is nitrogen atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-N (Ry) (Rz), and the group represented by-N (Ry) (Rz) is N, N- dimethylamino group, N-ethyl-N-methylamino group, N, N-diethylamino group, N- methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N- methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N- butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N- (2- ethylbutyl) amino group, N- (2-ethylbutyl)-N-methylamino group, N- cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N- (cyclopentylmethyl) amino group, N- (cyclopentylmethyl)-N-methylamino group, N- (cyclohexylmethyl) amino group, N- (cyclohexylmethyl)-N-methylamino group, N- (2- methylphenyl) amino group, N- (4-methylphenyl) amino group, N- (2- fluorophenyl) amino group, N' (3'fluorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (2-chlorophenyl) amino group, N- (3-chlorophenyl) amino group, N- (4- chlorophenyl) amino group, N- (indan-2-yl) amino group, N- (1-phenylethyl) amino group, N- [1- (2-fluorophenyl) ethyl] amino group, N- [1- (3-fluorophenyl) ethyl] amino group, N- [1- (4-fluorophenyl) ethyl] amino group, N- [l- (2-chlorophenyl) ethyl] amino group, N-[1-(3-chlorophenyl) ethyl] amino group, N- [1- (4-chlorophenyl) ethyl] amino group, N- (2-methylphenylmethyl) amino group, N-methyl-N- (2- methylphenylmethyl)amino group, N-(3-methylphenylmethyl)amino group, N- methyl-N- (3-methylphenylmethyl) amino group, N- (4-methylphenylmethyl) amino group, N-methyl-N- (4-methylphenylmethyl) amino group, N- (2- fluorophenylmethyl) amino group, N- (2-fluorophenylmethyl)-N-methylamino group, N- (3-fluorophenylmethyl) amino group, N- (3-fluorophenylmethyl)-N-methylamino group, N- (4-fluorophenylmethyl) amino group, N- (4-fluorophenylmethyl)-N- methylamino group, N- (2-chlorophenylmethyl) amino group, N- (2- chlorophenylmethyl)-N-methylamino group, N- (3-chlorophenylmethyl) amino group, N- (3-chlorophenylmethyl) -N-methylamino group, N- (4-chlorophenylmethyl) amino group, N- (4-chlorophenylmethyl)-N-methylamino group, N- (2, 3- difluorophenylmethyl) amino group, N- (2, 3-difluorophenylmethyl)-N-methylamino group, N- (2, 4-difluorophenylmethyl) amino group, N- (2, 4-difluorophenylmethyl)-N- methylamino group, N- (2, 5-difluorophenylmethyl) amino group, N- (2, 5- difluorophenylmethyl)-N-methylamino group, N- (3, 4-difluorophenylmethyl) amino group, N- (3, 4-difluorophenylmethyl)-N-methylamino group, N- (3, 5- difluorophenylmethyl) amino group, N- (3, 5-difluorophenylmethyl)-N-methylamino group, N- (2,3-dichlorophenylmethyl) amino group, N- (2,3-dichlorophenylmethyl)-N- methylamino group, N- (2, 4-dichlorophenylmethyl) amino group, N- (2, 4- dichlorophenylmethyl)-N-methylamino group, N- (2, 5-dichlorophenylmethyl) amino group, N- (2, 5-dichlorophenylmethyl)-N-methylamino group, N- (2, 6- dichlorophenylmethyl) amino group, N- (2, 6-dichlorophenylmethyl)-N-methylamino group, N-(3,4-dichlorophenylmethyl)amino group, N- (3, 4-dichlorophenylmethyl) -N- methylamino group, N- (3, 5-dichlorophenylmethyl) amino group, N- (3, 5- dichlorophenylmethyl)-N-methylamino group, N- [2- (trifluoromethyl) phenylmethyl] amino group, N-methyl-N- [2- (trifluoromethyl) phenylmethyl] amino group, N- [3- (trifluoromethyl) phenylmethyl] amino group, N-methyl-N- [3- (trifluoromethyl) phenylmethyl] amino group, N- [4- (trifluoromethyl) phenylmethyl] amino group, N-methyl-N- [4- (trifluoromethyl) phenylmethyl] amino group, 1-pyrrolidino group, 1- (4- methylpiperidino) group, 1-homopiperidino group, or 4-morpholino group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2,3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-1H-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-lH- indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-l-propyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-1H- indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethy)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

(66) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (1), n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is carbon atom substituted with- N (Rnl) (Rn2) (provided that one of Rnl and Rn2 is a substituent other than hydrogen atom), C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-O-Rx, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(67) The compound or salt thereof according to (4) mentioned above, wherein, in the formula (I), Link is- (CH2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is carbon atom substituted with -N (Rnl) (Rn2) (provided that one of Rnl and Rn2 is a substituent other than hydrogen atom), C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is- O-Rx, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(68) The compound or salt thereof according to (5) mentioned above, wherein, in the formula (I), Link is- (CH2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is carbon atom substituted with -N (Rnl) (Rn2) (provided that one of Rnl and Rn2 is a substituent other than hydrogen atom), C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is- O-Rx, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(69) The compound or salt thereof according to any one of (66) to (68) mentioned above, wherein, in the formula (I), Xa which may substitute on AR is methyl group, ethyl group, propyl group, hydroxyethyl group, carboxymethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, methylamino group, dimethylamino group, carboxyl group, carbamoyl group, acetyl group, methanesulfonyl group, sulfamoyl group, or N, N-dimethylsulfamoyl group.

(70) The compound or salt thereof according to any one of (66) to (69) mentioned above, wherein, in the formula (I), Rs is'O'Rx, Rx is a group selected from butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, and cyclohexylmethyl group, or Rb (provided that Q in Rb is phenyl group or indan-2-yl group), Al is a single bond, or methylene group substituted with methyl group or ethyl group or unsubstituted methylene group, or ethylene group substituted with methyl group or ethyl group or unsubstituted ethylene group, A2 represents a single bond, oxygen atom, sulfur atom,-N (methyl) -, or-N (ethyl) - (provided that when A2 is oxygen atom, sulfur atom, - N (methyl) -, or-N (ethyl)-, Al is ethylene), and R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, or dimethylamino group (provided that when Q is phenyl group, A is a single bond or unsubstituted methylene, and A2 is a single bond, one of R2 and R3 is a substituent other than hydrogen atom).

(71) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 2, C3 is carbon atom to which AR binds, C4 is carbon atom to which Rs binds, C5 is carbon atom substituted with Zx, C2 and C6 are unsubstituted ring- constituting carbon atoms, Zx is N-methylamino group, N-ethylamino group, N-propylamino group, N- isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, or N, N-dimethylsulfamoylamino group, Rs is'O'Rx, Rx is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1-(4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4- dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, or 2- (N-ethyl-N-phenylamino) ethyl group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6-(N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6-(2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3- dimethyl-lH-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1, 2-dimethyl-1H-indol- 5-yl group, 1, 3-dimethyl-1H-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-lH-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-1H- indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-1H- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-lH-indazol-5- yl group, imidazo [1, 2-a]pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolol2, 3-b] pyridin-5-yl group, l-ethyl-lH-pyrrolol2, 3-b] pyridin-5-yl group, l-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-1H- pyrrolo [2, 3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

(72) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is a ring-constituting carbon atom substituted with Zx, or an unsubstituted ring-constituting carbon atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-D-Rc, D is oxygen atom or sulfur atom, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(73) The compound or salt thereof according to (4) mentioned above, wherein, in the formula (I), Link is- H2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is a ring-constituting carbon atom substituted with Zx, or an unsubstituted ring-constituting carbon atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-O-Rc, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(74) The compound or salt thereof according to (5) mentioned above, wherein, in the formula (I), Link is- H2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is a ring-constituting carbon atom substituted with Zx, or an unsubstituted ring-constituting carbon atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-O-Rc, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(75) The compound or salt thereof according to any one of (72) to (74) mentioned above, wherein, in the formula (I), Xa which may substitute on AR is methyl group, ethyl group, propyl group, hydroxyethyl group, carboxymethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, methylamino group, dimethylamino group, carboxyl group, carbamoyl group, acetyl group, methanesulfonyl group, sulfamoyl group, or N, N-dimethylsulfamoyl group.

(76) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 1 to 3, C3 is carbon atom to which AR binds, C4 is carbon atom to which Rs binds, C5 may be replaced with V, C2 and C6 are unsubstituted ring-constituting carbon atoms, V is nitrogen atom, or carbon atom substituted with Zx, Zx is fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, or N, N-dimethylsulfamoylamino group, Rs is-D-Rc, D is oxygen atom or sulfur atom, p in Rc is an integer of 2 or 3, A4 is a single bond or methylene, A5 is-C (O)-,-C (S) -, or-S (0) 2-, Rd is hydrogen atom, or methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4- chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin- 3-yl group, or pyridin-4-yl group, Re is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t- butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4- methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N- isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- 4-methylphenyl) amino group, N- (4- chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2- yl) amino group, N- (furan-3-yl) amino group, N- (thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, or ethyloxycarbonylamino group, AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4- yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro- lH-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, lH-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [c]isothiazol-4-yl group, benzo [c]isothiazol-6-yl group, benzo [c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, 1H-pyrrolo [2,3- b]pyridin-5-yl group, 1H-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H- isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H- benzimidazol-5-yl group, lH-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H- pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, 1H- benzotriazol-5-yl group, lH-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2, 3- b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1, 3- dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H- benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5- yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3,2- c] pyridin-6-yl group, lH-pyrrolo [3, 2-c] pyridin-4-yl group, 1H-pyrrolo [2, 3-c] pyridin- 5-yl group, 1H-pyrrolo [2, 3-c] pyridin-4-yl group, 1H-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazolo [4, 3-b] pyridin-6-yl group, lH-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-c] pyridin-5-yl group, 1H- pyrazolo [3, 4-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H- pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-e] pyridin-2-yl group, thieno [3,2- c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b] pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3,2- b] pyridin-6-yl group, 1H-thieno [3, 2-c] pyrazol-5-yl group, lH-thieno [3, 2-c] pyrazol-4- yl group, benzo [d] isoxazol-5-yl group, benzo [d] isoxazol-4-yl group, benzo [d] isoxazol- 6-yl group, benzo [d] isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c]isoxazol-4-yl group, benzo [c]isoxazol-6-yl group, benzo [c] isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5- yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3,4- d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2, 4] triazolo [1, 5-a] pyrimidin-6-yl group, lH-pyrazolo [3, 4-b] pyrazin-5-yl group, lH-imidazo [4, 5-b] pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa), Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2- hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N- dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2- aminoacetylamino group, methylsulfonylamino group, (N, N- dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N- methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N, N-dimethylcarbamoyl group, and Y is hydrogen atom, methyl group, or ethyl group.

(77) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 2, C3 is carbon atom to which AR binds, C4 is carbon atom to which Rs binds, C5 may be replaced with V, C2 and C6 are unsubstituted ring-constituting carbon atoms, V is nitrogen atom, or carbon atom substituted with Zx, Zx is fluorine atom, chlorine atom, bromine atom, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N- isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, or N, N-dimethylsulfamoylamino group, Rs is-O-Rc, p in Rc is an integer of 2, A4 is a single bond or methylene, A5 is-C (O)-,-C (S) -, or-S (0) 2-, Rd is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, or 4-fluorophenylmethyl group, Re is isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t- butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4- methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, N- propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4-chlorophenyl) amino group, N- (4-fluorophenyl) amino group, pyrrolidino group, piperidino group, or morpholino group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2,3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-1H-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H- indol-5-yl group, 2-methyl-1-propyl-lH-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1propyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-1H- indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-1H-pyrrolo [2, 3-b]pyridin-5-yl group, 1- (2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

(78) The compound or salt thereof according to (7) mentioned above, wherein, in the formula (I), Link is- (CH2) n-, n is an integer of 2, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is a ring-constituting carbon atom substituted with Zx, or an unsubstituted ring-constituting carbon atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-O-Rx, and Y is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

(79) The compound or salt thereof according to (78) mentioned above, wherein, in the formula (1), Xa which may substitute on AR is methyl group, ethyl group, propyl group, hydroxyethyl group, carboxymethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, methylamino group, dimethylamino group, carboxyl group, carbamoyl group, acetyl group, methanesulfonyl group, sulfamoyl group, or N, N-dimethylsulfamoyl group.

(80) The compound or salt thereof according to (78) or (79) mentioned above, wherein, in the formula (I), Rs is-O-Rx, Rx is butyl group, isobutyl group, 2- ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, or cyclohexylmethyl group, or Rb (provided that Q in Rb is phenyl group or indan-2-yl group), Al is a single bond, or methylene group substituted with methyl group or ethyl group or unsubstituted methylene group, or ethylene group substituted with methyl group or ethyl group or unsubstituted ethylene group, A2 is a single bond, oxygen atom, sulfur atom,-N (methyl)-, or- N (ethyl)- (provided that when A2 is oxygen atom, sulfur atom,-N (methyl)-, or- N (ethyl)-, Al is ethylene), and R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, or dimethylamino group (provided that when Q is phenyl group, Al is a single bond or unsubstituted methylene, and A2 is a single bond, one of R2 and R3 is a substituent other than hydrogen atom).

(81) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 1 to 3, C3 is carbon atom to which AR binds, C4 is carbon atom to which Rs binds, C5 may be replaced with V, C2 and C6 are unsubstituted ring-constituting carbon atoms, V is nitrogen atom, or carbon atom substituted with Zx, Zx is fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, or N, N-dimethylsulfamoylamino group, Rs is-O-Rx, Rx is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-cyclopentylethyl group, or 2-cyclohexylethyl group, or Rb or Rc, Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group, A2 is a single bond, oxygen atom, sulfur atom,- N (methyl) -, or-N (ethyl) - (provided that when A2 is oxygen atom, sulfur atom,- N (methyl)-, or-N (ethyl)-, Al is ethylene), R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q is phenyl group, Al is a single bond or unsubstituted methylene, and A2 is a single bond, one of R2 and R3 is a substituent other than hydrogen atom), p in Rc is an integer of 2 or 3, A4 is a single bond or methylene, A5 is-C (O)-,-C (S) -, or'8 (0) 2-, Rd is hydrogen atom, or methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4- chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, or pyridin-4-yl group, Re is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen- 2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4- methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N- isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4- chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2- yl) amino group, N- (furan-3-yl) amino group, N- (thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, or ethyloxycarbonylamino group, AR is cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, lH-benzimidazol-5-yl group, lH-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3,2- b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, lH-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1,3- dihydropyrrolo [2, 3-b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1, 3-dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro- 3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H- benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3,2- c] pyridin-6-yl group, 1H-pyrrolo [3, 2-c] pyridin-4-yl group, lH-pyrrolo [2, 3-c] pyridin- 5-yl group, lH-pyrrolo [2, 3-c]pyridin-4-yl group, 1H-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazolo [4, 3-b] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-c] pyridin-5-yl group, 1H- pyrazolo [3, 4-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H- pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2- c] pyridin-3-yl group, thieno [3, 2-c]pyridin-6-yl group, thieno [3, 2-b]pyridin-2-yl group, thieno [3, 2-b]pyridin-3-yl group, thieno [3, 2-b]pyridin-5-yl group, thieno [3,2- b] pyridin-6-yl group, 1H-thieno [3, 2-c] pyrazol-5-yl group, 1H-thieno [3, 2-c]pyrazol-4- yl group, benzo [d] isoxazol-5-yl group, benzo [d] isoxazol-4-yl group, benzo [d]isoxazol- 6-yl group, benzo [d]isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c]isoxazol-6-yl group, benzo [c] isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5- yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, lH-pyrazolo [3,4- d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazololl, 5-a] pyrimidin-6-yl group, 1H-pyrazolo [3, 4-b] pyrazin-5-yl group, 1H-imidazo [4, 5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa), Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2- hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N- dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2- aminoacetylamino group, methylsulfonylamino group, (N, N- dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N- methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N, N-dimethylcarbamoyl group, and Y is hydrogen atom, methyl group, or ethyl group.

(82) The compound or salt thereof according to (6) mentioned above, wherein, in the formula (I), Link is- H2) n-, AR binds to C3 in the aromatic ring (E), Rs binds to C4 in the aromatic ring (E), C5 is a ring-constituting carbon atom substituted with Zx, or an unsubstituted ring-constituting carbon atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Rs is-O-Rx, and Rx is a linear or branched saturated alkyl group having 3 to 8 carbon atoms, or Ra or Rb.

(83) The compound or salt thereof according to (82) mentioned above, wherein, in the formula (I), Zx is fluorine atom, chlorine atom, nitro group, amino group, methyl group, or OR9.

(84) The compound or salt thereof according to (1-2) mentioned above, wherein, in the formula (I), n is an integer of 1 to 3, AR binds to C3, Rs binds to one of the ring- constituting atoms C4, C5, and C6, a ring-constituting carbon atom to which Rs does not bind among C4, C5, and C6 may be replaced with V, V is nitrogen atom or carbon atom substituted with Zx, Zx is fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, or N, N-dimethylsulfamoylamino group, Rs is-D-Rx or-N (Ry) (Rz), D is oxygen atom or sulfur atom, Rx is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2- cyclopentylethyl group, or 2-cyclohexylethyl group, or Rb or Re, Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group, A2 is a single bind, oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)- (provided that when A2 is oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)-, A1 is ethylene), R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q is phenyl group, A1 is a single bind or unsubstituted methylene, and A2 is a single bind, one of R2 and R3 is a substituent other than hydrogen atom), p in Ru vis an integer of 2 or 3, A4 is a single bind or methylene, A5 is-C (O)-,-C (S) -, or-S (0) 2-, Rd is hydrogen atom, or methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, or pyridin-4-yl group, Re is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4- chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4- chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin- 3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4- methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N- isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4- chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N-(pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2- yl) amino group, N- (furan-3-yl) amino group, N-(thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group or ethyloxyearbonylamino group, Rz is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4- methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2- yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2- yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2- yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan- 2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7- dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4- chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6- dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3, 5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2-(4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyllethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2-(N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4- methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4- chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4- fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N- isobutylthiocarbamoyl group, t'butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N- cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N- cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N- cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N-phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4- methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4- chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4- fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4- fluorophenyl) thiocarbamoyl group, (pyrrolidino-l-yl) carbonyl group, (piperidino-1- yl) carbonyl group, or (morpholino-4-yl) carbonyl group, Ry is hydrogen atom, methyl group, ethyl group or isobutyl group, or binds to Rz to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol- 1-yl group, or pyrazol-1-yl group together with the nitrogen atom, AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4- yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro- 1H-quinolin-5-yl group, benzold] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, lH-indazol-5-yl group, 1H-indazol-4-yl group, lH-indazol-6-yl group, benzo [c]isothiazol-5-yl group, benzo [c]isothiazol-4-yl group, benzo [c]isothiazol-6-yl group, benzo [c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, lH-pyrrolo [2,3- b] pyridin-5-yl group, 1H-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H- isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H- benzimidazol-5-yl group, lH-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H- pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, 1H- benzotriazol-5-yl group, l H-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2,3- b]pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1,3- dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H- benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5- yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3,2- c] pyridin-6-yl group, 1H-pyrrolo [3, 2-c] pyridin-4-yl group, lH-pyrrolo [2, 3-c] pyridin- 5-yl group, 1H-pyrrolo [2, 3-c] pyridin-4-yl group, 1H-pyrazolo [4, 3-b]pyridin-5-yl group, 1H-pyrazolo [4, 3-b] pyridin-6-yl group, lH-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-c] pyridin-5-yl group, 1H- pyrazolo [3, 4-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H- pyrazolo [3, 4-b]pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a]pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3,2- c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b]pyridin-3-yl group, thieno [3, 2-b]pyridin-5-yl group, thieno [3, 2- b] pyridin-6-yl group, 1H-thieno [3, 2-c] pyrazol-5-yl group, 1H-thieno [3, 2-c] pyrazol-4- yl group, benzo [d] isoxazol-5-yl group, benzo [d] isoxazol-4-yl group, benzo [d] isoxazol- 6-yl group, benzo [d]isoxazol-7-yl group, benzo [c]isoxazol-5-yl group, benzo [c]isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5- yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3,4- d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, 1H-pyrazolo [3, 4-b] pyrazin-5-yl group, 1H-imidazo [4, 5-b] pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa), Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2- hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N- dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2- aminoacetylamino group, methylsulfonylamino group, (N, N- dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N- methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N, N-dimethylcarbamoyl group, and Y is hydrogen atom, methyl group, or ethyl group.

(85) A medicament containing a compound represented by the aforementioned formula (I) or a pharmacologically acceptable salt thereof as an active ingredient.

(86) An agent for suppressing production of a prostaglandin and/or leukotriene, which contains a compound represented by the aforementioned formula (I) or a pharmacologically acceptable salt thereof as an active ingredient.

(87) The medicament according to (85) for prophylactic and/or therapeutic treatment of a disease caused by production of a prostaglandin and/or leukotriene.

(88) The medicament according to (85) for prophylactic and/or therapeutic treatment of an inflammatory disease of a mammal.

(89) The medicament according to (85) for prophylactic and/or therapeutic treatment of an autoimmune disease of a mammal.

(90) The medicament according to (85) for prophylactic and/or therapeutic treatment of an allergic disease of a mammal.

(91) The medicament according to (85) for defervescence and/or pain relief of a mammal.

(92) A pharmaceutical composition for prophylactic and/or therapeutic treatment of a condition of living body of a mammal exhibiting an acute or chronic inflammatory reaction, which comprises a prophylactically and/or therapeutically effective amount of a compound represented by the aforementioned formula (I) or a pharmacologically acceptable salt thereof and a pharmaceutically acceptable carrier.

(93) A method for prophylactic and/or therapeutic treatment of a condition of living body of a mammal exhibiting an acute or chronic inflammatory reaction, which comprises administering a prophylactically and/or therapeutically effective amount of a compound represented by the aforementioned formula (I) or a pharmacologically acceptable salt thereof to the mammal.

(94) A compound represented by the following formula (II) : [In the formula, each of C2', C3', C4', C5', and C6'in the aromatic ring (E') represents a ring-constituting carbon atom, any one of them to which Rs'and G does not bind may be replaced with V', V'represents nitrogen atom, or carbon atom substituted with Zx', Zx'has the same meaning as Zx mentioned above, provided that when Zx contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx contains amino group, the amino group may be protected with Rp2, Rs'represents-D-Rx'or-N (Ry') (Rz'), -D-Rx'and-N (Ry') (Rz') have the same meanings as-D-Rx and-N (Ry) (Rz), respectively, provided that when-D-Rx or-N (Ry) (Rz) contains hydroxyl group, the hydroxyl group may be protected with Rpl, when-D-Rx or-N (Ry) (Rz) contains amino group, the amino group may be protected with Rp2, G represents chlorine atom, bromine atom, iodine atom, mesylate group, triflate group, or an arenesulfonate group of which aromatic portion may be substituted with one of Tl or two or more of the same or different T1, and Y'represents a lower alkyl group having 1 to 4 carbon atoms].

(95) The compound according to (94) mentioned above, wherein, in the formula (II), G binds to the ring-constituting carbon atom C2'or C3'in the aromatic ring (E').

(96) The compound according to (94) or (95) mentioned above, wherein, in the formula (II), n is an integer of 2.

(97) The compound according to any one of (94) to (96) mentioned above, wherein, in the formula (II), Rs'is-O-Rx'.

(98) The compound according to any one of (94) to (97) mentioned above, wherein, in the formula (II), Rs'is-D-Rx'or-N (Ry') (Rz'), D is a single bind, oxygen atom, sulfur atom,-S (O)-,-S (0) 2-, or-C (O)-, Rx'is a linear or branched saturated alkyl group having 3 to 8 carbon atoms, or Ra, Rb, or Rc, k in Ra is 0 or an integer of 1 to 3, Rl is a saturated cyclic alkyl group having 3 to 7 carbon atoms or a condensed saturated cyclic alkyl group having 6 to 8 carbon atoms, Rl may be substituted with one of lower alkyl group having 1 to 4 carbon atoms or two or more of the same or different lower alkyl groups having 1 to 4 carbon atoms, Q in Rb is phenyl group, thienyl group, furyl group, pyrrolyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, indazolyl group, 4H-chromenyl group, dihydrobenzodioxyl group, benzoisoxazolyl group, pyrrolopyridinyl group, pyrazolopyridinyl group, triazolopyridinyl group, thienopyridinyl group, thienopyrazolyl group, 1,3-dihydrobenzimidazole group, dihydro-3H-benzoxazole group, or dihydro-3H-benzothiazole group, which binds to A2 at an arbitrary position on the ring, Al is a single bind or an alkylene (a) having 1 to 3 carbon atoms, the alkylene (a) may be substituted with a lower alkyl group having 1 to 4 carbon atoms or phenyl group, A2 is a single bind, oxygen atom, sulfur atom, -S (O)-,-S (0) 2-, or-N (R4)- (provided that when A2 is oxygen atom, sulfur atom, -S (O)-,-S (0) 2-, or-N (R4)-, Al is ethylene or trimethylene), R2 and R3 independently represent hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms, oxo group, thioxo group, fluorine atom, chlorine atom, bromine atom, trifluoromethyl group,-OR5,-N (R6) (R6'),-NHCOR7,-NHS02R8, or-A6-Qa, or they bind to each other to form methylenedioxy group, Qa may be substituted with one of T'or two or more of the same or different T1, and is phenyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, naphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, or indazolyl group, which binds to As at an arbitrary position on the ring, R4 and R6 independently represent hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R5 and R7 independently represent hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, or-A6-Qa, R8 represents a lower alkyl group having 1 to 4 carbon atoms, R6'has the same meaning as R6, or binds to R6 to form a 3-to 6-membered ring of a cycloalkyl group or morpholino group together with the nitrogen atom to which they bind, p in Rc is an integer of 2 to 4, A4 is a single bind or methylene or ethylene, A5 is-C (O)-,-C (S)-, or-S (0) 2-, Rd is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or Qa, Re is an alkyl group having 1 to 8 carbon atoms,-A6-Qa, - (CH2) iRl4,-OR28,-SR28, or-N (R29) (R30), i is an integer of 1 to 3, Ri4 is hydroxyl group, an alkoxy group having 1 to 4 carbon atoms, carboxyl group, or an N, N- dialkylcarbamoyl group having 1 to 4 carbon atoms, R28 is an alkyl group having 1 to 8 carbon atoms or-A6-Qa, R29 is an alkyl group having 1 to 8 carbon atoms, an alkoxycarbonyl group having 1 to 4 carbon atoms, or-A6-Qa, R30 represents hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, or binds to R29 to form a 3-to 6-membered ring of nitrogen-containing cycloalkyl group or morpholino group together with the nitrogen atom to which they bind, Rz'has the same meaning as Rx', or represents-A5-Re, Ry'represents hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or-A6-Qp, or binds to Rz'to form a saturated or unsaturated nitrogen-containing cyclic substituent having 3 to 7 atoms together with the nitrogen atom to which they bind, when-D-Rx'or-N (Ry') (Rz') contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when-D-Rx'or -N (Ry') (Rz') contains amino group, the amino group may be protected with Rp2.

(99) The compound according to (94) mentioned above, wherein, in the formula (II), n is an integer of 1 to 3, G binds to C3', Rs'binds to one of the ring-constituting carbon atoms C4', C5', and C6', a ring-constituting carbon atom to which Rs'does not bind among C4', C5', and C6'may be replaced with V', V is nitrogen atom or carbon atom substituted with Zx', Zx'is fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, or N, N-dimethylsulfamoylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx' contains amino group, the amino group may be protected with Rp2, Rs'is-D-Rx'or-N (Ry') (Rz'), D is oxygen atom or sulfur atom, Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2- cyclopentylethyl group, or 2-cyclohexylethyl group, or Rb or Rc, Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group, A2 is a single bind, oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)- (provided that when A2 is oxygen atom, sulfur atom, -N (methyl) -, or-N (ethyl)-, Al is ethylene), R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q is phenyl group, Al is a single bind or unsubstituted methylene, and A2 is a single bind, one of R2 and R3 is a substituent other than hydrogen atom), p in Rc is an integer of 2 or 3, A4 is a single bind or methylene, A5 is-C (O)-,-C (S) -, or-S (0) 2-, Rd is hydrogen atom, or methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, or pyridin-4-yl group, Re is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4- chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4- chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin- 3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4- methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N- isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4- chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2- yl) amino group, N- (furan-3-yl) amino group, N- (thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group or ethyloxyearbonylamino group, Rz is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4- methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2- yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2- yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2- yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan- 2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7- dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1-(3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1-(2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4- chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3, 5- dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4- methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4- chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4- fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N- isobutylthiocarbamoyl group, t'butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N- cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N- cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N- cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N-phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4- methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4- chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4- fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4- fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-1- yl) carbonyl group, or (morpholino-4-yl) carbonyl group, Ry is hydrogen atom, methyl group, ethyl group or isobutyl group, or binds to Rz to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol- 1-yl group, or pyrazol-1-yl group together with the nitrogen atom to which they binds, provided that when-D-Rx'or-N (Ry') (Rz') contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when-D-Rx'or-N (Ry') (Rz') contains amino group, the amino group may be protected with Rp2, G is chlorine atom, bromine atom, iodine atom, or triflate group, and Y'is methyl group or ethyl group.

(100) The compound according to any one of (94) to (96) mentioned above, wherein, in the formula (II), Rs'is-N (Ry') (Rz').

(101) The compound according to any one of (94) to (96) mentioned above, wherein, in the formula (II), Rs'is-D-Rx', and D is sulfur atom,-S (O)-,-S (0) 2- or-C (O) -.

(102) The compound according to (94) mentioned above, wherein, in the formula (II), G binds at the position of C2'in the aromatic ring (E'), Rs'binds to one of the ring- constituting carbon atoms C3', C4'and C5', and all of C2', C3', C4', C5'and C6'in the aromatic ring (E') are not replaced with V'.

(103) The compound according to (94) mentioned above, wherein, in the formula (II), n is an integer of 1 to 3, G binds to C2', Rs'binds to one of the ring-constituting carbon atoms C4', C5', and C6', a ring-constituting carbon atom to which Rs'does not bind among C3', C4', and C5'may be replaced with V', V'is nitrogen atom, or carbon atom substituted with Zx', Zx'is fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N- propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N- diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, or N, N-dimethylsulfamoylamino group, provided that when Zx' contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx'contains amino group, the amino group may be protected with Rp2, Rs'is-D-Rx'or-N (Ry') (Rz'), D is oxygen atom or sulfur atom, Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2- cyclopentylethyl group, 2-cyclohexylethyl group, or Rb or Rc, Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group, A2 is a single bind, oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)- (provided that when A2 is oxygen atom, sulfur atom, -N (methyl) -, or-N (ethyl)-, Al is ethylene), R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q is phenyl group, Al is a single bind or unsubstituted methylene, and A2 is a single bind, one of R2 and R3 is a substituent other than hydrogen atom), p in Rc is an integer of 2 or 3, A4 is a single bind or methylene, A5 is-C (O)-,-C (S) -, or-S (0) 2-, Rd is hydrogen atom, or methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, or pyridin-4-yl group, Re is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4- chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4- chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin- 3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4- methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N- isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4- chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N-(pyridin-2-yl) amino group, N-(pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2- yl) amino group, N- (furan-3-yl) amino group, N- (thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, or ethyloxycarbonylamino group, Rz is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4- methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4'chlorophenyl group, indan-2- yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2- yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2- yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5,6-dichloroindan- 2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7- dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4- chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2-13- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorop henyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4- methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4- chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4- fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N- isobutylthiocarbamoyl group, t-butyloxycarbonyl group, N-t-butylearbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N- cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N- cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N- cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N-phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4- methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4- chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4- fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4- fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-1- yl) carbonyl group, or (morpholino-4-yl) carbonyl group, Ry is hydrogen atom, methyl group, ethyl group or isobutyl group, or binds to Rz to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol- 1-yl group, or pyrazol-1-yl group together with the nitrogen atom, provided that when-D-Rx'or-N (Ry') (Rz') contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when-D-Rx'or-N (Ry') (Rz') contains amino group, the amino group may be protected with Rp2, G is chlorine atom, bromine atom, iodine atom, or triflate group, and Y'is methyl group or ethyl group.

(104) The compound according to (102) or (103) mentioned above, wherein, in the formula (II), n is an integer of 2, Rs'binds to C3'in the aromatic ring (E'), Rs'is-O- Rx', and Y'is methyl group or ethyl group.

(105) The compound according to (94) mentioned above, wherein, in the formula (II), n is an integer of 2, C22 is a ring-constituting carbon atom to which G binds, C3'is a ring- constituting carbon atom to which Rs'binds, C4'may be replaced with V', C5'and C6' are unsubstituted ring-constituting carbon atoms, V'is nitrogen atom, or carbon atom substituted with Zx', Zx'is fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, or N, N- dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx'contains amino group, the amino group may be protected with Rp2, Rs'is-O-Rx', Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, l- (3-fluorophenyl) ethyl group, 1-(4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2, 6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3, 5- dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4'fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorop henyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, or 2- (N-ethyl-N-phenylamino) ethyl group, G is bromine atom or iodine atom, and Y'is methyl group or ethyl group.

(106) The compound according to (102) or (103) mentioned above, wherein, in the formula (II), n is an integer of 2, Rs'binds at the position of C4'in the aromatic ring (E'), Rs'is-O-Rx', and Y'is methyl group or ethyl group.

(107) The compound according to (94) mentioned above, wherein, in the formula (II), n is an integer of 2, C2'is a ring-constituting carbon atom to which G binds, C4'is a ring- constituting carbon atom to which Rs'binds, C5'may be replaced with V', C3'and C6' are unsubstituted ring-constituting carbon atoms, V'is nitrogen atom, or carbon atom substituted with Zx', Zx'is fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, or N, N- dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx'contains amino group, the amino group may be protected with Rp2, < Rs'is-O-Rx', Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1- (2-fluorophenyl) ethyl group, l- (3'fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3,5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2-(N-phenyl-N-methylamino) ethyl group, or 2-(N-ethyl-N-phenylamino) ethyl group, G is bromine atom or iodine atom, and Y'is methyl group or ethyl group.

(108) The compound according to (102) or (103) mentioned above, wherein, in the formula (II), n is an integer of 2, Rs'binds at the position of C5'in the aromatic ring (E'), Rs'is-O-Rx', and Y'is methyl group or ethyl group.

(109) The compound according to (94) mentioned above, wherein, in the formula (II), G binds to C3'in the aromatic ring (E'), Rs'binds to C5'or C6'in the aromatic ring (E'), and all of C2', C3', C4', C5'and Cs'in the aromatic ring (E') are not replaced with V'.

(110) The compound according to (109) mentioned above, wherein, in the formula (II), n is an integer of 2, Rs'binds to C5'in the aromatic ring (E'), and Rs'is-0-Rx'.

(111) The compound according to (94) mentioned above, wherein, in the formula (II), n is an integer of 2, C3'iS carbon atom to which G binds, C5'iS carbon atom to which Rs'binds, C2', C4', and C6'are unsubstituted ring-constituting carbon atoms, Rs'is-O-Rx', Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, l- (3'fluorophenyl) ethyl group, l' (4'fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4- dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group or 2- (N-ethyl-N-phenylamino) ethyl group, G is bromine atom or iodine atom, and Y'is methyl group or ethyl group.

(112) The compound according to (109) mentioned above, wherein, in the formula (II), n is an integer of 2, Rs'binds to C6'in the aromatic ring (E'), and Rs'is-O-Rx'.

(113) The compound according to (94) mentioned above, wherein, in the formula (II), G binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), and C6'is V.

(114) The compound according to (113) mentioned above, wherein, in the formula (II), n is an integer of 2, V'is carbon atom substituted with Zx', and Rs'is-O-Rx' (115) The compound according to (94) mentioned above, wherein, in the formula (II), n is an integer of 2, C3'is carbon atom to which G binds, C4'is a carbon atom to which Rs'binds, C6 is carbon atom substituted with Zx', C2 and C5'are unsubstituted ring- constituting carbon atoms, Zx'is fluorine atom, methyl group, hydroxyl group, amino group, N- methylamino group, or N, N-dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx' contains amino group, the amino group may be protected with Rp2, Rs'is-O-Rx', Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, l' (3'chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl ! ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2-(N-phenyl-N-methylamino) ethyl group, or 2-(N-ethyl-N-phenylamino) ethyl group, G is bromine atom or iodine atom, and Y'is methyl group or ethyl group.

(116) The compound according to (94) mentioned above, wherein, in the formula (II), G binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5' is nitrogen atom, and C2'and C6'are unsubstituted ring-constituting carbon atoms.

(117) The compound according to (116) mentioned above, wherein, in the formula (II), n is an integer of 2, and Rs'is-O-Rx'.

(118) The compound according to (94) mentioned above, wherein, in the formula (II), n is an integer of 2, C3'is carbon atom to which G binds, C4'iS carbon atom to which Rs'binds, C5'is nitrogen atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, Rs'is-O-Rx', Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2-(2-fluorophenyl) ethyl group, 2-(3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, or 2- (N-ethyl-N-phenylamino) ethyl group, G is bromine atom or iodine atom, and Y'is methyl group or ethyl group.

(119) The compound according to (94) mentioned above, wherein, in the formula (II), G binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5' is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring- constituting carbon atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, Rs'is-D-Rx', and D is a single bind, sulfur atom,-S (O) -,-S (0) 2-, or-C (O)-.

(120) The compound according to (94) mentioned above, wherein, in the formula (II), n is an integer of 2, C3'iS carbon atom to which G binds, C4'is a carbon atom to which Rs'binds, C5'is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2 and C6 are unsubstituted ring-constituting carbon atoms, Zx'is fluorine atom, methyl group, hydroxyl group, amino group, N- methylamino group, or N, N-dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx' contains amino group, the amino group may be protected with Rp2, Rs'is-S-Rx', Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl ethyl group, 2- [4- (trifluoromethyl) phenyl) ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, or 2- (N-ethyl-N-phenylamino) ethyl group, G is bromine atom or iodine atom, and Y'is methyl group or ethyl group.

(121) The compound according to (94) mentioned above, wherein, in the formula (II), G binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5' is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring- constituting carbon atom, C2 and C6'are unsubstituted ring-constituting carbon atoms, and Rs'is-N (Ry') (Rz').

(122) The compound according to (94) mentioned above, wherein, in the formula (II), n is an integer of 2, C3'is carbon atom to which G binds, C4'is a carbon atom to which Rs'binds, C5'is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, Zx'is fluorine atom, methyl group, hydroxyl group, amino group, N- methylamino group, or N, N-dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx' contains amino group, the amino group may be protected with Rp2, Rs'is-N (Ry') (Rz'), Rz'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4'fluorophenylmethyl group, 2'chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorop henyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4- methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4- chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4- fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N- isobutylthiocarbamoyl group, t-butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N- cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N- cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N- cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N'phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4- methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4- chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4- fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4- fluorophenyl) thiocarbamoyl group, (pyrrolidino-l-yl) carbonyl group, (piperidino-l- yl) carbonyl group, or (morpholino-4-yl) carbonyl group, Ry'is hydrogen atom, methyl group, ethyl group or isobutyl group, or binds to Rz'to form pyrrolidino group, piperidino group, or morpholino group together with nitrogen atom to which they binds, provided that when-N (Ry') (Rz') contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when-N (Ry') (Rz') contains amino group, the amino group may be protected with Rp2, G is bromine atom or iodine atom, and Y'is methyl group or ethyl group.

(123) The compound according to (94) mentioned above, wherein, in the formula (II), n is an integer of 2, G binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'iS carbon atom substituted with-N (Rnl) (Rn2) group (provided that one of Rnl and Rn2 is a substituent other than hydrogen atom), C2'and C6'are unsubstituted ring-constituting carbon atoms, and Rs'is-O-Rx'.

(124) The compound according to (94) mentioned above, wherein, in the formula (II), n is an integer of 2, C3'iS carbon atom to which G binds, C4'iS carbon atom to which Rs'binds, C5'is carbon atom substituted with Zx', C2'and c6 are unsubstituted ring- constituting carbon atoms, Zx'is N-methylamino group, N-ethylamino group, N-propylamino group, N- isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, or N, N-dimethylsulfamoylamino group, provided that when Zx'contains amino group, the amino group may be protected with Rp2, Rs'is-O-Rx', Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, l' (4'fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2-(N-phenyl-N-methylamino) ethyl group, or 2-(N-ethyl-N-phenylamino) ethyl group, G is bromine atom or iodine atom, and Y'is methyl group or ethyl group.

(125) The compound according to (94) mentioned above, wherein, in the formula (II), G binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5' is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring- constituting carbon atom, C2'and and C6 are unsubstituted ring-constituting carbon atoms, Rs'is-D-Rx', and Rx'has the same meaning as Rc, provided that when Rc contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Rc contains amino group, the amino group may be protected with Rp2.

(126) The compound according to (94) mentioned above, wherein, in the formula (II), n is an integer of 2, C3'iS carbon atom to which G binds, C4'is a carbon atom to which Rs'binds, C5'is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, Zx'is fluorine atom, methyl group, hydroxyl group, amino group, N- methylamino group, or N, N-dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx' contains amino group, the amino group may be protected with Rp2, Rs'is-O-Rx', Rx'has the same meaning as Rc, provided that when Rc contains hydroxyl group, the hydroxyl group may be protected with Rpl, p in Rc is an integer of 2, A4 is a single bind or methylene, A5 is-C (O)-,-C (S) -, or-S (0) 2-, Rd is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, phenyl group, 4- methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4- chlorophenylmethyl group, or 4-fluorophenylmethyl group, Re is isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4- methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, N- propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N' (4'methylphenyl) amino group, N' (4'chlorophenyl) amino group, N- (4-fluorophenyl) amino group, pyrrolidino group, piperidino group, or morpholino group, G is bromine atom or iodine atom, and Y'is methyl group or ethyl group.

(127) The compound according to (94) mentioned above, wherein, in the formula (II), G binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5' is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring- constituting carbon atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, Rs'is-O-Rx', and Rx'is a linear or branched saturated alkyl group having 3 to 8 carbon atoms, or Ra or Rb.

(128) The compound according to (94) mentioned above, wherein, in the formula (II), n is an integer of 2, G binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is carbon atom substituted with nitro group, C2'and C6'are unsubstituted ring-constituting carbon atoms, and Rs'is-O-Rx'.

(129) A compound represented by the following formula (III) : [In the formula, C2', C3', C4', C5'and C6'in the aromatic ring (E') represent a ring- constituting carbon atom, any one of these atoms to which Rs'and AR'does not bind may be replaced with V', and AR'has the same meaning as that of AR, provided that when AR contains hydroxyl group, the hydroxyl group may be protected with Rp1, and when AR contains amino group, the amino group may be protected with Rp2.].

(130) The compound according to (129) mentioned above, wherein, in the formula (III), AR'binds to the atom of C2'or C3'in the aromatic ring (E').

(131) The compound according to (129) or (130) mentioned above, wherein, in the formula (III), AR'is a residue of naphthalene, benzofuran, benzo [b] thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-lH-quinoline, benzo [d] isothiazole, IH-indazole, benzo [c] isothiazole, 2H-indazole, imidazo [1, 2- a] pyridine, lH-pyrrolo [2, 3-b] pyridine, isoquinoline, dihydro-2H-isoquinoline, cinnoline, quinazoline, quinoxaline, 1H-benzimidazole, benzoxazole, lH-pyrrolo [3, 2- bjpyridine, benzo [1, 2,5] thiadiazole, 1H-benzotriazole, 1, 3-dihydropyrrolo [2,3- b] pyridine, 1, 3-dihydrobenzimidazole, dihydro-3H-benzoxazole, phthalazine, [1, 8] naphthalidine, [1, 5] naphthalidine, 1H-pyrrolo [3, 2-c] pyridine, lH-pyrrolo [2,3- c] pyridine, lH-pyrazolo [4, 3-b]pyridine, 1H-pyrazolo [4, 3-c]pyridine, 1H-pyrazolo [3,4- c] pyridine, lH-pyrazolo [3, 4-b] pyridine, [1, 2,4] triazolo [4, 3-a] pyridine, thieno [3,2- c] pyridine, thieno [3, 2-b]pyridine, 1H-thieno [3, 2-c] pyrazole, benzo [d] isoxazole, benzo [c] isoxazole, indolizine, 1,3-dihydroindole, lH-pyrazolo [3, 4-d] thiazole, 2H- isoindole, [1, 2,4] triazolo [1, 5-a]pyrimidine, 1H-pyrazolo [3, 4-b]pyrazine, 1H- imidazo [4, 5-b] pyrazine, 7H-purine, or 4H-chromene (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa, when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when AR'contains amino group, the amino group may be protected with Rp2).

(132) The compound according to (129) or (130) mentioned above, wherein, in the formula (III), AR'is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4- yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro- lH-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, 1H-indazol-5-yl group, lH-indazol-4-yl group, 1H-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [c] isothiazol-4-yl group, benzo [c] isothiazol-6-yl group, benzo [c] isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo [l, 2-a] pyridin-7-yl group, 1H-pyrrolo [2,3- b]pyridin-5-yl group, 1H-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H- isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H- benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H- pyrrolo [3, 2-b]pyridin-5-yl group, 1H-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, 1H- benzotriazol-5-yl group, lH-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2,3- b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1,3- dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H- benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5- yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3,2- c] pyridin-6-yl group, lH-pyrrolo [3, 2-c] pyridin-4-yl group, lH-pyrrolo [2, 3-c] pyridin- 5-yl group, 1H-pyrrolo [2, 3-c] pyridin-4-yl group, 1H-pyrazolo [4 ; 3-b] pyridin-5-yl group, lH-pyrazolo [4, 3-b] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-4-yl group, lH-pyrazolo [3, 4-c] pyridin-5-yl group, 1H- pyrazolo [3, 4-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H- pyrazolo [3, 4-b]pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c]pyridin-2-yl group, thieno [3,2- c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b]pyridin-2-yl group, thieno [3, 2-b] pyridin-3-yl group, thieno [3, 2-blpyridin-5-yl group, thieno [3,2- b] pyridin-6-yl group, lH-thieno [3, 2-c] pyrazol-5-yl group, lH-thieno [3, 2-c] pyrazol-4- yl group, benzo [d] isoxazol-5-yl group, benzo [d]isoxazol-4-yl group, benzo [d] isoxazol- 6-yl group, benzo [d]isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c]isoxazol-6-yl group, benzo [c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5- yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3,4- d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, 1H-pyrazolo [3, 4-b] pyrazin-5-yl group, 1H-imidazo [4, 5-b] pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa, when AR'contains hydroxyl group, the hydroxyl group may be protected with Rp, and whenAR'contains amino group, the amino group may be protected with Rp2).

(133) The compound according to (129) or (130) mentioned above, wherein, in the formula (III), AR'is a residue of naphthalene, benzofuran, benzo [b] thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-lH-quinoline, benzo [d] isothiazole, 1H-indazole, benzo [c] isothiazole, 2H-indazole, imidazol, 2- a] pyridine, lH-pyrrolo [2, 3-b] pyridine, isoquinoline, or dihydro-2H-isoquinoline (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa, when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and whenAR'contains amino group, the amino group may be protected with Rp2).

(134) The compound according to (129) or (130) mentioned above, wherein, in the formula (III), AR'is a residue of cinnoline, quinazoline, quinoxaline, 1H- benzimidazole, benzoxazole, lH-pyrrolo [3, 2-b] pyridine, benzo [1, 2,5] thiadiazole, 1H- benzotriazole, 1, 3-dihydropyrrolo [2, 3-b] pyridine, 1, 3-dihydrobenzimidazole, dihydro-3H-benzoxazole, phthalazine, [1, 8] naphthalidine, [1,5]naphthalidine, 1H- pyrrolo [3, 2-c]pyridine, 1H-pyrrolo [2, 3-c]pyridine, 1H-pyrazolo [4, 3-b] pyridine, 1H- pyrazolo [4, 3-c] pyridine, lH-pyrazolo [3, 4-c] pyridine, lH-pyrazolo [3, 4-b] pyridine, [1, 2,4] triazolo [4, 3-a] pyridine, thieno [3, 2-c] pyridine, thieno [3, 2-b] pyridine, 1H- thieno [3, 2-c] pyrazole, benzo [d] isoxazole, benzo [c] isoxazole, indolizine, 1,3- dihydroindole, 1H-pyrazolo [3, 4-d] thiazole, 2H-isoindole, [1, 2,4] triazolo[1, 5- a] pyrimidine, lH-pyrazolo [3, 4-b] pyrazine, lH-imidazo [4, 5-b] pyrazine, 7H-purine, or 4H-chromene (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa, when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when AR'contains amino group, the amino group may be protected with Rp2).

(135) The compound according to any one of (129) to (134) mentioned above, wherein, in the formula (III), Rs'is-O-Rx'.

(136) The compound according to any one of (129) to (135) mentioned above, wherein, in the formula (III), Rs'is-D-Rx'or-N (Ry') (Rz'), D is a single bind, oxygen atom, sulfur atom,-S (O)-,-S (0) 2-, or-C (O)-, Rx'is a linear or branched saturated alkyl group having 3 to 8 carbon atoms, or Ra, Rb, or Rc, k in Ra is 0 or an integer of 1 to 3, Rl is a saturated cyclic alkyl group having 3 to 7 carbon atoms or a condensed saturated cyclic alkyl group having 6 to 8 carbon atoms, Ri may be substituted with one of lower alkyl group having 1 to 4 carbon atoms or two or more of the same or different lower alkyl groups having 1 to 4 carbon atoms, Q in Rb is phenyl group, thienyl group, furyl group, pyrrolyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, indazolyl group, 4H-chromenyl group, dihydrobenzodioxyl group, benzoisoxazolyl group, pyrrolopyridinyl group, pyrazolopyridinyl group, triazolopyridinyl group, thienopyridinyl group, thienopyrazolyl group, 1, 3-dihydrobenzimidazole group, dihydro-3H-benzoxazole group, or dihydro-3H-benzothiazole group, which binds to A2 at an arbitrary position on the ring, Al is a single bind or an alkylene (a) having 1 to 3 carbon atoms, the alkylene (a) may be substituted with a lower alkyl group having 1 to 4 carbon atoms or phenyl group may be substituted with, A2 is a single bind, oxygen atom, sulfur atom,-S (O)-,-S (0) 2-, or-N (R4)- (provided that when A2 is oxygen atom, sulfur atom, -S (O)-,-S (O) 2-, or-N (R4)-, Al is ethylene or trimethylene), R2 and R3 independently represent hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms, oxo group, thioxo group, fluorine atom, chlorine atom, bromine atom, trifluoromethyl group,-OR5,-N (R6) (R6'),-NHCOR7,-NHSO2R8, or-A6-Qa, or they binds to each other to form methylenedioxy group, Qa is phenyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, naphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, or indazolyl group, which may be substituted with one of Tl or two or more of the same or different T1, and binds to A6 at an arbitrary position on the ring, R4 and R6 independently represent hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, R5 and R7 independently represent hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, or-A6-Qa, R8 is a lower alkyl group having 1 to 4 carbon atoms, Rs' has the same meaning as R6, or binds to R6 to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to form a saturated nitrogen- containing alkyl group or morpholino group, p in Rc is an integer of 2 to 4, A4 is a single bind or methylene or ethylene, A5 is-C (O)-,-C (S) -, or-S (0) 2-, Rd is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or Qa, Re is an alkyl group having 1 to 8 carbon atoms,-A6-Qa,- (CH2) iRl4, -OR28,-SR28, or-N (R29) (R30), i is an integer of 1 to 3, R14 is hydroxyl group, an alkoxy group having 1 to 4 carbon atoms, carboxyl group, or an N, N- dialkylcarbamoyl group having 1 to 4 carbon atoms, R28 is an alkyl group having 1 to 8 carbon atoms or-A6-Qa, R29 is an alkyl group having 1 to 8 carbon atoms, an alkoxycarbonyl group having 1 to 4 carbon atoms, or-A6-Qa, R3° is hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, or binds to R29 to form a 3-to 6- membered ring together with the nitrogen atom to which they bind to form a saturated nitrogen-containing alkyl group or morpholino group, Rz'has the same meaning as Rx', or represents-A5-Re, Ry'is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or-A6-Qp, or binds to Rz'to form a saturated or unsaturated nitrogen-containing cyclic substituent having 3 to 7 atoms, when-D-Rx'or- N (Ry') (Rz') contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when-D-Rx'or-N (Ry') (Rz') contains amino group, the amino group may be protected with Rp2.

(137) The compound according to any one of (129) to (136) mentioned above, wherein, in the formula (III), Rs'is-N (Ry') (Rz').

(138) The compound according to any one of (129) to (136) mentioned above, wherein, in the formula (III), Rs'is-D-Rx', D is sulfur atom,-S (O)-,-S (0) 2-, or- C (O)-.

(139) The compound according to (129) mentioned above, wherein, in the formula (III), AR'binds at the position of C2'in the aromatic ring (E'), and Rs'binds to one of the ring-constituting carbon atoms C3', C4', and C5'.

(140) The compound according to (129) mentioned above, wherein, in the formula (III), AR'binds to C2', Rs'binds to any one of the atoms C3', C4', and C5', a ring- constituting carbon atom to which Rs'does not bind among C3', C4', and C5'may be replaced with V', V'is nitrogen atom, or carbon atom substituted with Zx', Zx'is one kind of group selected from the group consisting of fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N- methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N- dimethylsulfamoylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx'contains amino group, the amino group may be protected with Rp2, Rs'is-D-Rx'or-N (Ry') (Rz'), D is oxygen atom or sulfur atom, Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2- cyclopentylethyl group, or 2-cyclohexylethyl group, or Rb or Rc, Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group, A2 is a single bind, oxygen atom, sulfur atom, -N (methyl) -, or-N (ethyl)- (provided that when A2 is oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl) -, Al is ethylene), R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q is phenyl group, Al is a single bind or unsubstituted methylene, and A2 is a single bind, one of R2 and R3 is a substituent other than hydrogen atom), p in Rc is an integer of 2 or 3, A4 is a single bind or methylene, A5 is-C (O)-,-C (S) -, or-S (O) 2-, Rd is hydrogen atom, or methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, or pyridin-4-yl group, Re is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4- chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4- chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin- 3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4- methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N- isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4- chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2- yl) amino group, N- (furan-3-yl) amino group, N- (thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, or ethyloxycarbonylamino group, Rz'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4- methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2- yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2- yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2- yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan- 2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7- dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4- chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4- dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6- dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2' (4'chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyllethyl group, 2- [3- (trifluoromethyl) phenyll ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2-(N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4- methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4- chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4- fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N- isobutylthiocarbamoyl group, t-butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N- cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N- cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N- cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N-phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4- methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4- chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4- fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4- fluorophenyl) thiocarbamoyl group, (pyrrolidino-l-yl) carbonyl group, (piperidino-l- yl) carbonyl group, or (morpholino-4-yl) carbonyl group, Ry'is hydrogen atom, methyl group, ethyl group or isobutyl group, or binds to Rz'to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol- 1-yl group or pyrazol-1-yl group together with the nitrogen atom, provided that when-D-Rx'or-N (Ry') (Rz') contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when-D-Rx'or-N (Ry') (Rz') contains amino group, the amino group may be protected with Rp2, AR'is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [blthiophen-4-yl group, benzo [blthiophen-2-yl group, indol-5-yl group, indol-4- yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro- 1H-quinolin-5-yl group, benzo [dlisothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, lH-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [clisothiazol-4-yl group, benzo [c] isothiazol-6-yl group, benzo [c] isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-alpyridin-7-yl group, 1H-pyrrolo [2, 3- blpyridin-5-yl group, 1H-pyrrolo [2, 3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H- isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group ; quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H- benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H- pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b]pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, 1H- benzotriazol-5-yl group, lH-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2,3- blpyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-blpyridin-4-yl group, 1,3- dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H- benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5- yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [l, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3, 2- c]pyridin-6-yl group, lH-pyrrolo [3, 2-c]pyridin-4-yl group, lH-pyrrolo [2, 3-c]pyridin- 5-yl group, 1H-pyrrolo [2, 3-c] pyridin-4-yl group, 1H-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazolo [4, 3-b]pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-4-yl group, lH-pyrazolol3, 4-clpyridin-5-yl group, 1H- pyrazolo [3, 4-c]pyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H- pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2, 4] triazolo [4, 3-a]pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c]pyridin-2-yl group, thieno [3, 2- clpyridin-3-yl group, thieno [3, 2-c]pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b]pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3,2- b] pyridin-6-yl group, 1H-thieno [3, 2-c] pyrazol-5-yl group, lH-thieno [3, 2-c]pyrazol-4- yl group, benzo [d]isoxazol-5-yl group, benzo [d]isoxazol-4-yl group, benzo [dlisoxazol- 6-yl group, benzo [d]isoxazol-7-yl group, benzo[c]isoxazol-5-yl group, benzo[c]isoxazol-4-yl group, benzo [c]isoxazol-6-yl group, benzo [c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5- yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3, 4- d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a]pyrimidin-6-yl group, 1H-pyrazolo [3, 4-b] pyrazin-5-yl group, 1H-imidazo [4, 5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa), and Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2- hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N- dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2- aminoacetylamino group, methylsulfonylamino group, (N, N- dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N- methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N, N-dimethylcarbamoyl group, provided that when AR' contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when AR'contains amino group, the amino group may be protected with Rp2.

(141) The compound according to (139) or (140) mentioned above, wherein, in the formula (III), Rs'is-O-Rx', and all of C2', C3', C4', C5'and C6'in the aromatic ring (E') are not replaced with V'.

(142) The compound according to (131) mentioned above, wherein, in the formula (III), AR'binds at the position of C2'in the aromatic ring (E'), Rs'binds to one of the ring-constituting carbon atoms C3', C4', and C5', Rs'is-O-Rx', and all of C2', C3', C4', C5'and C6'in the aromatic ring (E') are not replaced with V.

(143) The compound according to (132) mentioned above, wherein, in the formula (III), AR'binds at the position of C2'in the aromatic ring (E'), Rs'binds to one of the ring-constituting carbon atoms C3', C4', and C5', Rs'is-O-Rx', and all of C2', C3', C4', C5'and C6'in the aromatic ring (E') are not replaced with V.

(144) The compound according to any one of (139) to (143) mentioned above, wherein, in the formula (III), Rs'binds to C3'.

(145) The compound according to (129) mentioned above, wherein, in the formula (III), C2'is carbon atom to which AR'binds, C3'is carbon atom to which Rs'binds, C4'may be replaced with V', C5'and C6'are unsubstituted ring-constituting carbon atoms, V'is nitrogen atom, or carbon atom substituted with Zx', Zx'is fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, or N, N- dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx'contains amino group, the amino group may be protected with Rp2, Rs'is-O-Rx', Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1-(4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3,5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3, 5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2-(4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyll ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, or 2- (N-ethyl-N-phenylamino) ethyl group, and AR'is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) nap hthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2,3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-lH- indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-lH-indol-5-yl group, 1-(2-hydroxyethyl)-lH- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, l-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-IH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b]pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-1H- pyrrolo [2, 3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa), provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when AR'contains amino group, the amino group may be protected with Rp2.

(146) The compound according to (139) to (143) mentioned above, wherein, in the formula (III), Rs'binds to C4'.

(147) The compound according to (129) mentioned above, wherein, in the formula (III), C22 is carbon atom to which AR'binds, C4'iS carbon atom to which Rs'binds, C5'may be replaced with V', C3'and c6 are unsubstituted ring-constituting carbon atoms, V'is nitrogen atom, or carbon atom substituted with Zx', Zx'is fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, or N, N- dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx'contains amino group, the amino group may be protected with Rp2, Rs'is-O-Rx', Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, l' (4'chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyll ethyl group, 2- [3- (trifluoromethydphenyll ethyl group, 2- [4- (trifluoromethyl) phenyl ethyl group, 2- [4- (N, N-dimethylamino) phenyll ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2-(N-phenyl-N-methylamino) ethyl group, or 2-(N-ethyl-N-phenylamino) ethyl group, and AR'is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2,3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H- indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-lH-indol-5-yl group, 1-(2-hydroxyethyl)-1H- indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, l-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when AR'contains amino group, the amino group may be protected with Rp2.

(148) The compound according to any one of (139) to (143) mentioned above, wherein, in the formula (III), Rs'binds to C5'.

(149) The compound according to (129) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to the atom C5'or C6'in the aromatic ring (E').

(150) The compound according to (149) mentioned above, wherein, in the formula (III), Rs'is-O-Rx', and all of C2', C3', C4', C5'and C6'in the aromatic ring (E') are not replaced with V.

(151) The compound according to (131) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to the atom C5'or C6'in the aromatic ring (E'), Rs'is-O-Rx', and all of C2', C3', C4', C5'and C6'in the aromatic ring (E') are not replaced with V.

(152) The compound according to (132) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to the atom C5'or C6'in the aromatic ring (E'), Rs'is-0-Rx', and all of C2', C3', C4', C5'and C6'in the aromatic ring (E') are not replaced with V.

(153) The compound according to any one of (149) to (152) mentioned above, wherein, in the formula (III), Rs'binds to C5'.

(154) The compound according to (129) mentioned above, wherein, in the formula (III), C3'iS carbon atom to which AR'binds, C5'is carbon atom to which Rs'binds, C2', C4', and C6'are unsubstituted ring-constituting carbon atoms, Rs'is-O-Rx', Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, l- (3'fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3,5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4- dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, or 2-(N-ethyl-N-phenylamino) ethyl group, and AR'is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo[b]furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo[b]thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3- dimethyl-lH-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, l-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H- indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-lH- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-IH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol- 5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when AR'contains amino group, the amino group may be protected with Rp2.

(155) The compound according to any one of (149) to (152) mentioned above, wherein, in the formula (III), Rs'binds to C6'.

(156) The compound according to (129) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), and C6'is V'.

(157) The compound according to (131) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4' in the aromatic ring (E'), Cs'is carbon atom substituted with Zx, C2'and C5'are unsubstituted carbon atoms, and Rs' is -O-Rx'.

(158) The compound according to (132) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4' in the aromatic ring (E'), C6'is carbon atom substituted with Zx, C2'and C5'are unsubstituted ring- constituting carbon atoms, and Rs'is-O-Rx'.

(159) The compound according to (129) mentioned above, wherein, in the formula (III), C3' is carbon atom to which AR'binds, C4'is a carbon atom to which Rs'binds, C6 is carbon atom substituted with Zx', C2'and C5'are unsubstituted ring- constituting carbon atoms, Zx'is fluorine atom, methyl group, hydroxyl group, amino group, N- methylamino group, or N, N-dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx' contains amino group, the amino group may be protected with Rp2, Rs'is-O-Rx', Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2-[2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyll ethyl group, 2- [4- (N, N-dimethylamino) phenyl ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, or 2-(N-ethyl-N-phenylamino) ethyl group, and AR'is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2, 3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H- indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-lH- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-lH-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-1H- pyrrolo [2, 3-b]pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, provided that when Ar'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and whenAR'contains amino group, the amino group may be protected with Rp2.

(160) The compound according to (129) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is nitrogen atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, and Rs'is-O-Rx'.

(161) The compound according to (131) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is nitrogen atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, and Rs'is-O-Rx'.

(162) The compound according to (132) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is nitrogen atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, and Rs'is-O-Rx'.

(163) The compound according to (129) mentioned above, wherein, in the formula (III), C3'iS carbon atom to which AR'binds, C4'iS carbon atom to which Rs'binds, C5'is nitrogen atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, Rs'is-O-Rx', Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2-(4-chlorophenyl)ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3-(trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, or 2- (N-ethyl-N-p henylamino) ethyl group, and AR'is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzotb] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H- indol-5-yl group, 2-methyl-l-propyl-lH-indol-5-yl group, 3-methyl-1-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-lH- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol- 5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-lH-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1- (2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when AR'contains amino group, the amino group may be protected with Rp2.

(164) The compound according to (129) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, Rs'is-D-Rx', D is a single bind, sulfur atom,-S (O)-,-S (0) 2-, or-C (O)-.

(165) The compound according to (131) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5 iSo a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2'and C6 are unsubstituted ring-constituting carbon atoms, Rs'is-D-Rx', and D is a single bind, sulfur atom,-S (O)-,-S (0) 2-, or- C (O)-.

(166) The compound according to (132) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, Rs'is-D-Rx', and D is a single bind, sulfur atom,-S (O) -,-S (O) 2-, or- C (O)-.

(167) The compound according to (129) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2'and c62 are unsubstituted ring-constituting carbon atoms, and Rs'is-N (Ry') (Rz').

(168) The compound according to (131) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5 is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, and Rs'is-N (Ry') (Rz').

(169) The compound according to (132) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, and Rs'is-N (Ry') (Rz').

(170) The compound according to (129) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5 is carbon atom substituted with-N (Rnl) (Rn2) (provided that one of Rnl and Rn2 is a substituent other than hydrogen atom), C2'and C6 are unsubstituted ring- constituting carbon atoms, and Rs'is-O-Rx'.

(171) The compound according to (131) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'iS carbon atom substituted with-N (Rnl) (Rn2) (provided that one of Rnl and Rn2 is a substituent other than hydrogen atom), C2'and C6'are unsubstituted ring- constituting carbon atoms, and Rs'is-O-Rx'.

(172) The compound according to (123) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'iS carbon atom substituted with-N (Rnl) (Rn2) (provided that one of Rnl and Rn2 is a substituent other than hydrogen atom), C2'and C6' are unsubstituted ring- constituting carbon atoms, and Rs'is-O-Rx'.

(173) The compound according to (129) mentioned above, wherein, in the formula (III), C3'iS carbon atom to which AR'binds, C4' is carbon atom to which Rs'binds, C5' is carbon atom substituted with Zx', C2'and C6 are unsubstituted ring- constituting carbon atoms, Zx'is N-methylamino group, N-ethylamino group, N-propylamino group, N- isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, or N, N-dimethylsulfamoylamino group, provided that when Zx'contains amino group, the amino group may be protected with Rp2, Rs'is-O-Rx', Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2- fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4- methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2- chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4- methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4- difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4- dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2-(N-phenyl-N-methylamino) ethyl group, or 2-(N-ethyl-N-phenylamino) ethyl group, and AR'is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) nap hthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2,3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, l-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H- indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-lH- indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-lH- indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-1H- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-lH-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-blpyridin-5-yl group, 1-ethyl-lH-pyrrolo [2, 3-blpyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when AR'contains amino group, the amino group may be protected with Rp2.

(174) The compound according to (129) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2' and C6' are unsubstituted ring-constituting carbon atoms, Rs'is-D-Rx', and Rx'has the same meaning as Rc, provided that when Rc contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Rc contains amino group, the amino group may be protected with Rp2.

(175) The compound according to (131) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4in the aromatic ring (E'), C5'is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2' and C6' are unsubstituted ring-constituting carbon atoms, Rs'is-D-Rx', and Rx'has the same meaning as Rc, provided that when Rc contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Rc contains amino group, the amino group may be protected with Rp2.

(176) The compound according to (132) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, Rs'is-D-Rx', and Rx'has the same meaning as Rc, provided that when Rc contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Rc contains amino group, the amino group may be protected with Rp2.

(177) The compound according to (129) mentioned above, wherein, in the formula (III), C3'is carbon atom to which AR'binds, C4'is a carbon atom to which Rs'binds, C5'is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, Zx'is fluorine atom, methyl group, hydroxyl group, amino group, N- methylamino group, or N, N-dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx' contains amino group, the amino group may be protected with Rp2, Rs'is-O-Rx', Rx'has the same meaning as Rc, provided that when Rc contains hydroxyl group, the hydroxyl group may be protected with Rpl, p in Rc is an integer of 2, A4 is a single bind or methylene, A5 is-C (O) -,-C (S)-, or-S (0) 2-, Rd is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, phenyl group, 4- methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4- chlorophenylmethyl group, or 4-fluorophenylmethyl group, Re is isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4- methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, N- propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N' (4'methylphenyl) amino groups N' (4'chlorophenyl) amino group, N' (4'fluorophenyl) amino group, pyrrolidino group, piperidino group, or morpholino group, and AR'is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6- methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6- aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N- dimethylamino) nap hthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3- methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3- methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, 1H- indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3- dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-1H-indol- 5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1,2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3- methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-lH- indol-5-yl group, 2-methyl-l-propyl-lH-indol-5-yl group, 3-methyl-l-propyl-1H- indol-5-yl group, 2, 3-dimethyl-1-propyl-lH-indol-5-yl group, 1-(2-hydroxyethyl)-lH- indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1- (2- hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-l- (2-hydroxyethyl)-lH- indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2- methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3- dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3- dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2- dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 1- methyl-lH-indazol-5-yl group, 1-ethyl-lH-indazol-5-yl group, 1-propyl-lH-indazol- 5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-lH-indazol-5- yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-lH-pyrrolo 12, 3-b] pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-1H- pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2- dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when AR'contains amino group, the amino group may be protected with Rp.

(178) The compound according to (129) mentioned above, wherein, in the formula (III), AR'binds to C3', Rs'binds to any one of the atoms C4', C5', and C6', a ring- constituting carbon atom to which Rs' does not bind among C4', C5', and C6 may be replaced with V', V'is nitrogen atom, or carbon atom substituted with Zx', Zx'is fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N- propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N- diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, or N, N-dimethylsulfamoylamino group, provided that when Zx' contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Zx'contains amino group, the amino group may be protected with Rp2, Rs'is-D-Rx'or-N (Ry') (Rz'), D is oxygen atom or sulfur atom, Rx'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2- cyclopentylethyl group, or 2-cyclohexylethyl group, or Rb or Rc, Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group, A2 is a single bind, oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)- (provided that when A2 is oxygen atom, sulfur atom, -N (methyl) -, or-N (ethyl)-, Al is ethylene), R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q is phenyl group, Al is a single bind or unsubstituted methylene, and A2 is a single bind, one of R2 and R3 is a substituent other than hydrogen atom), p in Rc is an integer of 2 or 3, A4 is a single bind or methylene, A5 is-C (O)-,-C (S) -, or-S (0) 2-, Rd is hydrogen atom, or methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, or pyridin-4-yl group, Re is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4- chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4- chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin- 3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4- methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N- isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4- chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2- yl) amino group, N- (furan-3-yl) amino group, N- (thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group or ethyloxycarbonylamino group, Rz'is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4- methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2- yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2- yl group, 5, 6-dimethylindan-2-yl group, 4-fiuoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2- yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan- 2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7- dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, l- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4- chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5- dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3- chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4- difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4- dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2,6- dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5- dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3- methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2- methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4- methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3- chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3- chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4- methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4- chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4- fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N- isobutylthiocarbamoyl group, t'butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxyearbonyl group, N- cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N- cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N- cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N-phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4- methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4- chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4- fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4- fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-1- yl) carbonyl group, or (morpholino-4-yl) carbonyl group, Ry'is hydrogen atom, methyl group, ethyl group or isobutyl group, or binds to Rz'to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol- 1-yl group, or pyrazol-1-yl group together with the nitrogen atom, provided that when-D-Rx'or-N (Ry') (Rz') contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituent-D-Rx'or-N (Ry') (Rz') contains amino group, the amino group may be protected with Rp2, AR'is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4- yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro- lH-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, 1H-indazol-5-yl group, lH-indazol-4-yl group, lH-indazol-6-yl group, benzo [clisothiazol-5-yl group, benzo [c] isothiazol-4-yl group, benzo [c] isothiazol-6-yl group, benzo [c] isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, 1H-pyrrolo [2,3- b] pyridin-5-yl group, 1H-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H- isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H- benzimidazol-5-yl group, lH-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H- pyrrolo [3, 2-b] pyridin-5-yl group, lH-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, 1H- benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2, 3- b]pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b]pyridin-4-yl group, 1,3- dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H- benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5- yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3,2- clpyridin-6-yl group, 1H-pyrrolo [3, 2-c] pyridin-4-yl group, 1H-pyrrolo [2, 3-c] pyridin- 5-yl group, lH-pyrrolo [2, 3-c] pyridin-4-yl group, lH-pyrazolo [4, 3-b] pyridin-5-yl group, lH-pyrazolo [4, 3-blpyridin-6-yl group, lH-pyrazolo [4, 3-c]pyridin-6-yl group, 1H-pyrazolo [4, 3-c]pyridin-4-yl group, 1H-pyrazolo [3, 4-c]pyridin-5-yl group, 1H- pyrazolo[3,4-c]pyridin-4-yl group, 1H-pyrazolo [3, 4-b]pyridin-5-yl group, 1H- pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a]pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2- c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b] pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3,2- b] pyridin-6-yl group, lH-thieno [3, 2-c] pyrazol-5-yl group, 1H-thieno [3, 2-c] pyrazol-4- yl group, benzo [d] isoxazol-5-yl group, benzo [d] isoxazol-4-yl group, benzo [d] isoxazol- 6-yl group, benzo [d] isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5- yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3, 4- d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a]pyrimidin-6-yl group, 1H-pyrazolo [3, 4-b] pyrazin-5-yl group, 1H-imidazo [4, 5-b] pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa), and Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2- hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N- dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2- aminoacetylamino group, methylsulfonylamino group, (N, N- dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N- methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N, N-dimethylcarbamoyl group, provided that when AR' contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when AR'contains amino group, the amino group may be protected with Rp2.

(179) The compound according to (119) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, and Rs'is-O-Rx'.

(180) The compound according to (131) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is a ring-constituting carbon atom substituted with Zx, or an unsubstituted ring-constituting carbon atom, C2'and C62 are unsubstituted ring-constituting carbon atoms, and D is oxygen atom.

(181) The compound according to (132) mentioned above, wherein, in the formula (III), AR'binds to C-9'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is a ring-constituting carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, C2'and C6'are unsubstituted ring-constituting carbon atoms, and Rs'is-O-Rx'.

(182) The compound according to (129) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'iS carbon atom substituted with nitro group, C2'and C6'are unsubstituted ring-constituting carbon atoms, and Rs'is-O-Rx'.

(183) The compound according to (131) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is carbon atom substituted with nitro group, C2'and C6'are unsubstituted ring-constituting carbon atoms, and Rs'is-O-Rx'.

(184) The compound according to (132) mentioned above, wherein, in the formula (III), AR'binds to C3'in the aromatic ring (E'), Rs'binds to C4'in the aromatic ring (E'), C5'is carbon atom substituted with nitro group, C2'and C6'are unsubstituted ring-constituting carbon atoms, and Rs'is-O-Rx'.

(185) An agent for prophylactic and/or therapeutic treatment of fibrosis, which contains a type 4 PLA2 inhibitor as an active ingredient.

(186) An agent for prophylactic and/or therapeutic treatment of pulmonary fibrosis, which contains a type 4 PLA2 inhibitor as an active ingredient..

(187) The prophylactic and/or therapeutic agent according to (186), wherein the pulmonary fibrosis is drug-induced pulmonary fibrosis.

(188) The prophylactic and/or therapeutic agent according to (187), wherein the drug-induced pulmonary fibrosis is a disease induced by one or more kinds of medicaments among methotrexate, sodium aurothiomalate, auranofin, D- penicillamine, bucillamine, actarit, salazosulfapyridine, cyclophosphamide, Taxol, etoposide, cisplatin, vincristine, vinblastine, irinotecan, gefitinib, and bleomycin.

(189) The prophylactic and/or therapeutic agent according to (187), wherein the drug-induced pulmonary fibrosis is a disease induced by one or more kinds of medicaments among methotrexate and bleomycin.

(190) The prophylactic and/or therapeutic agent according to (186), wherein the type 4 PLA2 inhibitor is a compound represented by the formula (I) or a pharmacologically acceptable salt thereof.

(191) The prophylactic and/or therapeutic agent according to (186), wherein the type 4 PLA2 inhibitor is an inhibitor selected from the group consisting of 4- (1- benzhydryl-6-chloro-lH-indol-3-ylmethyl)-3-methoxybenzoic acid, 4- {4- [2- (2- [bis (4- chlorophenyl) methoxy] ethylsulfonyl) ethoxy] phenyl}-1, 1, 1-trifluoro-2-butanone, N- {1- [2- (2, 4-difluorobenzoyl) benzoyl]-4-tritylsulfanylpyrrolidin-2-ylmethyl}-4- (2, 4- dioxothiazolidin-5-ylidenemethyl) benzoic acid amide, 4-methyl-2-oxo-5- (5, 6,7, 8- tetrahydronaphthalen-2-yl) oxazolidine-3-carbonxylic acid (6- methoxytetrahydropyran-2-yl) amide, 4-methyl-2-oxo-5- (4- methylphenyl) thiazolidine-3-carbonxylic acid (tetrahydropyran-2-yl) amide, 4- [3- (4- decyloxyphenyloxy)-2-oxopropyloxyabenzoic acid, and 1- {2- [4- (carboxymethyl) phenoxy] ethyl}-3-dodecanoylindole-2-carbonxylic acid.

The compound (I) of the present invention or a pharmaceutically acceptable salt thereof has an action of suppressing the production of both of prostaglandins and leukotrienes, and said compound has characteristic features that, when administered to a human or animal, the compound exerts superior prophylactic and/or therapeutic effect on diseases or pathological conditions in which a prostaglandin and/or leukotriene is involved, and the compound has extremely low toxicity. The compounds (II) and (III) of the present invention are synthetic intermediates useful for the production of the compound (I) of the present invention.

Furthermore, it was confirmed that a type 4 PLA2 inhibitor is useful as a prophylactic and/or therapeutic agent for fibrosis, in particular, pulmonary fibrosis, especially drug-induced pulmonary fibrosis, which was induced as a side effect of a medicament.

Best Mode for Carrying out the Invention In the present specification, carbon atom may sometimes be represented simply by"C", hydrogen atom by"H", oxygen atom by"O", sulfur atom by"S", and nitrogen atom by"N".

Examples of Link in the aforementioned general formula (I) include a saturated straight hydrocarbon chain having 1 to 3 carbon atoms or an unsaturated straight hydrocarbon chain having 2 or 3 carbon atoms. In the present invention, the straight chain of the saturated straight hydrocarbon chain is preferably unsubstituted. The straight chain of the unsaturated straight hydrocarbon chain is also preferably unsubstituted. As the saturated straight hydrocarbon chain, - (CH2) n- is preferred. Symbol n is an integer of 1 to 3. When n is 1,2 or 3, the desired action is most characteristically exhibited. Methylene where n is 1, ethylene where n is 2 and trimethylene where n is 3 are preferred, and ethylene where n is 2 is particularly preferred.

The unsaturated hydrocarbon chain having 2 or 3 carbon atoms means a hydrocarbon chain which contains an unsaturated bond as a double bond or a triple bond among the carbon-carbon bonds. As the unsaturated hydrocarbon chain, an unsaturated hydrocarbon chain containing a double bond is preferred. When the chain contains one or more double bonds, the number of the double bond may preferably one. Specific examples include ethenylene which has two carbon atoms and contains one double bond, as well as ethynylene which has two carbon atoms and contains one triple bond, propen-3-yl which has three carbon atoms and contains one double bond, and propyn-3-yl which has three carbon atoms and contains one triple bond.

C2, C3, C4, C5 and C6 in the aromatic ring (E) in the formula (I) each represent a ring-constituting carbon atom. The ring-constituting carbon atoms form the aromatic ring (E), and accordingly, they are represented as C or CH.

Among them, any one of ring-constituting carbon atoms to which Rs or Ar does not bind may be replaced with V. The aforementioned expression"to be replaced with" means that any one of the ring-constituting carbon atoms C2, C3, C4, C5 and C6 is replaced with V, and thus V may sometimes be a ring-constituting component. Rs and AR each bind to any of the ring-constituting carbon atoms C2, C3, C4, C5 or C6 in the aromatic ring (E), and this means that, for example, when AR binds to C2, Rs binds to any of the ring-constituting carbon atoms C3, C4, C5 and C6, when AR binds to C3, Rs binds to any of the ring-constituting carbon atoms C2, C4, C5 and C6, and when AR bind to C4, Rs binds to the ring-constituting carbon atom C2 or C3.

Preferred examples of these combinations of substitution positions include a compound wherein AR binds to C2, and Rs binds to any of the atoms C3, C4, and C5, and particularly preferred examples include a compound wherein AR binds to C2, and Rs binds to C3 or C4. Preferred examples also include a compound wherein AR binds to C3, and Rs binds to any of the atoms C4, C5, and C6, and particularly preferred examples also include a compound wherein AR binds to C3, and Rs binds to the atom C4 or C5. A still more preferred example is a compound wherein AR binds to C3, and Rs binds to C4.

One of the atoms C2, C3, C4, C5 and C6 to which Rs and AR do not bind may be replaced with V. For example, when AR binds to C2, and Rs binds to C3, one of the ring-constituting carbon atoms C4, C5, and C6 may be replaced with V. As another example, it is meant that when AR binds to C3, and Rs binds to C4, one of the atoms C2, C5, and C6 may be replaced with V. Among them combinations and other combinations, preferred examples are a compound wherein AR binds to C2, Rs binds to C3, and C4 is replaced with V ; a compound wherein AR binds to C2, Rs binds to C4, and C5 is replaced with V a compound wherein AR binds to C2, Rs binds to C5, and C4 is replaced with V ; a compound wherein AR binds to C3, Rs binds to C4, and C5 is replaced with V ; a compound wherein AR binds to C3, Rs binds to C4, and C6 is replaced with V ; a compound wherein AR binds to C3, Rs binds to C5, and C4 is replaced with V ; a compound wherein AR binds to C3, Rs binds to C6, and C5 is replaced with V, and the like. Furthermore, particularly preferred examples include a compound wherein AR binds to C3, Rs binds to C4, and C5 is replaced with V and a compound wherein AR binds to C3, Rs binds to C4, and C6 is replaced with V, and an particularly preferred example is a compound wherein AR binds to C3, Rs binds to C4, and C5 is replaced with V.

V represents nitrogen atom, or carbon atom substituted with Zx. Namely, when V represent nitrogen atom, the aromatic ring (E) in the formula (I) represents a pyridine ring. When V represent carbon atom substituted with Zx, the aromatic ring (E) is a benzene ring having Zx. Both of the compounds are particularly preferred. Furthermore, a compound wherein AR binds to C3, Rs binds to C4, C5 is V replaced with V, and this V represents nitrogen atom is particularly preferred.

Zx is defined as a linear or branched saturated alkyl group having 1 to 4 carbon atoms, fluorine atom, chlorine atom, bromine atom, nitro group,-OR9, or -N (Rnl) (Rn2). Among them, fluorine atom, chlorine atom, bromine atom, and nitro group are preferred examples, and fluorine atom is particularly preferred.

As for Zx, examples of the linear or branched saturated alkyl group having 1 to 4 carbon atoms include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group and the like, and among them, methyl group is particularly preferred.

R9 represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, or-A6-Qp. Among them, hydrogen atom is a particularly preferred example.

Preferred examples of the lower alkyl group having 1 to 4 carbon atoms include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, and the like, and methyl group is particularly preferred.

As in-A6-Qp represents a single bond or methylene, and Qp represents a phenyl group which may be substituted with one of T1 or two or more of the same or different T1. The substituent T1 is a linear or branched saturated alkyl group having 1 to 4 carbon atoms, hydroxyl group, fluorine atom, chlorine atom, bromine atom, trifluoromethyl group, nitro group, an alkoxy group having 1 to 4 carbon atoms, or a mono-or dialkylamino group having 1 to 4 carbon atoms. Specific examples of-A6-Qp include phenyl group, methylphenyl group, chlorophenyl group, benzyl group, methylbenzyl group, chlorobenzyl group, dichlorobenzyl group, fluorobenzyl group, trifluoromethylbenzyl group, nitrobenzyl group, methoxyphenyl group, N-methylaminobenzyl group, N, N-dimethylaminobenzyl group, and the like.

Preferred examples of-OR9 include hydroxyl group, methoxy group, and the like, and hydroxyl group is particularly preferred.

Rnl represents hydrogen atom or a linear or branched saturated alkyl group having 1 to 4 carbon atoms, and hydrogen atom is particularly preferred. Examples of the linear or branched saturated alkyl group having 1 to 4 carbon atoms include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, or t-butyl group, and the like. Among them, methyl group, ethyl group, propyl group, isopropyl group, and the like are preferred examples, and methyl group is particularly preferred.

Rn2 has the same meaning as Rnl, or represents a-COR23 group or a-SO2R24 group, or binds to Rnl to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to form a saturated nitrogen-containing cycloalkyl group or morpholino group.

R23 represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms,-O-A6-Qp, or-N (R25) (R26).

R25 represents hydrogen atom, or a linear or branched saturated alkyl group having 1 to 4 carbon atoms. R26 has the same meaning as R25, or binds to R25 to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogen-containing cycloalkyl group or morpholino group. Examples of the compound wherein R26"binds to R25 to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to represent a saturated nitrogen-containing cycloalkyl group or morpholino group"include, for example, a compound wherein a cyclic aminoalkyl group containing nitrogen atom such as pyrrolidino group, piperazino group and morpholino group is formed.

Specific examples of-COR23 include formyl group, acetyl group, t-butyloxycarbonyl group, phenyloxycarbonyl group, benzyloxycarbonyl group, carbamoyl group, N'methylcarbamoyl group, N, N-dimethylcarbamoyl group, piperidine-l-carbonyl group, morpholine-4-carbonyl group, and the like, and preferred examples include formyl group, acetyl group, carbamoyl group, and the like. In the aforementioned formulas, as represented by As and Qp, for example, the same symbols may sometimes be used simultaneously at different positions.

These symbols are used to mean the same class of groups of substituents. However, because each substituent is independently chosen from each other, the same symbols do not mean that an identical substituent should be necessarily chosen, and as a result, selection of the same or different kind of substituent is not prohibited.

R24 represents a lower alkyl group having 1 to 4 carbon atoms, amino group, or a mono-or dialkylamino group having 1 to 4 carbon atoms. Specific examples of -SO2R24 include mesyl group, sulfamoyl group, N-methylsulfamoyl group, N, N-dimethylsulfamoyl group, and the like, and preferred examples include mesyl group, N, N-dimethylsulfamoyl group, and the like.

Specific examples of-N (Rnl) (Rn2) include amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, piperidino group, pyrrolidino group, morpholino group, formylamino group, acetylamino group, t-butyloxycarbonylamino group, phenyloxycarbonylamino group, benzyloxycarbonylamino group, carbamoylamino group, N-methylcarbamoylamino group, N, N-dimethylcarbamoylamino group, piperidine-1-carbonylamino group, morpholine-4-carbonylamino group, mesylamino group, sulfamoylamino group, N-methylsulfamoylamino group, N, N-dimethylsulfamoylamino group, and the like.

Among them, preferred examples include amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, N, N-dimethylsulfamoylamino group, and the like, and amino group, N-methylamino group, and N, N-dimethylamino group are particularly preferred.

Therefore, preferred examples of Zx include fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, N, N-dimethylsulfamoylamino group, and the like, and particularly preferred examples include fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, N, N-dimethylamino group, and the like.

In the formula (I), Rs is defined to represent-D-Rx or-N (Ry) (Rz).

D is defined to represent a single bond, oxygen atom, sulfur atom,-S (O) -, -S (0) 2-, or-C (O)-. Among them, oxygen atom and sulfur atom are preferred, and oxygen atom is particularly preferred. Another preferred examples include the compounds wherein D represent a single bond.

Rx represents a linear or branched saturated alkyl group having 3 to 8 carbon atoms, or represents Ra, Rb, or Rc mentioned above.

As for Rx, examples of the linear or branched saturated alkyl group having 3 to 8 carbon atoms include, for example, propyl group, isopropyl group, butyl group, isobutyl group, 1-methylpropyl group, t-butyl group, pentyl group, isopentyl group, 2-methylbutyl group, 2,2-dimethylpropyl group, hexyl group, 4-methylpentyl group, 2, 3-dimethylbutyl group, 2-ethylbutyl group, heptyl group, octyl group, and the like, and butyl group, isobutyl group, and 2-ethylbutyl group are particularly preferred.

As for Rx, Ru ouf Ra is defined to be a saturated cyclic alkyl group having 3 to 7 carbon atoms substituted with a lower alkyl group having 1 to 4 carbon atoms or an unsubstituted saturated cyclic alkyl group having 3 to 7 carbon atoms, or a condensed saturated cyclic alkyl group having 6 to 8 carbon atoms substituted with a lower alkyl group having 1 to 4 carbon atoms or an unsubstituted condensed saturated cyclic alkyl group having 6 to 8 carbon atoms. As for R1, examples of the saturated cyclic alkyl group having 3 to 7 carbon atoms include cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, and the like, and cyclopentyl group, cyclohexyl group, and cycloheptyl group are particularly preferred. As for RI, examples of the condensed saturated cyclic alkyl group having 6 to 8 carbon atoms group include bicyclo [2,2, heptyl group, bicyclo [2,2, 2] octyl group, and the like.

Examples of the lower alkyl group having 1 to 4 carbon atoms substituting on R1 include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, and the like. Examples of Rl substituted with a lower alkyl group having 1 to 4 carbon atoms include methylcyclopentyl group, methylcyclohexyl group, methylbicyclo [2,2, heptyl group, and the like.

Symbol k is defined to be 0 or an integer of 1 to 3. A single bond where k is 0, methylene where k is 1, and ethylene where k is 2 are preferred, and a bond where k is 0, and methylene where k is 1 are particularly preferred.

Examples of Ra include cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopropylmethyl group, cyclobutylmethyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, 3-cyclohexylpropyl group, 2-methylcyclopentyl group, 3'methylcyclopentyl group, 3,4-dimethylcyclopentyl group, 4-methylcyclohexyl group, 4, 4-dimethylcyclohexyl group, 4-ethylcyclohexyl group, 4-methylcyclohexylmethyl group, bicyclo [2,2, 1] heptane-2-methyl group, bicyclo [2,2, 2] octane-2-methyl group, 3-methylbicyclo [2,2, 1]heptane-2-methyl group, bicyclo [2, 2, 1] hept-1-ylmethyl group, bicyclo [2,2, 2] oct-1-ylmethyl group, and the like. Cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group are preferred, and cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group are particularly preferred.

As for Rx, A2 in Rb is defined to be a single bond, oxygen atom, sulfur atom, -S(O)-, -S(O)2-, or-N (R4)-. R4 is defined to be a lower alkyl group having 1 to 4 carbon atoms. Preferred examples are methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, and the like, and methyl group and ethyl group are particularly preferred examples. Therefore, particularly preferred examples of A2 include a single bond, oxygen atom, sulfur atom, -N (methyl) -, and-N (ethyl)-.

Al is defined to be a single bond or an alkylene (a) having 1 to 3 carbon atoms, i. e. , methylene, ethylene or trimethylene. However, when A2 represents oxygen atom, sulfur atom,-S (O)-,-S (0) 2-or-N (R4)-, Al is ethylene or trimethylene.

Further, the alkylene (a) may be substituted with a lower alkyl group having 1 to 4 carbon atoms or phenyl group. Examples of the lower alkyl group having 1 to 4 carbon atoms for the above compound include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, and the like, and methyl group, and ethyl group are preferred examples. Specific examples of Al include methylene, methylmethylene, ethylmethylene, phenylmethylene, ethylene, methylethylene, dimethylethylene, ethylethylene, phenylethylene, trimethylene, methyltrimethylene, and the like. Among them, when A2 represents a single bond, Al is most preferably a single bond, or methylene, methylmethylene, or ethylene.

Further, when A2 represents oxygen atom, sulfur atom,-S (O)-,-S (0) 2-or-N (R4)-, A is most preferably ethylene.

Q in Rb is defined to be a residue of a partially unsaturated or completely unsaturated monocyclic or condensed bicyclic carbon ring or heterocyclic ring (q), and the heterocyclic ring (q) means a ring containing 1 to 4 the same or different ring-constituting heteroatoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom. The term"residue"means a monovalent group formed by eliminating hydrogen atom bonding to a ring-constituting atom. The residue of monocyclic carbon ring or heterocyclic ring is a partially unsaturated or completely unsaturated substituent having 5 to 7 atoms, and examples include, for example, phenyl group, thienyl group, furyl group, pyrrolyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, and the like. Among them, phenyl group, thienyl group, furyl group, pyridyl group, and oxazolyl group are preferred examples, and phenyl group is particularly preferred.

The condensed bicyclic carbon ring or heterocyclic ring is a partially unsaturated or completely unsaturated ring having 8 to 11 atoms, and examples of residue thereof include, for example, naphthyl group, tetrahydronaphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, indazolyl group, 4H-chromenyl group, dihydrobenzodioxyl group, benzoisoxazolyl group, pyrrolopyridinyl group, pyrazolopyridinyl group, triazolopyridinyl group, thienopyridinyl group, thienopyrazolyl group, 1,3-dihydrobenzimidazole group, dihydro-3H-benzoxazole group, dihydro-3H-benzothiazole group, and the like. Among them, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, and dihydrobenzodioxyl group are preferred examples, and indanyl group is one of particularly preferred examples.

Q binds to A2 at an arbitrary position on the ring. Preferred examples of Q with indication of bonding position include phenyl group, 2-or 3-thienyl group, 2-or 3-furyl group, 2-, 3-or 4-pyridyl group, 2-, 4-or 5-oxazolyl group, 1-or 2-naphthyl group, 1-, 2-, 5-or 6-tetrahydronaphthyl group, indan-1-yl group, indan-2-yl group, indan-4-yl group, indan-5-yl group, 1-, 2-, 3-, 4-, 5-, 6-, or 7-indolyl group, 2-, 5-or 6-dihydrobenzodioxyl group, and the like. Among them, phenyl group, and indan-2-yl group are particularly preferred.

In Rb, R2 and R3 are defined to be substituents of Q, and independently represent hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms, oxo group, thioxo group, fluorine atom, chlorine atom, bromine atom, trifluoromethyl group,-OR5,-N (R6) (R6'),-NHCOR7,-NHS02R8, or-A6-Qa, or bind to each other to represent methylenedioxy group.

Examples of the linear or branched saturated alkyl group having 1 to 4 carbon atoms include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, and the like, and methyl group is particularly preferred.

R6 in-N (Rs) (R6') represents hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms. R6'has the same meaning as R6, or binds to R6 to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to form a saturated nitrogen-containing cycloalkyl group or morpholino group. Therefore, specific examples of-N (R6) (R6') include amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N'diethylamino group, piperidino group, pyrrolidino group, morpholino group, and the like. N, N-Dimethylamino group, piperidino group, morpholino group, and the like are preferred examples, and N, N-dimethylamino group is a particularly preferred example.

R5 and R7 are defined to independently represent hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, or a-A6-Qa group. Examples of the lower alkyl group having 1 to 4 carbon atoms include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, and the like, and among them, methyl group is a preferred example.

A6 in-A6-Qa has the same meaning as that defined above. Qa is defined to be a partially unsaturated or completely unsaturated monocyclic or condensed bicyclic carbon ring or heterocyclic ring (qa), and the heterocyclic ring (qa) means a substituent containing 1 to 4 the same or different ring-constituting heteroatoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom.

The monocyclic carbon ring or heterocyclic ring is a partially unsaturated or completely unsaturated ring having 5 to 7 atoms, and examples of residue thereof include, for example, phenyl group, thienyl group, furyl group, pyrrolyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, and the like. The condensed bicyclic carbon ring or heterocyclic ring is a partially unsaturated or completely unsaturated ring having 8 to 11 atoms, and examples of residue thereof include, for example, naphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, indazolyl group, and the like.

Qa binds to A6 at an arbitrary position on the ring. Further, Qa may be substituted with two or more of the same or different TI. Tl has the same meaning as defined above.

Specific examples of-A6-Qa include phenyl group, methylphenyl group, chlorophenyl group, benzyl group, methylbenzyl group, chlorobenzyl group, dichlorobenzyl group, fluorobenzyl group, trifluoromethylbenzyl group, nitrobenzyl group, methoxyphenyl group, N-methylaminobenzyl group, N, N-dimethylaminobenzyl group, furyl group, thienyl group, pyrrolyl group, pyridyl group, oxazolyl group, isoxazolyl group, thiazolyl group, isothiazolyl group, imidazolyl group, pyrazolyl group, oxadiazolyl group, thiadiazolyl group, triazolyl group, tetrazolyl group, naphthyl group, indanyl group, indenyl group, quinolyl group, isoquinolyl group, indolyl group, benzofuryl group, benzothienyl group, benzimidazolyl group, benzoxazolyl group, benzothiazolyl group, indazolyl group, and the like.

R3 each defined to be a lower alkyl group having 1 to 4 carbon atoms, and examples of the lower alkyl group having 1 to 4 carbon atoms include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, and the like.

Therefore, preferred examples of R2 and R3 include hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, and methylsulfonylamino group, and hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, and dimethylamino group are particularly preferred. When Q represents phenyl group, A1 represents a single bond, or unsubstituted methylene, and A2 represents a single bond, at least one of R2 and R3 preferably represents a substituent other than hydrogen atom.

Particularly preferred examples of Rb include 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2-[2-(trifluoromethyl) phenyllethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, and the like.

Symbol p in Rc is defined to be an integer of 2 to 4. Ethylene where p is 2, and trimethylene where p is 3 are preferred, and ethylene where p is 2 is particularly preferred. A4 represents a single bond, or represents methylene or ethylene, and a single bond and methylene are particularly preferred. A5 represents-C (O)-,-C (S) -, or-S (0) 2-, and all of them are preferred. Rd represents hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or group Qa. Re represents an alkyl group having 1 to 8 carbon atoms, a-As-Qa group, a- (CH2) iRl4 group, a-OR28 group, a-SR28 group, or a-N (R29) (R3Q) group. The group Qa and -A6-Qa have the same meanings as defined above.

The alkyl group having 1 to 8 carbon atoms is a linear or branched saturated alkyl group or a linear or branched partially unsaturated alkyl group, or an alkyl group which may contain a cycloalkyl group having 3 to 7 carbon atoms, and examples include, for example, methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, pentyl group, isopentyl group, 2-methylbutyl group, 2, 2-dimethylpropyl group, hexyl group, 4-methylpentyl group, 2, 3-dimethylbutyl group, 2-ethylbutyl group, heptyl group, octyl group, cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopropylmethyl group, cyclobutylmethyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, 2-methylcyclopentyl group, 3-methylcyclopentyl group, 3,4-dimethylcyclopentyl group, 4-methylcyclohexyl group, 4, 4-dimethylcyclohexyl group, 4-ethylcyclohexyl group, 4-methylcyclohexylmethyl group, and the like.

Symbol i in-(CH2) iRl4 represents an integer of 1 to 3, and R14 represents hydroxyl group, an alkoxy group having 1 to 4 carbon atoms, carboxyl group, or an N, N-dialkylcarbamoyl group having 1 to 4 carbon atoms. Examples of the alkoxy group having 1 to 4 carbon atoms include methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butoxy group, isobutyloxy group, t-butyloxy group, and the like. Examples of the N, N-dialkylcarbamoyl group having 1 to 4 carbon atoms include N, N-dimethylcarbamoyl group, N, N-diethylcarbamoyl group, and the like.

R28 in-OR28 or-SR28 represents an alkyl group having 1 to 8 carbon atoms, or-A6-Qa, and these have the same meanings as defined above.

R29 in-N (R29) (R30) represents an alkyl group having 1 to 8 carbon atoms, an alkoxycarbonyl group having 1 to 4 carbon atoms, or-A6-Qa. Among them, the alkyl group having 1 to 8 carbon atoms and-A6-Qa have the same meanings as those defined above. Examples of the alkoxycarbonyl group having 1 to 4 carbon atoms include methyloxycarbonyl group, ethyloxycarbonyl group, propyloxycarbonyl group, isopropyloxyearbonyl group, butyloxycarbonyl group, isobutyloxycarbonyl group, t'butyloxycarbonyl group, and the like. R30 represents hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms, or binds to R29 to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to form a saturated nitrogen-containing cycloalkyl group or morpholino group. The lower alkyl group having 1 to 4 carbon atoms has the same meaning as defined above. Examples of the compound where"R30 binds to R29 to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to form a saturated nitrogen-containing cycloalkyl group or morpholino group"include, for example, a compound wherein a cyclic aminoalkyl group containing nitrogen atom such as pyrrolidino group, piperazino group, and morpholino group is formed.

Preferred examples of Rd include hydrogen atom as well as methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorobenzyl group, 4-fluorobenzyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, and the like.

Particularly preferred examples of Rd include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, and the like.

Preferred examples of substituted-A4-Rd include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isoamyl group, cyclopropyl group, cyclopropylmethyl group, 2- (cyclopropyl) ethyl group, cyclopentyl group, cyclopentylmethyl group, 2- (cyclopentyl) ethyl group, cyclohexyl group, cyclohexylmethyl group, 2- (cyclohexyl) ethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, 2- (4'chlorophenyl) ethyl group, 2' (4'fluorophenyl) ethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, (pyridin-2-yl) methyl group, (pyridin-3-yl) methyl group, (pyridin-4-yl) methyl group, and the like.

Particularly preferred examples of substituted-A4-Rd include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, pentyl group, isoamyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, 2' (4'chlorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, and the like.

Preferred examples of Re include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, methylthioxo group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4-chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2-yl) amino group, N- (furan-3-yl) amino group, N-(thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, ethyloxycarbonylamino group, and the like.

Particularly preferred examples of Re include isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4-chlorophenyl) amino group, N- (4-fluorophenyl) amino group, pyrrolidino group, piperidino group, morpholino group, and the like.

Preferred examples of-A5-Re include acetyl group, thioacetyl group, methanesulfonyl group, propionyl group, ethylthiocarbonyl group, butyryl group, propylthiocarbonyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4-methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4-chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4-fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, phenylmethylcarbonyl group, 4-methylphenylmethylcarbonyl group, 4-chlorophenylmethylcarbonyl group, 4-fluorophenylmethylcarbonyl group, (pyridin-2-yl) carbonyl group, (pyridin-2-yl) thiocarbonyl group, (pyridin-3-yl) carbonyl group, (pyridin-4-yl) carbonyl group, (furan-2-yl) carbonyl group, (thiophen-2-yl) carbonyl group, methyloxycarbonyl group, methylsulfanylcarbonyl group, methyloxythiocarbonyl group, methyloxycarbonylaminocarbonyl group, carbamoyl group, N-methylcarbamoyl group, N-methylthiocarbamoyl group, N, N-dimethylcarbamoyl group, N, N-dimethylthiocarbamoyl group, N, N-dimethylsulfamoyl group, ethyloxycarbonyl group, ethyloxycarbonylaminocarbonyl group, N-ethylcarbamoyl group, N-ethylthiocarbamoyl group, N, N-diethylcarbamoyl group, N, N-diethylthiocarbamoyl group, N, N-diethylsulfamoyl group, propyloxycarbonyl group, N-propylcarbamoyl group, N-propylthiocarbamoyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N-isobutylthiocarbamoyl group, t'butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N-cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N-cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N-cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N'phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4-methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4-chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4-fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4-fluorophenyl) thiocarbamoyl group, phenylmethyloxycarbonyl group, 4-methylphenylmethyloxycarbonyl group, 4-chlorophenylmethyloxycarbonyl group, 4-fluorophenylmethyloxycarbonyl group, N- (pyridin-2-yl) carbamoyl group, N- (pyridin-2-yl) thiocarbamoyl group, N- (pyridin-3-yl) carbamoyl group, N- (pyridin-3-yl) thiocarbamoyl group, N- (pyridin-4-yl) carbamoyl group, N- (pyridin-4-yl) thiocarbamoyl group, N- (furan-2-yl) carbamoyl group, N- (thiophen-2-yl) carbamoyl group, (pyrrolidino-l-yl) carbonyl group, (piperidino-1-yl) carbonyl group, (morpholino-4-yl) carbonyl group, and the like.

Particularly preferred examples of-A5-Re include isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4-methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4-chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4-fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N-isobutylthiocarbamoyl group, t-butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N-cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N-cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N-cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N'phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4-methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4-chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4-fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4-fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-1-yl) carbonyl group, (morpholino-4-yl) carbonyl group, and the like.

Specific examples of Rc include 2-(N-isobutyryl-N-methylamino) ethyl group, 2- (N-ethyl-N-isobutyrylamino) ethyl group, 2- (N-isobutyryl-N-propylamino) ethyl group, 2- (N-isobutyryl-N-isopropylamino) ethyl group, 2- (N-butyl-N-isobutyrylamino) ethyl group, 2- (N-isobutyl-N-isobutyrylamino) ethyl group, 2- (N-cyclopropyl-N-isobutyrylamino) ethyl group, 2- (N-cyclop entyl-N-isobutyrylamino) ethyl group, 2- (N-cyclop entylmethyl-N-isobutyrylamino) ethyl group, 2- (N-cyclohexyl-N-isobutyrylamino) ethyl group, 2- (N-cyclohexylmethyl-N-isobutyrylamino) ethyl group, 2- (N-isobutyryl-N-phenylamino) ethyl group, 2- [N-isobutyryl-N- (4-methylphenyl) amino] ethyl group, 2- [N- (4-chlorophenyl)-N-isobutyrylamino] ethyl group, 2- [N- (4-fluorophenyl)-N-isobutyrylamino] ethyl group, 2- (N-benzyl-N-isobutyrylamino) ethyl group, 2- [N- (4-chlorophenylmethyl)-N-isobutyrylamino] ethyl group, 2- [N- (4-fluorophenylmethyl)-N-isobutyrylamino] ethyl group, 2- [N- [2- ( 4chlorophenyl) ethyl]-N-isobutyrylamino] ethyl group, 2- [N- [2- (4-fluorophenyl) ethyl]-N-isobutyrylamino] ethyl group, 2-(N-isobutylthiocarbonyl-N-methylamino) ethyl group, 2-(N-isobutylthiocarbonyl-N-isopropylamino) ethyl group, 2-(N-butyl-N-isobutylthiocarbonylamino) ethyl group, 2-(N-isobutyl-N-isobutylthiocarbonylamino) ethyl group, 2- (N-cyclopentyl-N-isobutylthiocarbonylamino) ethyl group, 2- (N-cyclop entylmethyl-N-isobutylthiocarbonylamino) ethyl group, 2- (N-isobutylthiocarbonyl-N-phenylamino) ethyl group, 2-(N-benzyl-N-isobutylthiocarbonylamino) ethyl group, 2- [N- (4-fluorophenylmethyl)-N-isobutylthiocarbonylamino] ethyl group, 2- (N-methyl-N-pivaloylamino) ethyl group, 2- (N-isopropyl-N-pivaloylamino) ethyl group, 2- (N-butyl-N-pivaloylamino) ethyl group, 2- (N-isobutyl-N-pivaloylamino) ethyl group, 2- (N-cyclohexyl-N-pivaloylamino) ethyl group, 2- (N-cyclohexylmethyl-N-pivaloylamino) ethyl group, 2- (N-phenyl-N-pivaloylamino) ethyl group, 2- (N-benzyl-N-pivaloylamino) ethyl group, 2- (N-cyclopentylcarbonyl-N-methylamino) ethyl group, 2- (N-butyl-N-cyclopentylcarbonylamino) ethyl group, 2-(N-cyclopentylcarbonyl-N-isobutylamino) ethyl group, 2- (N-cyclopentylcarbonyl-N-cyclopentylmethylamino) ethyl group, 2- (N-cyclopentylcarbonyl-N-phenylamino) ethyl group, 2- [N-cyclop entylcarbonyl-N- (4-fluorophenyl) amino] ethyl group, 2- (N-benzyl-N-cyclopentylcarbonylamino) ethyl group, 2- [N-cyclopentylcarbonyl-N-(4-fluorophenylmethyl) amino] ethyl group, 2- (N-methyl-N-phenylsulfonylamino) ethyl group, 2-(N-ethyl-N-phenylsulfonylamino) ethyl group, 2-(N-phenylsulfonyl-N-propylamino) ethyl group, 2- (N-isopropyl-N-phenylsulfonylamino) ethyl group, 2-(N-butyl-N-phenylsulfonylamino) ethyl group, 2-(N-isobutyl-N-phenylsulfonylamino) ethyl group, 2-(N-cyclopropyl-N-phenylsulfonylamino) ethyl group, 2- (N-cyclopentyl-N-phenylsulfonylamino) ethyl group, 2- (N-cyclopentylmethyl-N-phenylsulfonylamino) ethyl group, 2- (N-cyclohexyl-N-p henylsulfonylamino) ethyl group, 2-(N-cyclohexylmethyl-N-phenylsulfonylamino) ethyl group, 2- (N-phenyl-N-phenylsulfonylamino) ethyl group, 2- [N- (4-fluorophenyl)-N-phenylsulfonylamino] ethyl group, 2- (N-benzyl-N-phenylsulfonylamino) ethyl group, 2- [N- (N-butylcarbamoyl)-N-methylamino] ethyl group, 2- [N-butyl-N- (N-butylcarbamoyl) amino] ethyl group, 2- [N- (N-butylcarbamoyl)-N-isobutylamino] ethyl group, 2- [N- (N-butylcarbamoyl)-N-cyclopentylamino] ethyl group, 2- [N- (N-butylcarbamoyl)-N-cyclohexylmethylamino] ethyl group, 2- [N- (N-butylcarbamoyl)-N-phenylamino] ethyl group, 2-{N- (N-butylcarbamoyl) -N- (4-fluorophenyl) amino} ethyl group, 2- [N-benzyl-N- (N-butylcarbamoyl) amino] ethyl group, 2- {N- (N-butylcarbamoyl) -N- (4-fluorophenylmethyl) amino} ethyl group, 2-{N- (N-butylcarbamoyl)-N- [2- (4-fluorophenyl) ethyl] amino} ethyl group, 2-[N-(N-isopropylthiocarbamoyl)-N-methylamino] ethyl group, 2-[N-butyl-N-(N-isopropylthiocarbamoyl) amino] ethyl group, 2- [N-isobutyl-N- (N-isopropylthiocarbamoyl) amino] ethyl group, 2- [N-cyclopentyl-N-(N-isopropylthiocarbamoyl) amino] ethyl group, 2- [N-cyclohexylmethyl-N- (N-isopropylthiocarbamoyl) amino] ethyl group, 2- [N- (N-isopropylthiocarbamoyl)-N-phenylamino] ethyl group, 2-{N- (4-fluorophenyl) -N- (N-isopropylthiocarbamoyl) amino} ethyl group, 2- [N-benzyl-N- (N-isopropylthiocarbamoyl) amino] ethyl group, 2- (N-isobutyloxycarbonyl-N-methylamino) ethyl group, 2- (N-butyl-N-isobutyloxycarbonylamino) ethyl group, 2- (N-isobutyl-N-isobutyloxycarbonylamino) ethyl group, 2- (N-cyclopentyl-N-isobutyloxycarbonylamino) ethyl group, 2-(N-cyclohexylmethyl-N-isobutyloxycarbonylamino) ethyl group, 2- (N-isobutyloxycarbonyl-N-phenylamino) ethyl group, 2- [N- (4-fluorophenyl)-N-isobutyloxycarbonylamino] ethyl group, 2- (N-benzyl-N-isobutyloxycarbonylamino) ethyl group, 2- [N- (N-cyclopentylcarbamoyl)-N-methylamino] ethyl group, 2- [N-butyl-N- (N-cyclopentylcarbamoyl) amino] ethyl group, 2- [N- (N-cyclopentylcarbamoyl)-N-isobutylamino] ethyl group, 2-[N-cyclopentyl-N-(N-cyclopentylcarbamoyl)amino] ethyl group, 2- [N-cyclohexylmethyl-N- (N-cyclopentylcarbamoyl) amino] ethyl group, 2- [N- (N-cyclopentylcarbamoyl)-N-phenylamino] ethyl group, 2- [N-benzyl-N- (N-cyclopentylcarbamoyl) amino] ethyl group, 2- [N- (N-cyclohexylthiocarbamoyl)-N-methylamino] ethyl group, 2- [N-butyl-N- (N-cyclohexylthiocarbamoyl) amino] ethyl group, 2- [N- (N-cyclohexylthiocarbamoyl)-N-isobutylamino] ethyl group, 2- [N- (N-cyclohexylthiocarbamoyl)-N-cyclopentylamino] ethyl group, 2-[N-cyclohexylmethyl-N-(N-cyclohexylthiocarbamoyl) amino] ethyl group, 2- [N- (N-cyclohexylthiocarbamoyl)-N-phenylamino] ethyl group, 2- [N-benzyl-N- (N-cyclohexylthiocarbamoyl) amino] ethyl group, 2- (N-methyl-N-phenyloxycarbonylamino) ethyl group, 2- (N-butyl-N-phenyloxycarbonylamino) ethyl group, 2- (N-isobutyl-N-phenyloxycarbonylamino) ethyl group, 2-(N-cyclopentyl-N-phenyloxycarbonylamino)ethyl group, 2- (N-cyclohexylmethyl-N-phenyloxycarbonylamino) ethyl group, 2- (N-phenyl-N-phenyloxycarbonylamino) ethyl group, 2- (N-benzyl-N-phenyloxycarbonylamino) ethyl group, 2- [N-methyl-N- (N-phenylcarbamoyl) amino] ethyl group, 2- [N-butyl-N- (N-phenylcarbamoyl) amino] ethyl group, 2- [N-isobutyl-N- (N-phenylcarbamoyl) amino] ethyl group, 2- [N-cyclop entyl-N- (N-phenylcarbamoyl) amino] ethyl group, 2- [N-cyclohexylmethyl-N- (N-phenylcarbamoyl) amino] ethyl group, 2- [N-phenyl-N- (N-phenylcarbamoyl) amino] ethyl group, 2-[N-benzyl-N-(N-phenylcarbamoyl) amino] ethyl group, and the like.

When Rs in the formula (I) represents-N (Ry) (Rz), Rz is defined to have the same meaning as lAx, or Rz represents methyl group, ethyl group, or a-A5-Re group.

-A5-Re has the same meaning as defined above.

Particularly preferred examples of Rz include butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, l- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2-(N-phenyl-N-methylamino) ethyl group, 2-(N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4-methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4-chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4-fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N-isobutylthiocarbamoyl group, t-butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N-cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N-cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N-cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxyearbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N-phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4-methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4-chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4-fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4-fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-1-yl) carbonyl group, (morpholino-4-yl) carbonyl group, and the like.

Among the Rz, methyl group or ethyl group is particularly preferred when Ry is other than hydrogen atom.

Ry represents hydrogen atom, an alkyl group having 1 to 8 carbon atoms, or a-A6-Qp group, or binds to Rz to form a saturated or unsaturated nitrogen-containing cyclic substituent having 3 to 7 atoms together with nitrogen atom to which they bind. The alkyl group having 1 to 8 carbon atoms is a linear or branched saturated alkyl group, a linear or branched partially unsaturated alkyl group, or an alkyl group which may contain a cyclic alkyl group having 3 to 7 carbon atoms. Examples include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, pentyl group, isopentyl group, 2-methylbutyl group, 2,2-dimethylpropyl group, hexyl group, 4-methylpentyl group, 2,3-dimethylbutyl group, 2-ethylbutyl group, heptyl group, octyl group, cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopropylmethyl group, cyclobutylmethyl group, cyclopentylmethyl group, cyclohexylmethyl group, cycloheptylmethyl group, 2-cyclopentylethyl group, 2-cyclohexylethyl group, 2-methylcyclopentyl group, 3-methylcyclopentyl group, 3, 4-dimethylcyclopentyl group, 4-methylcyclohexyl group, 4, 4-dimethylcyclohexyl group, 4-ethylcyclohexyl group, 4-methylcyclohexylmethyl group, and the like.

-A6-Qp has the same meaning as defined above.

Particularly preferred examples of Ry include hydrogen atom, methyl group, ethyl group, isobutyl group, and the like.

Ry also binds to Rz to represents a saturated or unsaturated nitrogen-containing cyclic substituent having 3 to 7 atoms formed together with the nitrogen atom to which they bind. Specific examples thereof include cyclic substituents containing nitrogen atom such as 1-pyrrolidino group, 1-piperidino group, 1-homopiperidino group, 1'piperazino group, 4-morpholino group, pyrrol-1-yl group, imidazol-1-yl group, and pyrazol-1-yl group, and all of these are preferred.

The nitrogen-containing cyclic substituent may be substituted with one or two lower alkyl groups having 1 to 4 carbon atoms wherein the two alkyl groups may be the same or different. Examples of the lower alkyl having 1 to 4 carbon atoms include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, or t-butyl group.

Among the substituent-N (Ry) (Rz), particularly preferred examples include N, N-dimethylamino group, N-ethyl-N-methylamino group, N, N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N- (2-ethylbutyl) amino group, N-(2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N- (cyclopentylmethyl) amino group, N- (cyclopentylmethyl)-N-methylamino group, N- (cyclohexylmethyl) amino group, N- (cyclohexylmethyl)-N-methylamino group, N- (2-methylphenyl) amino group, N- (4-methylphenyl) amino group, N- (2-fluorophenyl) amino group, N- (3-fluorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (2-chlorophenyl) amino group, N' (3'chlorophenyl) amino group, N- (4-chlorophenyl) amino group, N- (indan-2-yl) amino group, N- (1-phenylethyl) amino group, N- [1- (2-fluorophenyl) ethyl] amino group, N- [1- (3-fluorophenyl) ethyl] amino group, N- [1- (4-fluorophenyl) ethyl] amino group, N- [1- (2-chlorophenyl) ethyfl amino group, N- [1- (3-chlorophenyl) ethyl] amino group, N- [1- (4-chlorophenyl) ethyl] amino group, N- (2-methylphenylmethyl) amino group, N-methyl-N- (2-methylphenylmethyl) amino group, N- (3-methylphenylmethyl) amino group, N-methyl-N- (3-methylphenylmethyl) amino group, N- (4-methylphenylmethyl) amino group, N-methyl-N- (4-methylphenylmethyl) amino group, N- (2-fluorophenylmethyl) amino group, N- (2-fluorophenylmethyl)-N-methylamino group, N- (3-fluorophenylmethyl) amino group, N- (3-fluorophenylmethyl) -N-methylamino group, N- (4-fluorophenylmethyl) amino group, N- (4-fluorophenylmethyl)-N-methylamino group, N- (2-chlorophenylmethyl) amino group, N- (2-chlorophenylmethyl)-N-methylamino group, N- (3-chlorophenylmethyl) amino group, N- (3-chlorophenylmethyl)-N-methylamino group, N- (4-chlorophenylmethyl) amino group, N- (4-chlorophenylmethyl)-N-methylamino group, N- (2, 3-difluorophenylmethyl) amino group, N- (2, 3-difluorophenylmethyl)-N-methylamino group, N-(2,4-difluorophenylmelthyl)amino group, N-(2, 4-difluorophenylmethyl)-N-methylamino group, N- (2, 5-difluorophenylmethyl) amino group, N- (2, 5-difluorophenylmethyl)-N-methylamino group, N- (3, 4-difluorophenylmethyl) amino group, N- (3, 4-difluorophenylmethyl)-N-methylamino group, N- (3, 5-difluorophenylmethyl) amino group, N- (3,5-difluorophenylmethyl)-N-methylamino group, N- (2, 3-dichlorophenylmethyl) amino group, N- (2, 3-dichlorophenylmethyl)-N-methylamino group, N- (2, 4-dichlorophenylmethyl) amino group, N- (2,4-dichlorophenylmethyl)-N-methylamino group, N- (2, 5-dichlorophenylmethyl) amino group, N- (2, 5-dichlorophenylmethyl)-N-methylamino group, N- (2, 6-dichlorophenylmethyl) amino group, N- (2, 6-dichlorophenylmethyl)-N-methylamino group, N- (3, 4-dichlorophenylmethyl) amino group, N- (3, 4-dichlorophenylmethyl) -N-methylamino group, N- (3,5-dichlorophenylmethyl) amino group, N- (3, 5-dichlorophenylmethyl)-N-methylamino group, N- [2- (trifluoromethyl) phenylmethyl] amino group, N-methyl-N- [2- (trifluoromethyl) phenylmethyll amino group, N- [3- (trifluoromethyl) phenylmethyll amino group, N-methyl-N- [3- (trifluoromethyl) phenylmethyll amino group, N- [4- (trifluoromethyl) phenylmethyl] amino group, N-methyl-N- [4- (trifluoromethyl) phenylmethyl] amino group, 1-pyrrolidino group, 1- (4-methylpiperidino) group, 1-homopiperidino group, and 4-morpholino group.

A most preferred example of Rs in the aforementioned general formula (I) include Rs which meets the conditions of : Rs is-D-Rx wherein D is a single bond and Rx represents Rb, and A1 and A2 in Rb are single bonds. Specific examples include phenyl group, 2-methylphenyl group, 3-methylphenyl group, 4-methylphenyl group, 2, 3-dimethylphenyl group, 3,5-dimethylphenyl group, 2-methoxyphenyl group, 3-methoxyphenyl group, 4-methoxyphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2, 3-difluorophenyl group, 2, 4-difluorophenyl group, 2, 5-difluorophenyl group, 3, 4-difluorophenyl group, 2, 3-dichlorophenyl group, 2,4-dichlorophenyl group, 2, 5-dichlorophenyl group, 2,6-dichlorophenyl group, 3, 4-dichlorophenyl group, 3, 5-dichlorophenyl group, 2-trifluoromethylphenyl group, 3-trifluoromethylphenyl group, 4-trifluoromethylphenyl group, 4- (N, N-dimethylamino) phenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, naphthalen-1-yl group, naphthalen-2-yl group, lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, lH-indazol-5-yl group, or 1-methyl-lH-indazol-5-yl group.

AR in the formula (I) is defined to be a residue of a partially unsaturated or completely unsaturated condensed bicyclic carbon ring or heterocyclic ring (ar).

Further, AR may be substituted with one of Xa or two or more of the same or different Xa. The heterocyclic ring (ar) means a ring containing 1 to 4 the same or different ring-constituting heteroatoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom.

The"condensed bicyclic carbon ring or heterocyclic ring"means a partially unsaturated or completely unsaturated ring having 8 to 11 atoms. Preferred examples include a partially unsaturated or completely unsaturated ring consisting of 8 atoms formed by fusion of 5-membered heterocyclic rings containing 1 or 2 ring-constituting heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur atoms, a partially unsaturated or completely unsaturated ring consisting of 9 atoms formed by fusion of a 5-membered heterocyclic ring containing 1 or 2 ring-constituting heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur atoms and a 6-membered carbon ring or a 6-membered heterocyclic ring containing 1 or 2 ring-constituting heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur atoms, and a partially unsaturated or completely unsaturated substituent consisting of 10 atoms formed by fusion of a 6-membered carbon ring or a 6-membered heterocyclic ring containing 1 or 2 ring-constituting heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur atoms and a 6-membered carbon ring or 6-membered heterocyclic rings containing 1 or 2 ring-constituting heteroatoms selected from the group consisting of nitrogen, oxygen, and sulfur atom. As the carbon ring constituting AR not containing a heteroatom, among the rings constituting AR, naphthalene ring is particularly preferred. Further, as the heterocyclic ring (ar) containing a heteroatom, among the rings constituting AR, those containing 1 or 2 ring-constituting heteroatoms are preferred.

As for AR in the formula (I), specific examples of preferred ring constituting AR include naphthalene, benzofuran, benzo [b] thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-1H-quinoline, benzo [d] isothiazole, 1H-indazole, benzo [c] isothiazole, 2H-indazole, imidazo l, 2-a] pyridine, 1H-pyrrolo [2, 3-b] pyridine, isoquinoline, dihydro-2H-isoquinoline, cinnoline, quinazoline, quinoxaline, 1H-benzimidazole, benzoxazole, lH-pyrrolo [3, 2-b] pyridine, benzo [1, 2,5] thiadiazole, IH-benzotriazole, 1, 3-dihydropyrrolo [2, 3-b] pyridine, 1, 3-dihydrobenzimidazole, dihydro-3H-benzoxazole, phthalazine, [l, 8]naphthalidine, [1, 5] naphthalidine, 1H-pyrrolo [3, 2-c]pyridine, 1H-pyrrolo [2, 3-c] pyridine, 1H-pyrazolo [4, 3-b]pyridine, 1H-pyrazolo [4, 3-c] pyridine, IH-pyrazolo [3, 4-c pyridine, 1H-pyrazolo [3, 4-b] pyridine, [1, 2,4] triazolo [4, 3-a] pyridine, thieno [3, 2-c] pyridine, thieno [3, 2-b]pyridine, 1H-thieno[3,2-c]pyrazole, benzo[d]isoxazole, benzo[c]isoxazole, indolizine, 1,3-dihydroindol, lH-pyrazolo [3, 4-d] thiazole, 2H-isoindol, [1, 2,4] triazolo [1, 5-a] pyrimidine, lH-pyrazolo [3, 4-b] pyrazine, 1H-imidazo [4, 5-b] pyrazine, 7H-purine, 4H-chromene, and the like. Among them, naphthalene, benzofuran, benzo [b] thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-1H-quinoline, benzo [d] isothiazole, 1H-indazole, benzo [c] isothiazole, 2H-indazole, imidazo l, 2-a] pyridine, lH-pyrrolo [2, 3-b] pyridine, isoquinoline and dihydro-2H-isoquinoline constitute a particularly preferred group, and cinnoline, quinazoline, quinoxaline, 1H-benzimidazole, benzoxazole, 1H-pyrrolo [3, 2-b] pyridine, benzo [1, 2,5] thiadiazole, 1H-benzotriazole, 1, 3-dihydropyrrolo [2, 3-b] pyridine, 1, 3-dihydrobenzimidazole and dihydro-3H-benzoxazole also constitute a particularly preferred group. Further, naphthalene, benzofuran, benzo [b] thiophene, indole, benzothiazole, quinoline, 1H-indazole and isoquinoline are particularly preferred.

AR binds to any of the ring-constituting carbon atoms C2, C3, C4, C5, and C6 in the aromatic ring (E) in the aforementioned formula (I) at an arbitrary carbon atom in AR. Preferred examples of the ring constituting AR include, as indicated with substitution position in the aromatic ring (E), naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro-lH-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, lH-indazol-5-yl group, lH-indazol-4-yl group, lH-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [c] isothiazol-4-yl group, benzo [c] isothiazol-6-yl group, benzo [c] isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1H-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, lH-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, lH-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1, 3-dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3, 2-c]pyridin-6-yl group, 1H-pyrrolo [3, 2-c] pyridin-4-yl group, 1H-pyrrolo [2, 3-c]pyridin-5-yl group, lH-pyrrolo [2, 3-c] pyridin-4-yl group, lH-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazaolo [4, 3-b] pyridin-6-yl group, lH-pyrazolo [4, 3-c] pyridin-6-yl group, lH-pyrazolo [4, 3-c] pyridin-4-yl group, lH-pyrazolo [3, 4-c]pyridin-5-yl group, 1H-pyrazolo [3, 4-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, lH-pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2-c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b]pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3, 2-b]pyridin-6-yl group, lH-thieno [3, 2-c] pyrazol-5-yl group, 1H-thieno [3, 2-c] pyrazol-4-yl group, benzo [d]isoxazol-5-yl group, benzo [d]isoxazol-4-yl group, benzo[d]isoxazo]-6-yl group, benzo [d]isoxazol-7-yl group, benzo [c]isoxazol-5-yl group, benzo [c]isoxazol-4-yl group, benzo [c]isoxazol-6-yl group, benzo [c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5-yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3, 4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, 1H-pyrazolo [3, 4-b]pyrazin-5-yl group, 1H-imidazo [4, 5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, 4H-chromen-5-yl group, and the like. Among them, naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, indol-5-yl group, indol-4-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, quinolin-6-yl group, quinolin-3-yl group, dihydro-lH-quinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, lH-indazol-4-yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, dihydro-2H-isoquinolin-6-yl group, cinnolin-6-yl group, benzoxazol-5-yl group, and the like constitute a particularly preferred group, and naphthalen-2-yl group, benzofuran-5-yl group, benzo [b] thiophen-5-yl group, indol-5-yl group, benzothiazol-6-yl group, quinolin-6-yl group, quinolin-3-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, cinnolin-6-yl group, benzoxazol-5-yl group and the like are particularly preferred.

Further, AR may be substituted with one of Xa or the same or different two or more of Xa. Examples of substitution position of Xa include a carbon atom of AR not bonding to the aromatic ring (E), and/or when nitrogen atom is present, that nitrogen atom.

The substituent Xa represents a linear or branched saturated alkyl group having 1 to 4 carbon atoms, a saturated cyclic alkyl group having 3 to 7 carbon atoms, oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, -(CH2) iRl4,-ORl°,-N (Rll) (Rl2),-SO2Rl3, or-COR27. However, when nitrogen atom is present in AR, Xa which may substitute on the nitrogen atom represents a linear or branched saturated alkyl group having 1 to 4 carbon atoms, a saturated cyclic alkyl group having 3 to 7 carbon atoms, or-(CH2) iRl4.

Preferred examples of the substituent Xa are oxo group, thioxo group, fluorine atom, chlorine atom, and trifluoromethyl group.

Examples of the linear or branched saturated alkyl group having 1 to 4 carbon atoms as the substituent Xa include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, and the like, and among them, methyl group, ethyl group, and propyl group are particularly preferred.

Further, examples of the saturated cyclic alkyl group having 3 to 7 carbon atoms include cyclopropyl group, cyclobutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, and the like.

- (CH2) iRl4 has the same meaning as defined above. Preferred examples are 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, and N, N-dimethylcarbamoylmethyl group, and a particularly preferred example is 2-hydroxyethyl group.

R10 in-ORl° represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, or a-(CH2) iRl4 group, and among them, hydrogen atom is a particularly preferred example. Examples of the lower alkyl group having 1 to 4 carbon atoms include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, and the like. Among them, methyl group is particularly preferred.-(CH2) iRl4 has the same meaning as defined above.

Therefore, preferred examples of-ORl° are hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N-dimethylcarbamoylmethyloxy group, and the like, and hydroxyl group, methoxy group, and 2-hydroxyethyloxy group are particularly preferred.

Rll in-N (R") (Rm) represents hydrogen atom, or a lower alkyl group having 1 to 4 carbon atoms, and R, 12 represents hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms, a hydroxyalkyl group having 2 to 4 carbon atoms,-COR15, or -SO2Rl6, or binds to Rll to form a 3-to 6-membered ring together with the nitrogen atom to which they bind to form a saturated nitrogen-containing cycloalkyl group or morpholino group. Rl5 in-COR15 represents a lower alkyl group having 1 to 4 carbon atoms, a hydroxyalkyl group having 2 to 4 carbon atoms, amino group, a mono-or dialkylamino group having 1 to 4 carbon atoms, or-A6-Qa. R16 in-S02Rl6 represents a lower alkyl group having 1 to 4 carbon atoms, amino group, or a mono- or dialkylamino group having 1 to 4 carbon atoms. Specific examples of-N (Rll) (Rl2) include amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, piperidino group, pyrrolidino group, morpholino group, 2-hydroxyethylamino group, formylamino group, acetylamino group, benzoyl group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, carbamoylamino group, N-methylcarbamoylamino group, N, N-dimethylcarbamoylamino group, methylsulfonylamino group, sulfamoylamino group, N-methylsulfamoylamino group, N, N-dimethylsulfamoylamino group, and the like. Among them, preferred examples are amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N, N-dimethylsulfamoyl) amino group, and the like, and amino group, N-methylamino group, N, N-dimethylamino group, and 2-hydroxyethylamino group are particularly preferred.

R13 in-SO2Rl3 represents a lower alkyl group having 1 to 4 carbon atoms, amino group, or a mono-or dialkylamino group having 1 to 4 carbon atoms.

Preferred examples of-SO2Rl3 include methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N, N-dimethylsulfamoyl group, and the like.

R27 in-COR27 represents hydrogen atom, hydroxyl group, an alkoxy group having 1 to 4 carbon atoms, a lower alkyl group having 1 to 4 carbon atoms, amino group, or a mono-or dialkylamino group having 1 to 4 carbon atoms. Specific examples of-COR27 include formyl group, carboxyl group, methoxycarbonyl group, ethoxycarbonyl group, acetyl group, propionyl group, carbamoyl group, N-methylcarbamoyl group, N, N-dimethylcarbamoyl group, and the like. Carboxyl group, acetyl group, carbamoyl group, N, N-dimethylcarbamoyl group, and the like are preferred examples, and carboxyl group is particularly preferred.

Preferred examples of the group Xa include oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N'dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N, N-dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, N, N-dimethylcarbamoyl group, and the like. Particularly preferred examples of the group Xa include oxo group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, amino group, N-methylamino group, N, N-dimethylamino group, 2-hydroxyethylamino group, carboxyl group, and the like. Preferred examples of the group Xa which may substitute on nitrogen atom include methyl group, ethyl group, propyl group, hydroxymethyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, and N, N-dimethylcarbamoylmethyl group. Among them, particularly preferred examples are methyl group, ethyl group, propyl group, and 2-hydroxyethyl group.

Preferred examples of AR substituted with the group Xa or unsubstituted AR include naphthalen-1-yl group, naphthalen-2-yl group, 6-fluoronaphthalen-2-yl group, 6-chloronaphthalen-2-yl group, 6- (trifluoromethyl) naphthalen-2-yl group, 5-hydroxynaphthalen-1-yl group, 5-hydroxynaphthalen-2-yl group, 6-hydroxynaphthalen-1-yl group, 6-hydroxynaphthalen-2-yl group, 7-hydroxynaphthalen-1-yl group, 7-hydroxynaphthalen-2-yl group, 5-methoxynaphthalen-1-yl group, 5-methoxynaphthalen-2-yl group, 6-methoxynaphthalen-1-yl group, 6-methoxynaphthalen-2-yl group, 7-methoxynaphthalen-1-yl group, 7-methoxynaphthalen-2-yl group, 5- (2-hydroxyethyloxy) naphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 7-(2-hydroxyethyloxy) naphthalen-2-yl group, 5- (carboxymethyloxy) naphthalen-2-yl group, 6- (carboxymethyloxy) naphthalen-2-yl group, 7- (carboxymethyloxy) naphthalen-2-yl group, 5- (N, N-dimethylcarbamoylmethyloxy) naphthalen-2-yl group, 6- (N, N-dimethylcarbamoylmethyloxy) naphthalen-2-yl group, 7- (N, N-dimethylcarbamoylmethyloxy) naphthalen-2-yl group, 5-aminonaphthalen-1-yl group, 5-aminonaphthalen-2-yl group, 6-aminonaphthalen-1-yl group, 6-aminonaphthalen-2-yl group, 7-aminonaphthalen-1-yl group, 7-aminonaphthalen-2-yl group, 5- (N-methylamino) naphthalen-1-yl group, 5- (N-methylamino) naphthalen-2-yl group, 6- (N-methylamino) naphthalen-1-yl group, 6- (N-methylamino) naphthalen-2-yl group, 7- (N-methylamino) naphthalen-1-yl group, 7- (N-methylamino) naphthalen-2-yl group, 5- (N, N-dimethylamino) naphthalen-1-yl group, 5- (N, N-dimethylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-l-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 7- (N, N-dimethylamino) naphthalen-1-yl group, 7-(N, N-dimethylamino) naphthalen-2-yl group, 5-(2-hydroxyethylamino) naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, 7- (2-hydroxyethylamino) naphthalen-2-yl group, 5-acetylaminonaphthalen-2-yl group, 6-acetylaminonaphthalen-2-yl group, 6- (2-aminoacetylamino) naphthalen-2-yl group, 6- (2-hydroxyacetylamino) naphthalen-2-yl group, 7- (2-hydroxyacetylamino) naphthalen-2-yl group, 6-[(furan-2-carbonyl) amino] naphthalen-2-yl group, 7- [(furan-2-carbonyl) amino] naphthalen-2-yl group, 6- [ (benzene-2-carbonyl) amino] nap hthalen-2-yl group, 7- [ (benzene-2-carbonyl) amino] nap hthalen-2-yl group, 6-carbamoylaminonaphthalen-2-yl group, 6-methylsulfonylaminonaphthalen-2-yl group, 6-sulfamoylaminonaphthalen-2-yl group, 6- (N, N-dimethylsulfamoylamino) naphthalen-2-yl group, 6-methanesulfonylnaphthalen-2-yl group, 6-sulfamoylnaphthalen-2-yl group, 6- (N-methylsulfamoyl) naphthalen-2-yl group, 6- (N, N-dimethylsulfamoyl) naphthalen-2-yl group, 6-carboxynaphthalen-2-yl group, benzo [b] furan-4-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-4-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-4-yl group, 3-methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-4-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, 2-carboxybenzo [b] furan-4-yl group, 2-carboxybenzo [b] furan-5-yl group, 2-carboxy-3-methylbenzo [b] furan-4-yl group, 2-carboxy-3-methylbenzo [b] furan-5-yl group, 3-acetylbenzo [b] furan-4-yl group, 3-acetylbenzo [b] furan-5-yl group, 3-acetyl-2-methylbenzo [b] furan-4-yl group, 3-acetyl-2-methylbenzo [b]furan-5-yl group, 3-hydroxymethylbenzo [b]furan-4-yl group, 3-hydroxymethylbenzo [blfuran-5-yl group, 3-hydroxymethyl-2-methylbenzo [b]furan-4-yl group, 3-hydroxymethyl-2-methylbenzo [b] furan-5-yl group, benzolb] thiophen-4-yl group, benzo [b]thiophen-5-yl group, 2-methylbenzo [b]thiophen-4-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-4-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-4-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, 2-carboxybenzo [b] thiophen-4-yl group, 2-carboxybenzo [b]thiophen-5-yl group, 2-carboxy-3-methylbenzo [b] thiophen-4-yl group, 2-carboxy-3-methylbenzo [b] thiophen-5-yl group, 3-acetylbenzo [b] thiophen-4-yl group, 3-acetylbenzo [b] thiophen-5-yl group, 3-acetyl-2-methylbenzo [b]thiophen-4-yl group, 3-acetyl-2-methylbenzo [b]thiophen-5-yl group, 3-hydroxymethylbenzo [b] thiophen-4-yl group, 3-hydroxymethylbenzo[b]thiophen-5-yl group, 3-hydroxymethyl-2-methylbenzo [b] thiophen-4-yl group, 3-hydroxymethyl-2-methylbenzo [b]thiophen-5-yl group, 1H-indol-4-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-4-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-4-yl group, 3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1H-indol-4-yl group, 2, 3-dimethyl-1H-indol-5-yl group, 2-carboxy-lH-indol-4-yl group, 2-carboxy-lH-indol-5-yl group, 2-carboxy-3-methyl-1H-indol-4-yl group, 2-carboxy-3-methyl-lH-indol-5-yl group, 3-acetyl-1H-indol-4-yl group, 3-acetyl-1H-indol-5-yl group, 3-acetyl-2-methyl-lH-indol-4-yl group, 3-acetyl-2-methyl-1H-indol-5-yl group, 3-hydroxymethyl-lH-indol-4-yl group, 3-hydroxymethyl-1H-indol-5-yl group, 3-hydroxymethyl-2-methyl-lH-indol-4-yl group, 3-hydroxymethyl-2-methyl-1H-indol-5-yl group, 1-methyl-1H-indol-4-yl group, 1-methyl-1H-indol-5-yl group, 1, 2-dimethyl-lH-indol-4-yl group, 1, 2-dimethyl-lH-indol-5-yl group, 1, 3-dimethyl-1H-indol-4-yl group, 1, 3-dimethyl-1H-indol-5-yl group, 1,2, 3-trimethyl-1H-indol-4-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, 2-carboxy-1-methyl-1H-indol-4-yl group, 2-carboxy-l-methyl-lH-indol-5-yl group, 2-carboxy-1, 3-dimethyl-lH-indol-4-yl group, 2-carboxy-1, 3-dimethyl-lH-indol-5-yl group, 3-acetyl-1-methyl-1H-indol-4-yl group, 3-acetyl-l-methyl-lH-indol-5-yl group, 3-acetyl-1, 2-dimethyl-lH-indol-4-yl group, 3-acetyl-1, 2-dimethyl-lH-indol-5-yl group, 3-hydroxymethyl-1-methyl-lH-indol-4-yl group, 3-hdyroxymethyl-1-methyl-1H-indol-5-yl group, 3-hydroxymethyl-1, 2-dimethyl-lH-indol-4-yl group, 3-hydroxymethyl-1, 2-dimethyl-lH-indol-5-yl group, 1-ethyl-1H-indol-4-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-4-yl group, 1-ethyl-2-methyl-lH-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-4-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-4-yl group, l-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 2-carboxy-1-ethyl-1H-indol-4-yl group, 2-carboxy-1-ethyl-1H-indol-5-yl group, 2-carboxy-l-ethyl-3-methyl-lH-indol-4-yl group, 2-carboxy-1-ethyl-3-methyl-1H-indol-5-yl group, 3-acetyl-1-ethyl-1H-indol-4-yl group, 3-acetyl-1-ethyl-1H-indol-5-yl group, 3-acetyl-1-ethyl-2-methyl-1H-indol-4-yl group, 3-acetyl-1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-hydroxymethyl-lH-indol-4-yl group, l-ethyl-3-hydroxymethyl-lH-indol-5-yl group, 1-ethyl-3-hydroxymethyl-2-methyl-1H-indol-4-yl group, 1-ethyl-3-hydroxymethyl-2-methyl-1H-indol-5-yl group, 1-propyl-lH-indol-4-yl group, l-propyl-lH-indol-5-yl group, 2-methyl-1-propyl-lH-indol-4-yl group, 2-methyl-1-propyl-lH-indol-5-yl group, 3-methyl-1-propyl-1H-indol-4-yl group, 3-methyl-l-propyl-lH-indol-5-yl group, 2, 3-dimethyl-l-propyl-lH-indol-4-yl group, 2, 3-dimethyl-1-propyl-lH-indol-5-yl group, 2-carboxy-1-propyl-1H-indol-4-yl group, 2-carboxy-1-propyl-lH-indol-5-yl group, 2-carboxy-3-methyl-1-propyl-1H-indol-4-yl group, 2-carboxy-3-methyl-1-propyl-1H-indol-5-yl group, 3-acetyl-l-propyl-lH-indol-4-yl group, 3-acetyl-1-propyl-1H-indol-5-yl group, 3-acetyl-2-methyl-1-propyl-1H-indol-4-yl group, 3-acetyl-2-methyl-1-propyl-1H-indol-5-yl group, 3-hydroxymethyl-1-propyl-1H-indol-4-yl group, 3-hydroxymethyl-l-propyl-lH-indol-5-yl group, 3-hydroxymethyl-2-methyl-1-propyl-1H-indol-4-yl group, 3-hydroxymethyl-2-methyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-lH-indol-4-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-4-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-4-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-1H-indol-4-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, 2-carboxy-1- (2-hydroxyethyl)-lH-indol-4-yl group, 2-carboxy-1- (2-hydroxyethyl)-lH-indol-5-yl group, 2-carboxy-1-(2-hydroxyethyl)-3-methyl-1H-indol-4-yl group, 2-carboxy-1-(2-hydroxyethyl)-3-methyl-1H-indol-5-yl group, 3-acetyl-1- (2-hydroxyethyl)-lH-indol-4-yl group, 3-acetyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, 3-acetyl-1- (2-hydroxyethyl)-2-methyl-lH-indol-4-yl group, 3-acetyl-1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-hydroxymethyl-lH-indol-4-yl group, 1- (2-hydroxyethyl)-3-hydroxymethyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-3-hydroxymethyl-2-methyl-lH-indol-4-yl group, 1- (2-hydroxyethyl)-3-hydroxymethyl-2-methyl-lH-indol-5-yl group, 1-carboxymethyl-1H-indol-4-yl group, 1-carboxymethyl-lH-indol-5-yl group, 1-carboxymethyl-2-methyl-lH-indol-4-yl group, 1-carboxymethyl-2-methyl-1H-indol-5-yl group, l-carboxymethyl-3-methyl-lH-indol-4-yl group, l-carboxymethyl-3-methyl-lH-indol-5-yl group, 1-carboxymethyl-2, 3-dimethyl-lH-indol-4-yl group, 1-carboxymethyl-2, 3-dimethyl-1H-indol-5-yl group, 2-carboxy-1-carboxymethyl-lH-indol-4-yl group, 2-carboxy-1-carboxymethyl-1H-indol-5-yl group, 2-carboxy-1-carboxymethyl-3-methyl-lH-indol-4-yl group, 2-carboxy-1-carboxymethyl-3-methyl-lH-indol-5-yl group, 3-acetyl-l-carboxymethyl-lH-indol-4-yl group, 3-acetyl-1-carboxymethyl-1H-indol-5-yl group, 3-acetyl-1-carboxymethyl-2-methyl-1H-indol-4-yl group, 3-acetyl-1-carboxymethyl-2-methyl-lH-indol-5-yl group, 1-carboxymethyl-3-hydroxymethyl-1H-indol-4-yl group, 1-carboxymethyl-3-hydroxymethyl-1H-indol-5-yl group, l-carboxymethyl-3-hydroxymethyl-2-methyl-lH-indol-4-yl group, 1-carboxymethyl-3-hydroxymethyl-2-methyl-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2- (N-methylamino) benzothiazol-6-yl group, 2- (N, N-dimethylamino) benzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, 2-methylquinolin-3-yl group, quinolin-6-yl group, 2-methylquinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 3-methylbenzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 3-methyl-lH-indazol-5-yl group, 1-methyl-lH-indazol-5-yl group, 1, 3-dimethyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-ethyl-3-methyl-1H-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 3-methyl-1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indazol-5-yl group, 1-(carboxymethyl)-1H-indazol-5-yl group, 1-(carboxymethyl)-3-methyl-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, benzo [c]isothiazol-5-yl group, 3-methylbenzo [c] isothiazol-5-yl group, 2-methyl-2H-indazol-5-yl group, 2, 3-dimethyl-2H-indazol-5-yl group, 2-ethyl-2H-indazol-5-yl group, 2-ethyl-3-methyl-2H-indazol-5-yl group, 2-propyl-2H-indazol-5-yl group, 3-methyl-2-propyl-2H-indazol-5-yl group, 2- (2-hydroxyethyl)-2H-indazol-5-yl group, 2- (2-hydroxyethyl) -3-methyl-2H-indazol-5-yl group, 2- (carboxymethyl) -2H-indazol-5-yl group, 2- (carboxymethyl)-3-methyl-2H-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, 2-methyl-imidazo [1, 2-a] pyridin-6-yl group, 3-methyl-imidazo [1, 2-a] pyridin-6-yl group, 2, 3-dimethyl-imidazo [l, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 3-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1, 2-dimethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1, 3-dimethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 2, 3-dimethyl-1H-pyrrolo [2, 3-b]pyridin-5-yl group, 1, 2, 3-trimethyl-1H-pyrrolo [2, 3-b]pyridin-5-yl group, l-ethyl-lH-pyrrolo [2, 3-b]pyridin-5-yl group, 1-ethyl-2-methyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, l-ethyl-3-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-ethyl-2, 3-dimethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-1H-pyrrolo [2, 3-b]pyridin-5-yl group, 2-methyl-l-propyl-lH-pyrrolo [2, 3-b]pyridin-5-yl group, 3-methyl-1-propyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 2, 3-dimethyl-1-propyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-3-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (carboxymethyl) lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (carboxymethyl)-2-methyl-IH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (carboxymethyl)-3-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (carboxymethyl)-2, 3-dimethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-methylisoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, 2-methylquinazolin-6-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 2-methylquinoxalin-6-yl group, lH-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, l-methyl-lH-benzimidazol-5-yl group, 2-methyl-lH-benzimidazol-5-yl group, 1, 2-dimethyl-1H-benzimidazol-5-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 2-methylbenzoxazol-5-yl group, lH-pyrrolo [3, 2-b] pyridin-5-yl group, lH-pyrrolo [3, 2-b] pyridin-6-yl group, l-methyl-lH-pyrrolo [3, 2-b] pyridin-5-yl group, l-ethyl-lH-pyrrolo [3, 2-b]pyridin-5-yl group, 2-methyl-1H-pyrrolo [3, 2-b]pyridin-5-yl group, 3-methyl-1H-pyrrolo [3, 2-b] pyridin-5-yl group, 1, 3-dimethyl-1H-pyrrolo [3, 2-b]pyridin-5-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzol, 2,5] thiadiazol-4-yl group, lH-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1-methyl-lH-benzotriazol-5-yl group, 1-ethyl-1H-benzotriazol-5-yl group, 1, 3-dihydropyrrolo [2, 3-b]pyridin-2-on-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-2-on-4-yl group, 1-methyl-1, 3-dihydropyrrolo[2,3-b]pyridin-2-on-5-yl group, 1, 3-dihydrobenzimidazol-2-on-5-yl group, 1, 3-dihydrobenzimidazol-2-on-4-yl group, 1-methyl-1, 3-dihydrobenzimidazol-2-on-5-yl group, 1, 3-dihydrobenzimidazole-2-thion-5-yl group, 1, 3-dihydrobenzimidazole-2-thion-4-yl group, l'methyl'l, 3-dihydrobenzimidazole-2-thion-5-yl group, 3H-benzoxazol-2-on-6-yl group, 3H-benzoxazol-2-on-7-yl group, 3H-benzoxazol-2-on-5-yl group, 3H-benzoxazol-2-on-4-yl group, 3-methyl-3H-benzoxazol-2-on-6-yl group, 3H-benzoxazole-2-thion-6-yl group, 3H-benzoxazole-2-thion-7-yl group, 3H-benzoxazole-2-thion-5-yl group, 3H-benzoxazole-2-thion-4-yl group, 3-methyl-3H-benzoxazole-2-thion-6-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3, 2-c] pyridin-6-yl group, lH-pyrrolo [3, 2-c] pyridin-4-yl group, 1-mnethyl-1H-pyrrolo [3, 2-c] pyridin-6-yl group, 1-ethyl-1H-pyrrolo [3, 2-c]pyridin-6-yl group, 2-methyl-1H-pyrrolo [3, 2-c] pyridin-6-yl group, 3-methyl-1H-pyrrolo [3, 2-c]pyridin-6-yl group, 1, 3-dimethyl-lH-pyrrolo [3, 2-c] pyridin-6-yl group, 1H-pyrrolo [2, 3-c] pyridin-5-yl group, 1H-pyrrolo [2, 3-c] pyridin-4-yl group, 1-methyl-1H-pyrrolo [2, 3-c] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-c] pyridin-5-yl group, 2-methyl-lH-pyrrolo [2, 3-c] pyridin-5-yl group, 3-methyl-1H-pyrrolo [2, 3-c] pyridin-5-yl group, 1, 3-dimethyl-1H-pyrrolo] [2, 3-c] pyridin-5-yl group, 1H-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazolo [4, 3-b] pyridin-6-yl group, 1-methyl-1H-pyrazolo [4, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrazolo [4, 3-b]pyridin-5-yl group, 3-methyl-lH-pyrazolo [4, 3-b] pyridin-5-yl group, 1, 3-dimethyl-lH-pyrazolo [4, 3-b]opyridin-5-yl group, 1H-pyrazolo [4, 3-c] pyridin-6-yl group, lH-pyrazolo [4, 3-c] pyridin-4-yl group, 1-methyl-lH-pyrazolo [4, 3-c] pyridin-6-yl group, 1-ethyl-1H-pyrazolo [4, 3-c] pyridin-6-yl group, 3-methyl-1H-pyrazolo [4, 3-c]pyridin-6-yl group, 1, 3-dimethyl-lH-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [3, 4-c] pyridin-5-yl group, 1H-pyrazolo [3, 4-c] pyridin-4-yl group, l-methyl-lH-pyrazolo [3, 4-c]pyridin-5-yl group, 1-ethyl-lH-pyrazolo [3, 4-c] pyridin-5-yl group, 3-methyl-lH-pyrazolo [3, 4-c] pyridin-5-yl group, 1, 3-dimethyl-lH-pyrazolo [3, 4-c] pyridin-5-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H-pyrazolo [3, 4-b]pyridin-4-yl group, 1-methyl-lH-pyrazolo [3, 4-b] pyridin-5-yl group, 1-ethyl-lH-pyrazolo [3, 4-b] pyridin-5-yl group, 3-methyl-lH-pyrazolo [3, 4-b]pyridin-5-yl group, 1, 3-dimethyl-1H-pyrazolo [3, 4-b] pyridin-5-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a]pyridin-7-yl group, 3-methyl [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2-c]pyridin-3-yl group, thieno [3, 2-c]pyridin-6-yl group, 2-methylthieno [3, 2-c] pyridin-2-yl group, 3-methylthieno [3, 2-c]pyridin-2-yl group, thieno [3, 2-b]pyridin-2-yl group, thieno [3, 2-b]pyridin-3-yl group, thieno [3, 2-b]pyridin-5-yl group, thieno [3, 2-b]pyridin-6-yl group, 2-methylthieno [3, 2-blpyridin-2-yl group, 3-methylthieno [3, 2-b]pyridin-2-yl group, lH-thieno [3, 2-c] pyrazol-5-yl group, lH-thieno [3, 2-c] pyrazol-4-yl group, 1-methyl-1H-thieno [3, 2-c] pyrazol-5-yl group, 1-ethyl-1H-thieno [3, 2-c] pyrazol-5-yl group, 3-methyl-1H-thieno [3, 2-c]pyrazol-5-yl group, 1, 3-dimethyl-1H-thieno [3, 2-c]pyrazol-5-yl group, benzo [d] isoxazol-5-yl group, benzo [d]isoxazol-4-yl group, benzo [d]isoxazol-6-yl group, benzo [d] isoxazol-7-yl group, 3-methylbenzo [d] isoxazol-5-yl group, benzo [c] isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c] isoxazol-7-yl group, 3-methylbenzo [c] isoxazol-5-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-2-on-5-yl group, 1, 3-dihydroindol-2-on-4-yl group, 1, 3-dihydroindol-2-on-6-yl group, 1-methyl-1, 3-dihydro-indol-2-on-5-yl group, lH-pyrazolo [3, 4-d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, 2-methyl-2H-isoindol-5-yl group, 4H-chromen-6-yl group, 4H-chromen-5-yl group, chromen-4-on-7-yl group, chromen-4-on-6-yl group, and the like.

Particularly preferred examples include naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b]furan-5-yl group, 2, 3-dimethylbenzo [b]furan-5-yl group, benzo [b]thiophen-5-yl group, 2-methylbenzo [b]thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b]thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, l-ethyl-2-methyl-lH-indol-5-yl-group, 1-ethyl-3-methyl-1H-indol-5-yl group, l-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-l-propyl-lH-indol-5-yl group, 2, 3-dimethyl-l-propyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1-methyl-lH-indazol-5-yl group, l-ethyl-lH-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, benzoxazol-5-yl group, and the like.

Particularly preferred examples include naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1-ethyl-lH-indol-5-yl group, benzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, benzoxazol-5-yl group, and the like.

In the formula (I), the group Y is defined to be hydrogen atom, a lower alkyl group having 1 to 4 carbon atoms,- (CH2). N (RI8) (R'9), or-C (R20) 20C (O) A3R21, and among them, hydrogen atom is particularly preferred.

Examples of the lower alkyl group having 1 to 4 carbon atoms include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, and the like. Among them, methyl group, and ethyl group are particularly preferred.

Symbol m in-(CH2) mN (R18) (Rl9) is defined to be an integer of 2 or 3. R18 is the same as R19, or binds to R19 to represent a saturated nitrogen-containing cycloalkyl group forming a 3-to 6-membered ring together with nitrogen atom, or form morpholino group together with nitrogen atom, and R19 is defined to be methyl group, ethyl group, or propyl group. Examples of-(CH2) mN (R18) (Rl3) include 2- (N, N-dimethylamino) ethyl group, 2- (N, N-diethylamino) ethyl group, 2- (N, N-dipropylamino) ethyl group, 3- (N, N-dimethylamino) propyl group, 3- (N, N-diethylamino) propyl group, 2- (N, N-dipropylamino) propyl group, 2-pyrrolidin-1-ylethyl group, 2-piperidin-1-ylethyl group, 2-morpholin-4-ylethyl group, 3-pyrrolidin-1-ylpropyl group, 3-piperidin-1-ylpropyl group, 3-morpholin-4-ylpropyl group, and the like.

R20 in-C (R20) 20C (O) A3R21 is defined to be hydrogen atom, methyl group, ethyl group, or propyl group. R21 is defined to be a lower alkyl group having 1 to 4 carbon atoms, a cyclic saturated alkyl group having 3 to 6 carbon atoms group, or phenyl group. Examples of the lower alkyl group having 1 to 4 carbon atoms include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, and the like, and examples of the cyclic saturated alkyl group having 3 to 6 carbon atoms group include cyclopropyl group, cyclobutyl group, cyclopentyl group, and cyclohexyl group. A3 is defined to be a single bond, or oxygen atom. Examples of-C (R20) 2OC (O) A3R2l include acetoxymethyl group, propionyloxymethyl group, butyryloxymethyl group, (2-methylpropionyl) oxymethyl group, (2, 2-dimethylpropionyl) oxymethyl group, cyclopropionyloxymethyl group, cyclopentanoyloxymethyl group, cyclohexanoyloxymethyl group, phenylcarboxymethyl group, 1-acetoxy-1-methylethyl group, 1-methyl-1-(2-methylpropionyloxy) ethyl group, 1-cyclopentanoyloxy-l-methylethyl group, 1-cyclohexanoyloxy-1-methylethyl group, methoxycarbonyloxymethyl group, ethoxycarbonyloxymethyl group, isopropyloxycarbonyloxymethyl group, t-butyloxycarbonyloxymethyl group, cyclopropyloxycarbonyloxymethyl group, cyclopentyloxycarbonyloxymethyl group, cyclohexyloxycarbonyloxymethyl group, phenyloxycarbonyloxymethyl group, 1-methoxycarbonyloxy-1-methylethyl group, 1-ethoxycarbonyloxy-1-methylethyl group, 1-isopropyloxycarbonyloxy-1-methylethyl group, 1-t-butyloxycarbonyloxy-1-methylethyl group, 1-cyclopropyloxycarbonyloxy-1-methylethyl group, 1-cyclopentyloxyearbonyloxy-1-methylethyl group, 1-cyclohexyloxycarbonyloxy-1-methylethyl group, 1-methyl-1-phenyloxycarbonyloxyethyl group, and the like.

In a preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- (CHz) n-, symbol n represents an integer of 1 to 3.

AR binds to C2, Rs binds to any of the atoms C3, C4 and C5, and a ring-constituting carbon atom to which Rs does not bind among C3, C4, and C5 may be replaced with V.

V represents nitrogen atom, or carbon atom substituted with Zx, and Zx represents a group as any one of fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N-dimethylsulfamoylamino group.

Rs represents-D-Rx, or-N (Ry) (Rz). D represents oxygen atom, or sulfur atom. Rx represents butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-cyclopentylethyl group, or 2-cyclohexylethyl group, or represents Rb or Rc. Q in Rb represents a group as any one of phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, and dihydrobenzodioxyl group. A2 represents a single bond, oxygen atom, sulfur atom,-N (methyl)-, or -N (ethyl)- (provided that when A2 represents oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)-, A1 represents ethylene). R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q represents phenyl group, A1 represents a single bond, or unsubstituted methylene, and A2 represents a single bond, one of R2 and R3 represents a substituent other than hydrogen atom). Symbol p in Rc represents an integer of 2 or 3, and A4 represents a single bond or methylene. A5 represents -C (O)-,-C (S)-, or-S (0) 2-. Rd represents hydrogen atom, or a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, and pyridin-4-yl group. Re represents a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N' (4'methylphenyl) amino group, N- (4-chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2-yl) amino group, N-(furan-3-yl) amino group, N-(thiophen-2-yl) amino group, N-(thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, and ethyloxyearbonylamino group.

Rz represents a group as any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, l' (4'fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2-(4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4-methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4-chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4-fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N-isobutylthiocarbamoyl group, t'butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N'cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N-cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N-cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N-phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4-methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4-chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4-fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4-fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-1-yl) carbonyl group, and (morpholino-4-yl) carbonyl group. Ry represents hydrogen atom, methyl group, ethyl group, or isobutyl group, or binds to Rz to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol-1-yl group, or pyrazol-1-yl group together with nitrogen atom.

AR represents naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro-lH-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, 1H-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [c] isothiazol-4-yl group, benzo [c] isothiazol-6-yl group, benzo [c] isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1H-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, lH-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, lH-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2, 3-b]pyridin-5-yl group, 1, 3-dihydroppyrrolo[2,3-b]pyridin-4-yl group, 1, 3-dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3, 2-c] pyridin-6-yl group, 1H-pyrrolo [3, 2-c] pyridin-4-yl group, lH-pyrrolo [2, 3-c] pyridin-5-yl group, 1H-pyrrolo [2, 3-c]pyridin-45-yl group, 1H-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazolo [4, 3-b] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [4, 3-clpyridin-4-yl group, 1H-pyrazolo [3, 4-c]pyridin-5-yl group, 1H-pyrazolo [3, 4-c] pyridin-4-yl group, lH-pyrazolo [3, 4-b] pyridin-5-yl group, lH-pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2-c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b] pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3, 2-b]pyridinb-6-yl group, 1H-thieno [3, 2-c]pyrazol-5-yl group, 1H-thieno [3, 2-c] pyrazol-4-yl group, benzo [d] isoxazol-5-yl group, benzo [d] isoxazol-4-yl group, benzo [d] isoxazol-6-yl group, benzo [d] isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c] isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5-yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3, 4-d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, lH-pyrazolo [3, 4-b] pyrazin-5-yl group, lH-imidazo [4, 5-b] pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (these groups may be substituted with one of Xa or two or more of the same or different Xa). The substituent Xa represents a group as any one of oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N, N-dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, and N, N-dimethylcarbamoyl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In another preferred embodiment of the present invention, the compound represented by the formula (1) or a salt thereof satisfies all of the following requirements.

Link represents-(CH2) n-, symbol n represents an integer of 1 to 3.

AR binds to C3, Rs binds to any of the atoms C4, C5, and C6, and a ring-constituting carbon atom to which Rs does not bind among C4, C5, and C6 may be replaced with V.

V represents nitrogen atom, or carbon atom substituted with Zx, and Zx represents a group as any one of fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N-dimethylsulfamoylamino group.

Rs represents-D-Rx, or-N (Ry) (Rz). D represents oxygen atom, or sulfur atom. Rx represents butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-cyclopentylethyl group, or 2-cyclohexylethyl group, or represents Rb, or Rc. Q in Rb represents a group as any one of phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, and dihydrobenzodioxyl group. A2 represents a single bond, oxygen atom, sulfur atom,-N (methyl)-, or -N (ethyl)- (provided that when A2 represents oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)-, A1 represents ethylene). R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q represents phenyl group, A1 represents a single bond, or unsubstituted methylene, and A2 represents a single bond, one of R2 and R3 represents a substituent other than hydrogen atom). Symbol p in Rc represents an integer of 2 or 3, and A4 represents a single bond or methylene. A5 represents -C (O)-,-C (S)-, or-S (0) 2-. Rd represents hydrogen atom, or a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, and pyridin-4-yl group. Re represents a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4-chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N-(pyridin-2-yl) amino group, N-(pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2-yl) amino group, N- (furan-3-yl) amino group, N-(thiophen-2-yl) amino group, N-(thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, and ethyloxycarbonylamino group. Rz represents a group as any of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, l' (4'fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4'chlorophenyl) ethyl group, 2-[2-(trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4'methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4-chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4-fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N-isobutylthiocarbamoyl group, t-butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N-cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N-cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N-cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N'phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4-methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4-chlorophenyl) carbamoyl group, N-(4-chlorophenyl)thiocarbamoyl group, 4-fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4-fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-l-yl) carbonyl group, and (morpholino-4-yl) carbonyl group. Ry represents hydrogen atom, methyl group, ethyl group, or isobutyl group, or binds to Rz to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol-1-yl group, or pyrazol-1-yl group together with the nitrogen atom to which they binds.

AR represents naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro-lH-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, 1H-indazol-5-yl group, lH-indazol-4-yl group, lH-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [c] isothiazol-4-yl group, benzo [c] isothiazol-6-yl group, benzo [c] isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo[1,2-a]pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1H-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, lH-benzimidazol-5-yl group, lH-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, lH-pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, lH-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1, 3-dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, lH-pyrrolo [3, 2-c] pyridin-6-yl group, lH-pyrrolo [3, 2-c] pyridin-4-yl group, lH-pyrrolo [2, 3-c] pyridin-5-yl group, 1H-pyrrolo [2, 3-c] pyridin-4-yl group, 1H-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazolo [4, 3-b] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-4-yl group, lH-pyrazolo [3, 4-c]pyridin-5-yl group, 1H-pyrazolo [3, 4-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H-pyrazolo [3, 4-b]pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2-c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b]pyridin-2-yl group, thieno [3, 2-b]pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3, 2-b] pyridin-6-yl group, lH-thieno [3, 2-c] pyrazol-5-yl group, 1H-thieno [3, 2-c] pyrazol-4-yl group, benzo [d] isoxazol-5-yl group, benzo [d] isoxazol-4-yl group, benzo [d] isoxazol-6-yl group, benzo [d] isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c] isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5-yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3, 4-d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, 1H-pyrazolo [3, 4-b] pyrazin-5-yl group, 1H-imidazo [4, 5-b] pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa). The substituent Xa represents a group as any one of oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N, N-dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, and N, N-dimethylcarbamoyl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In a preferred embodiment of the present invention, a compound or a salt thereof satisfying all of the following requirements is excluded from the compound represented by the formula (I) or a salt thereof.

Link represents- (CH2) n-, symbol n represents an integer of 1 to 3.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, C5 represents a ring-constituting carbon atom which may be substituted with Zx, and C2 and C6 represent unsubstituted ring-constituting carbon atom.

Zx represents fluorine atom, chlorine atom, nitro group, amino group, methyl group, or a OR9 group, and R9 represents hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms.

Rs represents-O-Rx. Rx represents a linear or branched saturated alkyl group having 3 to 8 carbon atoms, or represents Ra or Rb, Q in Rb represents a residue of a partially unsaturated or completely unsaturated monocyclic or condensed bicyclic carbon ring or heterocyclic ring (q), and binds to A2 at an arbitrary position on the ring. The heterocyclic ring (q) contains one or two of the same or different ring-constituting heteroatoms selected from the group consisting of nitrogen atom, oxygen atom, and sulfur atom.

AR represents a residue of naphthalene, benzofuran, benzo [b] thiophene, indole, benzothiazole, dihydro-3H-benzothiazole, quinoline, dihydro-lH-quinoline, benzo [d] isothiazole, IH-indazole, benzo [c] isothiazole, 2H-indazole, imidazo [1, 2-a] pyridine, lH-pyrrolo [2, 3-b] pyridine, isoquinoline, or dihydro-2H-isoquinoline (the aforementioned residue may be substituted with one of Xa or two or more of the same or different Xa).

In another preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents-(CH2) n-, symbol n represents an integer of 1 to 3.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, C5 may be replaced with V, and C2 and C6 represent unsubstituted ring-constituting carbon atom.

V represents nitrogen atom, or carbon atom substituted with Zx, and Zx represents a group as any one of fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N-dimethylsulfamoylamino group.

Rs represents'O'Rx. Rx represents butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-cyclopentylethyl group, or 2-cyclohexylethyl group, or represents Rb or Rc. Q in Rb represents a group as any one of phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, and dihydrobenzodioxyl group. A2 represents a single bond, oxygen atom, sulfur atom, -N (methyl)-, or-N (ethyl)- (provided that when A2 represents oxygen atom, sulfur atom, -N (methyl) -, or-N (ethyl)-, A1 represents ethylene). R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q represents phenyl group, Al represents a single bond, or unsubstituted methylene, and A2 represents a single bond, one of R2 and R3 represents a substituent other than hydrogen atom). Symbol p in Rc represents an integer of 2 or 3, and A4 represents a single bond or methylene.

A5 represents-C (O)-,-C (S)-, or-S (0) 2-. Rd represents hydrogen atom, or a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, and pyridin-4-yl group. Re represents a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N' (4'methylphenyl) amino group, N- (4-chlorophenyl) amino group, N' (4-fluorophenyl) amino group, N-(pyridin-2-yl) amino group, N-(pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2-yl) amino group, N- (furan-3-yl) amino group, N-(thiophen-2-yl) amino group, N-(thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, and ethyloxycarbonylamino group.

AR represents any one of cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, lH-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, lH-pyrrolo [3, 2-b] pyridin-5-yl group, lH-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, lH-benzotriazol-5-yl group, lH-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1, 3-dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3, 2-c] pyridin-6-yl group, lH-pyrrolo [3, 2-c]pyridin-4-yl group, lH-pyrrolo [2, 3-c]pyridin-5-yl group, 1H-pyrrolo [2, 3-c] pyridin-4-yl group, 1H-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazolo [4, 3-b] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [4, 3-c]pyridin-4-yl group, 1H-pyrazolo [3, 4-c] pyridin-5-yl group, 1H-pyrazolo [3, 4-c] pyridin-4-yl group, lH-pyrazolo [3, 4-b] pyridin-5-yl group, 1H-pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2-c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b]pyridin-2-yl group, thieno [3, 2-b]pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3, 2-b]pyridin-6-yl group, 1H-thieno [3, 2-c]pyrazol-5-yl group, 1H-thieno [3, 2-c] pyrazol-4-yl group, benzo [d] isoxazol-5-yl group, benzo[d]isoxazol-4-yl group, benzo [d] isoxazol-6-yl group, benzo [d] isoxazol-7-yl group, benzo [c]isoxazol-5-yl group, benzo [c]isoxazol-4-yl group, benzo [c]isoxazol-6-yl group, benzo [c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5-yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3, 4-d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, 1H-pyrazolo [3, 4-b] pyrazin-5-yl group, lH-imidazo [4, 5-b] pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, and 4H-chromen-5-yl group (these groups may be substituted with one of Xa or two or more of the same or different Xa). The substituent Xa represents a group as any one of oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N, N-dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, and N, N-dimethylcarbamoyl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In another preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- H2) n-symbol n represents an integer of 1 to 3.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, C5 may be replaced with, and C2 and C6 represent unsubstituted ring-constituting carbon atom.

V represents nitrogen atom, or carbon atom substituted with Zx, and Zx represents a group as any one of, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N-dimethylsulfamoylamino group.

Rs represents-S-Rx. Rx represents butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-cyclopentylethyl group, or 2-cyclohexylethyl group, or represents Rb or Rc. Q in Rb represents a group as any one of phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, and dihydrobenzodioxyl group. A2 represents a single bond, oxygen atom, sulfur atom, - N (methyl), or-N (ethyl) - (provided that when A2 represents oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)-, A1 represents ethylene). R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q represents phenyl group, Al represents a single bond, or unsubstituted methylene, and A2 represents a single bond, one of R2 and R3 represents a substituent other than hydrogen atom). Symbol p in Rc represents an integer of 2 or 3, and A4 represents a single bond or methylene.

A5 represents-C (O)-,-C (S) -, or-S (0) 2-. Rd represents hydrogen atom, or a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, and pyridin-4-yl group. Re represents a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4-chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2-yl) amino group, N- (furan-3-yl) amino group, N-(thiophen-2-yl) amino group, N-(thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, and ethyloxycarbonylamino group.

AR represents naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7'yl group, dihydro-lH-quinolin-6-yl group, dihydro-lH-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, lH-indazol-5-yl group, 1H-indazol-4-yl group, lH-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [c] isothiazol-4-yl group, benzo [c] isothiazol-6-yl group, benzo [c] isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1H-pyrrolo [2, 3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, lH-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1, 3-dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [l, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, lH-pyrrolo [3, 2-c] pyridin-6-yl group, l H-pyrrolo [3, 2-c] pyridin-4-yl group, 1H-pyrrolo [2, 3-c] pyridin-5-yl group, 1H-pyrrolo [2, 3-c] pyridin-4-yl group, l H-pyrazolo [4, 3-b] pyridin-5-yl group, III-pyrazolo [4, 3-b] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-6-yl group, lH-pyrazolo [4, 3-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-c] pyridin-5-yl group, 1H-pyrazolo [3, 4-c]pyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H-pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2-c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b] pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3, 2-b]pyridin-6-yl group, lH-thieno [3, 2-c] pyrazol-5-yl group, lH-thieno [3, 2-c] pyrazol-4-yl group, benzo [d] isoxazol-5-yl group, benzo [d] isoxazol-4-yl group, benzo [d] isoxazol-6-yl group, benzo [d] isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c] isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5-yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3, 4-d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a]pyrimidin-6-yl group, 1H-pyrazolo [3, 4-b]pyrazin-5-yl group, 1H-imidazo [4, 5-b] pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (these groups may be substituted with one of Xa or two or more of the same or different Xa). The substituent Xa represents a group as any one of oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N-dimethylcarbamoylmethoxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N, N-dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, and N, N-dimethylcarbamoyl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In another preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- (CH2) n-, symbol n represents an integer of 1 to 3.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, and C2, C5 and C6 represent unsubstituted ring-constituting carbon atom.

Rs represents-N (Ry) (Rz). Rz represents a group as any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1-(3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2-[3-(trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2-(phenylthio) ethyl group, 2-(N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4-methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4-chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4-fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N-isobutylthiocarbamoyl group, t-butyloxycarbonyl group, N-t-butylcarbamoyl. group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N-cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N-cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N'cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N'phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4-methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4-chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4-fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4-fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-l-yl) carbonyl group, and (morpholino-4-yl) carbonyl group. Ry represents hydrogen atom, methyl group, ethyl group, or isobutyl group, or binds to Rz to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol-1-yl group, or pyrazol-1-yl group together with the nitrogen atom to which they bind.

AR represents naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro'lH'quinolin'6'yl group, dihydro-lH-quinolin-5-yl group, benzo [dlisothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d]isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, 1H-indazol-5-yl group, lH-indazol-4-yl group, 1H-indazol-6-yl group, benzo [c]isothiazol-5-yl group, benzo [c]isothiazol-4-yl group, benzo [c]isothiazol-6-yl group, benzo [c] isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, l H-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, l H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b]pyridin-4-yl group, 1, 3-dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, lH-pyrrolo [3, 2-c]pyridin-6-yl group, 1H-pyrrolo [3, 2-c] pyridin-4-yl group, 1H-pyrrolo [2, 3-c]pyridin-5-yl group, 1H-pyrrolo [2, 3-c] pyridin-4-yl group, 1H-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazolo [4, 3-b] pyridin-6-yl group, lH-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-c] pyridin-5-yl group, 1H-pyrazolo [3, 4-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H-pyrazolo [3, 4-b]pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a]pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2-c]pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b] pyridin-3-yl group, thieno [3, 2-b]pyridin-5-yl group, thieno [3, 2-b] pyridin-6-yl group, lH-thieno [3, 2-c] pyrazol-5-yl group, lH-thieno [3, 2-c] pyrazol-4-yl group, benzo [d]isoxazol-5-yl group, benzo [d]isoxazol-4-yl group, benzo [d]isoxazol-6-yl group, benzo [d]isoxazol-7-yl group, benzo [c]isoxoazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c]isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5-yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, lH-pyrazolo [3, 4-d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, 1H-pyrazolo [3, 4-b] pyrazin-5-yl group, 1H-imidazo [4, 5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (these groups may be substituted with one of Xa or two or more of the same or different Xa). The substituent Xa represents a group as any one of oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N, N-dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, and N, N-dimethylcarbamoyl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In another preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- (CH2) n-, symbol n represents an integer of 1 to 3.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, C5 may be replaced with V, and C2 and C6 represent unsubstituted ring-constituting carbon atom.

V represents nitrogen atom, or carbon atom substituted with Zx, and Zx represents a group as any one of chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N-dimethylsulfamoylamino group.

Rs represents-D-Rc, and D represents oxygen atom or sulfur atom. Symbol p in Rc represents an integer of 2 or 3, and A4 represents a single bond or methylene.

A5 represents-C (O)-,-C (S)-, or-S (0) 2-. Rd represents hydrogen atom, or a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, and pyridin-4-yl group. Re represents a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4'methylphenyl) amino group, N' (4-chlorophenyl) amino group, N' (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2-yl) amino group, N- (furan-3-yl) amino group, N-(thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, and ethyloxycarbonylamino group.

AR represents naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, lH-indazol-5-yl group, lH-indazol-4-yl group, 1H-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [c] isothiazol-4-yl group, benzo [c] isothiazol-6-yl group, benzo [c] isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1H-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7~yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, lH-pyrrolo [3, 2-b]pyridin-5-yl group, lH-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzol, 2,5] thiadiazol-4-yl group, lH-benzotriazol-5-yl group, lH-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-5-yl group, 1, 3-dihdyropyrrolo[2,3-b]pyridin-4-yl group, 1, 3-dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [l, 5] naphthalidin-4-yl group, 1H-pyrrolo [3, 2-c] pyridin-6-yl group, lH-pyrrolo [3, 2-c]pyridin-4-yl group, 1H-pyrrolo [2, 3-c] pyridin-5-yl group, 1H-pyrrolo [2, 3-c] pyridin-4-yl group, 1H-pyrazolo [4, 3-b] pyridin-5-yl group, lH-pyrazolo [4, 3-b] pyridin-6-yl group, 1H-pyrazolo [4, 3-c] pyridin-6-yl group, 1H-pyrazolo [4, 3-c]pyridiin-4-yl group, 1H-pyrazolo [3, 4-c] pyridin-5-yl group, 1H-pyrazolo [3, 4-clpyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H-pyrazolo [3, 4-b]pyrridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2-c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b] pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3, 2-b] pyridin-6-yl group, 1H-thieno [3, 2-c] pyrazol-5-yl group, 1H-thieno [3, 2-c] pyrazol-4-yl group, benzo [d] isoxazol-5-yl group, benzo [d]isoxazol-4-yl group, benzo [d]isoxazol-6-yl group, benzo [d]isoxazol-7-yl group, benzo [c]isoxazol-5-yl group, benzo [c]isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c] isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5-yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3, 4-d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo[1,5-a]pyrimidin-6-yl group, lH-pyrazolo [3, 4-b] pyrazin-5-yl group, 1H-imidazo [4, 5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (these groups may be substituted with one of Xa or two or more of the same or different Xa). The substituent Xa represents a group as any one of oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N, N-dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, and N, N-dimethylcarbamoyl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In another preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link is- (CH2) n-, n is an integer of 1 to 3, C3 is carbon atom bound with AR, C4 is carbon atom bound with Rs, C5 may be replaced with V, C2 and C6 are unsubstituted ring-constituting carbon atoms, V is nitrogen atom or V is carbon atom substituted with Zx, Zx is any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, or N, N-dimethylamino group, Rs is-D-Rx, D is a single bond, Rx is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-cyclopentylethyl group, or 2-cyclohexylethyl group, or Rx is Rb or Rc (provided that Q in Rb is phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, or dihydrobenzodioxyl group), A2 is a single bond, oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)- (provided that when A2 represents oxygen atom, sulfur atom,-N (methyl)- or - N (ethyl) -, A1 represents ethylene), R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group, p in Rc is an integer of 2 or 3, A4 is a single bond or methylene, A5 is-C (O)-,-C (S) -, or -S (0) 2-, Rd is hydrogen atom, or methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, or pyridin-4-yl group, Re is methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4-chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2-yl) amino group, N- (furan-3-yl) amino group, N- (thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, or ethyloxycarbonylamino group, AR is naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [blthiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro-lH-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, lH-indazol-5-yl group, 1H-indazol-4-yl group, 1H-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [c] isothiazol-4-yl group, benzo [c]isothiazol-6-yl group, benzo [c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, lH-pyrrolo [2, 3-b]pyriodin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, lH-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, lH-benzotriazol-5-yl group, lH-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1, 3-dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3, 2-c] pyridin-6-yl group, 1H-pyrrolo [3, 2-c] pyridin-4-yl group, 1H-pyrrolo [2, 3-c] pyridin-5-yl group, 1H-pyrrolo [2, 3-c] pyridin-4-yl group, lH-pyrazolo [4, 3-b] pyridin-5-yl group, 1H-pyrazolo [4, 3-b]pyridin-6-yl group, lH-pyrazolo [4, 3-c]pyridin-6-yl group, lH-pyrazolo [4, 3-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-c] pyridin-5-yl group, 1H-pyrazolo [3, 4-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-b] pyridin-5-yl group, 1H-pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2-c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b] pyridin-3-yl group, thieno [3, 2-b]pyridin-5-yl group, thieno [3, 2-b] pyridin-6-yl group, 1H-thieno [3, 2-c] pyrazol-5-yl group, 1H-thieno [3, 2-c]pyrazol-4-yl group, benzo [d] isoxazol-5-yl group, benzo [d]isoxazol-4-yl group, benzo [d] isoxazol-6-yl group, benzo [d] isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c] isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5-yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3, 4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a]pyrimidin-6-yl group, 1H-pyrazolo [3, 4-b]pyrazin-5-yl group, 1H-imidazo [4, 5-b]pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, or 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of the same or different Xa), Xa is oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N, N-dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, or N, N-dimethylcarbamoyl group, and Y is hydrogen atom, methyl group, or ethyl group.

In a particularly preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- (CH2) n-, symbol n represents an integer of 2.

C2 represents carbon atom to which AR bonds, C3 represents carbon atom to which Rs bonds, C4 may be replaced with V, and C5 and C6 represent unsubstituted ring-constituting carbon atom.

V represents nitrogen atom, or carbon atom substituted with Zx, and Zx represents a group as any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, and N, N-dimethylamino group.

Rs represents-O-Rx. Rx represents a group as any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2-(2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2-(4-chlorophenyl) ethyl group, 2-[2-(trifluoromethyl)phenyl]ethyl group, 2- [3- (trifluoromethyl) phenyl ethyl group, 2- [4- (trifluoromethyl) phenyll ethyl group, 2- [4- (N, N- dimethylamino) phenyll ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

AR represents a group as any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydoryxethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, lH-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-1H-indol-5-yl group, 1, 3-dimethyl-1H-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, l-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, l-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-porpyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2, 3-dimethyl-1-propyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a3pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, l-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, l'oxo'l, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In another particularly preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents -(CH2) n, symbol n represents an integer of 2.

C2 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, C5 may be replaced with V, and C3 and C6 represent unsubstituted ring-constituting carbon atom.

V represents nitrogen atom, or carbon atom substituted with Zx, and Zx represents a group as any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, and N, N-dimethylamino group.

Rs represents-O-Rx. Rx represents a group as any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1-(3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1-(2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2-(4-methoxyphenyl)ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyll ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2-(N-phenyl-N-methylamino) ethyl group, and 2-(N-ethyl-N-phenylamino) ethyl group.

AR represents a group as any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy)naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6-(2-hydroxyethylamino)naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, lH-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1H-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-1H-indol-5-yl group, 1, 3-dimethyl-1H-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, l-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-lH-indol-5-yl group, l-ethyl-3-methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-lH-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1-methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, l-ethyl-3-hydroxy-lH-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-IH-pyrrolo [2, 3-b]pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In another particularly preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- (CH2) n-, symbol n represents an integer of 2.

C3 represents carbon atom to which AR bonds, C5 represents carbon atom to which Rs bonds, and C2, C4 and C6 represent unsubstituted ring-constituting carbon atom.

Rs represents'O'Rx. Rx represents a group as any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1-(3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2-(trifluoromethyl)phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyll ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2-(phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

AR represents a group as any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydorxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzolb] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, lH-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2, 3-dimethyl-1H-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-1H-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, l-ethyl-2, 3-dimethyl-1H-indol-5-yl group, l-propyl-lH-indol-5-yl group, 2-methyl-l-propyl-lH-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1-methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, l-propyl-lH-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroyx-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo [2, 3-b]pyridin-5-yl group, isoquinolin-6-yl group, l-oxorl, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In another particularly preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- (CH2) n-, symbol n represents an integer of 2.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, C5 represents nitrogen atom, and C2 and C6 represent unsubstituted ring-constituting carbon atom.

Rs represents-O-Rx. Rx represents a group as any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, l- (2-fluorophenyl) ethyl group, l- (3-fluorophenyl) ethyl group, l- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4-(trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2-(2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2-(phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

AR represents a group as any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6-(2-hydoryxethylamino)naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo[b]furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzolb] thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-lH-indol-5-yl group, 1-ethyl-3-methyl-lH-indol-5-yl group, l-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-IH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-1H-pyrrolo [2, 3-b]pyridin-5-yl group, 1- (2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In another preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- (CH2) n-, symbol n represents an integer of 2.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, C6 represents carbon atom substituted with Zx, and C2 and C5 represent unsubstituted ring-constituting carbon atom.

Zx represents fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, or N, N-dimethylamino group.

Rs represents'O'Rx. Rx represents a group as any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2Eyl group, 4, 7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, l' (3'chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3-(trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2-(4-fouorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4-(trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

AR represents a group as any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo[b]furan-5-yl group, 3-methylbenzo lb] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, lH-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, l-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-l-propyl-lH-indol-5-yl group, 2, 3-dimethyl-l-propyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d]isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazoll, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-lH-pyrrolo [2, 3-b]pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b]pyridin-5-yl group, l-propyl-lH-pyrrolo [2, 3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo [2, 3-b]pyrridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In another particularly preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- (CH2) n-symbol n represents an integer of 2.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, and C2, C5 and C6 represent unsubstituted ring-constituting carbon atom.

Rs represents-N (Ry) (Rz). Rz represents a group as any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5'dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4-methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4-chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4'fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N-isobutylthiocarbamoyl group, t-butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N-cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N-cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N-cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N-phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4-methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4-chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4-fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4-fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-1-yl) carbonyl group, and (morpholino-4-yl) carbonyl group. Ry represents hydrogen atom, methyl group, ethyl group, or isobutyl group, or binds to Rz to form pyrrolidino group, piperidino group, or morpholino group together with nitrogen atom to which they bonds.

AR represents a group as any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [blfuran-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1,2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-lH-indol-5-yl group, l-ethyl-2-methyl-lH-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1-methyl-lH-indazol-5-yl group, 1-ethyl-lH-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, l'oxo'l, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In another particularly preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- (CH2) n-, symbol n represents an integer of 2.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, and C2, C5 and C6 represent unsubstituted ring-constituting carbon atom.

Rs represents-N (Ry) (Rz). -N (Ry) (Rz) is any one of N, N-dimethylamino group, N-ethyl-N-methylamino group, N, N-diethylamino group, N-methyl-N-propylamino group, N-ethyl-N-propylamino group, N-isopropyl-N-methylamino group, N-ethyl-N-isopropylamino group, N-butylamino group, N-butyl-N-methylamino group, N-butyl-N-ethylamino group, N-isobutylamino group, N-isobutyl-N-methylamino group, N-ethyl-N-isobutylamino group, N- (2-ethylbutyl) amino group, N- (2-ethylbutyl)-N-methylamino group, N-cyclopentylamino group, N-cyclopentyl-N-methylamino group, N-cyclohexylamino group, N-cyclohexyl-N-methylamino group, N-cycloheptylamino group, N' (cyclopentylmethyl) amino group, N- (cyclopentylmethyl)-N-methylamino group, N- (cyclohexylmethyl) amino group, N-(cyclohexylmethyl)-N-methylamino group, N- (2-methylphenyl) amino group, N- (4-methylphenyl) amino group, N- (2-fluorophenyl) amino group, N- (3-fluorophenyl) amino group, N- 4-fluorophenyl) amino group, N- (2-chlorophenyl) amino group, N- (3-chlorophenyl) amino group, N- (4-chlorophenyl) amino group, N-(indan-2-yl) amino group, N- (1-phenylethyl) amino group, N- [1- (2-fluorophenyl) ethyl] amino group, N- [1- (3-fluorophenyl) ethyl] amino group, N- [1- (4-fluorophenyl) ethyl] amino group, N- [1- (2-chlorophenyl) ethyl] amino group, N- [1- (3-chlorophenyl) ethyl] amino group, N- [1- (4-chlorophenyl) ethyl] amino group, N- (2-methylphenylmethyl) amino group, N-methyl-N- (2-methylphenylmethyl) amino group, N- (3-methylphenylmethyl) amino group, N-methyl-N- (3-methylphenylmethyl) amino group, N- (4-methylphenylmethyl) amino group, N-methyl-N- (4-methylphenylmethyl) amino group, N- (2-fluorophenylmethyl) amino group, N- (2-fluorophenylmethyl)-N-methylamino group, N- (3-fluorophenylmethyl) amino'group, N- (3-fluorophenylmethyl)-N-methylamino group, N- (4-fluorophenylmethyl) amino group, N- (4-fluorophenylmethyl)-N-methylamino group, N- (2-chlorophenylmethyl) amino group, N- (2-chlorophenylmethyl)-N-methylamino group, N- (3-chlorophenylmethyl) amino group, N- (3-chlorophenylmethyl)-N-methylamino group, N- (4-chlorophenylmethyl) amino group, N- (4-chlorophenylmethyl)-N-methylamino group, N- (2, henylmethyl) amino group, N- (2, 3-difluorophenylmethyl)-N-methylamino group, N- (2, 4-difluorophenylmethyl) amino group, N- (2, 4-difluorophenylmethyl)-N-methylamino group, N- (2, 5-difluorophenylmethyl) amino group, N- (2,5-difluorophenylmethyl)-N-methylamino group, N- (3, 4-difluorophenylmethyl) amino group, N- (3, 4-difluorophenylmethyl)-N-methylamino group, N- (3, 5-difluorophenylmethyl) amino group, N- (3, 5-difluorophenylmethyl)-N-methylamino group, N- (2, 3-dichlorophenylmethyl) amino group, N- (2, 3-dichlorophenylmethyl)-N-methylamino group, N- (2, 4-dichlorophenylmethyl) amino group, N- (2,4-dichlorophenylmethyl)-N-methylamino group, N- (2, 5-dichlorophenylmethyl) amino group, N- (2, 5-dichlorophenylmethyl)-N-methylamino group, N- (2, 6-dichlorophenylmethyl) amino group, N- (2, 6-dichlorophenylmethyl)-N-methylamino group, N- (3, 4-dichlorophenylmethyl) amino group, N- (3, 4-dichlorophenylmethyl)-N-methylamino group, N- (3, 5-dichlorophenylmethyl) amino group, N- (3,5-dichlorophenylmethyl)-N-methylamino group, N- [2- (trifluoromethyl) phenylmethyl] amino group, N-methyl-N- [2- (trifluoromethyl) phenylmethyll amino group, N- [3- (trifluoromethyl) p henylmethyl] amino group, N-methyl-N- [3- (trifluoromethyl) phenylmethyll amino group, N- [4- (trifluoromethyl) p henylmethyl] amino group, N-methyl-N- [4- (trifluoromethyl) phenylmethyl] amino group, 1'pyrrolidino group, 1- (4-methylpiperidino) group, 1-homopiperidino group, or 4-morpholino group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzolb] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, lH-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1, 2-dimethyl-lH-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-lH-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-lH-indol-5-yl group, 2, 3-dimethyl-1-propyl-lH-indol-5-yl group, 1-(2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3'dimethyl'l' (2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-lH-indazol-5-yl group, 1-ethyl-lH-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b]pyridin-5-yl group, 1-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b]pyrridin-5-yl group, 1-propyl-lH-pyrrolol2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

In another particularly preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- (CH2) n-, symbol n represents an integer of 2.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, C5 represents carbon atom substituted with Zx, and C2 and C6 represent unsubstituted ring-constituting carbon atom.

Zx represents N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N-dimethylsulfamoylamino group.

Rs represents'O'Rx. Rx represents a group as any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2-(2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

AR represents a group as any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6-(2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, lH-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1H-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-1H-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1,2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, l-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-lH-indol-5-yl group, 2, 3-dimethyl-1-propyl-lH-indol-5-yl group, 1-(2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-IH-indol-5-yl group, 2, 3'dimethyl'l' (2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [dlisothiazol-5-yl group, lH-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In another particularly preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- (CH2) n-, symbol n represents an integer of 2.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, C5 may be replaced with V, and C2 and C6 represent unsubstituted ring-constituting carbon atom.

V represents nitrogen atom, or carbon atom substituted with Zx, and Zx represents a group as any one of chlorine atom, bromine atom, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N-dimethylsulfamoylamino group.

Rs represents-O-Rc. p in Rc represents an integer of 2, and A4 represents a single bond or methylene. A5 represents-C (O)-,-C (S)-, or-S (O) 2-. Rd represents a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, and 4-fluorophenylmethyl group. Re represents a group as any one of isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N' (4'methylphenyl) amino group, N- (4-chlorophenyl) amino group, N- (4-fluorophenyl) amino group, pyrrolidino group, piperidino group, and morpholino group.

AR represents a group as any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b]thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, lH-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1H-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1,2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-lH-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, l-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-lH-indol-5-yl group, 2-methyl-l-propyl-lH-indol-5-yl group, 3-methyl-l-propyl-lH-indol-5-yl group, 2, 3-dimethyl-l-propyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-IH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2-, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1-methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yl group.

The group Y represents hydrogen atom, methyl group, or ethyl group.

In another particularly preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents -(CH2)n-, symbol n represents an integer of 2.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, C5 may be replaced with V, and C2 and C6 represent unsubstituted ring-constituting carbon atom.

V represents nitrogen atom, or carbon atom substituted with Zx, Zx is any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, or N, N-dimethylamino group, Rs represents-D-Rx and D represents a single bond. Rx is butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 2-methylphenyl group, 3-methylphenyl group, 4-methylphenyl group, 2,3-dimethylphenyl group, 3,5-dimethylphenyl group, 2-methoxyphenyl group, 3-methoxyphenyl group, 4-methoxyphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2,3-difluorophenyl group, 2, 4-difluorophenyl group, 2, 5-difluorophenyl group, 3,4-difluorophenyl group, 2, 3-dichlorophenyl group, 2, 4-dichlorophenyl group, 2, 5-dichlorophenyl group, 2, 6-dichlorophenyl group, 3, 4-dichlorophenyl group, 3, 5-dichlorophenyl group, 2-trifluoromethylphenyl group, 3-trifluoromethylphenyl group, 4-trifluoromethylphenyl group, 4- (N, N-dimethylamino) phenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, naphthalen-1-yl group, naphthalen-2-yl group, lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, biphenyl-2-yl group, biphenyl 3-yl group, biphenyl-4-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2-(2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, or 2- (N-ethyl-N-phenylamino) ethyl group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b]thiophen-5-yl group, 3-methylbenzo [b]thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, lH-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol-5-yl group, 1, 3-dimethyl-1H-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, l-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-lH-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, l-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-l-propyl-lH-indol-5-yl group, 3-methyl-l-propyl-lH-indol-5-yl group, 2, 3-dimethyl-1-propyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, l-ethyl-lH-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, l-ethyl-3-hydroxy-lH-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2,3-b] pyridin-5-yl group, l-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

In another particularly preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- (CH2) n-, symbol n represents an integer of 2.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, C5 may be replaced with V, and C2 and C6 represent unsubstituted ring-constituting carbon atom.

V represents nitrogen atom, or carbon atom substituted with Zx, Zx is any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, or N, N-dimethylamino group, Rs represents-D-Rx and D represents a single bond. Rx is phenyl group, 2-methylphenyl group, 3-methylphenyl group, 4-methylphenyl group, 2, 3-dimethylphenyl group, 3,5-dimethylphenyl group, 2-methoxyphenyl group, 3-methoxyphenyl group, 4-methoxyphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2,3-difluorophenyl group, 2,4-difluorophenyl group, 2,5-difluorophenyl group, 3, 4-difluorophenyl group, 2, 3-dichlorophenyl group, 2, 4-dichlorophenyl group, 2, 5-dichlorophenyl group, 2, 6-dichlorophenyl group, 3,4-dichlorophenyl group, 3,5-dichlorophenyl group, 2-trifluoromethylphenyl group, 3-trifluoromethylphenyl group, 4-trifluoromethylphenyl group, 4- (N, N-dimethylamino) phenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, naphthalen-1-yl group, naphthalen-2-yl group, 1H-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1H-indazol-5-yl group, or 1-methyl-1H-indazol-5-yl group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6-(N-methylamino) naphthalen-2-yl group, 6-(N,N-dimethylamino)naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [blfuran-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo[b]thiophen-5-yl group, lH-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1,2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-lH-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, l-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-lH-indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1 (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-lH-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-1H-pyrrolo [2, 3-b]pyridin-5-yl group, 1- (2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

In another particularly preferred embodiment of the present invention, the compound represented by the formula (I) or a salt thereof satisfies all of the following requirements.

Link represents- (CH2) n-, symbol n represents an integer of 2.

C3 represents carbon atom to which AR bonds, C4 represents carbon atom to which Rs bonds, and C2, C5, and C6 represent unsubstituted ring-constituting carbon atom.

Rs represents-D-Rx and D represents a single bond. Rx is phenyl group, 2-methylphenyl group, 3-methylphenyl group, 4-methylphenyl group, 2, 3-dimethylphenyl group, 3,5-dimethylphenyl group, 2-methoxyphenyl group, 3-methoxyphenyl group, 4-methoxyphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, 2, 3-difluorophenyl group, 2,4-difluorophenyl group, 2,5-difluorophenyl group, 3,4-difluorophenyl group, 2, 3-dichlorophenyl group, 2, 4-dichlorophenyl group, 2, 5-dichlorophenyl group, 2, 6-dichlorophenyl group, 3, 4-dichlorophenyl group, 3, 5-dichlorophenyl group, 2-trifluoromethylphenyl group, 3-trifluoromethylphenyl group, 4-trifluoromethylphenyl group, 4-(N, N-dimethylamino) phenyl group, indan-2-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, naphthalen-1-yl group, naphthalen-2-yl group, lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, lH-indazol-5-yl group, or 1-methyl-lH-indazol-5-yl group, AR is naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6-(2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-1H-indol-5-yl group, 1, 2-dimethyl-1H-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, l-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-lH-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-lH-indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a]pyridin-6-yl group, 1H-pyrrolo [2,3-b]pyridin-5-yl group, l-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, or benzoxazol-5-yl group, and Y is hydrogen atom, methyl group, or ethyl group.

Compound (I) of the present invention may have one or more asymmetric carbons depending on types of substituents. For example, as for a compound wherein the group Rs contains one or more asymmetric carbons, two kinds of optical isomers exist when the number of asymmetric carbon is 1, and when the number of asymmetric carbons is 2, four kinds of optical isomers and two kinds of diastereomers exist. Pure stereoisomers including optical isomers and diastereoisomers, any mixtures thereof, racemates and the like of the stereoisomers fall within the scope of the present invention. Further, Compound (I) of the present invention may exist as geometrical isomers based on a cycloalkyl ring structure, and any geometrical isomers in pure forms, and any mixtures of the geometrical isomers also fall within the scope of the present invention. Mixtures such as racemates may sometimes be preferred from a viewpoint of easiness for manufacture.

As a salt of Compound (I) of the present invention, a pharmaceutically acceptable salt is preferred. It is meant that, when at least one of the conditions (1) to (3) is satisfied: (1) Y is hydrogen atom ; (2) the group AR contains carboxyl group or phenolic hydroxyl group ; (3) the group Zx is phenolic hydroxyl group, and the like, then the compound forms 1 to 3 alkali salts depending on the number of acidic groups. Examples the alkali salts include, for example, salts with inorganic bases such as sodium and ammonia and salts with organic bases such as triethylamine.

Alternatively, it is meant that, when at least one of the conditions (1) to (4) is satisfied : (1) the group Rs has properties as a base as in a compound wherein Rs contains a substituted or unsubstituted amino group and the like ; (2) AR itself is a cyclic substituent having properties as a base ; (3) the group Ar contains a substituted or unsubstituted amino group ; (4) any carbon atom in the aromatic ring (E) is replaced with V, and V is nitrogen atom, V is carbon atom substituted with Zx, and Zx is a substituted or unsubstituted amino group and the like, then the compound forms 1 to 4 acidic salts depending on the number of basic groups.

Examples of the acidic salts include, for example, salts with inorganic acids such as hydrochloric acid and sulfuric acid and salts with organic acids such as acetic acid and citric acid.

C2', C3', C4', C5', and C6'in the aromatic ring (E') in the aforementioned formula (II) each represent a ring-constituting carbon atom. Among them, any ring-constituting carbon atom to which Rs'and G do not bind may be replaced with V. The substitution positions of Rs', G, and V are similar to those described in the explanations of the substitution positions of Rs (corresponding to the position of Rs'), AR (corresponding to the position of the group G), and V (corresponding to the position of V') in the aforementioned formula (I).

V'represents nitrogen atom, or represents carbon atom substituted with Zx'.

Zx'has the same meaning as that of Zx, provided that when Zx contains hydroxyl group (OH), the hydroxyl group may be protected with Rpl, and when Zx contains amino group (NH), the amino group may be protected with Rp2.

Rs'represents-D-Rx'or-N (Ry') (Rz'). -D-Rx'and-N (Ry') (Rz') have the same meanings as those of-D-Rx and-N (Ry) (Rz) mentioned above, respectively.

Provided that when-D-Rx and-N (Ry) (Rz) contain hydroxyl group, the hydroxyl group may be protected with Rpl, and when-D-Rx and-N (Ry) (Rz) contains amino group (NH), the amino group may be protected with Rp2.

Rpl represents, for example, a silyl group substituted with 3 of identical or different linear or branched saturated alkyl groups having 1 to 4 carbon atoms or phenyl groups, tetrahydropyranyl group, tetrahydrofuryl group, allyl group, propargyl group, benzyl group which may be substituted with one Tl or two or more identical or different T1,-CH2-U-Rp3,-C (O) Rp3, -C (O) ORp3, or the like. U represents oxygen atom, or sulfur atom, and Rp3 represents hydrogen atom, a linear or branched saturated alkyl group having 1 to 4 carbon atoms, trimethylsilylethyl group, chloromethyl group, trichloromethyl group, trifluoromethyl group, 9-fluorenylmethyl group, adamantyl group, allyl group,-A6-Qp, or the like. Rp2 represents, for example, benzyl group which may be substituted with one of T1 or two or more of identical or different T,-C (O) Rp3, -C (O) ORp3, or the like. However, the protective groups of hydroxyl group and amino group are not limited to these, and they can be chosen by referring and examining methods for introduction of protective groups and deprotection described in usual publications in the chemical field, for example, Protective Groups In Organic Synthesis, THIRD EDITION, published by John Wiley & Sons or the references cited therein.

G represents chlorine atom, bromine atom, iodine atom, mesylate group, triflate group, or an arenesulfonate group of which aromatic moiety may be substituted with one of T1 or two or more identical or different Tl. Examples of the arenesulfonate group include, for example, benzenesulfonate group, p-toluenesulfonate group, mesitylenesulfonate group, 2,4, 6-triisopropylbenzenesulfonate group, 4-fluorobenzenesulfonate group, 2, 5-dichlorobenzenesulfonate group, 3- (trifluoromethyl) benzenesulfonate group, pentafluorobenzenesulfonate group, 2-nitrobenzenesulfonate group, 2, 4-dinitrobenzenesulfonate group, and the like. Preferred examples of G include chlorine atom, bromine atom, iodine atom, triflate group, and the like, and bromine atom and iodine atom are particularly preferred examples.

Y'represents a lower alkyl group having 1 to 4 carbon atoms. Examples of the lower alkyl group having 1 to 4 carbon atoms include methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, and the like. Among these, methyl group, and ethyl group are particularly preferred examples.

In the aforementioned formula (II), n and D have the same meaning as defined above.

In a preferred embodiment, the compound represented by the formula (II) satisfies all of the following requirements.

Symbol n represents an integer of 1 to 3.

The group G binds to C2', Rs'binds to any of the atoms C3', C4'and C5', and a ring-constituting carbon atom to which Rs'does not bind among C3', C4', and C5'may be substituted with V'.

V'represents nitrogen atom, or carbon atom substituted with Zx', and Zx' represents any one of fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N-dimethylsulfamoylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituted Zx' contains amino group, the amino group may be protected with Rp2.

Rs'represents-D-Rx'or-N (Ry') (Rz'). D represents oxygen atom or sulfur atom. Rx'represents butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-cyclopentylethyl group, or 2-cyclohexylethyl group, or represents Rb or Rc. Q in Rb represents a group as any one of phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, and dihydrobenzodioxyl group. A2 represents a single bond, oxygen atom, sulfur atom,-N (methyl)-, or -N (ethyl)- (provided that when A2 represents oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)-, Al represents ethylene). R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q represents phenyl group, A1 represents a single bond, or unsubstituted methylene, and A2 represents a single bond, one of R2 and R3 represents a substituent other than hydrogen atom). Symbol p in Rc represents an integer of 2 or 3, and A4 represents a single bond or methylene. A5 represents -C (O)-,-C (S) -, or-S (0) 2-. Rd represents hydrogen atom, or a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, and pyridin-4-yl group. Re represents any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4-chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N-(pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2-yl) amino group, N- (furan-3-yl) amino group, N-(thiophen-2-yl) amino group, N-(thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, and ethyloxyearbonylamino group. Rz'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyllethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4-methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4-chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4-fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N-isobutylthiocarbamoyl group, t-butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N-cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N-cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group,- N-cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N'phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4-methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4-chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4-fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4-fluorophenyl) thiocarbamoyl group, (pyrrolidino-l-yl) carbonyl group, (piperidino-1-yl) carbonyl group, and (morpholino-4-yl) carbonyl group. Ry' represents hydrogen atom, methyl group, ethyl group, or isobutyl group, or binds to Rz'to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol-1-yl group, or pyrazol-1-yl group together with the nitrogen atom to which they bonds. Provided that when-D-Rx'or-N (Ry') (Rz') contains hydroxyl group (OH), the hydroxyl group may be protected with Rpl, and when-D-Rx'or-N (Ry') (Rz') contains amino group, the amino group may be protected with Rp2.

The group G represents chlorine atom, bromine atom, iodine atom, or triflate group.

The group Y'represents methyl group, or ethyl group.

In another preferred embodiment, the compound represented by the formula (II) satisfies all of the following requirements.

Symbol n represents an integer of 1 to 3.

The group G binds to C3', Rs'binds to any of the atoms C4', C5', and C6', and a ring-constituting carbon atom to which Rs'does not bind among C4', C5'and C6'may be replaced with V'.

V'represents nitrogen atom, or carbon atom substituted with Zx', and Zx' represents any one of fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N-dimethylsulfamoylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituted Zx' contains amino group, the amino group may be protected with Rp2.

Rs'represents-D-Rx', or-N (Ry') (Rz'). D represents oxygen atom or sulfur atom. Rx'represents butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-cyclopentylethyl group, or 2-cyclohexylethyl group, or represents Rb or Rc. Q in Rb represents a group as any one of phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, and dihydrobenzodioxyl group. A2 represents a single bond, oxygen atom, sulfur atom,-N (methyl)-, or -N (ethyl)- (provided that when A2 represents oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)-, A1 represents ethylene). R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q represents phenyl group, A1 represents a single bond, or unsubstituted methylene, and A2 represents a single bond, one of R2 and R3 represents a substituent other than hydrogen atom). Symbol p in Rc represents an integer of 2 or 3, and A4 represents a single bond or methylene. A5 represents -C (O)-,-C (S) -, or-S (0) 2-. Rd represents hydrogen atom, or a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, and pyridin-4-yl group. Re represents any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- 4-methylphenyl) amino group, N- (4-chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2-yl) amino group, N- (furan-3-yl) amino group, N- (thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, and ethyloxycarbonylamino group. Rz'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1-(4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2-(phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2-(N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4-methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4-chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4-fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylearbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N-isobutylthiocarbamoyl group, t'butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N-cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N-cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N-cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N-phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4-methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4-chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4-fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4-fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-l-yl) carbonyl group, and (morpholino-4-yl) carbonyl group. Ry' represents hydrogen atom, methyl group, ethyl group, or isobutyl group, or binds to Rz'to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol-1-yl group, or pyrazol-1-yl group together with nitrogen atom. Provided that when-D-Rx'or-N (Ry') (Rz') contains hydroxyl group, the hydroxyl group may be protected with Rpl, and-D-Rx'or-N (Ry') (Rz') contains amino group, the amino group may be protected with Rp2.

The group G represents chlorine atom, bromine atom, iodine atom, or triflate group.

The group Y'represents methyl group, or ethyl group.

In a particularly preferred embodiment, the compound represented by the formula (II) satisfies all of the following requirements.

Symbol n represents an integer of 2.

C2'represents carbon atom to which the group G bonds, C3'represents carbon atom to which Rs'binds, C4'may be replaced with V', and C5'and C6'represent an unsubstituted ring-constituting carbon atom.

V'represents nitrogen atom, or carbon atom substituted with Zx', and Zx' represents any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, and N, N-dimethylamino group, provided that when Zx' contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituted Zx'contains amino group, the amino group may be protected with Rp2 Rs'represents-O-Rx'. Rx'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2' (4'fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyll ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

The group G represents bromine atom, or iodine atom.

The group Y'represents methyl group, or ethyl group.

In another particularly preferred embodiment, the compound represented by the formula (II) satisfies all of the following requirements.

Symbol n represents an integer of 2.

C2'represents carbon atom to which the group G bonds, C4'represents carbon atom to which Rs'binds, C5'may be replaced with V', and C3'and C6'represent an unsubstituted ring-constituting carbon atom.

V'represents nitrogen atom, or carbon atom substituted with Zx', and Zx' represents any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, and N, N-dimethylamino group, provided that when Zx' contains hydroxyl group, the hydroxyl group may be protected with Rp 1, and when the substituted Zx'contains amino group, the amino group may be protected with Rp2.

Rs'represents-O-Rx'. Rx'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2-[2-(trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2-14-(trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

The group G represents bromine atom, or iodine atom.

The group Y'represents methyl group, or ethyl group.

In another particularly preferred embodiment, the compound represented by the formula (II) satisfies all of the following requirements.

Symbol n represents an integer of 2.

C3'represents carbon atom to which the group G bonds, C5'represents carbon atom to which Rs'binds, and C2', C4'and C6'represent an unsubstituted ring-constituting carbon atom.

Rs'represents-O-Rx'. Rx'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, l-phenylethyl group, l- (2-fluorophenyl) ethyl group, 1-(3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

The group G represents bromine atom, or iodine atom.

The group Y'represents methyl group, or ethyl group.

In another particularly preferred embodiment, the compound represented by the formula (II) satisfies all of the following requirements.

Symbol n represents an integer of 2.

C3'represents carbon atom to which the group G bonds, C4'represents carbon atom to which Rs'binds, C5'represents nitrogen atom, and C2'and C6' represent an unsubstituted ring-constituting carbon atom.

Rs'represents-O-Rx'. Rx'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2-[2-(trifluoromethyl) phenyl] ethyl group, 2-13- (trifluoromethyl) phenyl] ethyl group, 2- [4-(trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

The group G represents bromine atom, or iodine atom.

The group Y'represents methyl group, or ethyl group.

In another particularly preferred embodiment, the compound represented by the formula (II) satisfies all of the following requirements.

Symbol n represents an integer of 2.

C3'represents carbon atom to which the group G bonds, C4'represents carbon atom to which Rs'binds, C6'represents carbon atom substituted with Zx', and C2'and C5'represent an unsubstituted ring-constituting carbon atom.

Zx'represents any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, and N, N-dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituted Zx'contains amino group, the amino group may be protected with Rp2.

Rs'represents-O-Rx'. Rx'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

The group G represents bromine atom, or iodine atom.

The group Y'represents methyl group, or ethyl group.

In another particularly preferred embodiment, the compound represented by the formula (II) satisfies all of the following requirements.

Symbol n represents an integer of 2.

C3'represents carbon atom to which the group G bonds, C4'represents carbon atom to which Rs'binds, C5'represents carbon atom substituted with Zx', or unsubstituted carbon atom, and C2'and C6'represent an unsubstituted ring-constituting carbon atom.

Zx'represents any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, and N, N-dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituted Zx'contains amino group, the amino group may be protected with Rp2.

Rs'represents-S-Rx'. Rx'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3-(trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2-[2-(trifluoromethyl) phenyllethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyll ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

The group G represents bromine atom, or iodine atom.

The group Y'represents methyl group, or ethyl group.

In another particularly preferred embodiment, the compound represented by the formula (II) satisfies all of the following requirements.

Symbol n represents an integer of 2.

C3'represents carbon atom to which the group G bonds, C4'represents carbon atom to which Rs'binds, C5'represents carbon atom substituted with Zx', or unsubstituted ring-constituting carbon atom, and C2'and C6'represent an unsubstituted ring-constituting carbon atom.

Zx'represents any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, and N, N-dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituted Zx'contains amino group, the amino group may be protected with Rp2.

Rs'represents-N (Ry') (Rz'). Rz'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1-(4-fluorophenyl) ethyl group, 1-(2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2,5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) p henyll ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4-methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4-chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4-fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N-isobutylthiocarbamoyl group, t'butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N-cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N-cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N-cyclohexylcarbamoyl group, N-cyelohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N-phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4-methylphenyl) thiocarbamoyl group, 4-chlorophenyloxyearbonyl group, N- (4-chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4-fluorophenyloxyearbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4-fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-1-yl) carbonyl group, and (morpholino-4-yl) carbonyl group. Ry' represents hydrogen atom, methyl group, ethyl group, or isobutyl group, or binds to Rz'to form pyrrolidino group, piperidino group, or morpholino group together with the nitrogen atom to which they bonds. Provided that when-N (Ry') (Rz') contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when Ry'or Rz' contains amino group, the amino group may be protected with Rp2.

The group G represents bromine atom, or iodine atom.

The group Y'represents methyl group, or ethyl group.

In another particularly preferred embodiment, the compound represented by the formula (II) satisfies all of the following requirements.

Symbol n represents an integer of 2.

C3'represents carbon atom to which the group G bonds, C4'represents carbon atom to which Rs'binds, C5'represents carbon atom substituted with Zx', and C2'and C6'represent an unsubstituted ring-constituting carbon atom.

Zx'represents any one of N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N-dimethylsulfamoylamino group. Provided that when the substituted Zx'contains amino group (NH), the amino group may be protected with Rp2.

Rs'represents-O-Rx'. Rx'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1-(3-fluorophenyl) ethyl group, l' (4'fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1-(3-chlorophenyl) ethyl group, l- (4'chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2,5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N N-dimethylamino) p henyll ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

The group G represents bromine atom, or iodine atom.

The group Y'represents methyl group, or ethyl group.

In another particularly preferred embodiment, the compound represented by the formula (II) satisfies all of the following requirements.

Symbol n represents an integer of 2.

C3'represents carbon atom to which the group G bonds, C4'represents carbon atom to which Rs'binds, C5'represents carbon atom substituted with Zx', or unsubstituted carbon atom, and C2'and C6'represent an unsubstituted ring-constituting carbon atom.

Zx'represents any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, and N, N-dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituted Zx'contains amino group, the amino group may be protected with Rp2.

Rs'represents-O-Rx'. Rx'have the same meaning as that of Rc, provided that when Rc contains hydroxyl group (OH), the hydroxyl group may be protected with Rpl. p in Rc represents an integer of 2, and A4 represents a single bond or methylene. A5 represents-C (O)-,-C (S) -, or-S (0) 2-. Rd represents a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, and 4-fluorophenylmethyl group. Re represents a group as any one of isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4-chlorophenyl) amino group, N- (4-fluorophenyl) amino group, pyrrolidino group, piperidino group, and morpholino group.

The group G represents bromine atom, or iodine atom.

The group Y'represents methyl group, or ethyl group.

C2', C3', C4', C5', and C6'in the aromatic ring (E') in the aforementioned formula (III) each represent a ring-constituting carbon atom. Any ring-constituting carbon atom to which Rs'and AR'do not bond among them may be replaced with V'.

The substitution positions of Rs', AR', and V'are similar to those described in the explanations of the substitution positions of Rs (corresponding to the position of Rs'), AR (corresponding to the position of the group AR'), and V (corresponding to the position of V') in the aforementioned formula (I).

AR'has the same meaning as that of AR mentioned above, provided that when AR contains hydroxyl group, the hydroxyl group may be protected with Rpl.

In this case, the hydroxyl group includes OH in carboxyl group (COOH). When the substituted AR contains amino group, the amino group represents a substituent, which may be protected with Rp2. Examples of the amino group, which may be protected include NH present in a ring constituting AR, for example, as in indole ring, indazole ring, and the like.

Rs', V', n, and D in the aforementioned formula (III) have the same meanings as those defined above. Rpl, and Rp2 also have the same meanings as those defined above.

In a preferred embodiment, the compound represented by the formula (III) satisfies all of the following requirements.

AR'binds to C2', Rs'binds to any of the atoms C3', C4', and C5', and a ring-constituting carbon atom to which Rs'does not bind among C3', C4', and C5'may be replaced with V.

V'represents nitrogen atom, or carbon atom substituted with Zx', and Zx' represents any one of fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N-dimethylsulfamoylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituted Zx' contains amino group, the amino group may be protected with Rp2.

Rs'represents-D-Rx'or-N (Ry') (Rz'). D represents oxygen atom or sulfur atom. Rx'represents butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-cyclopentylethyl group, or 2-cyclohexylethyl group, or represents Rb or Rc. Q in Rb represents a group as any one of phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, and dihydrobenzodioxyl group. A2 represents a single bond, oxygen atom, sulfur atom,-N (methyl)-, or -N (ethyl)- (provided that when A2 represents oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)-, A1 represents ethylene). R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q represents phenyl group, Al represents a single bond, or unsubstituted methylene, and A2 represents a single bond, one of R2 and R3 represents a substituent other than hydrogen atom). Symbol p in Rc represents an integer of 2 or 3, and A4 represents a single bond or methylene. A5 represents -C (O)-,-C (S)-, or-S (0) 2-. Rd represents hydrogen atom, or a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, and pyridin-4-yl group. Re represents any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N- (4-chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2-yl) amino group, N- (furan-3-yl) amino group, N- (thiophen-2-yl) amino group, N- (thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, and ethyloxycarbonylamino group. Rz'represents butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, l' (4'fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4-(trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2-(2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2- (N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4-methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4-chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4'fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylearbamoyl group, N-isobutylthiocarbamoyl group, t-butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N'cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N-cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N-cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N-phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4-methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4-chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4-fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4-fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-l-yl) carbonyl group, and (morpholino-4-yl) carbonyl group. Ry' represents hydrogen atom, methyl group, ethyl group, or isobutyl group, or binds to Rz to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol-1-yl group, or pyrazol-1-yl group together with the nitrogen atom to which they bond. However,-D-Rx'or-N (Ry') (Rz') contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when-D-Rx'or - N (Ry') (Rz') contains amino group, the amino group may be protected with Rp2.

AR'represents any one of naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-1H-quinolin-6-yl group, dihydro-lH-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, 1H-indazol-5-yl group, lH-indazol-4-yl group, lH-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [c]isothiazol-4-yl group, benzo [c]isothiazol-6-yl group, benzo[c]isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1H-pyrrolo [2, 3-b] pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, lH-benzimidazol-5-yl group, lH-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, 1H-pyrrolo [3, 2-b] pyridin-5-yl group, 1H-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, lH-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2, 3-b]pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1, 3-dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3, 2-c] pyridin-6-yl group, lH-pyrrolo [3, 2-c] pyridin-4-yl group, 1H-pyrrolo [2, 3-c]pyridin-5-yl group, lH-pyrrolo [2, 3-c] pyridin-4-yl group, lH-pyrazolo [4, 3-b]pyridin-5-yl group, lH-pyrazolo [4, 3-b]pyridin-6-yl group, lH-pyrazolo [4, 3-c]pyridin-6-yl group, lH-pyrazolo [4, 3-c] pyridin-4-yl group, 1H-pyrazolo [3, 4-c] pyridin-5-yl group, 1H-pyrazolo [3, 4-c] pyridin-4-yl group, lH-pyrazolo [3, 4-b] pyridin-5-yl group, 1H-pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a]pyridin-6-yl group, [1, 2,4] triazolo [4, 3-a]pyridin-7-yl group, thieno [3, 2-c] pyridin-2-yl group, thieno [3, 2-c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3,2-b] pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3, 2-b] pyridin-6-yl group, 1H-thieno [3, 2-c] pyrazol-5-yl group, lH-thieno [3, 2-c] pyrazol-4-yl group, benzo [d] isoxazol-5-yl group, benzo [d] isoxazol-4-yl group, benzo [d] isoxazol-6-yl group, benzo [d] isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c] isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5-yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3, 4-d] thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, lH-pyrazolo [3, 4-b] pyrazin-5-yl group, 1H-imidazo [4, 5-b] pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, and 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of identical or different Xa). The substituent Xa represents a group as any one of oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N, N-dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, and N, N-dimethylcarbamoyl group. Provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when substituted AR'contains amino group, the amino group may be protected with Rp2.

In another preferred embodiment, the compound represented by the formula (III) satisfies all of the following requirements.

AR'binds to C3', Rs'binds to any of the ring-constituting carbon atoms C4', C5', and C6', and a ring-constituting carbon atom to which Rs'does not bind among C4', C5', and C6'may be replaced with V'.

V'represents nitrogen atom, or carbon atom substituted with Zx', and Zx' represents any one of fluorine atom, chlorine atom, bromine atom, nitro group, methyl group, hydroxyl group, methoxy group, amino group, N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N-dimethylsulfamoylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituted Zx' contains amino group, the amino group may be protected with Rp2.

Rs'represents-D-Rx'or-N (Ry') (Rz'). D represents oxygen atom or sulfur atom. Rx'represents butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-cyclopentylethyl group, or 2-cyclohexylethyl group, or represents Rb or Rc. Q in Rb represents a group as any one of phenyl group, thienyl group, furyl group, pyridyl group, oxazolyl group, naphthyl group, tetrahydronaphthyl group, indanyl group, indolyl group, and dihydrobenzodioxyl group. A2 represents a single bond, oxygen atom, sulfur atom, -N (methyl) -, or - N (ethyl) - (provided that when A2 represents oxygen atom, sulfur atom,-N (methyl)-, or-N (ethyl)-, A1 represents ethylene). R2 and R3 independently represent hydrogen atom, methyl group, fluorine atom, chlorine atom, trifluoromethyl group, methoxy group, dimethylamino group, acetylamino group, or methylsulfonylamino group (provided that when Q represents phenyl group, A1 represents a single bond, or unsubstituted methylene, and A2 represents a single bond, one of R2 and R3 represents a substituent other than hydrogen atom). Symbol p in Rc represents an integer of 2 or 3, and A4 represents a single bond or methylene. A5 represents -C (O)-,-C (S) -, or-S (0) 2-. Rd represents hydrogen atom, or a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopropylmethyl group, cyclopentyl group, cyclopentylmethyl group, cyclohexyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, and pyridin-4-yl group. Re represents any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, phenylmethyl group, 4-chlorophenylmethyl group, 4-fluorophenylmethyl group, pyridin-2-yl group, pyridin-3-yl group, pyridin-4-yl group, furan-2-yl group, furan-3-yl group, thiophen-2-yl group, thiophen-3-yl group, methoxy group, ethoxy group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, thiomethoxy group, amino group, N-methylamino group, N, N-dimethylamino group, N-ethylamino group, N, N-diethylamino group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N' (4-methylphenyl) amino group, N- (4-chlorophenyl) amino group, N- (4-fluorophenyl) amino group, N- (pyridin-2-yl) amino group, N- (pyridin-3-yl) amino group, N- (pyridin-4-yl) amino group, N- (furan-2-yl) amino group, N- (furan-3-yl) amino group, N- (thiophen-2-yl) amino group, N-(thiophen-3-yl) amino group, pyrrolidino group, piperidino group, morpholino group, methyloxycarbonylamino group, and ethyloxycarbonylamino group. Rz'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3'chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, 2-(N-ethyl-N-phenylamino) ethyl group, isobutyryl group, isopropylthiocarbonyl group, isopropylsulfonyl group, valeryl group, butylthiocarbonyl group, isovaleryl group, isobutylthiocarbonyl group, pivaloyl group, t-butylthiocarbonyl group, cyclopropylcarbonyl group, cyclopropylthiocarbonyl group, cyclopentylcarbonyl group, cyclopentylthiocarbonyl group, cyclohexylcarbonyl group, cyclohexylthiocarbonyl group, cyclopentylmethylcarbonyl group, cyclopentylmethylthiocarbonyl group, cyclohexylmethylcarbonyl group, cyclohexylmethylthiocarbonyl group, benzoyl group, thiobenzoyl group, phenylsulfonyl group, 4-methylphenylcarbonyl group, 4-methylphenylthiocarbonyl group, 4-methylphenylsulfonyl group, 4-chlorophenylcarbonyl group, 4-chlorophenylthiocarbonyl group, 4-fluorophenylcarbonyl group, 4-fluorophenylthiocarbonyl group, isopropyloxycarbonyl group, N-isopropylcarbamoyl group, N-isopropylthiocarbamoyl group, butyloxycarbonyl group, N-butylcarbamoyl group, N-butylthiocarbamoyl group, isobutyloxycarbonyl group, N-isobutylcarbamoyl group, N-isobutylthiocarbamoyl group, t-butyloxycarbonyl group, N-t-butylcarbamoyl group, N-t-butylthiocarbamoyl group, cyclopropyloxycarbonyl group, N-cyclopropylcarbamoyl group, N-cyclopropylthiocarbamoyl group, cyclopentyloxycarbonyl group, N-cyclopentylcarbamoyl group, N-cyclopentylthiocarbamoyl group, cyclohexyloxycarbonyl group, N-cyclohexylcarbamoyl group, N-cyclohexylthiocarbamoyl group, cyclopentylmethyloxycarbonyl group, cyclohexylmethyloxycarbonyl group, phenyloxycarbonyl group, N'phenylcarbamoyl group, N-phenylthiocarbamoyl group, 4-methylphenyloxycarbonyl group, N- (4-methylphenyl) carbamoyl group, N- (4-methylphenyl) thiocarbamoyl group, 4-chlorophenyloxycarbonyl group, N- (4-chlorophenyl) carbamoyl group, N- (4-chlorophenyl) thiocarbamoyl group, 4-fluorophenyloxycarbonyl group, N- (4-fluorophenyl) carbamoyl group, N- (4-fluorophenyl) thiocarbamoyl group, (pyrrolidino-1-yl) carbonyl group, (piperidino-1-yl) carbonyl group, and (morpholino-4-yl) carbonyl group. Ry' represents hydrogen atom, methyl group, ethyl group, or isobutyl group, or binds to Rz'to form pyrrolidino group, piperidino group, piperazino group, morpholino group, pyrrol-1-yl group, imidazol-1-yl group, or pyrazol-1-yl group together with nitrogen atom. Provided that when-D-Rx'or-N (Ry') (Rz') contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when-D-Rx'or-N (Ry') (Rz') contains amino group, the amino group may be protected with Rp2.

AR'represents any one of naphthalen-2-yl group, naphthalen-1-yl group, benzofuran-5-yl group, benzofuran-4-yl group, benzofuran-2-yl group, benzo [b] thiophen-5-yl group, benzo [b] thiophen-4-yl group, benzo [b] thiophen-2-yl group, indol-5-yl group, indol-4-yl group, indol-6-yl group, benzothiazol-6-yl group, benzothiazol-7-yl group, benzothiazol-5-yl group, benzothiazol-4-yl group, dihydro-3H-benzothiazol-6-yl group, dihydro-3H-benzothiazol-7-yl group, dihydro-3H-benzothiazol-5-yl group, dihydro-3H-benzothiazol-4-yl group, quinolin-6-yl group, quinolin-3-yl group, quinolin-5-yl group, quinolin-7-yl group, dihydro-lH-quinolin-6-yl group, dihydro-1H-quinolin-5-yl group, benzo [d] isothiazol-5-yl group, benzo [d] isothiazol-4-yl group, benzo [d] isothiazol-6-yl group, benzo [d] isothiazol-7-yl group, lH-indazol-5-yl group, lH-indazol-4-yl group, 1H-indazol-6-yl group, benzo [c] isothiazol-5-yl group, benzo [c]isothiazol-4-yl group, benzo [c] isothiazol-6-yl group, benzo [c] isothiazol-7-yl group, 2H-indazol-5-yl group, 2H-indazol-4-yl group, 2H-indazol-6-yl group, imidazo [1, 2-a] pyridin-6-yl group, imidazo [1, 2-a] pyridin-7-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, lH-pyrrolo [2, 3-b]pyridin-4-yl group, isoquinolin-6-yl group, isoquinolin-3-yl group, isoquinolin-5-yl group, isoquinolin-7-yl group, dihydro-2H-isoquinolin-6-yl group, dihydro-2H-isoquinolin-5-yl group, cinnolin-6-yl group, cinnolin-5-yl group, quinazolin-6-yl group, quinazolin-7-yl group, quinazolin-5-yl group, quinoxalin-2-yl group, quinoxalin-6-yl group, quinoxalin-5-yl group, 1H-benzimidazol-5-yl group, 1H-benzimidazol-4-yl group, benzoxazol-5-yl group, benzoxazol-6-yl group, benzoxazol-4-yl group, benzoxazol-7-yl group, lH-pyrrolo [3, 2-b] pyridin-5-yl group, lH-pyrrolo [3, 2-b] pyridin-6-yl group, benzo [1, 2,5] thiadiazol-5-yl group, benzo [1, 2,5] thiadiazol-4-yl group, 1H-benzotriazol-5-yl group, 1H-benzotriazol-4-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-5-yl group, 1, 3-dihydropyrrolo [2, 3-b] pyridin-4-yl group, 1, 3-dihydrobenzimidazol-5-yl group, 1, 3-dihydrobenzimidazol-4-yl group, dihydro-3H-benzoxazol-6-yl group, dihydro-3H-benzoxazol-7-yl group, dihydro-3H-benzoxazol-5-yl group, dihydro-3H-benzoxazol-4-yl group, phthalazin-6-yl group, phthalazin-5-yl group, [1, 8] naphthalidin-3-yl group, [1, 8] naphthalidin-4-yl group, [1, 5] naphthalidin-3-yl group, [1, 5] naphthalidin-4-yl group, 1H-pyrrolo [3, 2-c] pyridin-6-yl group, 1H-pyrrolo [3, 2-c] pyridin-4-yl group, 1H-pyrrolo [2, 3-c] pyridin-5-yl group, 1H-pyrrolo [2, 3-c] pyridin-4-yl group, 1H-pyrazolo [4, 3-b] pyridin-5-yl group, lH-pyrazolo [4, 3-b] pyridin-6-yl group, lH-pyrazolo [4, 3-c] pyridin-6-yl group, lH-pyrazolo [4, 3-c] pyridin-4-yl group, lH-pyrazolo [3, 4-c] pyridin-5-yl group, lH-pyrazolo [3, 4-c] pyridin-4-yl group, lH-pyrazolo [3, 4-b] pyridin-5-yl group, 1H-pyrazolo [3, 4-b] pyridin-4-yl group, [1, 2,4] triazolo [4, 3-a] pyridin-6-yl group, [1, 2, 4] triazolo [4, 3-a]pyridin-7-yl group, thieno [3, 2-c]pyridin-2-yl group, thieno [3, 2-c] pyridin-3-yl group, thieno [3, 2-c] pyridin-6-yl group, thieno [3, 2-b] pyridin-2-yl group, thieno [3, 2-b] pyridin-3-yl group, thieno [3, 2-b] pyridin-5-yl group, thieno [3, 2-b] pyridin-6-yl group, lH-thieno [3, 2-c]pyrazol-5-yl group, 1H-thieno [3, 2-c] pyrazol-4-yl group, benzo [d] isoxazol-5-yl group, benzo [d] isoxazol-4-yl group, benzo [d] isoxazol-6-yl group, benzo [d] isoxazol-7-yl group, benzo [c] isoxazol-5-yl group, benzo [c] isoxazol-4-yl group, benzo [c] isoxazol-6-yl group, benzo [c] isoxazol-7-yl group, indolizin-7-yl group, indolizin-6-yl group, indolizine-8-yl group, 1, 3-dihydroindol-5-yl group, 1, 3-dihydroindol-4-yl group, 1, 3-dihydroindol-6-yl group, 1H-pyrazolo [3, 4-d]thiazol-5-yl group, 2H-isoindol-5-yl group, 2H-isoindol-4-yl group, [1, 2,4] triazolo [1, 5-a] pyrimidin-6-yl group, lH-pyrazolo [3, 4-b]pyrazin-5-yl group, 1H-imidazo [4, 5-b] pyrazin-5-yl group, 7H-purin-2-yl group, 4H-chromen-6-yl group, and 4H-chromen-5-yl group (the aforementioned groups may be substituted with one of Xa or two or more of identical or different Xa). The substituent Xa represents a group as any one of oxo group, thioxo group, fluorine atom, chlorine atom, trifluoromethyl group, methyl group, ethyl group, propyl group, 2-hydroxyethyl group, carboxymethyl group, 2-carboxyethyl group, N, N-dimethylcarbamoylmethyl group, hydroxyl group, methoxy group, 2-hydroxyethyloxy group, carboxymethyloxy group, 2-carboxyethyloxy group, N, N-dimethylcarbamoylmethyloxy group, amino group, methylamino group, dimethylamino group, 2-hydroxyethylamino group, carbamoylamino group, acetylamino group, furan-2-carboxyamino group, 2-hydroxyacetylamino group, 2-aminoacetylamino group, methylsulfonylamino group, (N, N-dimethylsulfamoyl) amino group, methanesulfonyl group, sulfamoyl group, N-methylsulfamoyl group, N, N-dimethylsulfamoyl group, carboxyl group, acetyl group, carbamoyl group, and N, N-dimethylcarbamoyl group. Provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when substituted AR'contains amino group, the amino group may be protected with Rp2.

In a particularly preferred embodiment, the compound represented by the formula (III) satisfies all of the following requirements.

C2'represents carbon atom to which AR'binds, C3'represents carbon atom to which Rs'binds, C4'may be replaced with V', and C5'and C6'represent an unsubstituted ring-constituting carbon atom.

V'represents nitrogen atom, or carbon atom substituted with Zx', and Zx' represents any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, and N, N-dimethylamino group, provided that when Zx' contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituted Zx'contains amino group, the amino group may be protected with Rp2.

Rs'represents-O-Rx'. Rx'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl) ethyl group, l- (3'fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2-(3-fluorophenyl) ethyl group, 2' (4'fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyll ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyll ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2-(N-ethyl-N-phenylamino) ethyl group.

AR'represents any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b]thiophen-5-yl group, 2-methylbenzo [blthiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-1H-indol-5-yl group, 1, 3-dimethyl-1H-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-lH-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-lH-indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1-(2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1-methyl-lH-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-lH-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, l-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-1H-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, einnolin-6-yl group, and benzoxazol-5-yl group. Provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when substituted AR'contains amino group, the amino group may be protected with Rp2.

In another particularly preferred embodiment, the compound represented by the formula (III) satisfies all of the following requirements.

C2'represents carbon atom to which AR'binds, C4'represents carbon atom to which Rs'binds, C5'may be replaced with V', and C3'and C6'represent an unsubstituted ring-constituting carbon atom.

V'represents nitrogen atom, or carbon atom substituted with Zx', and Zx' represents any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, and N, N-dimethylamino group. Provided that when Zx' contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituted Zx'contains amino group, the amino group may be protected with Rp2.

Rs'represents-O-Rx'. Rx'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5, 6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, l' (2'fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1-(4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3, 5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4-(trifluoromethyl)phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyllethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

AR'represents any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo[b]furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, lH-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1,2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-lH-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1-(2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1-methyl-lH-indazol-5-yl group, l-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo l, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yl group. Provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rp l, and when substituted AR'contains amino group, the amino group may be protected with Rp2.

In another particularly preferred embodiment, the compound represented by the formula (III) satisfies all of the following requirements.

C3'represents carbon atom to which AR'binds, C5'represents carbon atom to which Rs'binds, and C2', C4'and C6'represent an unsubstituted ring-constituting carbon atom.

Rs'represents-O-Rx'. Rx'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1-(2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, l- (4'chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2-(N-ethyl-N-phenylamino) ethyl group.

AR'represents any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol-5-yl group, 1, 3-dimethyl-1H-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-lH-indol-5-yl group, 1-ethyl-2-methyl-lH-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, l-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-lH-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-l-propyl-lH-indol-5-yl group, 2, 3-dimethyl-1-propyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-1H-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, l-ethyl-lH-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-lH-indazol-5-yl group, imidazoll, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yt group. Provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when substituted AR'contains amino group, the amino group may be protected with Rp2.

In another particularly preferred embodiment, the compound represented by the formula (III) satisfies all of the following requirements.

C3'represents carbon atom to which AR'binds, C4'represents carbon atom to which Rs'binds, C5'represents nitrogen atom, and C2'and C6'represent an unsubstituted ring-constituting carbon atom.

Rs' represents -O-Rx'. Rx'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4,7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4,7-dichloroindan-2-yl group, 5,6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4, 7-dimethoxyindan-2-yl group, 5, 6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1-(2-chlorophenyl) ethyl group, l' (3'chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3,5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2, 4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3,4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2-[2-(trifluoromethyl)phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

AR'represents any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo[b]furan-5-yl group, 2, 3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, 1H-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol-5-yl group, 1, 3-dimethyl-1H-indol-5-yl group, 1,2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-lH-indol-5-yl group, l-ethyl-2-methyl-1H-indol-5-yl group, l-ethyl-3-methyl-lH-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-l-propyl-lH-indol-5-yl group, 2, 3-dimethyl-1-propyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1-(2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1-(2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2,3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-lH-indazol-5-yl group, 1-ethyl-lH-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 1- (2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-1H-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo[1,2-a]pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b]pyridin-5-yl group, l-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, l'oxo'l, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yl group. Provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when substituted AR'contains amino group, the amino group may be protected with Rp2.

In another particularly preferred embodiment, the compound represented by the formula (III) satisfies all of the following requirements.

C3'represents carbon atom to which AR'binds, C4'represents carbon atom to which Rs'binds, C6'represents carbon atom substituted with Zx', and C2'and C5' represent an unsubstituted ring-constituting carbon atom.

Zx'represents any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, and N, N-dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituted Zx'contains amino group, the amino group may be protected with Rp2.

Rs'represents-O-Rx'. Rx'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4, 7-difluoroindan-2-yl group, 5, 6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1'phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, l' (4'fluorophenyl) ethyl group, 1- (2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2,3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2, 3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3,4-difluorophenylmethyl group, 2, 3-dichlorophenylmethyl group, 2,4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2,6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3, 6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2- (4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2-(2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4-(trifluoromethyl)phenyl]ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2-(phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

AR'represents any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzoMthiophen-5-yl group, 2-methylbenzo [bjthiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, lH-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-lH-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-lH-indol-5-yl group, l-ethyl-2-methyl-lH-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2, 3-dimethyl-1H-indol-5-yl group, l-propyl-lH-indol-5-yl group, 2-methyl-l-propyl-lH-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2, 3-dimethyl-l-propyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-1H-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-1H-indazol-5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-lH-pyrrolo [2, 3-b]pyridin-5-yl group, l-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-propyl-1H-pyrrolo [2, 3-b]pyridin-5-yl group, 1-(2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, l'oxo'l, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yl group. Provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when substituted AR'contains amino group, the amino group may be protected with Rp2.

In another particularly preferred embodiment, the compound represented by the formula (III) satisfies all of the following requirements..

C3'represents carbon atom to which AR'binds, C4'represents carbon atom to which Rs'binds, C5'represents carbon atom substituted with Zx', and C2'and C6' represent an unsubstituted ring-constituting carbon atom.

Zx'represents any one of N-methylamino group, N-ethylamino group, N-propylamino group, N-isopropylamino group, N, N-dimethylamino group, N, N-diethylamino group, formylamino group, acetylamino group, carbamoylamino group, mesylamino group, and N, N-dimethylsulfamoylamino group. Provided that when the substituted Zx'contains amino group (NH), the amino group may be protected with Rp2.

Rs'represents-O-Rx'. Rx'represents any one of butyl group, isobutyl group, 2-ethylbutyl group, cyclopentyl group, cyclohexyl group, cycloheptyl group, cyclopentylmethyl group, cyclohexylmethyl group, 2-methylphenyl group, 4-methylphenyl group, 2-fluorophenyl group, 3-fluorophenyl group, 4-fluorophenyl group, 2-chlorophenyl group, 3-chlorophenyl group, 4-chlorophenyl group, indan-2-yl group, 4-methylindan-2-yl group, 5-methylindan-2-yl group, 4, 7-dimethylindan-2-yl group, 5,6-dimethylindan-2-yl group, 4-fluoroindan-2-yl group, 5-fluoroindan-2-yl group, 4,7-difluoroindan-2-yl group, 5,6-difluoroindan-2-yl group, 4-chloroindan-2-yl group, 5-chloroindan-2-yl group, 4, 7-dichloroindan-2-yl group, 5, 6-dichloroindan-2-yl group, 4-methoxyindan-2-yl group, 5-methoxyindan-2-yl group, 4,7-dimethoxyindan-2-yl group, 5,6-dimethoxyindan-2-yl group, 1-phenylethyl group, 1- (2-fluorophenyl) ethyl group, 1- (3-fluorophenyl) ethyl group, 1- (4-fluorophenyl) ethyl group, 1-(2-chlorophenyl) ethyl group, 1- (3-chlorophenyl) ethyl group, 1- (4-chlorophenyl) ethyl group, 2-methylphenylmethyl group, 3-methylphenylmethyl group, 4-methylphenylmethyl group, 2, 3-dimethylphenylmethyl group, 3, 5-dimethylphenylmethyl group, 2-fluorophenylmethyl group, 3-fluorophenylmethyl group, 4-fluorophenylmethyl group, 2-chlorophenylmethyl group, 3-chlorophenylmethyl group, 4-chlorophenylmethyl group, 2,3-difluorophenylmethyl group, 2,4-difluorophenylmethyl group, 2, 5-difluorophenylmethyl group, 3, 4-difluorophenylmethyl group, 2,3-dichlorophenylmethyl group, 2, 4-dichlorophenylmethyl group, 2, 5-dichlorophenylmethyl group, 2, 6-dichlorophenylmethyl group, 3, 4-dichlorophenylmethyl group, 3,5-dichlorophenylmethyl group, 3,6-dichlorophenylmethyl group, 2- (trifluoromethyl) phenylmethyl group, 3- (trifluoromethyl) phenylmethyl group, 4- (trifluoromethyl) phenylmethyl group, 2- (2-methylphenyl) ethyl group, 2- (3-methylphenyl) ethyl group, 2-(4-methylphenyl) ethyl group, 2- (2-methoxyphenyl) ethyl group, 2- (3-methoxyphenyl) ethyl group, 2- (4-methoxyphenyl) ethyl group, 2- (2-fluorophenyl) ethyl group, 2- (3-fluorophenyl) ethyl group, 2- (4-fluorophenyl) ethyl group, 2- (2-chlorophenyl) ethyl group, 2- (3-chlorophenyl) ethyl group, 2- (4-chlorophenyl) ethyl group, 2- [2- (trifluoromethyl) phenyl] ethyl group, 2- [3- (trifluoromethyl) phenyl] ethyl group, 2- [4- (trifluoromethyl) phenyl] ethyl group, 2- [4- (N, N-dimethylamino) phenyl] ethyl group, 2-phenyloxyethyl group, 2- (2-chlorophenyloxy) ethyl group, 2- (3-chlorophenyloxy) ethyl group, 2- (4-chlorophenyloxy) ethyl group, 2- (phenylthio) ethyl group, 2- (N-phenyl-N-methylamino) ethyl group, and 2- (N-ethyl-N-phenylamino) ethyl group.

AR'represents any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2, 3-dimethylbenzo [b] thiophen-5-yl group, lH-indol-5-yl group, 2-methyl-1H-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2, 3-dimethyl-1h-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-1H-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1, 2, 3-trimethyl-1H-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, 1-ethyl-2-methyl-1H-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2, 3-dimethyl-1H-indol-5-yl group, 1-propyl-lH-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-l-propyl-lH-indol-5-yl group, 2, 3-dimethyl-l-propyl-lH-indol-5-yl group, 1-(2-hydroxyethyl)-1H-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2, 3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, 1H-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, 1-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 1-(2-hydroxyethyl)-1H-indazol-5-yl group, 3-hydroxy-1H-indazol-5-yl group, 3-hydroxy-1-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1-ethyl-1H-pyrrolo [2, 3-b] pyridin-5-yl group, l-propyl-lH-pyrrolol2, 3-b] pyridin-5-yl group, 1-(2-hydroxyethyl)-1H-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yl group. Provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when substituted AR'contains amino group, the amino group may be protected with Rp2.

In another particularly preferred embodiment, the compound represented by the formula (III) satisfies all of the following requirements.

C3'represents carbon atom to which AR'binds, C4'represents carbon atom to which Rs'binds, C5'represents carbon atom substituted with Zx', or an unsubstituted ring-constituting carbon atom, and C2'and C6'represent an unsubstituted ring-constituting carbon atom.

Zx'represents any one of fluorine atom, methyl group, hydroxyl group, amino group, N-methylamino group, and N, N-dimethylamino group, provided that when Zx'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when the substituted Zx'contains amino group, the amino group may be protected with Rp2.

Rs'represents-O-Rx'. Rx'have the same meaning as that of Re, provided that when Rc contains hydroxyl group, the hydroxyl group may be protected with Rpl. p in Rc represents an integer of 2, and A4 represents a single bond or methylene. A5 represents-C (O)-,-C (S)-, or-S (0) 2-. Rd represents a group as any one of methyl group, ethyl group, propyl group, isopropyl group, butyl group, isobutyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, benzyl group, 4-chlorophenylmethyl group, and 4-fluorophenylmethyl group. Re represents a group as any one of isopropyl group, butyl group, isobutyl group, t-butyl group, cyclopropyl group, cyclopentyl group, cyclohexyl group, cyclopentylmethyl group, cyclohexylmethyl'group, phenyl group, 4-methylphenyl group, 4-chlorophenyl group, 4-fluorophenyl group, propyloxy group, isopropyloxy group, butyloxy group, isobutyloxy group, t-butyloxy group, cyclopropyloxy group, cyclopentyloxy group, cyclohexyloxy group, cyclopentylmethyloxy group, cyclohexylmethyloxy group, phenyloxy group, 4-methylphenyloxy group, 4-chlorophenyloxy group, 4-fluorophenyloxy group, N-propylamino group, N-isopropylamino group, N-butylamino group, N-isobutylamino group, N-t-butylamino group, N-cyclopropylamino group, N-cyclopentylamino group, N-cyclohexylamino group, N-phenylamino group, N- (4-methylphenyl) amino group, N' (4'chlorophenyl) amino group, N- (4-fluorophenyl) amino group, pyrrolidino group, piperidino group, and morpholino group.

AR'represents any one of naphthalen-2-yl group, 6-hydroxynaphthalen-2-yl group, 6-methoxynaphthalen-2-yl group, 6- (2-hydroxyethyloxy) naphthalen-2-yl group, 6-aminonaphthalen-2-yl group, 6- (N-methylamino) naphthalen-2-yl group, 6- (N, N-dimethylamino) naphthalen-2-yl group, 6- (2-hydroxyethylamino) naphthalen-2-yl group, benzo [b] furan-5-yl group, 2-methylbenzo [b] furan-5-yl group, 3-methylbenzo [b] furan-5-yl group, 2,3-dimethylbenzo [b] furan-5-yl group, benzo [b] thiophen-5-yl group, 2-methylbenzo [b] thiophen-5-yl group, 3-methylbenzo [b] thiophen-5-yl group, 2,3-dimethylbenzo [b] thiophen-5-yl group, lH-indol-5-yl group, 2-methyl-lH-indol-5-yl group, 3-methyl-1H-indol-5-yl group, 2, 3-dimethyl-lH-indol-5-yl group, 1-methyl-lH-indol-5-yl group, 1, 2-dimethyl-1H-indol-5-yl group, 1, 3-dimethyl-lH-indol-5-yl group, 1,2, 3-trimethyl-lH-indol-5-yl group, 1-ethyl-1H-indol-5-yl group, l-ethyl-2-methyl-lH-indol-5-yl group, 1-ethyl-3-methyl-1H-indol-5-yl group, 1-ethyl-2, 3-dimethyl-lH-indol-5-yl group, 1-propyl-1H-indol-5-yl group, 2-methyl-1-propyl-1H-indol-5-yl group, 3-methyl-1-propyl-1H-indol-5-yl group, 2, 3-dimethyl-l-propyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-lH-indol-5-yl group, 1- (2-hydroxyethyl)-2-methyl-lH-indol-5-yl group, 1- (2-hydroxyethyl)-3-methyl-lH-indol-5-yl group, 2, 3-dimethyl-1- (2-hydroxyethyl)-lH-indol-5-yl group, benzothiazol-6-yl group, 2-methylbenzothiazol-6-yl group, 2-methoxybenzothiazol-6-yl group, 2-aminobenzothiazol-6-yl group, 2-oxo-2,3-dihydrobenzothiazol-6-yl group, 2-oxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-2, 3-dihydrobenzothiazol-6-yl group, 2-thioxo-3-methyl-2, 3-dihydrobenzothiazol-6-yl group, quinolin-3-yl group, quinolin-6-yl group, 2-oxo-1, 2-dihydroquinolin-6-yl group, benzo [d] isothiazol-5-yl group, lH-indazol-5-yl group, 1-methyl-1H-indazol-5-yl group, l-ethyl-1H-indazol-5-yl group, 1-propyl-lH-indazol-5-yl group, 1-(2-hydroxyethyl)-lH-indazol-5-yl group, 3-hydroxy-lH-indazol-5-yl group, 3-hydroxy-l-methyl-lH-indazol-5-yl group, 1-ethyl-3-hydroxy-1H-indazol-5-yl group, imidazo [1, 2-a] pyridin-6-yl group, 1H-pyrrolo[2,3-b]pyridin-5-yl group, 1-methyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-ethyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, l-propyl-lH-pyrrolo [2, 3-b] pyridin-5-yl group, 1- (2-hydroxyethyl)-lH-pyrrolo [2, 3-b] pyridin-5-yl group, isoquinolin-6-yl group, 1-oxo-1, 2-dihydroisoquinolin-6-yl group, cinnolin-6-yl group, and benzoxazol-5-yl group. Provided that when AR'contains hydroxyl group, the hydroxyl group may be protected with Rpl, and when substituted AR'contains amino group, the amino group may be protected with Rp2.

Compound (I) of the present invention can be produced by, for example, employing the reactions according to the following various methods.

[Preparation Method 1] (Step a-1) As shown in the following scheme 1 : (Schemel) a compound of the present invention represented by the formula (Ia') wherein Y represents a lower alkyl group having 1 to 4 carbon atoms, and Rs, AR, and V on or in the aromatic ring (E) may be protected [hereinafter simply referred to as "Compound (Ia')"], which falls within the scope of Compound (I) of the present invention, can be prepared by reacting a compound represented by the formula (II) [simply referred to as"Compound (II)"hereinafter] with a boronic acid derivative represented by the formula (IV) [hereinafter simply referred to as"Compound (IV)"]. n, C2'to C6', Rs', AR', Y'and G in the formulas have the same meanings as defined above. In the formula of Compound (IV), Ll and L2 independently represent hydroxyl group, an alkoxyl group having 1 to 8 carbon atoms (e. g. , methoxy group, ethoxy group, propoxy group, isopropoxy group, cyclohexyloxy group), or a substituted or unsubstituted phenyloxy group, or Ll and L2 bind to each other to represent a 5-or 6-membered cyclic ester of an arylboric acid (e. g., 9- borabicyclo [3,3, l] nonane, 1,3, 2-dioxaborolane, 4,4, 5, 5-tetramethyl-1, 3, 2- dioxaborolane), which forms a ring containing boron atom [this ring may be saturated or unsaturated, may be a ring containing a heteroatom other than boron (e. g. , oxygen atom), and may be further substituted].

Further, as shown in the following scheme 2: Rs'C5'=C6, '1-a-1 C X (CH2)"-COOY' 3<_ AR' (Ia) Rs'c5 C"2) AR'-G /3'-Cz' Ll_ B c-I-C I (V) (VI) 12 L2 (Scheme2) an example of the method for preparing Compound (Ia') includes a method of reacting a combination of a compound represented by the formula (V) [hereinafter simply referred to as"Compound (V)"] and a compound represented by the formula (VI) [hereinafter simply referred to as"Compound (VI)"].

Examples include a method of preparing Compound (Ia') by performing the Suzuki reaction described in, for example, Jikken Kagaku Koza, 4th Edition (edited by Chemical Society of Japan, published by Maruzen Co. , Ltd. ), vol. 25, p. 403 with a combination mentioned either in the scheme l or scheme 2 or the both. A specific example includes a reaction of Compound (II) [or Compound (V)] with Compound (IV) [or Compound (VI)] in a solvent in the presence of a commercially available palladium catalyst or a catalyst prepared from a palladium complex and a ligand, and a base.

As the palladium catalyst, a commercially available catalyst such as tetrakis (triphenylphosphine) palladium, tetrakis (methyldiphenylphosphine) palladium, dichlorobis (triphenylphosphine) palladium, dichlorobis (tri-o- tolylphosphine) palladium, dichlorobis (tricyclohexylphosphine) palladium, dichlorobis (triethylphosphine) palladium, palladium acetate, palladium chloride, bis (acetonitrile) palladium chloride, tris (dibenzylideneacetone) dipalladium and bis (diphenylphosphinoferrocene) palladium chloride may be purchased and added to the reaction system, per se, or a catalyst may be added which is separately prepared from palladium acetate, tris (dibenzylideneacetone) dipalladium or the like and arbitrary ligands and isolated. Further, a catalyst considered to actually participate in the reaction may also be prepared by mixing palladium acetate, tris (dibenzylideneacetone) dipalladium or the like and arbitrary ligands in the reaction system. The valence of palladium may be 0 or may be +2. Examples of the ligand include phosphine ligands such as trifurylphosphine, tri (o- tolyl) phosphine, tri (cyclohexyl) phosphine, tri (t-butyl) phosphine, dicyclohexylphenylphosphine, 1, 1'-bis (di-t-butylphosphino) ferrocen, 2- dicyclohexylphosphino-2'-dimethylamino-1, 1'-biphenyl and 2- (di-t- butylphosphino) biphenyl and phosphine mimic ligands such as imidazol-2- ylidenecarbenes. Chemical equivalents of the palladium catalyst may be one equivalent or a catalytic amount, and the amount may preferably be 0.01 to 20.0 mol %, and most preferably be 0.10 to 10.0 mol %.

Examples of the base include sodium carbonate, potassium carbonate, cesium carbonate, cesium fluoride, potassium fluoride, potassium phosphate, potassium acetate, triethylamine, potassium hydroxide, sodium hydroxide, sodium methoxide, lithium methoxide and the like. The reaction temperature is, for example, preferably 20°C to 150°C, and particularly preferable examples include 20°C to 120°C.

The reaction system may be either a two-phase system of water and an organic solvent, or a homogeneous system of a water-containing organic solvent or an organic solvent. As for the organic solvent, examples include uses of hydrocarbon-type solvents such as toluene, xylene and hexane, halogen-type solvents such as methylene chloride, sulfoxide-type solvents such as dimethyl sulfoxide, amide-type solvents such as dimethylformamide, ether-type solvents such as tetrahydrofuran, dioxane and diglyme, alcohol-type solvents such as methanol and ethanol, nitrile-type solvents such as acetonitrile, ketone-type solvents such as acetone and cyclohexanone, ester-type solvents such as ethyl acetate, heterocyclic- type solvents such as pyridine and the like. Two or more kinds of organic solvents may be mixed and used.

For the reaction conditions, Miyaura, N. , Suzuki, A. , Chemical Review, 1995, vol. 95, p. 2457 ; Snieckus, V., Chemical Review, 1990, vol. 90, p. 879 and the like and references cited therein can be referred to.

When hydroxyl group or amino group reactive under the aforementioned reaction conditions or inhibiting the reactions exists in the group AR', Rs'or V'in the aromatic ring (E'), this substituent is preferably protected.

When a protective group of hydroxyl group or amino group exist in the group AR', Rs'or V in the aromatic ring (E') of the compound (Ia') prepared as described above, such a protective group can be eliminated during or after the preparation of Compound (Ia') to convert the compound into Compound (I) of the present invention. As for selection, introduction and deprotection of these protective groups of hydroxyl group and amino group, ordinary chemical publications, for example, Protective Groups In Organic Synthesis THIRD EDITION, John Wiley & Sons) and references cited therein can be referred to.

[Preparation Method 1] (Step a-2) As Compound (IV), a compound commercially available as a reagent may be used, or as shown in the following scheme 3: L1 1-a-2 <BR> <BR> <BR> <BR> <BR> AR'-B < AR'-G <BR> <BR> <BR> <BR> <BR> <BR> <BR> <BR> <BR> (vol) (IV) (Scheme3) the compound can be produced from Compound (VI), which is commercially available or can be synthesized by a known method or a similar method thereto, according to the method described in the aforementioned reference (Chemical Review, vol. 95, p. 2457,1995) or the method described in Satoh, Y. et al., SYNTHESIS, p. 1146,1994 or according to the references cited therein.

For example, examples include a method of preparing Compound (VI) by converting Compound (VI) into a lithio-compound using an alkyl lithium such as n- butyl lithium and t-butyl lithium, then reacting the product with a trialkyl borate and treating the product with a mineral acid such as hydrochloric acid, sulfuric acid, and phosphoric acid and a method of to preparing Compound (VI) by performing a cross-coupling reaction of Compound (VI) and an (alkoxyl) diboron in the presence of a palladium catalyst and a base.

An example of the preparation method of Compound (V) includes a method of subjecting Compound (II) to a reaction similar to that of the aforementioned Step a-2, as shown in the following scheme 4 : Rs'c5=cs, C4\\/ (E) -- n-COOY- /C3 B C5,-r61 1-a-2 C 3l-c2l mu (Scheme4) [Preparation Method 1] (Step b) As shown in the following scheme 5 : Rs'C51 C f I), - Hai l-b Rs-= C6 1* C3'C2 (VII) (Scheme5) a compound represented by the formula (IIh) (hereinafter simply referred to as "Compound (IIh)"), which correspond to the compounds (II) wherein G represents a halogen atom such as chlorine atom, bromine atom or iodine atom, can be prepared by halogenating a compound represented by the formula (VII) [this compound is simply referred to as"Compound (VII)"], which is commercially available or can be prepared by a known method or a method similar thereto. In the formula of Compound (IIh), the group Hal represents a halogen atom, which may be any of chlorine atom, bromine atom and iodine atom. As for the halogenation, examples of chlorination include a preparation method described in ordinary publications in the filed of chemistry, for example, Shin Jikken Kagaku Koza (edited by Chemical Society of Japan, published by Maruzen Co. , Ltd. ), vol. 14, p. 354. Examples of the method include a method utilizing chlorine (Cl2), a method utilizing sulfuryl chloride, and the like. Examples of bromination include a preparation method described in ordinary publications in the filed of chemistry, for example, Shin Jikken Kagaku Koza (edited by Chemical Society of Japan, published by Maruzen Co. , Ltd. ), vol. 14, p. 354. Examples of the method include a method utilizing bromine (Br2), a method utilizing N-bromosuccinimide, and the like. Examples of iodination include a preparation method described in ordinary publications in the filed of chemistry, for example, Shin Jikken Kagaku Koza (edited by Chemical Society of Japan, published by Maruzen Co. , Ltd. ), vol. 14, p. 423. Examples of the method include a method utilizing iodine (I2), a method utilizing potassium triiodide, and the like.

[Preparation Method 1] (Step c) As shown in the following scheme 6 : Rs''= 41* (E') -- n-COOY- /C3'C2' Su0 (IIs) Rs' c C (CH2) n-COOY' 3 HO (VIII) (Scheme6) a compound represented by the formula (IIs) (this compound is hereinafter simply referred to as"Compound (ITs)"), which corresponds to Compound (II) wherein G represents mesylate group, triflate group, or an arenesulfonate group, can be prepared by converting a compound represented by the formula (VIII) (this compound is simply referred to as"Compound (VIII) "), which is commercially available or can be prepared by a known method or a method similar thereto, into a sulfonic acid ester. In the formula of Compound (IIs), the group Su represents methanesulfonyl group, trifluoromethanesulfonyl group, or arenesulfonyl group of which aromatic ring may be substituted with one of T'or two or more of identical or different T1. Examples of the method for the conversion into sulfonic acid ester include a preparation method described in ordinary publications in the filed of chemistry, for example, Shin Jikken Kagaku Koza (edited by Chemical Society of Japan, published by Maruzen Co. , Ltd. ), vol. 14, p. 1793. Examples of the method include a method utilizing sulfonyl chloride, a method utilizing sulfonic anhydride, and the like.

[Preparation Method 2] (Step d) As shown in the following scheme 7: (Scheme7) a compound represented by the formula (Ib') wherein Y represents hydrogen atom, and Rs, AR, and V on or in the aromatic ring (E) may be protected (this compound is hereinafter simply referred to as"Compound (Ib') "), which constitutes a part of the scope of Compound (I) of the present invention, can be prepared by hydrolyzing Compound (Ia') so as to convert the group OY'into hydroxyl group.

For the reaction of converting Compound (Ia') into Compound (Ib'), in general, the compound is preferably reacted in a base. Further, for the reaction of converting Compound (Ia') to Compound (Ib'), in general, the compound is preferably reacted in an inert medium that does not inhibit the reaction, preferably a polar solvent.

Examples of the base used in the above reaction include, for example, alkali metal bases such as sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, sodium methoxide and potassium t-butoxide and organic bases such as triethylamine. As for amounts of the bases, generally 1 to 20 moles, preferably 1 to 10 moles, for alkali metal bases, or 1 to a large excess moles for organic bases based on Compound (Ia').

Examples of the polar solvent include water, methanol, ethanol, tetrahydrofuran, dioxane and the like, and these solvents may be used as a mixture as required. As the reaction temperature, an appropriate temperature of, for example, from room temperature to a refluxing temperature of solvent is chosen.

The reaction time is, for example, generally 0.5 to 72 hours, preferably 1 to 48 hours, when an alkali metal base is used, or generally 5 hours to 14 days when an organic base is used. Since progress of the reaction can be monitored by thin layer chromatography (TLC), high performance liquid chromatography (HPLC) or the like, the reaction can generally be terminated appropriately so as to maximize the yield of Compound (Ib').

For collection of Compound (Ib') obtained as described above from the reaction solution as a free carboxylic acid, operations may preferably be carried out by, when the polar solvent is a water-soluble solvent, evaporating the solvent, neutralizing the residue with an inorganic acid such as aqueous hydrochloric acid, dissolving the residue in a water-insoluble solvent, then washing the solution with a weakly acidic aqueous solution, water or the like, and evaporating the solvent.

When the polar solvent is a water-insoluble solvent, operations may preferably carried out by neutralizing the reaction solution with an inorganic acid, washing the solution with a weakly acidic aqueous solution, water or the like, and then evaporating the solvent.

Further, when Compound (Ib') forms a salt with the base used after the reaction to give a solid, the salt of Compound (Ib') can be obtained by isolation and purification of the solid in a conventional manner.

When a protective group of hydroxyl group or amino group exists in the group AR', Rs'or V'in the aromatic ring (E') of Compound (Ia') prepared as described above, Compound (Ia') can be converted into Compound (I) of the present invention by removing the protective group during or after the preparation of Compound (Ia').

[Preparation Method 3] (Step e) As shown by the following scheme 8 : (Scheme8) a compound represented by the formula (Ic') [hereinafter simply referred to as "Compound (Ic')"] as Compound (I) of the present invention wherein the group Y represents Y", and Rs, AR, and V in the aromatic ring (E) may be protected, can be produced by esterifying the carboxyl group (COOH) of Compound (Ib') in a conventional manner. In the formula of Compound (Ib'), Y"represents a lower alkyl group having 1 to 4 carbon atoms, a-(CH2) mNRl8Rl9 group, or- C (Rzo) 20C (O) A3R21.

Examples of the method for producing Compound (Ic') include a method of allowing Compound (Ib') to react with an inorganic halide without solvent or in an inert solvent to convert the compound into an acid halide and then allowing the acid halide per se or the same dissolved in an inert solvent to react with an excess amount of hydroxide of the targeted Y". Examples of the inorganic halide used in this method include thionyl chloride, phosphoryl chloride, phosphorus pentachloride, phosphorus trichloride and the like, and thionyl chloride is a preferred example. Examples of an amount used include generally an equimolar to a large excess amount, preferably 1.5 to 5 moles based on Compound (Ib').

Examples of the inert solvent used in this reaction include, for example, halogenated hydrocarbons such as dichloromethane, chloroform and 1, 2- dichloroethane, ethers such as tetrahydrofuran and dioxane, and benzene compounds such as benzene, toluene, xylene and chlorobenzene. These solvents can be used, for example, each alone or as a mixed solvent. In order to promote the reaction, a catalytic amount of N, N-dimethylformamide may be added. As a reaction temperature, an appropriate temperature of from room temperature to a refluxing temperature of the solvent is generally chosen. Examples of the reaction time include generally 0.5 to 24 hours, preferably 1 to 6 hours.

Examples of the inert solvent used for the reaction with hydroxide of the targeted Y"include, for example, halogenated hydrocarbons such as dichloromethane, chloroform and 1, 2-dichloroethane, ethers such as tetrahydrofuran and dioxane, and benzene compounds such as benzene, toluene, and xylene. The reaction can also be performed with an excess amount of the hydroxide of the targeted Y"without using a solvent. As the reaction temperature, an appropriate temperature of from-10°C to room temperature is chosen.

Examples of the reaction time include generally 0.5 to 24 hours, preferably 0.5 to 6 hours.

Other methods for producing Compound (Ic') include, for example, the "esterification using an alcohol"described in Shin Jikken Kagaku Koza (edited by the Chemical Society of Japan, published by Maruzen Co. , Ltd. ), vol. 14, p. 1002, "esterification using an 0-alkylating agent", ibid, the same volume, p. 1002, "esterification using an alkyl halide", ibid, the same volume, p. 1008,"esterification reaction using a dehydrating agent", ibid, vol. 22, p. 45 and the like.

When hydroxyl group or amino group reactive under the aforementioned reaction conditions or inhibiting the reactions exists in AR', Rs'or V'in the aromatic ring (E'), this substituent is preferably protected.

When a protective group of hydroxyl group or amino group exist in AR', Rs' or V'in the aromatic ring (E') of the compound (Ic') prepared as described above, such a protecting group can be eliminated during or after the preparation of Compound (Ic') to convert the compound into Compound (I) of the present invention.

[Preparation Method 4] As shown in the following scheme 9 : Rs'C5=C6, (E') z AR' (Id') 5= RsX5 Rs'-.., ,- /COOY' p41 AR,... AR (Scheme9) UHZ) 2-COOY' 4--fa compound represented by the formula (Id') (hereinafter this compound is simply referred to as"Compound (Id') ") as Compound (I) of the present invention wherein n in the methylene moiety is an integer of 2, and wherein Rs, AR, and V in the aromatic ring (E) may be protected, can also be prepared by the method shown below.

[Preparation Method 4] (Step f) Compound (Id') can be prepared by reducing the double bond of a compound represented by the formula (IX) (hereinafter this compound is simply referred to as "Compound (IX) ") using a reduction reaction described in ordinary publications in the filed of chemistry. Examples of the reaction include a method of converting the double bond of Compound (IX) into a single bond by hydrogenation using a hydrogen source such as hydrogen gas, ammonium formate, and hydrazine hydrate in a single solvent or a mixed solvent of alcoholic-type solvents such as methanol, ester'type solvents such as ethyl acetate in the presence of a catalyst such as palladium/carbon powder, platinum oxide (PtO2), and activated nickel.

When hydroxyl group or amino group reactive under the aforementioned reaction conditions or inhibiting the reactions exists in AR', Rs'or V'in the aromatic ring (E'), this substituent is preferably protected.

When a protective group of hydroxyl group or amino group exist in AR', Rs' or V'in the aromatic ring (E') of the compound (Id') prepared as described above, such a protecting group can be eliminated during or after the preparation of Compound (Id') to convert the compound into Compound (I) of the present invention.

[Preparation Method 4] (Step g) Compound (IX) can be prepared from a compound represented by the formula (III) [hereinafter this compound is simply referred to as"Compound (III)"].

Examples of the preparation method include a method utilizing the Horner-Emonds reaction described in Shin Jikken Kagaku Koza (edited by Chemical Society of Japan, published by Maruzen Co. , Ltd. ), vol. 14, p. 238. Specifically, the compound can be obtained by reacting Compound (III) with a commercially available dialkylphosphonoacetic acid ester in an inert solvent, for example, an alcohol-type solvent such as methanol and ethanol or ether-type solvent such as tetrahydrofuran and dimethoxyethane in the presence of a base such as sodium hydride and sodium alkoxide. As the reaction temperature, an appropriate temperature of from-10°C to a refluxing temperature of a solvent is generally chosen, and preferred examples include a temperature of from 0°C to room temperature. The reaction time is generally 1 to 16 hours, preferably 2 to 8 hours. Since progress of the reaction can be monitored by thin layer chromatography (TLC), high performance liquid chromatography (HPLC) or the like, the reaction can generally be terminated appropriately so as to maximize the yield of Compound (IX).

[Preparation Method 4] (Step a) As shown in the following scheme 10 : Rs', C5'=, CE'M-CHO -CHO c I), CHO 00 4-a N, r F-')/ "" c31-C2, AR (III) G (Scheme Compound (III) can be prepared by introducing the substituent AR'into a compound represented by the formula (X) [hereinafter this compound is simply referred to as "Compound (X)"] according to any of the methods described in the step a-1 of the preparation method 1 mentioned above.

[Preparation Method 5] As shown in the following scheme 11 : , s, Rs, C. COOH CN 2 \. AR (ive') Rsw 5 C /back AR' (Scheme1 a compound represented by the formula (Ie') [hereinafter this compound is simply referred to as"Compound (Ie')"], as Compound (I) of the present invention wherein n in the methylene moiety is an integer of 1, Y represents hydrogen atom, and Rs, AR, and V in the aromatic ring (E) may be protected, can also be prepared by the method shown below.

[Preparation Method 7] (Step d) Specifically, Compound (Ie') can be prepared by hydrolyzing nitrile group of a compound represented by the formula (XI) [hereinafter this compound is simply referred to as"Compound (XI)"] into carboxyl group according to a method similar to the method shown in the step d of the preparation method 2 mentioned above.

When a protective group of hydroxyl group or amino group exist in AR', Rs' or V'in the aromatic ring (E') of the compound (Ie') prepared as described above, such a protecting group can be eliminated during or after the preparation of Compound (Ie') to convert the compound into Compound (I) of the present invention.

[Preparation Method 5] (Step h) Compound (XI) can be produced from Compound (III) mentioned above.

For example, Compound (III) is reacted with a trimethylsilyl cyanide using a Lewis acid, particularly zinc iodide, as a catalyst in an inert solvent such as tetrahydrofuran as described in Jikken Kagaku Koza, 4th Edition (edited by Chemical Society of Japan, published by Maruzen Co. , Ltd. ), vol. 20, p. 445. Then, the reduction reaction using a hydrosilane described in Jikken Kagaku Koza, 4th Edition (edited by Chemical Society of Japan, published by Maruzen Co. , Ltd.), vol.

26, p. 197 is performed. Examples of the method of the reduction reaction include a method of performing the reduction with a hydrosilane such as triethylsilane and a protonic acid such as trifluoroacetic acid or a Lewis acid such as boron trifluoride in a halogenated solvent such as dichloromethane.

The preparation method of Compound (I) is not limited to the methods described herein. For example, the compounds of the present invention can be produced by modifying or converting a substituent of a compound serving as a precursor of the compounds according to a method or a combination of methods described in ordinary publications in the filed of chemistry.

Examples of the preparation method for Compound (I) of the present invention which contains an asymmetric carbon in the substituent Rs include a method of using a starting material in which a moiety corresponding to the asymmetric carbon in the substituent Rs is already optically active, which is commercially available (or can be prepared by a known method or a method similar thereto). A method is also available in which the compound of the present invention or a precursor thereof is separated as an optically active isomer in a conventional manner. Examples of such method include, for example, a method utilizing high performance liquid chromatography (HPLC) using a chiral column, a method comprising condensation with an optically active regent to form a diastereomer, successive separation and purification, followed by decomposition.

When a precursor is separated to obtain an optical isomer, optically active Compound (I) of the present invention can then be prepared by performing the aforementioned preparation methods.

When Compound (I) of the present invention contains an acidic functional group such as carboxyl group or phenolic hydroxyl group, the compound can be converted into pharmaceutically acceptable salt (e. g. , inorganic salts with sodium, ammonia and the like, or organic salts with triethylamine and the like) by a known means. For example, when an inorganic salt is to be obtained, it is preferable to dissolve Compound (I) of the present invention in water containing at least 1 equivalence of hydroxide, carbonate, bicarbonate or the like corresponding to a desired inorganic salt. For the reaction, an inactive water-miscible organic solvent such as methanol, ethanol, acetone, and dioxane may be mixed. For example, by using sodium hydroxide, sodium carbonate, or sodium hydrogencarbonate, a solution of sodium salt can be obtained.

When Compound (I) of the present invention contains a basic functional group such as amino group, or when Compound (I) of the present invention contains an aromatic ring which itself has properties of base (e. g. , pyridine ring), the compound can be converted into a pharmaceutically acceptable salt (e. g. , salt with inorganic acids such as hydrochloric acid and sulfuric acid, or salts with organic acids such as acetic acid and citric acid) by a known means. For example, when an inorganic salt is to be obtained, it is preferable to dissolve Compound (I) of the present invention in water containing at least 1 equivalence of a desired inorganic acid. For the reaction, an inactive water-miscible organic solvent such as methanol, ethanol, acetone, and dioxane may be mixed. For example, by using hydrochloric acid, a solution of hydrochloride can be obtained.

When a solid salt is desired, a solution may be evaporated, or a water- miscible organic solvent having polarity to some extent, such as butanol or ethyl methyl ketone, can be added to obtain a solid salt thereof.

The various compounds disclosed by the present invention can be purified by known methods such as recrystallization, and variety of chromatography techniques (column chromatography, flash column chromatography, thin layer chromatography, high performance liquid chromatography).

Compound (I) of the present invention and pharmaceutically acceptable salts thereof have an action of suppressing the production of both of prostaglandins and leukotrienes. The action of suppressing the production of prostaglandins and/or leukotrienes includes, for example, an action of suppressing PGE2 production, observed when cultured cells of MG-63 which is a human osteosarcoma cell line are stimulated with IL-1 ß and/or PGD2 and LTB4 production observed when cultured cells of RBL-2H3 which is a rat mastocytoma cell line are stimulated with IgE, by 10% or more, preferably 30% or more, most preferably 50% or more, compared with a positive control at a concentration of the compound not having cytotoxicity. As for a mode of action at a molecular level, it is considered that the compound of the present invention inhibits both of COX-1 and/or COX-2, which produce prostaglandins, and 5-LO, which produces leukotrienes. It is also considered that the compound of the present invention suppresses the production of arachidonic acid by inhibiting enzymatic activity of type 2A, 4, or 5 PLA2 involved in prostaglandin and leukotrien production.

It is considered that, in these molecular action mechanisms, Compound (I) of the present invention inhibits the enzymatic activity of type 4 PLA2. For the judgment, for example, the enzyme inhibitory action against type 4 PLA2 can be examined, and known methods for measuring the enzymatic activity of type 4 PLA2 are preferably utilized [Clark et al. , Proceeding of National Academy of Science USA (Proc. Natl. Acad. Sci. USA), 1990, vol. 87, p. 7708 ; Gronich et al., Biochemical Journal (Biochem. J. ), 1990, vol. 271, p. 37 ; Clark et al., Cell, 1991, vol. 65, p. 1043 ; Kramer et al. , Journal of Biological Chemistry (J. Biol. Chem), 1991, vol. 266, p. 5268]. The type 4 PLA2 inhibitory action of the compounds of the present invention can be elucidated by employing these methods.

Compounds (I) of the present invention and pharmaceutically acceptable salts thereof inhibited mouse inflammatory edema, allergic edema, acetic acid writhing reaction, and rat adjuvant arthritis by oral administration at a dose of 0. 1 to 500 mg/kg, and caused no death of the mice by oral administration at a dose of 500 mg/kg/day for 3 days. Therefore, they are safe compounds as drugs for mammals, preferably humans, pets or companion animals such as dogs and cats, and farm animals, and they are useful substances as active ingredients of medicaments. Preferred examples of the medicaments for mammals, preferably humans, pets or companion animals such as dogs and cats, and farm animals include agents for prophylactic and/or therapeutic treatment of various conditions, various diseases, and pathological conditions in which an acute or chronic inflammatory reaction resulted from production of prostaglandin and/or leukotriene is observed, specifically inflammatory diseases, allergic diseases, autoimmune diseases, and pain.

More specifically, the conditions or diseases include arthritis, chronic rheumatoid arthritis, malignant rheumatoid arthritis, juvenile rheumatoid arthritis, Felty's syndrome, adult Still's disease, osteoarthritis, synovitis, gout, slack of artificial joint implant, fervescence, common cold, algesia, burn, thermal injury, keloplasty, menstrual pain, dysmenorrhea, menstrual cramp, allergic reaction, allergic contact hypersensitivity, allergic rhinitis, pollinosis, allergic conjunctivitis, hypersensitivity pneumonitis, allergic bronchopulmonary mycosis, emphysema, acute respiratory distress syndrome, asthma, bronchitis, chronic obstructive pulmonary disease, chronic bronchitis, pulmonary emphysema, diffuse panbronchiolitis, respiratory obstruction, graft versus host syndrome, urticaria, ultraviolet radiation dermatitis, atopic dermatitis, cancer, myelogenous leukemia, sarcomata, brain tumor, cachexia, tissue ulcer, digestive ulcer, gastritis, acute and chronic pancreatitis, regional enteritis, ulcerative colitis, diverticulitis, recurrent gastroenteric disorder, gastroenteric bleeding, inflammatory bowel disease, Crohn's disease, intestinal tract type Behcet's disease, infectious enteritis, ischemic enteritis, radiation enteritis, drug-induced enteritis, irritable bowel syndrome, hepatic diseases (hepatopathies, liver failures) such as acute hepatitis, fulminant hepatitis, chronic hepatitis, hepatic cirrhosis, fatty liver, alcoholic liver injury, drug liver injury (drug-induced hepatitis), congestive hepatitis, autoimmune hepatitis, primary biliary cirrhosis and hepatic porphyria, coagulation, anemia, ankylosing spondilitis, restenosis, periodontosis, epidermolysis bullosa, atherosclerosis, aortic aneurysm, periarteritis nodosa, congestive cardiac failure, arrhythmia, myocardial infarction, cerebral infarction, attack, cerebral ischemia, head injury, spinal cord injury, myelopathic muscular atrophy, neuralgia, neurodegenerative disease, Alzheimer's disease, Lewy body disease, Shy-Drager syndrome, Reye's syndrome, progressive supranuclear palsy, progressive multifocal leukoencephalopathy, normal pressure hydrocephalus, subacute sclerosing panencephalitis, frontal lobe type dementia, acute anterior poliomyelitis (poliomyelitis), poliomyelitis neurosis, viral encephalitis, Creutzfeldt-Jakob disease, Kuru disease, bovine spongiform encephalopathy (mad cow disease), scrapie, epilepsy, cerebral amyloid angiopathy, autoimmune disease, Huntington's disease, Parkinson's disease, migraine, depression, mania, manic-depressive psychosis, hereditary cerebellar ataxia, peripheral neuropathy, glaucoma, pain, gingivitis, postoperative pain, amyotrophic lateral sclerosis, osteoporosis, multiple sclerosis, ocular angiogenesis, cornea damage, macular degeneration, conjunctivitis, abnormal wound healing, sprain or strain of muscle or joint, tendinitis, skin disease, psoriasis vulgaris, pustular psoriasis, erythroderma psoriaticum, arthritic psoriasis, myasthenia gravis, multiple myositis, myositis, bursitis, diabetes mellitus, tumor invasion, tumor growth, tumor metastasis, cornea scar, scleritis, immunodeficiency disease, pachydermia, eosinophilic fasciitis, sepsis, endotoxin shock, premature delivery, hypoprothrombinemia, hemophilia, thyroiditis, sarcoidosis, Behcet's syndrome, hypersensitivity, renal disease, rickettsial infectious disease, protozoal disease, reproduction disease, sepsis shock and the like. Other specific conditions and diseases include toothache, pain after tooth extraction, back or low back pain, periarthritis humeroscapularis, cervico-omo-brachial syndrome, tenosynovitis, acute upper respiratory inflammation, herpes zoster, fibrosis, pulmonary fibrosis, pneumoconiosis, chronic interstitial pneumonia, granulomatous interstitial pneumonia, fibrosing interstitial pneumonia, renal fibrosis, nephropyelitis, various types of secondary contracted kidney, glomerular nephritis, chronic nephritis, glomerulosclerosis, hepatic fibrosis, cardiac fibrosis after myocardial infarction, idiopathic cardiomyopathy, pancreatic sclerosis, pancreatic fibrosis, pancreatolithiasis, Takayasu's arteritis, chronic thyroiditis, dermatomyositis, multiple myositis, myelofibrosis, Banti disease, retroperitoneal fibrosis, various radiation injuries and the like. Further, the medicament comprising Compound (I) of the present invention as an active ingredient can be used for the aforementioned conditions or diseases of mammals, preferably humans, pets or companion animals such as dogs and cats or farm animals together with or in combination with one or more kinds of other prophylactic or therapeutic drugs.

Examples of the drugs that can be used together or in combination include, for example, the following drugs : immunomodulation-type antirheumatic drugs and antimetabolite used as therapeutic drugs for rheumatoid arthritis, specifically, gold preparations, bucillamine, lobenzarit, salazosulfapyridine, methotrexate, azathiopurin, mizoribine, leflunomide, tacrolimus, cyclosporin and the like and preparations containing the same; anti-cytokine antibody preparations directed to cytokines such as interleukin (IL) 1, IL-6, and tumor necrosis factor (TNF)-a or preparations of soluble receptors for those cytokines, which are biological preparations, specifically, infliximab, etanercept and the like and preparations containing the same ; steroid preparations, specifically, dexamethasone, betamethasone, prednisolone, fluticasone, beclometasone and the like and preparations containing the same ; bronchodilators used as therapeutic agents for chronic bronchial asthma, specifically, salmeterol and salbutamol, which are adrenalin B 2 stimulants, ipratropium, which is an anticholinergic drug, and the like and preparations containing the same ; therapeutic drugs for allergic diseases, for example, theophyline, which is a xanthine analogue drug, and the like, fexoquinadine, epinastatine, cetirizine, ketotifen, disodium cromoglycate, pemirolast and the like, which are antiallergic agents, fexoquinadine, cetirizine and the like, which are antihistaminic agents, and preparations containing the same ; irinotecan, 5-fluorouracil and the like, which are antitumor agents, and preparations containing the same. Further, the medicament comprising Compound (I) of the present invention as an active ingredient is used, for example, together with or in combination with radiotherapy.

In order to use Compound (I) of the present invention or pharmaceutically acceptable salts thereof for the medicaments described above, an effective amount of Compound (I) of the present invention or a pharmaceutically acceptable salt thereof, per se, may be used, or the substance may be mixed with a pharmaceutically acceptable carrier to form a pharmaceutical composition. The carrier may be, for example, a suspending agent such as carboxymethylcellulose, or purified water, physiological saline or the like, if desired. Other known carriers can also be used. Examples include a method of dissolving Compound (I) of the present invention or a pharmaceutically acceptable salt thereof in purified water containing 0.5% carboxymethylcellulose and using the solution.

Examples of formulations for preparing the aforementioned pharmaceutical composition include tablet, powder, granule, syrup, suspension, capsule, and injection. For the manufacture of these formulations, various carriers suitable for these preparations are used. For example, examples of the carrier for oral preparations include excipients, binders, lubricants, fluid accelerators, and colorants.

When the compound of the present invention is formulated as a parenteral preparation such as an injection, water for injection, physiological saline, glucose aqueous solution, vegetable oil for injection, propylene glycol, polyethylene glycol and the like can generally be used as a diluent. Disinfectants, antiseptics, stabilizers, isotonic agents, soothing agents and the like may be further added, as required.

When the compound of the present invention is administered to a mammal, e. g. , human, the compound can be administered in the form of a tablet, a powder, a granule, a suspension, a capsule or the like. The compound can also be parenterally administered in the form of a suppository, a gel, a lotion, an ointment, a cream, or a spray. A dose thereof varies depending on a disease to be applied, administration route, age, weight, degree of symptom of a patient and the like.

Examples of the dose include generally an administration at a dose of 1 to 1,000 mg per day for an adult once to three times a day. Every day administration for a period of several days to two months is commonly applied. The daily dose and the administration period may be increased or decreased depending on symptoms of a patient.

Fibrosis, which is a disease characterized by fibrosing of tissues, is known as a severe disease which is often mortal. Fibrosing of tissues is caused by proliferation of interstitial cells, which represented by fibroblasts, and production of extracellular matrix such as collagen. Fibrosing is considered a repair mechanism against tissue affections in organs. Excessive fibrosing causes fibrosing diseases of organs, and further progression of fibrosing causes sclerotic diseases. Many of such sclerotic diseases are intractable, progressive and irreversible. Although fibrosing varies in various organs, etiological hypotheses of fibrosing have many similarities. That is, a certain inflammatory lesion precedes, and in its healing process, various kinds of cytokines and growth factors are produced mainly from immunocompetent cells and platelets as well as interstitial cells such as fibroblasts themselves involved in the healing, and activated to cause deposition of extracellular matrix (Takehara, Molecular Medicine, 2001, vol. 38, p. 854).

Among fibroses, pulmonary fibrosis is one of the representative diseases.

Pulmonary fibrosis is a disease in which disruption of alveolar structure is caused by chronic inflammation and increase of collagenic fibers in alveolar walls, and which eventually leads to respiratory failure and death. For example, pulmonary fibrosis occurs following infectious pneumonia and the like. Examples of the infectious pneumonia include severe acute respiratory syndrome (SARS) and influenzal pneumonia. It has been reported that, in SARS, in particular, severe inflammation is caused in pulmonary stroma, and as a result, it highly likely to develop into pulmonary fibrosis (Antonino et al. , Radiology, 2003). In addition, pulmonary fibrosis is also caused by various medicaments.

In recent years, with increase of medicaments used for diagnosis, prophylactic and therapeutic treatments of various kinds of diseases, drug-induced pulmonary fibrosis caused by such drugs is increasing. Drug-induced pulmonary fibrosis is a severe disease that eventually leads to death, and it causes serious problems in therapeutic treatments of various diseases. Therefore, prophylactic and therapeutic treatments of drug-induced pulmonary fibrosis constitute a particularly important subject of concern.

Against drug-induced pulmonary fibrosis, steroid therapy is currently used.

However, effective rate of the steroid therapy is low and the effect is only partial and transient, and thus lesions often remain [Igaku no Ayumi, 2001, vol. 197, p. 313]. Further, side effect of steroid agents and acute aggravation due to decrease of doses or termination of their administrations are also often observed, which remains clinically far unsatisfactory level.

As a recent finding, it was reported that administration of pirfenidone was effective against pulmonary fibrosis in clinical tests in the United States (Raghu et al. , American Journal of Respiratory and Critical Care Medicine, 1999, vol. 159, p. 1061) and Japan (Nagai et al., Internal Medicine, 2002, vol. 41, p. 1118).

However, development of novel prophylactic and/or therapeutic agents highly effective for these diseases is desired at all events.

The medicament provided by the present invention is useful as a medicament containing a type 4 PLA2 inhibitor as an active ingredient for prophylactic and/or therapeutic treatment of fibrosis, preferably pulmonary fibrosis, further preferably drug-induced pulmonary fibrosis.

As described above, fibrosis, in particular, pulmonary fibrosis, is a severe disease and is an important object of prophylactic and/or therapeutic treatment.

As for pulmonary fibrosis, more than 100 kinds of factors including toxic gases and various medicaments have been elucidated as the causes of early alveolopathy. As described above, with the increase of medicaments used for diagnosis, prophylactic and therapeutic treatments of various kinds of diseases, drug-induced pulmonary fibrosis caused by such drugs is increasing.

As for drug-induced pulmonary fibrosis, causality between expression of pathological conditions such as coughing, difficulty of breathing, or fervescence and the administration of medicaments is suspected, and it is considered that a diffuse interstitial shadow appears on a thoracic X-ray photograph simultaneously with or slightly after the administration of medicaments.

As medicaments reported to cause drug-induced pulmonary fibrosis, anticancer agents, anti-rheumatic agents, immunosuppressants, antibiotics, chemotherapeutants, antihypertensive agents, diuretics, anti- inflammatory/analgesic agents, biologics, Chinese medicines are known (Inooka et al. , Therapeutics, 1995, vol. 29, p. 1295). Typical medicaments are shown in Table 1.

Table 1 Classification Examples of agent 1) Anticancer agent, Peplomycin, bleomycin, cychlophosphamide, nitrosourea, immunosuppressant busulfan, methotrexate, azathioprine, mitomycin-C, tegafur, carmofur, tegafur/uracil preparation, cisplatin, doxorubicin, 6-mercaptopurine, daunomycin, vincristine, vinblastine, vindesine, procarbazine, neocarzinostatin, melphalan, thiotepa, nimustine, cytarabine, zinostatin stimalamer, chlorambucil, carmustine, lomustine, semustine, teniposide, etoposide, Taxol, taxotere, irinotecan, gefitinib, tamoxifen and the like. 2) Antihypertensive a-methyldopa, trichlormethiazide, hydrochlorothiazide, agent, diuretic enalapril, hexamethonium, mecamylamine, pentolinium, practolol, pindolol, propranolol, acebutolol, hydralazine 3) Antibiotic, Cephem antibiotics (cephaloridine, cephalothin, chemotherapeutant cephalexin, cefradine, cefazolin, cefaclor, cefmenoxime, cefmetazole, cefoperazone, cefotiam, cefroxadin, ceftizoxime, latamoxef and the like), tetracyclines (minocycline, oxycycline), antituberculous agents (isoniazid, paraaminosalicylic acid, rifampicin, streptomycin), penicillin antibiotics (ampicillin, piperacillin, vastcillin, pentcillin, amoxicillin), aminoglycoside antibiotics (streptomycin), macrolide antibiotics (midecamycin), phosphomycin, aminoglycosides (tobramycin, Micromycin), new quinolone drugs (enoxacin, ofloxacin, norfloxacin), antifungal agents (amphotericin) and the like 4) Others Inhalants (cromoglicic acid and the like), gold preparations (aurothiomalic acid and the like), psychotropic agents and nervines (aminotriptyline, diphenylhydantoin, carbamazepine, phenobarbital, valproate salt, imipramine, mephenesin, meprobamate), antiphlogistic and analgesics (naproxen, acetaminophen, acetylsalicylic acid, phenacetin, diclofenac, loxoprofen, fenbufen, nabumetone, aluminoprophen and the like), antiarrhythmic agents (amiodarone, procainamide, aprindine), antidiabetic agents (chlorpropamide), antithyroid agents (thiouracil), proteolytic enzymes (serrapeptidase), antiparkinsonic agents (levodopa, bromocriptine), antirheumatic agents (bucillamine, auranofin, actarit), sho-saiko-to, chai-ling-tang, rikkunshi-to, interferon, warfarin, salazosulfapyridine, dichloroferamide, fominoben, D-penicillamine, propylthiouracil, corticosteroid, flavoxate, allopurinol, ethoxysclerol and the like In therapeutic treatment of rheumatoid arthritis, for example, agents that cause pulmonary fibrosis at high frequency such as methotrexate and sodium aurothiomalate are used as disease-modifying antirheumatic drugs. Further, disease-modifying antirheumatic drugs that may cause pulmonary fibrosis at a relatively low frequency, such as actarit, bucillamine, auranofin, salazosulfapyridine, and D-penicillamine are also used. Although these disease- modifying antirheumatic drugs are useful agent in the rheumatoid arthritis treatment system, pulmonary fibrosis caused as a side effect is a factor of restricting use of these drugs. In recent years, methotrexate, in particular, has come to be used as an antirheumatic agent, and onset of pulmonary fibrosis that is also histopathologically called interstitial pneumonia as the side effect of methotrexate becomes a problem in the rheumatoid arthritis treatment system.

Further, in cancer therapy, cychlophosphamide, Taxol, etoposide, cisplatin, vincristine, vinblastine, irinotecan, gefitinib, and bleomycin are useful as anticancer agents. However, because all of these anticancer agents cause pulmonary fibrosis that is also histopathologically called as interstitial pneumonia as a side effect at a high frequency, they have a problem in the therapeutic treatment system. Bleomycin, gefitinib, irinotecan, and cisplatin are used for therapeutic treatment of lung cancer. However, if patients with lung cancer develop pulmonary fibrosis, the condition is most likely for the patients to be fatal.

Among these drugs, bleomycin suffers from a problem that it causes pulmonary fibrosis at a high frequency.

Preferred objects of application of the medicament of present invention are drug-induced pulmonary fibroses caused by these drugs.

In present invention, the type 4 PLA2 inhibitor is not particularly limited so long as the inhibitor has type 4 PLA2 inhibitory activity. For example, known type 4 PLA2 inhibitors can be chosen. Examples of the known type 4 PLA2 inhibitors include the following inhibitors : the compounds described in U. S. Patent No. 5,462, 954, preferably 2-phenyl-4-ethyl-5- [6- (2H-tetrazol-5-yl)-6- methylheptyloxy] phenol, 8-propyl-7- {3- [4- (4-fluorophenyl)-2-ethyl-5- hydroxyphenyloxy] propyloxy}-3, 4-dihydro-2H-1-benzopyran-2-carboxylic acid, and 2- {3- [3- ([5-ethyl-2-hydroxy (l, 1'-bip henyl)-4-yl] oxy) propyloxy]-2- propylphenyloxy} propionic acid ; the compounds described in W099/43654, preferably 4- (1-benzhydryl-6-chloro-lH-indol-3-ylmethyl)-3-methoxybenzoic acid ; the compounds described in W098/33797, preferably N-14- (biphenyl-2-ylmethyl- isobutylamino)-1- [2- (4-fluorobenzoyl) benzoyl] pyrrolidin-2-ylmethyl}-3- [4- (2,4- dioxothiazolidin-5-ylidenemethyl) phenyl] acrylamide and the like ; the compounds described in WO01/30387, preferably N- [2- (2,4-difluorobenzoyl) benzoyl]-4- tritylsulfanylpyrrolidin-2-ylmethyl}-4- (2, 4-dioxothiazolidin-5-ylidenemethyl) benzoic acid amide and the like; the compounds described in W099/15129, preferably 4-{4- [2- (2- [bis (4-chlorophenyl) methoxy] ethylsulfonyl) ethoxy] phenyl}-1, 1, 1-trifluoro-2- butanone and the like ; the compounds described in W098/05637, preferably 1- {2- [4- (carboxymethyl) phenoxy] ethyl}-3-dodecanoylindole-2-carboxylic acid and the like ; the compounds described in Japanese Patent Unexamined Publication (Kokai) No.

2002-80368, preferably 4-methyl-2-oxo-5- (5, 6,7, 8-tetrahydronaphthalen-2- yl) oxazolidine-3-carboxylic acid (6-methoxytetrahydropyran-2-yl) amide, 4-methyl-2- oxo-5- (4-methylphenyl) thiazolidine-3-carboxylic acid (tetrahydropyran-2-yl) amide and the like ; and the type 4 PLA2 inhibitors selected from the compounds described in W098/08818, the compounds described in W099/43651, the compounds described in W099/43672, the compounds described in W003/048122, the compounds described in W095/10508, the compounds described in W097/05135, the compounds described in Japanese Patent Unexamined Publication No. 7-126166, the compounds described in Japanese Patent Unexamined Publication No. 7-224076, the compounds described in Japanese Patent Unexamined Publication No. 7-224076, the compounds described in Japanese Patent Unexamined Publication No. 2000- 119292, the compounds described in Japanese Patent Unexamined Publication No.

2000-109432, the compounds described in Japanese Patent Unexamined Publication No. 7-223997, the compounds described in the U. S. Patent No. 5,994, 398, the compounds described in WO00/27824, the compounds described in Japanese Patent Unexamined Publication No. 2000-38380, the compounds described in WOOO/71118, the compounds described in Japanese Patent No. 3107613, the compounds described in W003/031414, the compounds described in U. S. Patent No. 5,453, 443, and the compounds described in W002/038575. Examples further include the following known type 4 PLA2 inhibitors described in references arachidonyl trifluoromethyl ketone (Street et al. , Biochemistry, 1993, vol. 32, p. 5935) ; methyl arachidonyl fluorophosphate (Kennedy et al. , Mediators of Inflammation, 1994, vol.

3, p. 337) ; (3-lactam derivatives (Burke et al. , J. Enzyme Inhibition, 1998, vol. 13, p. 195) ; choline derivatives (Burke et al. , J. Biol. Chem. , 1999, vol. 274, p. 18864) ; 1, 3-disubstituted propan-2-one derivatives, especially 4- [3- (4-decyloxyphenyloxy)-2- oxopropyloxy] benzoic acid (Connolly et al. , J. Med. Chem. , 2002, vol. 45, p. 1348) ; Surfactin (Kim et al. , Biochem. Pharmacol. , 1998, vol. 55, p. 975) ; 1,1, 1- trifluorononadeca-10, 13,16-trien-2-one and 1, 1, 1-trifluorononadeca-10, 13-dien-2- one (Amandi-Burgermeister et al. , Eur. J. Pharmacol. , 1997, vol. 326, p. 237); and 2- oxoamide derivatives (Kokotos et al. , J. Med. Chem. , 2002, vol. 45, p. 2891).

In the present invention, preferred examples of type 4 PLA2 inhibitor further include the compounds represented by the aforementioned formula (I) and pharmacologically acceptable salts thereof. Various combinations of the compounds represented by the formula (I) and pharmacologically acceptable salts thereof described in the specification can also be arbitrarily chosen.

When a medicament comprising a type 4 PLA2 inhibitor as an active ingredient is used as a prophylactic and/or therapeutic agent for fibrosis, as for Compound (1) of the present invention, for example, Compound (I) of the present invention or a pharmaceutically acceptable salt thereof, per se, may be used in an effective amount, or the substance may be used after preparation of a pharmaceutical composition in the form of solid, liquid or gel by mixing the substance with a pharmaceutically acceptable carrier. As for the pharmaceutically acceptable carrier, known information and the information about carriers described in this specification can be referred to. As for known type 4 PLA2 inhibitors, a known type 4 PLA2 inhibitor or a pharmaceutically acceptable salt thereof, per se, may be used in an effective amount, or as mentioned above, the inhibitors may be used after preparation of a pharmaceutical composition by mixing the inhibitor with a pharmaceutically acceptable carrier.

It would be readily understood by those skilled in the art that progression- preventing agents, that is used for preventing progression of pathological conditions, occasionally fall within the scope of the agent for prophylactic and/or therapeutic treatment of the present invention.

Examples of the dosage form for preparation of the aforementioned pharmaceutical composition, tablet, powder, granule, syrup, suspension, capsule, inhalant, injection, and the like, and in order to prepare the compositions, various carriers are used depending on the type of the composition. Examples of the carrier for oral agents include, for example, excipients, binders, lubricants, flowability improvers, and colorants. When an inhalant is prepared (examples of administration method include a method of inhaling powder of the pharmaceutical composition or a solution obtained by dissolving or suspending the pharmaceutical composition in a solvent, per se, a method of inhaling mist of the composition prepared by using a sprayer called atomizer or nebulizer), the preparation the aforementioned pharmaceutical composition in the form of solid can be referred to for preparation of a powder for the inhalation, and a powder obtained is preferably further made into micropowder. When the composition is inhaled as a liquid, preferred examples of the preparation method include a method of dissolving a solid pharmaceutical composition, which is prepared by referring to the above explanation, in distilled water or a suitable solvent to obtain a solution of medicament upon use, and a method of preparing a liquid pharmaceutical composition prepared by referring the above explanation to obtain a solution of medicament. As for a size of the aforementioned powder or mist of a solution of a medicament to be inhaled, a particle size may be suitable for inhalation. For example, an upper limit is preferably 100, u m or less, further preferably 50, u m or less, most preferably 10 ju m or less. A lower limit is not particularly limited, and a smaller particle size is more preferred. When an injection and the like are prepared, distilled water for injection, physiological saline, glucose solution, vegetable oil for injection, propylene glycol, polyethylene glycols and the like can generally be used as diluents. Further, antimicrobial agents, antiseptics, stabilizers, isotonic agents, soothing agents, and the like may be added, as required.

When the aforementioned prophylactic and/or therapeutic agent is administered, a suitable dosage form can be chosen and administered via a suitable route. For example, the agent can be orally administered in the form of a tablet, a powder, a granule, a syrup, a suspension, or a capsule. The agent can also be administered via transairway route in the form of an inhalant. Further, the agent can be administered subcutaneously, intradermally, intravascularly, intramuscularly or intraperitoneally in the form of injection including a drip infusion. Furthermore, the agent can be transmucosally administered in the form of a sublingual agent or a suppository, and can be transdermally administered in the form of a gel, a lotion, an ointment, a cream, or a spray.

A dose thereof varies depending on the dosage form, and the age, weight, degree of symptoms of a patient and the like. Examples of the dose include generally an administration at a dose of 1 to 1,000 mg per day for an adult once to three times a day. Every day administration for a period of several days to two months is commonly applied. The daily dose and the administration period may be increased or decreased depending on symptoms of a patient.

As for the application of the aforementioned prophylactic and/or therapeutic agent, the agent may be administered to patients with pulmonary fibrosis as explained above. In addition, the prophylactic and/or therapeutic agent of the present invention containing a type PLA2 inhibitor as an active ingredient may preferably be administered after the administration of, most preferably immediately after the administration of an agent, which may possibly induces pulmonary fibrosis as an adverse reaction. Furthermore, as for the administration time, the prophylactic and/or therapeutic agent of the present invention may be administered simultaneously with an agent which may possibly induces pulmonary fibrosis as an adverse reaction, or the agent of the present invention may be administered beforehand.

Examples The present invention will be further specifically explained with reference to examples. However, the scope of the present invention is not limited to the following examples. In the examples, for thin layer chromatography (TLC), Precoated Silica Gel 60 F254 (produced by Merck, product number: 5715-1M)) was used. After development with chloroform: methanol (1 : 0 to 1: 1), acetonitrile: acetic acid: water (200: 1: 1 to 100: 4: 4) or ethyl acetate: hexane (1: 0 to 0: 1), spots were observed by UV irradiation (254 nm) or color development with ninhydrine or dinitrophenylhydrazine solution in hydrochloric acid. For drying organic solvent, anhydrous magnesium sulfate or anhydrous sodium sulfate was used. As for column chromatography, the indication of"Quad"means use of Quad 1 preparative chromatography system (produced by Biotage), and one or several columns selected from cartridge columns KP-Sil-12M, 40S and 40M produced by the same manufacturer were used depending on the amount of sample. For flash column chromatography, Silica gel 60N (spherical shape, neutral, 40 to 100, u m, produced by Kanto Chemicals) was used. Preparative thin layer chromatography (hereinafter abbreviated as"PTLC") was performed by using one or several plates of PLC Plate Silica Gel 60 F254 (20 x 20 cm, thickness: 2 mm, concentration zone : 4 cm, produced by Merck, product number: 13793-1M) were used depending on the amount of sample.

The indication of"LCMS"means that mass spectrum was measured by liquid chromatography-mass spectrometry (LC-MS). Platform-LC type mass spectrometry apparatus (produced by Micromass) was used as the mass spectrometer, and the measurement was performed by the electrospray ionization (ESI) method. As a liquid chromatography apparatus, an apparatus produced by GILSON was used. As a separation column, Mightysil RP-18 GP 50-4.6 (produced by Kanto Chemicals) was used. Elution was generally performed at a flow rate of 2 mllminute, and Solution A = water [containing 0. 1% (v/v) acetic acid] and Solution B = acetonitrile [containing 0.1% (v/v) acetic acid] were used as solvents.

In the tables mentioned below, data indicated by"LCMS"mean data of liquid chromatography-mass spectrometry spectra. In the columns of"Mass", data of mass spectrometry were shown (the indication"N. D" means that no molecular ion peak was detected). In the columns of"method", elution conditions of the liquid chromatography are described. In the columns of"RTime", retention times in the liquid chromatography are shown. For the indication of retention time in the liquid chromatography, the indication"A"for elution condition means that measurement was performed by elution with a linear gradient of 5 to 100% (v/v) Solution B from 0 minute to 5 minutes and then with 100% Solution B until 6 minutes. Similarly, the indication"B"for elution condition means that measurement was performed by elution with 30% (v/v) Solution B from 0 minute to 0.5 minute, then with a linear gradient of 30 to 95% (v/v) Solution B from 0.5 minute to 4 minutes and then with 95% (v/v) Solution B until 6 minutes. For the compounds with the indication C in the columns of elution conditions, data of mass spectrometry measured by fast atomic bombardment mass spectrometry (FAB-MS) using JEOL-JMS-SX102 (produced by JEOL Co. , Ltd. ) were mentioned in the columns of"Mass". Further, for the compounds with the indication D in the elution conditions, an apparatus manufactured by Waters Ltd. was used as a liquid chromatography apparatus. As a column for separation, Develosil C30-UG-5 (50 x 4.6 mm, Nomura Kagaku Co. , Ltd. ) was used. Measurement was performed under elution condition with a linear gradient of 5 to 98% (v/v) Solution B from 0 minute to 4 minutes and then with 100% Solution B until 6 minutes.

In the columns indicated as"Exp.", compound numbers are shown. When the tables include a column indicated as"position", substituting positions of substituents are indicated in the column. The abbreviations used in the tables have the following meanings. n: normal, i : iso, s: secondary, t: tertiary, c: cyclo, D : di, Me: methyl, Et: ethyl, Pr: propyl, Bu: butyl, Pen: pentyl, Hex: hexyl, Hep: heptyl, Ph: phenyl, Bn: benzyl, Py: pyridyl, Indan: indanyl, Ac: acetyl, CHO: formyl, COOH : carboxyl, N02 : nitro, DMA : dimethylamino, NH2 : amino, CF3: trifluoromethyl, F: fluoro, Cl: chloro, Br: bromo, OMe : methoxy, OH : hydroxy, TFA: trifluoroacetyl, S02 : sulfonyl, CO: carbonyl, Nap: naphthyl, Ind : lH-indolyl, lHIdz : 1H-indazolyl, 2HIdz: 2H-indazolyl, Bzt: benzothiazole, 2ABzt: 2-aminobenzothiazole, BF : benzofuranyl, BT : benzo [b] thienyl, Qu : Quinolyl, IQ: isoquinolyl The numbers given before the substituents indicate substituting positions.

The numbers given with hyphens before abbreviations of aromatic rings indicate substituting positions of the aromatic rings. (S) indicates optically active substances with S-configuration, and (R) indicates optically active substances with R-configuration. Representative examples of the substituents shown in the tables with abbreviations are listed in Table 2 mentioned below.

Table 2 Structure abbreviation abbreviation Structure cPenMeO 2EtBuO--Iro 3DMeBuO aO cPenO 1 cHexO zu ce t o 2-Indano (4FPh) EtO (4DMAPh) EtO . F 2 o 2 (PhO) EtO F 4 (OMe) BnC 2-Nap Ne » N St N @ 3-Qu N The manufacturers of the regents used may sometimes be indicated with the following abbreviations.

TCI: Tokyo Kasei Kogyo Co. , Ltd., Ald : Aldrich Co. , KANTO: Kanto Kagaku, WAKO: Wako Pure Chemical Industries, Ltd., LANC : Lancaster Synthesis, MAYB: Maybridge, plc.

[Example A-1] Synthesis of methyl 3- (4-hydroxyphenyl) propionate (Intermediate 1) A solution obtained beforehand by adding thionyl chloride (18.3 ml, WAKO) dropwise to methanol (250 ml) and mixing the mixture under ice cooling was added dropwise with a solution of 3- (4-hydroxyphenyl) propionic acid (16. 6g, TCI) in methanol (50 ml) under ice cooling, stirred for 30 minutes, warmed to room temperature, and further stirred for 1.5 hours. The reaction mixture was concentrated under reduced pressure, and then extracted with diethyl ether (200 ml). The organic layer was washed successively with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride and saturated brine.

The organic layer was dried, and then the solvent was evaporated under reduced pressure to obtain the title compound (Intermediate 1,17. 95 g).

Synthesis of methyl 3- (4-cyclopentylmethyloxyphenyl) propionate (Intermediate 2) A solution of cyclopentane methanol (4.05 ml, Ald) in anhydrous tetrahydrofuran (abbreviated as"THF"hereinafter, 40 ml) was added with triethylamine (6.49 ml, WAKO), added dropwise with methanesulfonyl chloride (3.48 ml, WAKO) under ice cooling, and stirred for 30 minutes. The reaction mixture was added with water (50 ml), and extracted with diethyl ether (80 ml x 2).

The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure. A solution obtained beforehand by adding 60% sodium hydride (1.15 g, KANTO) to a solution of Intermediate 1 (4.50 g) in N, N-dimethylformamide (abbreviated as"DMF"hereinafter, 35 ml) under ice cooling and stirring the solution for 15 minutes was added with a solution of the aforementioned residue in DMF (10 ml) under ice cooling. The reaction mixture was stirred for 15 minutes, then warmed to room temperature, stirred for 45 minutes, and further stirred at 60°C for 15 hours. The reaction mixture was added with water (100 ml) and diethyl ether (200 ml) for extraction. The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by flash column chromatography (hexane : isopropyl ether = 9: 1) to obtain the title compound (Intermediate 2,5. 58 g).

Synthesis of methyl 3- (3-bromo-4-cyclopentylmethyloxyphenyl) propionate (Compound No. A-1) A solution of Intermediate 2 (1.31 g) in acetonitrile (50 ml) was added with N-bromosuccinimide (hereinafter abbreviated as"NBS", 979 mg, KANTO), stirred at room temperature for 2 hours, then warmed to 40°C, and stirred for 3 hours.

The reaction mixture was concentrated under reduced pressure, then added with ethyl acetate (200 ml) and washed successively with saturated aqueous ammonium chloride, 5% aqueous sodium sulfite, saturated aqueous sodium hydrogencarbonate and saturated brine. The organic layer was dried, and then the solvent was evaporated under reduced pressure to obtain the title compound (Compound No. A- 1,1. 69 g).

[Example A-2] Synthesis of 3- (3-bromo-4-methoxyphenyl) propionic acid (Intermediate 3) According to the procedure described in the synthesis method of Compound No. A-1 provided that the reaction was carried out under ice cooling for 30 minutes and at room temperature for 3 hours, 3- (4-methoxyphenyl) propionic acid (27.0 g, TCI) and NBS (29.4 g) were reacted and treated to obtain the title compound (Intermediate 3,38. 1 g).

Synthesis of 3- (3-bromo-4-hydroxyphenyl) propionic acid (Intermediate 4) According to a procedure described in a literature (Carreno, M. C. , J. Org.

Chem. , 1995, vol. 60, p. 5328), a 1 M solution of boron tribromide in methylene chloride (200 ml, Fluka) was added dropwise with a solution of Intermediate 4 (23.5 g) in methylene chloride (200 ml) at-78°C, warmed to room temperature after 30 minutes, and further stirred for 1.5 hours. The reaction mixture was poured into ice water (750 ml), and stirred at room temperature for 1 hour. The reaction mixture was added with diethyl ether (750 ml) ) for extraction. The organic layer was added with 2 N aqueous sodium hydroxide (250ml x 2) for extraction, and then the aqueous layer was made acidic with 5 N aqueous hydrochloric acid under ice cooling, and extracted with diethyl ether (375 ml x 2) again. The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure. The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure to obtain the title compound (Intermediate 4,23. 5 g).

Synthesis of methyl 3- (3-bromo-4-hydroxyphenyl) propionate (Intermediate 5) According to the procedure described in the synthesis method of Intermediate 1 provided that the purification was performed by flash column chromatography (hexane : ethyl acetate = 4: 1), Intermediate 4 (21.15 g) and thionyl chloride (15.0 ml) were reacted and treated in methanol to obtain the title compound (Intermediate 5,20. 36 g).

Synthesis of methyl (3-bromo-4-cyclohexylmethyloxyphenyl) propionate (Compound No. A-2) A solution of Intermediate 5 (1.29 g) in DMF (25 ml) was added with potassium carbonate (0. 86 g) and bromomethylcyclohexane (1.05 ml, TCI), stirred under argon atmosphere at room temperature for 2 hours, then warmed to 60°C, and stirred for 17 hours. The reaction mixture was poured into ice water, and extracted with isopropyl ether (200 ml). The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by flash column chromatography (hexane : isopropyl ether = 9: 1) to obtain the title compound (Compound No. A-2,1. 45 g).

[Example A-5] Synthesis of methyl 3- (3-bromo-4-cyclopentyloxyphenyl) propionate (Compound No.

A-5) A solution of Intermediate 5 (4.50 g) in DMF (20 ml) was added with 60% sodium hydride (440 mg, KANTO) under ice cooling. The reaction mixture was stirred for 10 minutes, then added with bromocyclopentane (1.61 ml, TCI), warmed to room temperature, stirred for 1.5 hours, then warmed to 60°C, and further stirred for 16 hours. The reaction mixture was added with water (50 ml) and isopropyl ether (300 ml) ) for extraction. The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by flash column chromatography (hexane: isopropyl ether = 7: 1) to obtain the title compound (Compound No. A-5,2. 50 g).

[Example A-6] Synthesis of methyl 3- (3-bromo-4-cyclohexyloxyphenyl) propionate (Compound No.

A-6) A solution of Intermediate 5 (2.06 g), triphenylphosphine (hereinafter abbreviated as"PhsP", 6. 28 g, WAKO) and cyclohexanol (2.53 ml, WAKO) in anhydrous THF (60 ml) was added dropwise with a 40% solution of diisopropylazodicarboxylic acid ester in toluene (hereinafter abbreviated as"40% DIAD", 11.35 ml, WAKO) under ice cooling over 10 minutes. The reaction mixture was stirred for 10 minutes, then warmed to room temperature, and stirred for 18.5 hours. The reaction mixture was added with water (50 ml) and ethyl acetate (200 ml) ) for extraction. The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: isopropyl ether = 8: 1) to obtain the title compound (Compound No. A-6,2. 35 g).

[Example A-20] Synthesis of methyl 3- (3-bromo-5-chloro-4-hydroxyphenyl) propionate (Intermediate 6) A solution of Intermediate 5 (516mg) in chloroform (5 ml) was added with sulfuryl chloride (177 u 1), and stirred at room temperature for 21 hours. The reaction mixture was poured into aqueous saturated sodium hydrogencarbonate (20 ml), and extracted with ethyl acetate. The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 10 : 1) to obtain the title compound (Intermediate 6,290mg).

Synthesis of methyl 3- (3-bromo-5-chloro-4-cyclopentylmethyloxyphenyl) propionate (Compound No. A-20) According to the procedure described in the synthesis method of Compound No. A-6 provided that the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 30: 1), Intermediate 6 (278 mg), PhsP (747 mg), cyclopentane methanol (308 A 1), and 40% DIAD (1.34 ml) were reacted and treated to obtain the title compound (Compound No. A-20,337mg).

[Example A-21] Synthesis of ethyl 3- (3-fluoro-4-methyloxyphenyl) acrylate (Intermediate 7) A solution of 3-fluoro-4-methoxybenzaldehyde (2.20 g, Ald) in 1,2- diethoxyethane (5 ml) was added with ethyl diethylphosphonoacetate (3.12 ml, TCI) and added with 60% sodium hydride (624mg) under ice cooling. After being stirred for 10 minutes, the reaction mixture was warmed to room temperature, and stirred for 5 hours. The reaction mixture was added with ethyl acetate (90 ml), and washed successively with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride and saturated brine. The organic layer was dried, and then the solvent was evaporated under reduced pressure. The residue was purified by flash column chromatography (Quad, hexane : ethyl acetate = 10: 1) to obtain the title compound (Intermediate 7,3. 16 g).

Synthesis of ethyl 3- (3-fluoro-4-methoxyphenyl) propionate (Intermediate 8) A solution of Intermediate 7 (3.01 g) in ethyl acetate (50 ml) and methanol (25 ml) was added with 10% palladium/carbon (300 mg, Merck), and stirred at room temperature for 2 hours under hydrogen atmosphere. The reaction mixture was filtered, and the solvent of the filtrate was evaporated under reduced pressure to obtain the title compound (Intermediate 8,3. 02 g).

Synthesis of 3- (3-fluoro-4-methoxyphenyl) propionic acid (Intermediate 9) A solution of Intermediate 8 (2. 97 g) in methanol (40.0 ml) was added with 2 N aqueous sodium hydroxide (15.0 ml) and stirred at 60°C for 16 hours. The reaction mixture was concentrated under reduced pressure, then made acidic with aqueous 5% hydrochloric acid under ice cooling, and extracted with ethyl acetate (200 ml). The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure to obtain the title compound (Intermediate 9,2. 40 g).

Synthesis of 3- (3-fluoro-4-hydroxyphenyl) propionic acid (Intermediate 10) A pyridine/hydrochloric acid complex prepared by mixing pyridine (30 ml) and concentrated hydrochloric acid (30 ml) and heating the mixture at 190°C for 1 hour was added with Intermediate 9 (2.40 g) and stirred at 190°C for 1.5 hours.

The reaction mixture was poured into 1 N hydrochloric acid (100 ml) cooled with ice, and extracted with. ethyl acetate (200 ml). The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure to obtain the title compound (Intermediate 10,1. 98 g).

Synthesis of methyl 3- (3-fluoro-4-hydroxyphenyl) propionate (Intermediate 11) According to the procedure described in the synthesis method of Intermediate 1, Intermediate 10 (1.77 g) and thionyl chloride (1.65 ml) were reacted and treated in methanol to obtain the title compound (Intermediate 11,1. 85 g).

Synthesis of methyl 3- (3-bromo-5-fluoro-4-hydroxyphenyl) propionate (Intermediate 12) According to the procedure described in the synthesis method of Compound No. A-1 with the modifications that the reaction was carried out for 2 hours under ice cooling, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 10: 1), Intermediate 11 (1.84 g) and NBS (1.74 g) were reacted and treated to obtain the title compound (Intermediate 12,1. 74 g).

Synthesis of methyl 3- (3-bromo-4-cyclopentylmethyloxy-5-fluorophenyl) propionate (Compound No. A-21) According to the procedure described in the synthesis method of Compound No. A-6 with the modifications that the reaction was carried out for 22 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 50: 1), Intermediate 11 (310 mg), tributylphosphine (hereinafter abbreviated as"nBusP", 405 u 1, WAKO) instead of Ph3P, cyclopentane methanol (176, u 1), and N, N, N', N'-tetramethylazodicarboxamide (hereinafter abbreviated as "TMAD", 279 mg, TCI) instead of 40% DIAD were reacted and treated to obtain the title compound (Compound No. A-21, 386 mg).

[Example A-24] Synthesis of 4-cyclopentyloxy-3-methylbenzaldehyde (Intermediate 13) According to the procedure described in the synthesis method of Compound No. A-2 with the modifications that the reaction was carried out for 16 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 9 : 1), 4-hydroxy-3-methylbenzaldehyde (283 mg, TCI), potassium carbonate (578 mg) and bromocyclopentane (430, u 1) were reacted and treated to obtain the title compound (Intermediate 13,350 mg).

Synthesis of ethyl 3- (4-cyclopentyl-3-methylphenyl) acrylate (Intermediate 14) According to the procedure described in the synthesis method of Intermediate 7 with the modifications that the reaction was carried out for 2 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 9 : 1), Intermediate 13 (342 mg), ethyl diethylphosphonoacetate (408 u 1) and 60% sodium hydride (82 mg) were reacted and treated to obtain the title compound (Intermediate 14,450 mg).

Synthesis of ethyl 3- (4-cyclopentyl-3-methylphenyl) propionate (Intermediate 15) According to the procedure described in the synthesis method of Intermediate 8, Intermediate 14 (446 mg) and 10% palladium/carbon (20 mg) were reacted and treated under hydrogen gas atmosphere to obtain the title compound (Intermediate 15, 439 mg).

Synthesis of ethyl 3- (3-bromo-4-cyclopentyl-5-methylphenyl) propionate (Compound No. A-24) According to the procedure described in the synthesis method of Compound No. A-l, Intermediate 15 (437 mg) and NBS (320 mg) were reacted and treated to obtain the title compound (Compound No. A-24, 545 mg).

[Example A-25] Synthesis of 3-bromo-4- (t-butyldimethylsilyloxy)-5-methoxybenzaldehyde (Intermediate 16) A solution of 3-bromovanillin (1.16 g, TCI) in anhydrous DMF (20 ml) was added with imidazole (408 mg, TCI), added dropwise with a solution of 4-(N, N- dimethylamino) pyridine (25 mg) and t-butyldimethylsilyl chloride (904 mg, TCI) in DMF (15 ml) under ice cooling, stirred 30 minutes, then warmed to room temperature, and further stirred 3 hours. The reaction mixture was added with water (100 ml), and extracted with ethyl acetate (100 ml). The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by flash column chromatography (hexane : ethyl acetate = 9 : 1) to obtain the title compound (Intermediate 16,1. 75 g).

Synthesis of ethyl 3- [3-bromo-4- (t-butyldimethylsilyloxy)-5-methoxyphenyl] acrylate (Intermediate 17) According to the procedure described in the synthesis method of Intermediate 7 with the modifications that the reaction was carried out for 1.5 hours, and the purification was performed by flash column chromatography (hexane : ethyl acetate = 9 : 1), Intermediate 16 (910 mg), ethyl diethylphosphonoacetate (530 u 1) and 60% sodium hydride (120 mg) were reacted and treated to obtain the title compound (Intermediate 17,937 mg).

Synthesis of ethyl 3- [3-bromo-4- (t-butyldimethylsilyloxy)-5- methoxyphenyl] propionate (Intermediate 18) According to the procedure described in the synthesis method of Intermediate 8, Intermediate 17 (945 mg) and 10% palladium/carbon (95 mg) were reacted and treated under hydrogen gas atmosphere to obtain the title compound (Intermediate 18,760 mg).

Synthesis of ethyl 3- (3-bromo-4-hydroxy-5-methoxyphenyl) propionate (Intermediate 19) A solution of Intermediate 18 (750 mg) in THF (50 ml) was added with a 1 M solution of tetrabutylammonium fluoride in THF (5 ml, TCI), and stirred for 1.5 hours. The reaction mixture was added with saturated aqueous sodium hydrogencarbonate (30 ml), and extracted with ethyl acetate (50 ml). The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by flash column chromatography (hexane : ethyl acetate = 4: 1) to obtain the title compound (Intermediate 19,542 mg).

Synthesis of ethyl 3- (3-bromo-4-cyclopentyloxy-5-methoxyphenyl) propionate (Compound No. A-25) According to the procedure described in the synthesis method of Compound No. A-6 with the modifications that the reaction was carried out for 16 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 7: 1), Intermediate 19 (400 mg), Ph3P (1.31 g), cyclopentanol (450, u 1), and TMAD (860 mg) were reacted and treated to obtain the title compound (Compound No. A-25,376 mg).

[Example A-26] Synthesis of methyl 3- (3-bromo-4-cyclopentylmethyloxy-5-nitrophenyl) propionate (Compound No. A-26) A solution obtained beforehand by adding 70% nitric acid (3.9 ml) to acetic anhydride (30 ml) under ice cooling and stirring the mixture for 10 minutes was added with a solution of Compound No. A-1 (5.12 g) in acetonitrile (25 ml) at-15°C over 15 minutes, and stirred further for 15 minutes. The reaction mixture was poured into 1 N aqueous sodium hydroxide (500 ml) containing ice, and extracted with diethyl ether (300 ml x 2). The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 10: 1) to obtain the title compound (Compound No. A-26,3. 68 g).

[Example A-31] Synthesis of methyl 3- (3-bromo-4-phenoxyphenyl) propionate (Compound No. A-31) A solution of Intermediate 5 (3.08 g) in anhydrous N-methylpyrrolidone (9.5 ml, WAKO) was successively added with cesium carbonate (3.58 g, WAKO), iodobenzene (1.4 ml, TCI), dipivaloylmethane (0.12 ml, TCI) and copper (I) chloride (275 mg, WAKO), and stirred 120°C for 16 hours under argon gas atmosphere. The reaction mixture was added with t-butyl methyl ether (25 ml), and insoluble solids were removed by filtration. The filtrate was washed successively with 2 N aqueous hydrochloric acid and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by flash column chromatography (hexane: ethyl acetate = 1: 10) to obtain the title compound (Compound No. A-31, 1.00 g).

[Example B-96] Synthesis of methyl 3- (3-bromo-4-methoxyphenyl) propionate (Intermediate 20) According to the procedure described in the synthesis method of Intermediate 1 provided that the purification was performed by flash column chromatography (hexane: ethyl acetate = 6: 1), Intermediate 3 (1.60 g) and thionyl chloride (1.44 ml) were reacted and treated in methanol to obtain the title compound (Intermediate 20,1. 63 g).

Synthesis of methyl 3- (3-bromo-4-methoxy-5-nitrophenyl) propionate (Intermediate 21) A solution of Intermediate 20 (3.20 g) in acetic anhydride (25 ml) was added with potassium nitrate (1.30 g) under ice cooling and stirred for 10 minutes, and the solution was added dropwise with concentrated sulfuric acid (730, u 1) over 10 minutes. The reaction mixture was stirred for 10 minutes for 10 minutes at the same temperature, then warmed to room temperature, and further stirred for 30 minutes. The reaction mixture was poured into 1 N aqueous sodium hydroxide (250 ml) containing ice, and extracted with isopropyl ether (200 ml x 2). The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane : ethyl acetate = 10: 1) to obtain the title compound (Intermediate 21,2. 73 g).

Synthesis of 3- (3-bromo-4-methoxy-5-nitrophenyl) propionic acid (Intermediate 22) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 1 hour, Intermediate 21 (12.73 g) and 2 N aqueous sodium hydroxide (40 ml) were reacted and treated to obtain the title compound (Intermediate 22,11. 53 g).

Synthesis of 3- (3-bromo-4-hydroxy-5-nitrophenyl) propionic acid (Intermediate 23) According to the procedure described in the synthesis method of Intermediate 4 provided that the reaction was carried out for 2 hours, Intermediate 22 (11.53 g) and a 1 M solution of boron tribromide in methylene chloride (100 ml) were reacted and treated to obtain the title compound (Intermediate 23,10. 68 g).

Synthesis of methyl 3- (3-bromo-4-hydroxy-5-nitrophenyl) propionate (Intermediate 24) According to the procedure described in the synthesis method of Intermediate 1 provided that the reaction was carried out for 17.5 hours, Intermediate 23 (10. 68 g) and thionyl chloride (8.06 ml) were reacted and treated to obtain the title compound (Intermediate 24,8. 27 g).

Synthesis of methyl 3- [3-bromo-4- (indan-2-yloxy)-5-nitrophenyl] propionate (Compound No. B-96) According to the procedure described in the synthesis method of Compound No. A-6 with the modifications that the reaction was carried out for 15 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 19 : 1), Intermediate 24 (151 mg), Ph3P (260 mg), 2-hydroxyindane (133 mg, TCI) and 40% DIAD (470, u 1) were reacted and treated to obtain the title compound (Compound No. B-96, 192 mg).

Example B-99] Synthesis of methyl 3- (3-amino-5-bromo-4-cyclopentyloxyphenyl) propionate (Compound No. B-99) A solution of Compound No. A-28 (416 mg) in a mixture of THF (5 ml) and methanol (5 ml) was added with Raney 2800 nickel (230 mg, Ald) and stirred at room temperature for 6 hours under hydrogen atmosphere. The reaction mixture was filtered, and the solvent of the filtrate was evaporated under reduced pressure.

The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 5 : 2) to obtain the title compound (Compound No. B-99, 143 mg).

[Example B-103] Synthesis of methyl 3- [4-benzyloxy-5-bromo-3- (2, 2,2- trifluoroacetylamino) phenyl] propionate (Compound No. B-103) A solution of Compound No. B-100 (58.7 mg) in methylene chloride (2 ml) was added with triethylamine (76 u 1), added dropwise trifluoroacetic anhydride (91 u 1, TCI) under ice cooling, stirred for 30 minutes, then warmed to room temperature, and further stirred for 2 hours. The reaction mixture was added with water (5 ml), and extracted with methylene chloride (20 ml). The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 3: 1) to obtain the title compound (Compound No. B-103,59. 1 mg).

[Example B-105] Synthesis of methyl 3- [4-benzyloxy-5-bromo-3- (N-methylamino) phenyl] propionate (Compound No. B-105) A solution of Compound No. B-100 (105 mg) in DMF (3 ml) was added with 60% sodium hydride (20 mg) under ice cooling, and stirred for 10 minutes. This reaction mixture was added dropwise with methyl iodide (32 It 1), stirred for 10 minutes, then warmed to room temperature, and further stirred for 2 hours. The reaction mixture was poured into water, and added with ethyl acetate (30 ml) for extraction. The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure.

The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 6: 1) to obtain the title compound (Compound No. B-105, 17 mg).

[Example B-109] Synthesis of 3- [4-benzyloxy-5-bromo-3- (N, N-dimethylamino) phenyl] propionic acid (Compound No. B-109) A solution of Compound No. B-100 (105 mg) in DMF (3 ml) was added with 60% sodium hydride (40 mg) under ice cooling, and stirred for 10 minutes. This reaction mixture was added dropwise with methyl iodide (300/ l), stirred for 10 minutes, then warmed to room temperature, and further stirred for 16 hours. The reaction mixture was poured into water, and added with ethyl acetate (30 ml) for extraction. The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure.

The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 6: 1) to obtain the title compound (Compound No. B-109,88 mg).

[Examples B-113 and B-114] Syntheses of 3- (3-bromo-4-cyclopentyloxy-5-hydroxyphenyl) propionic acid (Compound No. B-113) and 3- (5-acetoxy-3-bromo-4-cyclopentyloxyphenyl) propionic acid (Compound No. B-114) A solution of Compound No. B-99 (415 mg) in acetic acid (1.5 ml) was added with 20% sulfuric acid (1.0 ml). This reaction mixture was added dropwise with an aqueous solution (0.5 ml) of sodium nitrite (78 mg) over 10 minutes, while the temperature of the reaction mixture was maintained below 10°C, and further stirred for 5 minutes. This reaction mixture was added dropwise to a solution of sodium acetate (348 mg) in acetic acid (3.5 ml) heated and stirred at 100°C beforehand over 5 minutes, and further stirred for 10 minutes with heating. The reaction solution was poured into ice water (50 ml), and extracted with isopropyl ether (100 ml x 2). The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 10: 1) to obtain the title compounds (Compound No. B-113, 47mg and Compound No. B-114,105 mg).

[Example B-117] Synthesis of methyl 3- (3, 5-dibromo-4-cyclopentylmethyloxyphenyl) propionate (Compound No. B-117) A solution of Intermediate 1 (670 mg) in acetonitrile (30 ml) was added with NBS (990 mg), stirred at room temperature for 2 hours, then warmed to 40°C, and stirred for 18 hours. The reaction mixture was concentrated under reduced pressure, then added with ethyl acetate (100 ml), and washed successively with saturated aqueous ammonium chloride, 5% aqueous sodium sulfite, saturated aqueous sodium hydrogencarbonate and saturated brine. The organic layer was dried, and then the solvent was evaporated under reduced pressure. According to the procedure described in the synthesis method of Compound No. A-6 with the modifications that the reaction was carried out for 18 hours under ice cooling, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 10: 1), the residue was reacted with Ph3P (1460 mg), cyclopentane methanol (560 mg) and 40% DIAD (2.6 ml) and treated to obtain the title compound (Compound No. B-117,710 mg).

Examples A-1 to A-33] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-A-1. The compounds were prepared according to the preparation methods of the compound numbers (e. g.,"A-1") or the intermediate numbers (e. g. ,"Int 2") shown in the columns of"Syn"in the tables. "Int"means an intermediate compound number. When the preparation required a plurality of steps, a plurality of compound numbers or intermediate compound numbers are mentioned in the columns of"Syn". For example, an indication of"Int 2, A-1"in a column of"Syn"means that"the compound is prepared from a compound prepared according to the procedure described in the synthesis method of Intermediate 2 according to the procedure described in the synthesis method of Compound No. A- 1."When the compounds were synthesized according to the procedure described in the synthesis method of Compound No. A-6, TMAD or di-t-butyl azodicarboxylate (hereinafter abbreviated as"DBAB") was sometimes used instead of 40% DIAD. Ex' RX G O Table-A-1 Exp. Rx'O Y, method RTime Mass A-1 cPenMeO Me H Br A-1 C A-2 cHexMeO Me H Br A-2 C A-3 iBuO Me H Br A-2 A 5. 34 N. D A-4 2EtBuO Me H Br A-2 A-5 cPenO Me H Br A-5 C A-6 cHexO Me H Br A-6 C A-7 cHepO Me H Br A-6 A-8 BnO Me H Br A-2 A-9 lPhEtO Me H Br A-2 A-10 2FBn0 Me H Br A-2 A-11 4FBnO Me H Br A-2 A-12 2CIBnO Me H Br A-13 4CIBnO H Br A-2 A 4. 85 N. D A-14 4MeBnO Me H Br A-2 A-15 Me H Br A-2 A-16 2 (4DMAPh) EtO Me H Br A-6 A-17 2 (PhO) EtO Me H Br A-6 A 5. 04 N. D A-18 1 (2FPh) EtO Me H Br A-6 A-19 Me H Br A-6 A 4. 82 N. D A-20 cPenMeO Me Cl Br A-20 A-21 cPenMeO Me F Br A-21 A-22 cPenO Me F Br A-21| C A-23 cHexO Me F Br A-21 A-24 cPenO Et Me Br A-24 A 5. 82 N. D A-25 cPenO OMe Br A-25 A-26 cPenMeO Me N02 Br A-26| C A-27 cHexMeO Me N02 Br A-26 A-28 cPenO Me N02 Br A-26 C A-29 cHexO Me N02 Br A-26 A-30 2-IndanO Me NO2 Br A-26 A 5. 03 N. D A-31 PhO Me H Br A-31 A 5. 15 D A-32 4CIPhO Me H Br A-31 A 5. 47 N. D A-33 4MeOPhO Me H Br 5. 02 N. D [Examples B-1 to B-119] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-B-1 to Table B-3. zxt , Rx- G O Table-B-1 i nn r Exp. Rx'O Y'Zx'G method Mass B-1 nPrO Me H Br B-2 Me H Br A-2 B-3 Me H Br A-6 B-4 iPenO Me H Br A-6 B-5 1, 3DMeBuO Me H Br A-6 B-6 2MeBuO Me H Br A-6 B-7 Me H Br A-6 B-8 A-6 B-9 2, 3DMeBuO Me H. Br A-6 B-10 cPenO Me H Cl A-6 C B-11 cPenO Me H Br A-6 B-12 3Me, cPenO Me H Br A-6 B-13 cHexO Me H Br A-6 B-14 cHexO Me H Br A-6 B-15 cHexO Me H Br A-6 C B-16 cHexO Me H Br A-6 B-17 2, 3DMe, cHexO Me H Br A-6 B-18 cHexO Me H Br A-6 C l B-19 3, 5DMe, cHexO Me H Br A-6 B-20 Me H Br A-6 B-21 Me H Br A-6 0 B-22 4to Me H Br A-6 H B-23 1 H Br A-6 B-24 (S) 1 Me H Br B-25 BenzhydrylO Me H Br A-6 B-26 H Br A-6 C 391 (M++1) 0 B-27 Meo _ ° Me Br A-6 F B-28 2Ph, 1 Me H Br A-6 B-29 2Ph, 2MeEtO Me H Br A-6 B-30 2 (2FPh), 1 Me H Br A-6 B-31 2 (3CF3Ph), 1 H Br B-32 3PhBuO Me H Br A-6 B-33 50Me-2-IndanO Me H Br A-6 B-34 5, Me H Br A-6 B-35 5F-2-IndaneO Me H Br A-6 B-36 1-IndaneO Me H Br A-6 B-37 mu Me H Br A-6 O Y'Table-B-2 viz B-38 j Me H Br A-6 B-39 B-39 B-40 Me H Br A-6 C B-41 3MeBnO Me H Br A-6 B-42 3, 5DMeBnO Me H Br A-6 B-43 4tBuBnO Me H Br A-6 B-44 2CF3BnO Me H Br A-6 B-45 4CF3BnO Me H Br A-6 B-46 3 (CF30) BnO Me H Br A-6 B-47 4 (CF30) BnO Me H Br A-6 B-48 4 (nBuO) Me H Br A-6 S B-49 Me 406 (M++1) B-50 Me H B-51 2, 4DFBnO Me H Br A-6 B-52 4Br, 2FBnO Me H Br A-6 B-53 2, 4DCIBnO Me H Br A-6 B-54 3, Me H Br A-6 B-55 2, Br A-6 B-56 2, 6DCIBnO Me H Br A-6 B-57 3, 5DCIBnO Me H Br A-6 B-58 2-NapMeO Me H Br A-6 C399 +1) B-59 1-NapMeO Me H Br A-6 B-60 _0 Me H Br A-6 B-61 Me H Br A-6 B-62 >° Me H Br A-6 C 339 (M++1) oll B-63 2PhBnO Me H Br A-6 B-64 4PhBnO Me H Br A-6 B-65 2PhEtO Me H Br A-6 B-66 2 (2MePh) EtO Me H Br A-6 B-67 2 (3MePh) EtO Me H Br A-6 B-68 2 (4MePh) EtO Me H Br A-6 B-69 2 (3FPh) EtO Me H Br A-6 B-70 2 Me H Br A-6 B-71 2 (2CF3Ph) EtO Me H Br A-6 B-72 2 (4CF3Ph) EtO Me H Br A-6 B-73 2 (20MePh) EtO Me H Br A-6 B-74 2 (2-Nap) EtO Me H Br A-6 C B-75 2 (3-Ind) EtO Me H Br A-6 s 0 B-76 Me H Br A-6 N B-77 B-78 2 (2CIPhO) Me H Br A-6 B-79 2 (4CIPhO) Me H Br jTable-B-3 0 B-80 "° Br A-6 C 407 (M++1) B-81 Me H Br A-6 B-82 Me H Br A-6 r B-83 r"""° Me H Br A-6 B-84 2 (PhS) EtO Me H 379 (M++1) B-85 2-BztO Me H Br A-6 B-86 (60Me-2-Bzt) O Me H Br A-6 B-87 cPenO Me Cl Br A-20 B-88 1 (4FPh) EtO Me CI Br B-89 1 Me F Br A-21 B-90 1 (4FPh) EtO Me F Br A-21 B-91 1 Et Me Br A-24 B-92 1 (4FPh) EtO Et Me Br A-24 B-93 1 Me OMe Br A-25 B-94 1 (4FPh) EtO Me OMe Br A-25 B-95 BnO Me N02 Br A-26 B-96 2-IndanO Me N02 Br A-26 A 4. 44 N. D B-97 50Me-2-IndanO Me N02 Br A-26 B-98 4CF3BnO Me N02 Br A-26 B-99 cPenO Me NH2 Br B-99 C B-100 BnO Me NH2 Br B-99 B-101 1 Me NH2 Br B-99 B-102 50Me-2-IndanO Me NH2 Br B-99 B-103 BnO Me NHTFA Br B-103 B-104 cPenO Me NHTFA Br B-103 C B-105 BnO Me NHMe Br B-105 B-106 cPenO Me NHMe Br B-105 C B-107 1 Me NHMe Br B-105 B-108 1 (4FPh) EtO Me NHMe Br B-105 B-109 BnO Me NMe2 Br B-109 B-110 cPenO Me NMe2 Br B-109 C B-111 1 Me NMe2 Br B-109 B-112 1 (4FPh) EtO Me NMe2 Br B-109 B-113 cPenO Me OH Br B-113 C B-114 cPenO Me COM Br B-114 B-115 1 (4FPh) EtO Me OH Br B-113 B-116 1 (4FPh) EtO Me COM Br B-114 B-117 cPenMeO Me Br. Br B-117 B-118 cPenO Me Br Br B-117 A 5. 98 N. D B-119 1 (4FPh) EtO Me Br Br B-117 [Example C-1] Synthesis of 3-bromo-4-cyclohexylmethyloxybenzaldehyde (Intermediate 25) According to the procedure described in the synthesis method of Compound No. A-2 provided that the purification was performed by flash column chromatography (hexane : isopropyl ether = 5: 1), 3-bromo-4-hydroxybenzaldehyde (17. 4 g), potassium carbonate (23.9 g) and bromomethylcyclohexane (36.2 ml) were reacted and treated to obtain the title compound (Intermediate 25,18. 7 g).

Synthesis of 4-cyclohexylmethyloxy-3- (naphthalen-2-yl) benzaldehyde (Compound No. C-1) A solution of 2-naphthaleneboronic acid (535 mg) in methanol (5.0 ml), Intermediate 25 (1.16 g), and 2 M aqueous sodium carbonate (0.9 ml) were added with toluene (10. 0 ml) and tetrakistriphenylphosphinepalladium (0) [hereinafter abbreviated as"(Ph3P) 4Pd"] (116 mg, Nakarai Tecs), and stirred at 80°C for 17 hours. The reaction mixture was added with ethyl acetate (100 ml), and washed successively with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride and saturated brine. The organic layer was dried, and then the solvent was evaporated under reduced pressure. The residue was purified by flash column chromatography (hexane : ethyl acetate = 10 : 1) to obtain the title compound (Compound No. C-1, 345 mg).

[Example D-10] Synthesis of 3-bromo-4-hydroxy-5-nitrobenzaldehyde (Intermediate 26) A solution of 3-bromo-4-hydroxybenzaldehyde (6.30 g) in acetic acid (45 ml) was added dropwise with 70% nitric acid (5.85 ml) on a water bath, then added with sodium nitrite (62 mg), and further stirred for 2 hours. The reaction mixture was poured into ice water (300 ml), and precipitates were taken by filtration, and washed with water (50ml x 3). The precipitates were dried under reduced pressure for 24 hours to obtain the title compound (Intermediate 26,5. 88 g).

Synthesis of 3-bromo-4-cyclohexylmethyloxy-5-nitrobenzaldehyde (Intermediate 27) According to the procedure described in the synthesis method of Compound No. A-2 provided that the purification was performed by flash column chromatography (hexane : ethyl acetate = 7: 1), Intermediate 26 (5.5 g), potassium carbonate (3.94 g) and bromomethylcyclohexane (3.94 ml) were reacted and treated to obtain the title compound (Intermediate 27,5. 2 g).

Synthesis of 4-cyclohexylmethyloxy-3- (naphthalen-2-yl)-5-nitrobenzaldehyde (Compound No. D-10) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 15 hours at 80°C, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 7: 1), Intermediate 27 (2.65 g), 2-naphthaleneboronic acid (3.01 g), 2 M aqueous sodium carbonate (7.5 ml) and (Ph3P) 4Pd (960 mg) were reacted and treated to obtain the title compound (Compound No. D-10, 2.96 g).

[Examples C-1 to C-8] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-C-1. zx Zx' Rx'-0 CHO AR Table-C-1 Rx'O Position RTime Mass C-1 cHexMeO 4 H-2-Nap C-2 cHexMeO 4 H-1-Nap 5 C-1 C-3 cHexMeO 4 H-20Me-6-Nap C-4 cHexMeO 4 H-5-Ind 5 C-1 C-5 cPenMeO 4 H-2-Nap C-6 cPenMeO 4 H-5-Ind 5 C-1 C-7 cPenO 5 C-1 C C-8 cPenO 4 5 C-1 C [Examples D-1 to D-29] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-D-1. zxw Rx'-0 ,-l 44 Table-D-1 2 Exp. Exp. Position PositonPosttion Postton method RTtme Mass D-1 cHexMeO 4 H-2-BT 3 C-1 D-2 cHexMeO 4 H-2-BF 3 C-1 D-3 cHexMeO 4 H-1 D-4 cHexMeO 4 H-5-1HIdz D-5 cHexMeO 4 H 3 C-1 D-6 2 (2FPh) EtO 4 H-2-Nap 3 C-1 D-7 2 (2FPh) EtO 4 H-5-Ind 3 C-1 D-8 2-IndanO 4 H-5-Ind 3 C-1 D D-9 2-IndanO 4 H-5-1HIdz 3 C-1 D-10 cPenMeO 4 N02 5 2-Nap 3 D-10 C D-11 cPenMeO 4 N02 5 5-Ind 3 D-10 D-12 cHexMeO 4 5 2-Nap 3 D-10 D-13 cHexMeO 4 N02 5 2-BF 3 D-10 D-14 cPenO 4 NO2 5 2-Nap 3 D-10 D-15 cPenO 5 5-Ind 3 D-10 C D-16 2 4 N02 5 2-Nap 3 D-10 D-17 2 (2FPh) 4 N02 5 5-Ind 3 D-10 D-18 2-IndanO 4 N02 5 5-Ind 3 D-10 D_l82_lndano D-19 2-IndanO 4 N02 5 1 3 D-10 A 3. 85 414 (M++1) D-20 cPenO 2 H-2-Nap D-21 cPenO 2 H-5-Ind 5 C-1 C D-22 cPenO 3 H-2-Nap 5 C-1 D-23 cPenO 3 H-5-Ind 5 C-1 D-24 cPenO 5 H 2 C-1 D-25 cPenO 5 H-5-Ind 2 C-1 D-26 cPenO 4 H 2 C-1. D-27 cPenO 4 H-5-Ind 2 C-1 D-28 cPenO 3 H 2 C-1 D-29 cPenO 3 H 2 C-1 [Example E-1] Synthesis of 5-bromo-2-cyclopentylmethyloxypyridine (Intermediate 28) A solution of potassium t-butoxid (550.6 mg, WAKO) in dehydrated THF (10 ml) was added with cyclopentane methanol (450 u 1), and then added with a solution of 2, 5-dibromopyridine (982.8 mg, TCI) in dehydrated THF (15 ml) under ice cooling. The reaction mixture was stirred for 30 minutes, then warmed to room temperature, and stirred for 11 hours. The reaction mixture was added with water (100 ml) and ethyl acetate (60 ml) for extraction. The organic layer was washed successively with saturated aqueous sodium hydrogencarbonate and saturated brine sequentially, and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 15: 1) to obtain the title compound (Intermediate 28, 896 mg).

Synthesis of 2-cyclopentylmethyloxypyridine-5-carbaldehyde (Intermediate 29) A solution of Intermediate 28 (895 mg) in anhydrous THF (10 ml) was added dropwise with a 1.6 M solution of n-butyllithium in hexane (2.70 ml, Ald) over 5 minutes with cooling at'78°C under argon gas atmosphere, and stirred for 20 minutes. This reaction mixture was added with dehydrated DMF (330, u 1, WAKO) over 3 minutes, stirred for 30 minutes, then warmed to room temperature, and further stirred for 1 hour. The reaction mixture was added with water (10 ml), and extracted with ethyl acetate (30ml x 3). The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 10: 1) to obtain the title compound (Intermediate 29,1. 04 g).

Synthesis of ethyl 3- (2-cyclopentylmethyloxypyridin-5-yl) acrylate (Intermediate 30) According to the procedure described in the synthesis method of Intermediate 7 with the modification that the reaction was carried out for 1 hour, Intermediate 29 (450 mg), ethyl diethylphosphonoacetate (530 u 1) and 60% sodium hydride (120 mg) were reacted and treated to obtain the title compound (Intermediate 30,394 mg).

Synthesis of ethyl 3- (2-cyclopentylmethyloxypyridine-5-yl) propionate (Intermediate 31) According to the procedure described in the synthesis method of Intermediate 8 with the modifications that the reaction was carried out for 1 hour, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 15 : 1), Intermediate 30 (392 mg) and 10% palladium/carbon (30 mg) were reacted and treated to obtain the title compound (Intermediate 31,246 mg).

Synthesis of ethyl 3- (3-bromo-2-cyclopentylmethyloxypyridin-5-yl) propionate (Compound No. E-1) A solution of Intermediate 31 (5.20 g) in acetonitrile (50 ml) was warmed to 35°C, added dropwise with bromine (1.1 ml, WAKO), then added with NBS (3.72 g), and stirred at room temperature for 2 hours. The reaction mixture was concentrated under reduced pressure, then added with ethyl acetate (200 ml), and washed successively with saturated aqueous ammonium chloride, 5% aqueous sodium sulfite, saturated aqueous sodium hydrogencarbonate and saturated brine.

The organic layer was dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane : ethyl acetate = 10 : 1) to obtain the title compound (Compound No. E-1, 6.51 g).

[Example E-7] Synthesis of 2-benzyloxy-5-bromopyridine (Intermediate 32) According to the procedure described in the synthesis method of Intermediate 28 provided that the reaction was carried out for 1 hour, potassium t- butoxide (3.13 g), benzyl alcohol (3.10 ml) and 2,5-dibromopyridine (4.79 g) were reacted and treated to obtain the title compound (Intermediate 32,5. 36 g).

Synthesis of 2-benzyloxypyridine-5-carbaldehyde (Intermediate 33) According to the procedure described in the synthesis method of Intermediate 29, Intermediate 32 (5.10 g), a 1.6M solution of n-butyllithium in hexane (15.5 ml) and dehydrated DMF (1.9 ml) were reacted and treated to obtain the title compound (Intermediate 33,2. 75 g).

Synthesis of ethyl 3- (2-benzyloxypyridin-5-yl) acrylate (Intermediate 34) According to the procedure described in the synthesis method of Intermediate 7, Intermediate 33 (2. 74 g), ethyl diethylphosphonoacetate (3.12 ml) and 60% sodium hydride (635 mg) were reacted and treated to obtain the title compound (Intermediate 34,2. 12 g).

Synthesis of ethyl 3- (2-hydroxypyridin-5-yl) propionate (Intermediate 35) According to the procedure described in the synthesis method of Intermediate 8 provided that the reaction was carried out for 2.5 hours, Intermediate 54 (2.12 g) and 10% palladium/carbon (120 mg) were reacted and treated to obtain the title compound (Intermediate 35,1. 26 g).

Synthesis of ethyl 3- (3-bromo-2-hydroxypyridin-5-yl) propionate (Intermediate 36) According to the procedure described in the synthesis method of Compound No. E-1 with the modifications that the reaction was carried out for 2.5 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 1 : 2), Intermediate 35 (1.23 g), bromine (340, u 1) and NBS (1.19 g) were reacted and treated to obtain the title compound (Compound No. 36,1. 42 g).

Synthesis of ethyl 3- [5-bromo-6- [(S)-l-phenylethyloxy] pyridin-3-yl] propionate (Compound No. E-7) According to the procedure described in the synthesis method of Compound No. A-6 with the modifications that the reaction was carried out for 11 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 4 : 1), Intermediate 36 (137 mg), PhsP (273 mg), (R)-l-phenylethanol (150 , u 1, TCI) and 40% DIAD (400 u 1) were reacted and treated to obtain the title compound (Compound No. E-7, 167 mg).

[Example E-13] Synthesis of ethyl 3- (5-bromo-6- (4-trifluoromethylbenzyloxy) pyridin-3-yl) propionate (Compound No. E-13) A solution of Intermediate 36 (71.5 mg) in chloroform (7 ml) was added with 4-trifluoromethylbenzyl bromide (109.2 mg, TCI) and silver carbonate (120 mg, WAKO), and stirred at room temperature for 11 hours under light shielding. The reaction mixture was filtered, and the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane : ethyl acetate = 6: 1) to obtain the title compound (Compound No. E-13, 114 mg).

[Example E-1 to 16] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-E-1. Rx'-O Table-E-1 Exp. Rx'O method RTime Mass E-1 cPenMeO E-2 cHexMeO Et Br E-1 E-2 E-3 Br E-1 A 5. 57 N. D E-4 2EtBuO Et Br E-1 E-5 cPenO Et Br E-1 A 5. 62 342 (M+) E-6 cHexO Et Br E-1 E-7 (R) 1 Et Br E-7 A 5. 60 N. D E-8 2 (4DMAPh) EtO Et Br E-7 E-9 2 (2FPh) EtO Et Br E-10 2 (3FPh) EtO Et Br E-7 E-11 2 (4CIPh) Et Br E-7 E-12 2 (PhO) EtO Et Br E-7 E-13 4CF3BnO Et Br E-13 A 5. 78 432 (M+) E-14 2MeBnO Et Br E-13 E-15 2CIBnO Et Br E-13 E-16 1 (4FPh) EtO Et Br E-7 G[Example F-1] Synthesis of 4- (3-bromo-4-methoxyphenyl) butyric acid (Intermediate 37) According to the procedure described in the synthesis method of Compound No. A-1 provided that the reaction was carried out under ice cooling for 30 minutes and for 20 hours at room temperature, 4- (4-methoxyphenyl) butyric acid (11.64 g, Ald) and NBS (11.21 g) were reacted and treated to obtain the title compound (Intermediate 37,16. 30 g).

Synthesis of methyl 4- (3-bromo-4-hydroxyphenyl) butyrate (Intermediate 38) According to the procedure described in the synthesis method of Intermediate 4, Intermediate 37 (12.51 g) and a 1 M solution of boron tribromide in methylene chloride (100 ml) were reacted and treated, and the obtained residue was reacted with thionyl chloride (8.4 ml) in methanol and treated according to the procedure described in the synthesis method of Intermediate 1 to obtain the title compound (Intermediate 38,10. 48 g).

Synthesis of methyl 4- (3-bromo-4-cyclopentylmethyloxyphenyl) butyrate (Compound No. F-1) According to the procedure described in the synthesis method of Compound No. A-6 provided that the purification was performed by column chromatography (Quad, hexane: isopropyl alcohol = 10 : 1), Intermediate 38 (2.72 g), PhsP (7.86 g), cyclopentane methanol (3.24 ml) and 40% DIAD (14.2 ml) were reacted and treated to obtain the title compound (Compound No. F-1, 3.33 g).

[Examples F-1 to F-4] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-F-l. zx Ru'-ou (CH2) nCOOY' Table-F-1 LCMS Exp. Rx'O Y'Zx'G n Syn I method RTime _ Mass F-1 cPenMeO Me H Br 3 F-1 F-2 cPenO Me H Br 3 F-3 cHexO Me 3 F-1 C F-4 (4FPh) EtO Me [Example G-1] Synthesis of methyl 3- [4-methoxy-3- (naphthalen-2-yl) phenyl] propionate (Intermediate 39) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 2 hours, and the purification was performed by flash column chromatography (hexane : isopropyl ether = 8 : 1), Intermediate 20 (460 mg), 2-naphthaleneboronic acid (886 mg), 2 M aqueous sodium carbonate (1.6 ml) and (Ph3P) 4Pd (298 mg) were reacted and treated to obtain the title compound (Intermediate 39,580 mg).

Synthesis of 3- [4-methoxy-3- (naphthalen-2-yl) phenyl] propionic acid (Intermediate 40) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 2 hours, Intermediate 39 (773 mg) and 2 N aqueous sodium hydroxide (2.3 ml) were reacted and treated to obtain the title compound (Intermediate 40,674 mg).

Synthesis of methyl 3- [4-hydroxy-3- (naphthalen-2-yl) phenyl] propionate (Intermediate 41) According to the procedure described in the synthesis method of Intermediate 10, pyridine (5 ml), concentrated hydrochloric acid (5 ml), and Intermediate 40 (551 mg) were reacted and treated to obtain crude powder substance. This substance was reacted with thionyl chloride (282 g 1) in methanol and treated according to the procedure described in the synthesis method of Intermediate 1 to obtain the title compound (Intermediate 41,531 mg).

Synthesis of methyl 3- [4-cyclopentyloxy-3- (naphthalen-2-yl) phenyl] propionate (Compound No. G-1) According to the procedure described in the synthesis method of Compound No. A-6 with the modifications that the reaction was carried out for 15 hours, and the purification was performed by flash column chromatography (hexane: isopropyl ether = 6: 1), Intermediate 41 (100 mg), PhsP (262 mg), cyclopentanol (91 u 1, TCI) and 40% DIAD (473 u 1) were reacted and treated to obtain the title compound (Compound No. G-1, 120 mg).

[Example G-2] Synthesis of 3- [4-cyclopentyloxy-3- (naphthalen-2-yl) phenyl] propionic acid (Compound No. G-2) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 4 hours, Compound No. G-1 (115 mg), and 2 N aqueous sodium hydroxide (0.75 ml) were reacted and treated to obtain the title compound (Compound No. G-2,108 mg).

[Example G-3] Synthesis of methyl 3- [4-cyclopentyloxy-3- (lH-indol-5-yl) phenyl] propionate (Compound No. G-3) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 3 hours, and the purification was performed by flash column chromatography (hexane: ethyl acetate = 4: 1), Compound No. A-5 (833 mg), 5-indoleboronic acid (657 mg), 2 M aqueous sodium carbonate (2.4 ml) and (PhsP) 4Pd (233 mg) were reacted and treated to obtain the title compound (Compound No. G-3, 900 mg).

[Example G-4] Synthesis of 3- [4-cyclopentyloxy-3- (lH-indole-5-yl) phenyl] propionic acid (Compound No. G-4) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 2 hours, Compound No. G-3 (144 mg) and 2 N aqueous sodium hydroxide (420 u 1) were reacted and treated to obtain the title compound (Compound No. G-4, 127 mg).

[Example G-9] Synthesis of methyl 3- [4-benzyloxy-5- (I-methyl-lH-indazol-5-yl) phenyl] propionate (Compound No. G-9) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out at 80°C for 6 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 4 : 1), Compound No. A-8 (349 mg), 1-methyl-lH-indazole-5-boronic acid (283 mg), 2 M aqueous sodium carbonate (0.9 ml) and (Ph3P) 4Pd (94.3 mg) were reacted and treated to obtain the title compound (Compound No. G-9, 370 mg).

[Example G-10] Synthesis of 3- [4-benzyloxy-5- (1-methyl-lH-indazol-5-yl) phenyl] propionic acid (Compound No. G-10) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 4 hours, Compound No. G-9 (80 mg) and 2 N aqueous sodium hydroxide (0.20 ml) were reacted and treated to obtain the title compound (Compound No. Go-10, 71 mg).

Synthesis of methyl 3- [4-hydroxy-5- (l-methyl-lH-indazol-5-yl) pheny propionate (Intermediate 42) A solution of Compound No. G-9 (314 mg) in a mixture of ethyl acetate (3 ml) and methanol (3 ml) was added with 10% palladium/carbon (12 mg), and stirred at room temperature for 16 hours under hydrogen atmosphere. The reaction mixture was filtered, and the solvent of the filtrate was evaporated under reduced pressure to obtain the title compound (Intermediate 48,288 mg).

[Example G-23] Synthesis of methyl 3- (3-bromo-4-t-butyldimethylsilyloxyphenyl) propionate (Intermediate 43) According to the procedure described in the synthesis method of Intermediate 16 provided that the reaction was carried out for 16 hours, Intermediate 5 (5.18 g), imidazole (2.04 g) and t-butyldimethylsilyl chloride (4.52 g) were reacted and treated to obtain the title compound (Intermediate 43, 8. 42 g).

Synthesis of methyl 3- [4- (t-butyldimethylsilyloxy-3- (lH-indol-5- yl) phenyl) propionate (Intermediate 44) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that reaction was performed for 12.5 hours, and the purification was performed by flash column chromatography (hexane : ethyl acetate = 9 : 1), 5-indoleboronic acid (4.83 g), Intermediate 34 (7.46 g), 2 M aqueous sodium carbonate (18 ml) and (Ph3P) 4Pd (1.62 g) were reacted and treated to obtain the title compound (Intermediate 44,5. 04 g).

Synthesis of methyl 3- [4-hydroxy-3- (lH-indol-5-yl) phenyl propionate (Intermediate 45) According to the procedure described in the synthesis method of Intermediate 19 with the modifications that the reaction was carried out for 2 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 3: 1), Intermediate 35 (5.04 g), acetic acid (2.8 ml) and a 1 M solution of tetrabutylammonium fluoride in THF (49 ml, TCI) were reacted and treated to obtain the title compound (Intermediate 45,3. 13 g).

Synthesis of methyl 3- [3- (lH-indol-5-yl)-4- (4-methylphenylmethyloxy) phenyl]- propionate (Compound No. G-23) According to the procedure described in the synthesis method of Compound No. A-2 with the modifications that the reaction was carried out for 15 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 5 : 1), Intermediate 45 (80 mg), potassium carbonate (114 mg) and 4- methylbenzyl bromide (54 u 1, TCI) were reacted and treated to obtain the title compound (Compound No. G-23,104 mg).

[Example G-24] Synthesis of 3- [3- (lH-indol-5-yl)-4- (4-methylphenylmethyloxy) phenyl] propionic acid (Compound No. G-24) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 3 hours, Compound No. G-23 (99 mg) and 2 N aqueous sodium hydroxide (500, u 1) were reacted and treated to obtain the title compound (Compound No. G-24, 84 mg).

[Example G-106] Synthesis of N- [2- (t-butyldiphenylsilyloxy) ethyl] aniline (Intermediate 46) A solution of 2-anilinoethanol (5.82 g, TCI) in anhydrous DMF (50 ml) was added with imidazole (3.23 g, TCI), added dropwise with a solution of t-butyldiphenylsilyl chloride (12.48 g, TCI) in DMF (50 ml) under ice cooling, stirred for 30 minutes, then warmed to room temperature, and further stirred for 3.5 hours. The reaction mixture was added with water (100 ml), and extracted with ethyl acetate (100 ml). The organic layer was washed successively with water and saturated brine, and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by flash column chromatography (hexane : ethyl acetate = 9: 1) to obtain the title compound (Intermediate 46,15. 61 g).

Synthesis of N-benzyl-N- [2- (t-butyldiphenylsilyloxy) ethyl] aniline (Intermediate 47) According to the procedure described in the synthesis method of Compound No. A-2 with the modifications that the reaction was carried out for 15 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 5 : 1), Intermediate 46 (15.60 g), potassium carbonate (8.91 g) and benzyl bromide (6.05 ml, TCI) were reacted and treated to obtain the title compound (Intermediate 47,19. 23 g).

Synthesis of 2- (N-benzyl-N-phenylamino) ethanol (Intermediate 48) According to the procedure described in the synthesis method of Intermediate 9 with the modifications that the reaction was carried out for 1 hour, and the purification was performed by flash column chromatography (hexane: ethyl acetate = 5: 1), Intermediate 47 (19.22 g) and a 1 M solution of tetrabutylammonium fluoride in THF (86 ml) were reacted and treated to obtain the title compound (Intermediate 48,9. 06 g).

Synthesis of methyl 3- {4- [2- (N-benzyl-N-phenylamino) ethyloxy]-3- (naphthalen-2- yl) phenyl} propionate (Compound No. G-106) According to the procedure described in the synthesis method of Compound No. A-6 with the modifications that the reaction was carried out for 15 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 7: 1), Intermediate 41 (1.26 g), PhsP (1.34 g), Intermediate 48 (1.01 g) and DBAB (1. 18 g) instead of 40% DIAD were reacted and treated to obtain the title compound (Compound No. G-106,1. 39 g).

[Example G-107] Synthesis of methyl 3-{3-(naphthalen-2-yl)-4-[2-(N- phenylamino) ethyloxylphenyllpropionate (Compound No. G-107) A solution of Compound No. G-106 (1.39 g) in a mixture of THF (10 ml) and methanol (20 ml) was added with concentrated hydrochloric acid (75 u 1, WAKO) and 10% palladium/carbon (142 mg), and stirred at room temperature for 3 hours under hydrogen gas atmosphere. The reaction mixture was filtered, and the solvent of the filtrate was evaporated under reduced pressure to obtain the title compound (Compound No. G-107, 842 mg).

[Example G-108] Synthesis of 3-{3- (naphthalen-2-yl)-4- [2- (phenylamino) ethyloxy] phenyl} propionic acid (Compound No. G-108) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 2 hours, Compound No. G-107 (46 mg) and 2 N aqueous sodium hydroxide (0.25 ml) were reacted and treated to obtain the title compound (Compound No. Go-108, 41 mg).

[Examples G-1 to G-121] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-G-1 to Table-G-4. Zx Rx-O AR Table-G-1 Exp. RxO Y Zx AR Syn LCMS method Mass G-1 cPenMeO Me H 2-Nap G-1 C 388 (M+) G-2 cPenMeO H H 2-Nap G-2 C G-3 cPenMeO Me H 5-Ind G-3 G-4 cPenMeO H H 5-Ind G-4 C 363 (M+) G-5 cPenMeO Me H 1 Me-5-Ind G-6 cPenMeO H H lMe-5-lnd G-7 cPenMeO Me H 5-1 Hldz G-3 G-8 cPenMeO H H 5-1 HIdz G-4 G-9 BnO Me H G-10 BnO H H 1 G-11 cPenMeO Me H 1 G-3 G-12 cPenMeO H H 1 G-4 G-13 H H 2-Nap G-1, G-2 A G-14 2EtBuO H H 5-Ind G-4 G-15 4Me, cHexO H 2-Nap G-1. G-2 G-16 4Me, cHexO H H 5-Ind G-3. G-4 D 5. 46 378 (M++1) G-17 H H 2-Nap G-1, G-2 qp"o G-13 H H 5-Ind G-4 G-19 cHepO G-4 G-20 3PhPrO H H 2-Nap G-1, G-2 G-21 4PhBuO H H 5-Ind G-3, G-4 G-22 t< H 2-Nap G-1, G-2 D 5. 414 (M++1) 6 G-23 4MeBnO Me H 5-Ind G-23 G-24 4MeBnO H H 5-Ind G-25 2 (4MePh) EtO H H 2-Nap G-1, G-2 G-26 2 (4MePh) EtO H H 5-Ind G-1. G-2 G-27 4CIBnO H H 2-Nap G-23, G-24 G-28 4CF3BnO H H 5-Ind G-23, G-24 G-29 3F, 4 (OMe) BnO H H 2-Nap G-1. G-2 G-30 3F, 4 (OMe) BnO H H 5-Ind G-1, G-2 G-31 H H 2-Nap G-1, G-2 G-32 H H 5-Ind G-1, G-2 0 G-33 CFy H H 2-Nap G-1, G-2 G-34 H 5-Ind G-1, G-2 CF3 G-35 H H 2-Nap G-1, G-2 H H 5-Ind G-1, G-2 O YTable-G-2 G-37 11ndanO H H G-2 D G-38 2IndanO 2-Nap G-1, G-2 G-39 21ndanO H H 5-lnd G-40 H H 2-Nap G-1, G-2 G G-41 5, 6D (OMe)-2-IndanO H H 5-Ind G-1, G-2 C G-42 5F-2-IndanO 2-Nap G-l, G-2 G-43 5F-2-IndanO H H 5-Ind G-2 C G-44 WO G-1, G-2 G-45 cao H H 5-Ind G-2 A 5. 46 412 (M"+1) o G-46 H H 2-Nap G-1, G-2 o G-47 H H 5-1 HInd G-48 G-2 G-49 2 (2MePh) EtO H H 5-Ind G-1, G-2 G-50 2 (3FPh) EtO H H 2-Nap G-1, G-2 G-51 2 (2CIPh) H H 2-Nap G-1, G-2 G-52 2 (3CIPh) H H 5-Ind G-1, G-2 G-53 2 (2CF3Ph) EtO H H 5-Ind G-1. G-2 G-54 4 (CF3Ph) EtO H H 2-Nap G-1, G-2 G-55 2 (20MePh) EtO H H 2-Nap G-1, G-2 C G-56 2 (40MePh) EtO H H 5-Ind G-1, G-2 G-57 2 (1-NapEt) O H H 2-Nap G-1. G-2 G-58 2 (2-Nap) EtO H H 2-Nap G-1, G-2 G-59 2 (2-Nap) EtO H H 5-Ind G-1, G-2 C G-60 2 (4CIPh) H H 2-Nap G-1, G-2 G-61 Con H H 5-Ind G-1, G-2 D 5. 11 430 (M++1) G-62 Ct>) G-2 G-63 2 (PhS) EtO H H 2-Nap G-2 A G-64 2 (PhS) EtO H H 5-Ind G-1, G-2 G-65 3PhPrO H H 5-Ind G-1, G-2 G-66 2CIBnO H H 2-Nap G-1. G-2 G-67 2BrBnO H H 5-Ind G-1, G-2 C G-68 3, 5DMeBnO H H 5-Ind G-1, G-2 G-69 4tBuBnO H H 2-Nap G-1, G-2 G-70 2CF3BnO H H 2-Nap G-1, G-2 G-71 4CF3BnO H H 5-Ind G-1, G-2 G-72 4nBuBnO H H 5-Ind G-73 3, 5DCIBnO H H 2-Nap G-1, G-2 G-74 2, H H 5-Ind G-1, G-2 G-75 2PhBnO H H 2-Nap G-1, G-2 G-76 4PhBnO H H 5-Ind G-1, G-2 A 5-Ind G-1,Table-G-3 i G-77 p'NN 2-Nap G-1. G-2 m G-78 fL<N H H 5-Ind G-2 0 1 G-79 H H 2-Nap G-1, G-2 IN' G-80 H H 5-Ind G-1, G-2 nul' G-81 t H H 2-Nap G-1, G-2 C 386 (M++1) G-82 '\o H H 5-Ind G-1, G-2 _o G-83 o H H 2-Nap G-1, G-2 tJO G-84 at G-2 o. G-B6 H H 2-Nap G-1, G-2 G-86 G-2 0 G-67 H H 2-Nap G-1, G-2 0 G-88 9 H 5-Ind G-1, G-2 0 G-89 Q G-90 9 H H 5-Ind G-1, G-2 G-91 H 2-Nap G-1, G-2 G-91 I'O H G-92 G-2 G-93 F3 H H 2-Nap G-1, G-2 C, 10, ll'0 G-94 . H H 2-Nap G-1, G-2 C 384 (M++1) Lo G-95 H H 5-Ind G-1, G-2 G-96 H H 2-Nap G-1, G-2 G-97 H H 5-Ind G-1, G-2 N H NTable-G-4 G-96 H 2-Nap G-1, G-2 0 H G-2 G-100 H H 2-Nap G-1, G-2 <- G-101 C H H 5-Ind G-1, G-2 C 423 (M++1) G-1, G-2 G-102 rio H H 2-Nap G-103 4 H H 5-Ind G-1, G-2 G-104 ° G-105 ° H H 5-Ind G-1, G-2 G-106 2 (Ph, BnN) EtO Me G-107 2 (PhNH) EtO Me G-107 G-108 2 (PhNH) EtO H H 2-Nap G-108 C G-109 2 (PhNH) EtO Me H 5-Ind G-107 G-110 2 (PhNH) EtO H H 5-Ind G-108 G-111 2 (PhNH) EtO Me H 1Me-5-Ind G-112 2 (PhNH) EtO H H 1 Me-5-Ind G-108 C G-113 Me H 5-1 G-114 2 (PhNH) EtO H H 5-1 Hldz G-108 G-115 2 (PhNH) EtO Me H 1Me-5-lHIdz A 4. 76 430 (M++1) G-116 2 (PhNH) EtO H H 1 G-117 H H 1 G-2 C G-118 H H G-2 C G-119 H H G-4 A 4. 10 373 (M++1) G-120 H H 1 G-4 A 4. 46 G-121 H H 1 G-4 A 4. 12 403 (M++l) t H [Examples H-1 to H-32] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification are shown in Table-H-1 and Table-H-2. Zx Rx-O AR Table-H-1 Exp. RxO Y Zx AR Syn method RTime Mass N--N H-1 Me H 2-Nap G-1 0 r4=N H-2 H 2-Nap G-2 N=N N=N H-3 N Me H 5-Ind G-1 C 375 (M \ H-4 cr H H 5-Ind G-2 NZN H-5 Cr, Me H G-1 0 N=N H-6 H NON H-7 Me H 5-1 G-1 0 H-8 ' H H 5-1 Hldz G-2 0 N=N H-9 Me H 1 G-1 N= H-10 G-2 C 454 (M++1) H-11 H 2-Nap G-1, G-2 H-12 H 1 Me-5-Ind G-1 G-2 G 452 (M++1) rop H-13 N H H 2-Nap G-1, G-2 0 H-14 » H 1 Me-5-Ind G-1, G-2 _ H-15 N. -b H H 2-Nap G-1, G-2 464 (M++1) H-16 O$b H 1 Me-5-Ind G-1, G-2 H-17 H H 2-Nap G-1, G-2 C 450 (M++1) H-1 8 H 1 Me-5-Ind G-1, G-2 LCMSTable-H-2 H-19 A H 2-Nap G-1, G-2 H-20 ° o H-21 H 2-Nap G-1, G-2 0 H-22 r-N H 1 G-2 C 471 (M++1) 0--Y H-23 0-mi H H 2-Nap G-1, G-2 H-24 H H 1 G-2 H-25 H H 2-Nap G-1, G-2 H-26 0 H H 1Me-5-Ind G-2 H-27 Xb H 2-Nap G-1, G-2 H-28 H H 1 G-2 C 460 (M++1) H-29 H H 2-Nap G-1, G-2 H-30 fit-\ H 1 Me-5-Ind G-1, G-2 H-31 H G-2 C 452 (M++l) H-32 H H H Me-5-Ind G-2 [Example J-1] Synthesis of methyl 3- [4-cyclopentylmethyloxy-3-fluoro-5- (lH-indol-5- yl) phenyllpropionate (Compound No. J-1) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 13 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 10: 1), Compound No. A-21 (154 mg), 5-indoleboronic acid (100 mg), 2 M aqueous sodium carbonate (1.5 ml) and (Ph3P) 4Pd (50 mg) were reacted and treated to obtain the title compound (Compound No. J-1, 125 mg).

[Example J-2] Synthesis of 3- [4-cyclopentylmethyloxy-3-fluoro-5- (lH-indol-5-yl) phenyl] propionic acid (Compound No. J-2) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 2 hours, Compound No. J-1 (124 mg) and 2 N aqueous sodium hydroxide (630 1) were reacted and treated to obtain the title compound (Compound No. J-2, 97 mg).

[Example J-3] Synthesis of methyl 3- [3-chloro-4-cyclopentylmethyloxy-5- (lH-indol-5- yl) phenyl] propionate (Compound No. J-3) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 13 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 10: 1), Compound No. A-20 (151 mg), 5-indoleboronic acid (97 mg), 2 M aqueous sodium carbonate (1.5 ml) and (Ph3P) 4Pd (46 mg) were reacted and treated to obtain the title compound (Compound No. J-3, 160 mg).

[Example J-4] Synthesis of 3- [3-chloro-4-cyclopentylmethyloxy-5- (lH-indol-5-yl) phenyl] propionic acid (Compound No. J-4) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 2 hours, Compound No. J-3 (135 mg) and 2 N aqueous sodium hydroxide (660 u 1) were reacted and treated to obtain the title compound (Compound No. J-4, 97 mg).

[Examples J-1 to J-92] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table'J'l to Table-J-3 Zx Rx-O AR Table-J-1 .."_..- Exp. RxO Y Zx AR Syn method mr mn J-1 cPenMeO Me F 5-lnd J-2 cPenMeO H F 5-Ind J-2 J-3 cPenMeO Me J-4 cPenMeO H CI 5-Ind J-5 cPenMeO Me F 2-Nap J-1 J-6 J-6 J-7 cPenMeO Me F 1 J-1 J-8 cPenMeO H F J-9 cPenMeO Me-F J-10 cPenMeO H F 5-1 J-2 J-11 cPenMeO Me F 1 J-12 cPenMeO H F'i J-2 C J-13 2EtBuO H F 2-Nap G-1, G-2 J-14 2EtBuO H F 5-tnd G-2 J-15 4Me, cHexO H F 2-Nap G-1, G-2 J-16 4Me. cHexO H F 1Me-5-Ind G-2 Lo J-17 H F 2-Nap G-1, G-2 Wo - Jo J-18 H F 1 G-2 C 452 I J-19 H F 2-Nap G-1, G-2 J-20 3PhPrO H F lMe-5-Ind G-2 J-21 4PhBuO H F 2-Nap G-1, G-2 J-22 G-2 J-23 1 (4MePh) EtO H F 2-Nap J-24 4CIBnO H F 1Me-5-Ind G-2 J-25 4CF3BnO H F 2-Nap G-1, G-2 J-26 3F, 4 (OMe) BnO H F 1Me-5-Ind G-2 J-27 H F 2-Nap G-1, G-2 C 429 (M++1) J-28 @ H F 1Me-5-Ind G-2 0 J-29 Cv H F 1Me-5-Ind G-2 0 J-30 H F 2-Nap G-1, G-2 F J-31 C/~ G-2 X °-YTable-J-2 J-32 1-IndanO H F 2-Nap G-1, G-2 J-33 2-IndaneO H F 1Me-5-Ind G-2 J-34 2-IndaneO H F 2-Nap G-1, G-2 J-35 50Me-2-IndanO H F 1Me-5-Ind G-2 J-36 5, OD (OMe)-2-lNdanO F 2-Nap G-1, G-2 J-37 5F-2-IndanO H F 2-Nap G-1, G-2 J-38 5F-2-IndanO H F 1Me-5-Ind G-2 J-39 Qdo H F 2-Nap G-1, G-2 G _ J-40 0 H F 1 G-2 ' J-41 2 (3MePh) Et0 2-Nap G-1, G-2 J-42 2 (4MePh) EtO H F 1Me-5-Ind G-2 J-43 2 (2CIPh) H F 1 J-44 2 (3CIPh) H F 2-Nap G-1, G-2 J-45 2 (2CF3Ph) H F 2-Nap G-1, G-2 J-46 2 (20MePh) EtO H F 1 J-47 2 (40MePh) EtO H F 2-Nap G-1. G-2 J-48 2 (2-Nap) EtO H F lMe-5-Ind G-2 J-49 Q° H F 2-Nap G-1, G-2 C 458 (M++l) Xco J-50 0 H F 1 G-2 J-51 2 (PhS) EtO H F 1Me-5-Ind J-52 3PhPrO H F 2-Nap G-1, G-2 J-53 2CIBnO H F 1Me-5-Ind G-2 J-54 2BrBnO H F 2-Nap G-1, G-2 J-55 3, 5DMeBnO H F 2-Nap G-1, G-2 v J-56 4tBuBnO H F 1 G-2 C J-57 2CF3BnO H F 1Me-5-Ind G-2 J-58 4CF3BnO H F 2-Nap G-1, G-2 J-59 4nBuOBnO H F 2-Nap G-1. J-60 3, H F 1Me-5-Ind G-2 J-61 2, 3DCIBnO H F 2-Nap G-1, G-2 J-62 2-NapMeO H F 2-Nap G-1, G-2 C J-63 1-NapMeO H F 1 J-64 2PhBnO H F 1Me-5-Ind G-2 J-65 4PhBnO H F I G-2 J-66 50Me-2-Indano H F 2-Nap G-1, J-67 50Me-2-IndanO H F 1 G-2 J-68 5, 6D (OMe)-2-IndanOH F 2-Nap G-1, G-2 J-69 5, 6D (OMe)-2-lndanO F 1 G-2 J-70 5F-2-IndanO F 2-Nap J-71 G-1,Table-J-3 J-72 ; H 1 G-2 C)'\ N J-73 H F 2-Nap G-2 C 481 J-74 G-2 i J-75 Chxo J-76 4N5o H F 1 G-2 0 J-77/CGC H F 1Me-5-lHldz G-2 C 410 o. J-78 H F 1Me-5-Ind zoo 0-\ J-79 G-2 . J-80 H F N_, J-81 I G-2 J-82 F3C G-2 J-83 1 u,-o I J-84 G-2 1q"0 J-85 H F G-2 C 419 (M++l) J-86 G-2 J-asz H F 2-Nap G-1, G-2 J-88 N,, G-2 J-89 li-S r-S H F 2-Nap G-1, G-2 C 436 (M++1) J-90 G-2 S J-91 \o 2-Nap G-l, G-2 ---------------------------------------------- J-92 H G-2 [Example K-11] Synthesis of methyl 3- [3-bromo-4-cyclopentylmethyloxy-5- (naphthalen-2- yl)phenyl]propionate (Compound No. K-11) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 15 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 9: 1), Compound No. B-117 (306 mg), 2-naphthaleneboronic acid (163 mg), 2 M aqueous sodium carbonate (689 A l) and (Ph3P) 4Pd (74.2 mg) were reacted and treated to obtain the title compound (Compound No. K-11, 261 mg).

Synthesis of 3- [3-bromo-4-cyclopentylmethyloxy-5- (lH-indol-5-yl) phenyl] propionic acid (Compound No. K-12) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 2 hours, Compound No. K-11 (131 mg) and 2 N aqueous sodium hydroxide (400, u 1) were reacted and treated to obtain the title compound (Compound No. K-12, 109 mg).

[Example K-13] Synthesis of methyl 3- [3-bromo-4-cyclopentylmethyloxy-5- (lH-indol-5- yl) phenyl] propionate (Compound No. K-13) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 13 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 5: 1), Compound No. B-117 (102 mg), 5-indoleboronic acid (97 mg), 2 M aqueous sodium carbonate (1.5 ml) and (Ph3P) 4Pd (46 mg) were reacted and treated to obtain the title compound (Compound No. K-13, 85 mg).

[Example K-14] Synthesis of 3- [3-bromo-4-cyclopentylmethyloxy-5- (lH-indol-5-yl) phenyl] propionic acid (Compound No. K-14) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 2 hours, Compound No. K-13 (85 mg) and 2 N aqueous sodium hydroxide (200 u 1) were reacted and treated to obtain the title compound (Compound No. K-14,79 mg).

[Example K-17] Synthesis of methyl 3- [3-bromo-4-cyclopentyloxy-5- (1-methyl-lH-indazol-5- yl) phenyl] propionate (Compound No. K-17) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 14 hours at 80°C, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 4 : 1), Compound No. B-118 (306 mg), 1-methyl-lH-indazole- 5-boronic acid (175 mg), 2 M aqueous sodium carbonate (0.68 ml) and (Ph3P) 4Pd (70. 1 mg) were reacted and treated to obtain the title compound (Compound No. K- 17,148 mg).

[Examples K-1 to K-40] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-K-l and Table-K-2. Zx -K-1 able A _ Exp. RxO Y Zx AR Syn LCMS method Mass K-1 ONT Me F 2-Nap G-1 K-2 ON>o H F 2-Nap G-2 FN. K-3 AN Me F 5-Ind G-1 0 K-4 C H F 5-Ind G-2 C 457 (M-'*+l) _ K-5 Crß G-1 0 1 1 1 K-6 G-2 C 471 (M++l) N-N. K-7 > Me F 5-1 G-1 . K-8 Q""o F 5-1 G-2 1'IV K-9 aN N K-10 G-2 K-11 K-12 cPenMeO H Br 2-Nap K-12 K-13 cPenMeO Me Br 2-Nap K-13 K-14 cPenMeO H Br 5-Ind Int50, K-15 cPenO H Br 2-Nap K-11 K-16 cPenO H Br 1 K-17 cPenO Me Br 1 K-18 cPenO H Br 1 A 4. 78 443 (M+) K-19 H F 2-Nap G-1, G-2 K-20 H G-1, G-2 K-21 H F 2-Nap G-1, G-2 o K-22 » F 1 G-2 o K-23 -NN G-1, G-2 (t-0 K-24 O#NSO H F 1Me-5-Ind G-1, G-2 C 485 (M++1) 0 K-25 eok H F 2-Nap G-1, G-2 vo K-26 owN H F 1 G-1, G-2 Rx-o,Table-K-2 o K-27 N H F 2-Nap G-1, G-2 _ K-28 H H F 1Me-5-Ind G-2 s K-29 G-2 01-Y K-30 H H F 1Me-5-Ind G-2 0-i I F G-2 C 486 (M++1) 0 K-32 @ G-2 K-33 ag H F 2-Nap G-1, G-2 K-34 0-0 F 1 G-2 C 511 (M++1) K-35 H F 2-Nap G-1, G-2 K-36 X H F 1Me-5-Ind G-2 K-37 G-2 4f, K-38'''-° G-2 SJ-S K-39 0 G-2 K-40-0 G-2 [Example L-1] Synthesis of 3- [4-cyclop entyloxy-3-methyl-5- (naphthalen-2-yl) phenyl] propionic acid (Compound No. L-1) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out at 80°C for 6 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 20: 1), Compound A-24 (63 mg), 2-naphthaleneboronic acid (67 mg), 2 M aqueous sodium carbonate (130, u 1) and (Ph3P) 4Pd (18 mg) were reacted and treated. The obtained substance was reacted with 2 N aqueous sodium hydroxide (200 u 1) and treated according to the procedure described in the synthesis method of Intermediate 9 to obtain the title compound (Compound No. L-1, 25 mg).

[Example L-2] Synthesis of methyl 3- [4-cyclopentyloxy-3-methyl-5- (1-methyl-lH-indazol-5- yl) phenyl] propionate (Compound No. L-2) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out at 80°C for 12 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 4: 1), Compound No. K-17 (115 mg), methylboronic acid (66 mg, Ald), 2 M aqueous sodium carbonate (0.40 ml) and (Ph3P) 4Pd (39.4 mg) were reacted and treated to obtain the title compound (Intermediate 52,84 mg).

[Example L-3] Synthesis of 3- [4-cyclopentyloxy-3-methyl-5- (1-methyl-lH-indazol-5- yl) phenyl] propionic acid (Compound No. L-3) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 1.5 hours, Compound No. L-2 (82 mg) and 2 N aqueous sodium hydroxide (0.26 ml) were reacted and treated to obtain the title compound (Compound No. L-3, 62 mg).

[Examples L-1 to L-95] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-L-1 to Table-L-3. Rx Rx-O AR Table-L-1 Exp. RxO Y Zx AR Syn. LCMS method r L-1 cPenO H Me 2-Nap L-1 A 5. 65 375 (M++l) L-2 cPenO Me Me 1 L-3 cPenO H Me 1 L-3 A 4. 50 379 (M++1) L-4 2EtBuO Me Me 2-Nap L-2 L-5 2EtBuO H Me 2-Nap L-3 C L-6 2EtBuO H Me 6-OMe-2-Nap L-2, L-3 L-7 2EtBuO Me Me 5-Ind L-2 L-8 2EtBuO H Me 5-Ind L-3 L-9 2EtBuO Me Me L-10 H Me 1Me-5-Ind L-11 Me Me 5-1 Hldz L-2 L-12 H Me 5-1 HIdz L-3 L-13 Me Me 1 L-14 H Me lMe-5-lHIdz L-3 C L-15 Me Me 5-Bzt L-2 L-1 H Me 5-Bzt L-3 L-17 Me Me 5-2ABzt L-2 L-18 H Me 5-2ABzt L-3 L-19 Me Me 2Me-5-Bzt L-2 L-20 2EtBuO H Me 2Me-5-Bzt L-3 L-21 4Me, cHexO H Me 1Me-5-Ind G-2 , L-22 Me 2-Nap G-1, G-2 L-23 cHepO Me 2-Nap G-1, G-2 L-24 cHepO H Me 1Me-5-Ind G-2 C L-25 3PhPrO H Me 2-Nap G-1, G-2 L-26 4PhBuO H Me G-2 L-27 Me 2-Nap G-1, G-2 L-28 1 (4MePh) EtO H Me 1 G-2 C L-29 4CIBnO H Me 2-Nap G-1, G-2 L-30 4CF3BnO H Me 1Me-5-Ind G-2 L-31 3F, 4 (OMe) BnO H Me 2-Nap G-1, G-2 L-32 ( G-2 / L-33 H Me 2-Nap G-1, G-2 0 t34 H Me 2-Nap G-1, G-2 . L-35 H Me 1Me-5-Ind G-2 CF3 ATable-L-2 L-36 CH G-2 L-37 H Me 1Me-5-Ind G-1, G-2 L-38 L-39 2-IndanO H Me G-2 C L-40 2-IndanO H Me 1Me-5-Ind G-2 L-41 50Me-2-IndanO H Me 1 L-42 5, 6D (OMe)-2-lndanO H Me 2-Nap G-1, G-2 L-43 5F-2-IndaneO H Me 2-Nap G-1, G-2 L-44 5F-2-IndaneO H Me 1Me-5-Ind G-2 L-45 calo H Me 1Me-5-Ind G-1, G-2 L-46 H Me 2-Nap G-1, G-2 L-47 2 (3MePh) EtO H Me 2-Nap G-1, G-2 L-48 2 (3FPh) EtO H Me lMe-5-lnd G-2 C L-49 2 (2CIPh) H Me 1Me-5-Ind G-2 L-50 2 (4CF3Ph) EtO H Me 1 G-2 L-51 2 (20MePh) EtO H Me 2-Nap G-1, G-2 C L-52 2 (40MePh) EtO H Me 1 G-2 L-53 2 H Me 2-Nap L-54 2 (2-Nap) EtO H Me 1 G-2 L-55 0""° H Me G-2 L-56 CEOF H Me 1 G-1, G-2 C 459 (M++1) L-57 2 (PhS) EtO L-58 3PhPrO H Me 1Me-5-Ind G-1, G-2 L-59 2CIBnO H Me 2-Nap G-1, G-2 L-60 2BrBnO H Me 1Me-5-Ind G-1, G-2 L-61 3, 5DMeBnO H Me 2-Nap G-1, G-2 L-62 4tBuBnO H Me 2-Nap G-1, G-2 L-63 2CF3BnO H Me 2-Nap G-1, G-2 L-64 4tBuBnO H Me 1Me-5-Ind G-1, G-2 L-65 4nBuBnO H Me 2-Nap G-1, G-2 C L-66 3, 5DCIBnO H Me 2-Nap G-1. G-2 L-67 2, 3DCIBnO H Me 1Me-5-Ind G-1, G-2 L-68 2-NapMeO H Me 1Me-5-Ind G-2 L-69 1-NapMeO H Me 2-Nap G-1, G-2 L-70 2PhBnO H Me 1Me-5-Ind G-1, G-2 L-71 4PhBnO H Me 2-Nap G-1, G-2 C L-72 50Me-2-IndanO H Me 1Me-5-Ind G-1, G-2 L-73 5F-2-IndaneO H H Me 1 Me-5-Ind G-1,Table-L-3 L-74 N H Me 2-Nap G-1, G-2 C 401 (M++1) N L-75 H G-2 L-76 H Me 2-Nap G-1, G-2 N L-77 H Me L-78 H Me 2-Nap G-1, G-2 (cl) L-79 Me 1 G-2 0 L-80 @_|g Me 2-Nap G-1, G-2 _. o L-81 9 H Me 1 G-2 o> H Me 2-Nap G-1, G-2 C 412 L-82'O L-83 N"H G-2 0, :) l' L-84 F3C, G-2 L-84 ( :) Io L-85 L-86 bX G-2 L-67 H Me 1 G-2 L-88 Me 2-Nap G-1, G-2 t--0 L-89 N,, Me 1 G-2 C 415 (M++1) L-90 0 Me 2-Nap G-1, G-2 L-91 -0 H Me 1 G-2 L-92 t Me 2-Nap G-1, G-2 ,'S L-93 Nap H G-2 C 435 (M++1) \S L-94 1-' G-2 L-95 H Me G-2 [Examples M-1 to M-32] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification are shown in Table-M-1 and Table-M-2. Zx RO- {YO-Y Table-M-1 Exp Exp. RxO Y Zx AR Syn method M-1 Me Me 2-Nap G-1 C 478 (M++1) o M-2 H Me 2-Nap G-2 C 464 (M++1) N=N M-3 Me Me 5-Ind G-1 N=N M-4 H Me 5-Ind G-2 N-N M-5 Me Me G-1 I I M-6 ONNW G-2 C 467 (M++1) Nt. M-7 CrtP, Me Me 5-1 G-1 N-N M-8 ONNm H Me 5-1 G-2 N2. M-9 aNW Me Me 1 G-1 Q N"N M-10 H Me G-2 Q M-11'o C 463 (M++1) M-'12 G-1, G-2 M-13 Me 2-Nap G-1, G-2 0 M-14 O ''N, H Me 1Me-5-Ind G-2 C 465 (M++1 0 M-15 H Me 2-Nap G-1, G-2 N< M-16 6 H Me 1 Me-5-Ind G-2 v M-1 H Me 2-Nap G-1, G-2 C 464 (M++1) C) M-18 < H Me G-1, G-2 0 M-19 9 H Me 2-Nap G-1, G-2 _ M-20 tof H Me 1Me-5-Ind G-2 0 M-21 N H Me 2-Nap G-1, G-2 ATable-M-2 o-, M-22 C6-, C) M-23 H Me 2-Nap G-1, G-2 N H Me 1 G-2 C 0 M-25 H Me 2-Nap G-1, G-2 M-26 e M-26 M-27 Me 2-Nap G-1, G-2 M-28 H G-2 M-29 H Me 2-Nap G-1, G-2 M-30 H Me G-2 C 472 (M++1) M-31 H Me 2-Nap G-1, G-2 0 M-32 QfN~O H G-2 [Example N-1] Synthesis of methyl 3- {4- [2- (N-acetyl-N-phenylamino) ethyloxy]-3- (naphthalen-2- yl) phenyl} propionate (Compound No. N-1) A solution of Compound No. G-107 (32 mg) in methylene chloride (1 ml) was added with pyridine (24 u 1, TCI) and acetyl chloride (21 u 1, TCI), and stirred for 17 hours. The reaction mixture was added with water (3 ml), and extracted with methylene chloride (10 ml). The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane : ethyl acetate = 2 : 1) to obtain the title compound (Compound No. N-1, 28. 1 mg).

[Example N-2] Synthesis of 3-{4- [2- (N-acetyl-N-phenylamino) ethyloxy]-3- (naphthalen-2- yl) phenyl} propionic acid (Compound No. N-2) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 3 hours, Compound No. N-1 (28 mg) and 2 N aqueous sodium hydroxide (0.25 ml) were reacted and treated to obtain the title compound (Compound No. N-2, 22 mg).

[Example N-29] Synthesis of methyl 3- {4- [2- (N-methoxycarbonyl-N-phenylamino) ethyloxy]-3- (naphthalen-2-yl) phenyl} propionate (Compound No. N-29) According to the procedure described in the synthesis method of Compound No. N-1, Compound No. G-107 (32 mg), pyridine (23 u 1) and methyl chloroformate (23 u 1, TCI) were reacted and treated to obtain the title compound (Compound No.

N-29,17. 3 mg).

[Example N-30] Synthesis of 3- {4- [2- (N-methoxycarbonyl-N-phenylamino) ethyloxy]-3- (naphthalen-2- yl) phenyl} propionic acid (Compound No. N-30) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 3 hours, Compound No. N-29 (17 mg) and 2 N aqueous sodium hydroxide (0.25 ml) were reacted and treated to obtain the title compound (Compound No. N-30, 10.1 mg).

[Example N-48] Synthesis of methyl 3- {4- [2- (N-methylsulfonyl-N-phenylamino) ethyloxy]-3- (naphthalen-2-yl) phenyl} propionate (Compound No. N-48) According to the procedure described in the synthesis method of Compound No. N-1, Compound No. G-107 (32 mg), pyridine (24 u 1) and methanesulfonyl chloride (23 u 1) were reacted and treated to obtain the title compound (Compound No. N-48,32. 3 mg).

[Example N-49] Synthesis of 3- {4- [2- (N-methylsulfonyl-N-phenylamino) ethyloxy]-3- (naphthalen-2- yl) phenyl} propionic acid (Compound No. N-49) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 3 hours, Compound No. N-48 (32 mg) and 2 N aqueous sodium hydroxide (0.25 ml) were reacted and treated to obtain the title compound (Compound No. N-49, 17 mg).

[Example N-55] Synthesis of methyl 3- {4- [2- (3-ethyl-1-phenylureido) ethyloxy]-3- (naphthalen-2- yl) phenyl} propionate (Compound No. N-55) According to the procedure described in the synthesis method of Compound No. N-1 provided that the reaction was carried out for 41 hours, Compound No. G- 107 (32 mg), pyridine (24 u 1) and ethyl isocyanate (24 u 1, Nakarai Tecs) were reacted and treated to obtain the title compound (Compound No. N-55, 31.2 mg).

[Example N-56] Synthesis of 3- {4- [2- (3-ethyl-1-phenylureido) ethyloxy]-3- (naphthalen-2- yl) phenyl} propionic acid (Compound No. N-56) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 3 hours, Compound No. N-55 (31 mg) and 2 N aqueous sodium hydroxide (0.25 ml) were reacted and treated to obtain the title compound (Compound No. N-56,15 mg).

[Example N-64] Synthesis of methyl 3-{4-[2-(3-ethyl-1-phenylthioureido) ethyloxy]-3-(naphthalen-2- yl) phenyl} propionate (Compound No. N-64) According to the procedure described in the synthesis method of Compound No. N-1 provided that the reaction was carried out for 41 hours, Compound No. G- 107 (32 mg), pyridine (24 u 1) and ethyl isothiocyanate (21 1, Nakarai Tecs) were reacted and treated to obtain the title compound (Compound No. N-64, 27.4 mg).

[Example N-65] Synthesis of 3- {4- [2- (3-ethyl-1-phenylthioureido) ethyloxy]-3- (naphthalen-2- yl) phenyl} propionic acid (Compound No. N-65) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 3 hours, Compound No. N-64 (27 mg) and 2 N aqueous sodium hydroxide (0.25 ml) were reacted and treated to obtain the title compound (Compound No. N-65, 8.9 mg).

[Examples N-1 to N-74] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-N-1 and Table-N-2. Zx 03 w N5 O f O Table-N-1 m Exp. A'Re Y Zx AR Syn Method RTime Mass N-1 COMe Me H 2-Nap N-1 N-2 COMe H H 2-Nap N-2 N-3 COMe Me H N-1 N-4 COMe H H 5-Ind N-2 C N-5 COMe Me H 1 N-1 N-6 COMe H H 1 N-2 N-7 COMe Me H 5-1 N-8 COMe H H 5-1HIdz N-2 N-9 COMe Me H 1 N-1 N-10 H H 1 N-2 N-11 H H 2-Nap N-1, N-2 C N-12 H H 1 N-2 N-13 H H N-2 N-14 H H 1 N-2 N-15 COiPr H H 2-Nap N-1, N-2 C N-16 COiPr H H 1Me-5-Ind N-2 N-17 (Et) nBu H H 2-Nap N-1, N'2 N-18 COCH (Et) nBu H H N-2 N-19 H H 2-Nap N-1, N-2 N-20 COCH2OMe H H 1Me-5-Ind N-2 N-21 COCH=CHMe H H 2-Nap N-1, N-2 N-22 COCH=CHMe H H 1 N-1, N-2 C N-23 COiBu H H 2-Nap N-1, N-2 N-24 COiBu H H 1Me-5-Ind N-2 N-25 COcPr H H 2-Nap N-1. N-2 N-26 COcPr H H 1Me-5-Ind N-2 C N-27 CO (CH2) H H 2-Nap N-1, N-2 N-28 CO H H 1Me-5-Ind N-1, N-2 N-29 COOMe Me H 2-Nap N-29 N-30 COOMe H H 2-Nap N-30 N-31 COOMe H H 1 N-30 N-32 COOPh H H 2-Nap N-29, N-30 C N-33 COOPh H H 1 N-30 N-34 CONMe2 H H 2-Nap N-29, N-30 C N-35 CONMe2 H H 1Me-5-Ind N-30 N-36 COOiBu H N-30 N-37 COOiBu H H iMe-5-lnd N-30 N-38 C (O) SMe H H 2-Nap N-29, N-30 N-39 C (O) SMe H H 1 N-30 N-40 *tNi H H 2-Nap N-29, N-30 . N-41 tNv N-30 C 528 (M++1) ZXTable-N-2 N-42 H H 2-Nap Int53, N-29 4--F N-43 SN3 H 1 Me-5-Ind Int53, N-29 N-44 COO (CH2) 2OMe H H 2-Nap Int53 N-29 N-45 COO (CH2) 2OMe H H 1 N-46 O*ND H H 2-Nap Int53, N-29 N-47 H 1 Me-5-Ind Int53, N-29 N-48 SO2Me Me H 2-Nap N-48 N-49 SO2Me H H 2-Nap N-49 N-50 SO2Me H H 1 N-49 C N-51 SO2Ph H H 2-Nap N-52 SO2Ph H H 1 N-49 N-53 SO2NMe2 H H 2-Nap N-48, N-49 C N-54 SO2NMe2 H H 1 N-49 N-55 CONHEt Me H 2-Nap N-55 N-56 CONHEt H H 2-Nap N-56 C N-57 CONHEt H H 1 N-56 N-58 CONHPh H H 2-Nap N-55, N-56 N-59 CONHPh H H 1 N-56 N-60 CONHcHex H H 2-Nap N-55, N-56 N-61 CONHcHex H H 1 N-56 C N-62 CONHBn H H 2-Nap N-55, N-56 N-63 CONHBn H H 1 N-56 N-64 CSNHMe Me H 2-Nap N-64 N-65 CSNHMe H H N-66 CSNHMe H H 1 N-65 N-67 CSNHPh H H 2-Nap N-64, N-65 N-68 CSNHPh H H 1 N-65 N-69 CSNH (3-Py) H H 2-Nap N-64, N-65 C N-70 CSNH (3-Py) H H 1 N-65 N-71 CSNHiPr H H 2-Nap N-64, N-65 N-72 CSNHiPr H H 1 N-65 C N-73 CSNHBn H H N-74 CSNHBn H H 1 N-65 [Example P-1] Synthesis of ethyl 3- [2-cyclopentylmethyloxy-3- (naphthalen-2-yl) pyridin-5- yl] propionate (Compound No. P-1) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 14 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 5: 1), 2-naphthaleneboronic acid (119 mg), Compound No. E-1 (83 mg), 2 M aqueous sodium carbonate (0.3 ml) and (PhsP) 4Pd (38.1 mg) were reacted and treated to obtain the title compound (Compound No. P-1, 76 mg).

[Example P-2] Synthesis of 3- [2-cyclopentylmethyloxy-3- (naphthalen-2-yl) pyridin-5-yllpropionic acid (Compound No. P-2) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 2 hours, Compound No. P-1 (47.8 mg) and 2 N aqueous sodium hydroxide (0.2 ml) were reacted and treated to obtain the title compound (Compound No. P-2, 20 mg).

[Example P-36] Synthesis of ethyl 3-{3-(naphthalen-2-yl)-2- [(R)-l-phenylethyloxy] pyridin-5- yl} propionate (Compound No. P-36) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 2 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 6: 1), 2-naphthaleneboronic acid (44 mg), Compound No. E-7 (73.3 mg), 2 M aqueous sodium carbonate (120, u 1) and (Ph3P) 4Pd (21.3 mg) were reacted and treated to obtain the title compound (Compound No. P-36, 44 mg).

[Example P-37] Synthesis of 3- {3- (naphthalen-2-yl)-2- [(R)-1-phenylethyloxy] pyridin-5-yl} propionic acid (Compound No. P-37) According to the procedure described in the synthesis method of Intermediate 9, Compound No. P-36 (41.2 mg) and 2 N aqueous sodium hydroxide (0.1 ml) were reacted and treated to obtain the title compound (Compound No. P-37, 38 mg).

[Example P-42] Synthesis of ethyl 3- {3- (naphthalen-2-yl)-2- [4- (trifluoromethyl) phenylmethyloxy] pyridin-5-yl} propionate (Compound No. P-42) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 2 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 6 : 1), 2-naphthaleneboronic acid (37.4 mg), Compound No. E-13 (42.4 mg), 2 M aqueous sodium carbonate (90 u 1) and (Ph3P) 4Pd (21.4 mg) were reacted and treated to obtain the title compound (Compound No. P-42,30. 4 mg).

[Example P-43] Synthesis of 3- {3- (naphthalen-2-yl) -2- [4- (trifluoromethyl) phenylmethyloxy] pyridin- 5-yl} propionic acid (Compound No. P-43) According to the procedure described in the synthesis method of Intermediate 9, Compound No. P-42 (29.5 mg) and 2 N aqueous sodium hydroxide (0.15 ml) were reacted and treated to obtain the title compound (Compound No. P- 43,24. 1 mg).

[Examples P-1 to P-50] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-P-1 and Table-P-2. Rx AR Table-P-1 ,..,. Exp. RxO Y AR Syn method irs P-1 cPenMeO Et 2-Nap P-1 P-2 cPenMeO H 2-Nap P-2 A 5. 60 376 (M++1) P-3 cPenMeO Et 5-Ind P-1 A 5. 37 393 (M++1) P-4 cPenMeO H 5-Ind P-2 P-5 cPenMeO Et 1 P-6 cPenMeO H 1Me-5-Ind P-2 A 4. 90 379 P-7 cPenMeO Et 1 Me-5-lnd P-8 cPenMeO H 5-1 HIdz P-9 cPenMeO Et 5-1 HIdz P-1 P-10 cPenMeO H 1Me-5-1HIdz P-2 P-11 cPenMeO Et 5-Bzt P-1 P-12 cPenMeO H 5-Bzt P-2 P-13 cPenMeO Et 5-2ABzt P-1 P-14 cPenMeO H 5-2ABzt P-2 Tr% P-15 H 6-IQ P-2 C P-16 cPenO H 2-Nap P-1, P-2 l P-17 cPenO H 5-Ind P-1, P-2 C P-18 cPenO H 1 P-2 P-19 cPenO H 5-1 P-2 P-20 cPenO H 1 P-2 P-21 cPenO H 5-Bzt P-1. P-2 P-22 cPenO H 5-2ABzt P-1, P-2 P-23 cHexO H 2-Nap P-1, P-2 A 5. 51 376 (M++1) P-24 cHexO. H 5-Ind P-1, P-2 P-25 cHexO H 1 P-26 cHexO H 1 P-2 P-27 2EtBuO H 2-Nap P-1, P-2 A 5. 68 378 (M++1) P-28 2EtBuO H 5-Ind P-1, P-2 P-29 2EtBuO H 1 P-2 P-30 iBuO H 2-Nap P-1, P-2 A 5. 13 350 (M++1) P-31 iBuO H 5-Ind P-1, P-2 P-32 iBuO H 1 P-1, P-2 P-33 iBuO P-34 BnO H 2-Nap P-1, P-2 P-35 BnO H 1Me-5-Ind P-36 (R) l Et 2-Nap P-36 P-37 (R) lPhEtO H 2-Nap P-37 P-38 (S) l H 2-Nap P-36, P37 A 5. 31 398 (M++1) P-39 (S) H 1 4. 75 401 (M++1) P-40 2MeBnO H 2-Nap P-1, P-2 P-41 2MeBnO H 1 P-2 OTable-P-2 P-42 4CF3BnO Et 2-Nap P-42 P-43 4CF3BnO H 2-Nap P-43 A 5. 52 452 (M++1) P-44 4CF3BnO H 1 P-2 P-45 3PhBuO H 1Me-5-Ind P-2 P-46 2 (2-Nap) EtO H 2-Nap P-2 P-47 2 (2-Nap) EtO H 1 P-2 P-48 2 (2FPh) EtO H P-49 2 (2FPh) EtO H 5-Ind P-1, P-2 A 4. 18 405 (M++1) P-50 2 (2FPh) EtO H 1 [Example Q-1] Synthesis of methyl 3- [4-methoxy-3- (naphthalen-2-yl)-5-nitrophenyl] propionate (Intermediate 49) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out at 80°C for 15 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 10: 1), Intermediate 21 (2.65 g), 2-naphthaleneboronic acid (2.87 g), 2 M aqueous sodium carbonate (7.5 ml) and (Ph3P) 4Pd (960 mg) were reacted and treated to obtain the title compound (Intermediate 49,2. 47 g).

Synthesis of 3- [4-methoxy-3- (naphthalen-2-yl)-5-nitrophenyl] propionic acid (Intermediate 50) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 40 minutes, Intermediate 49 (2.45 g) and 2 N aqueous sodium hydroxide (6.7 ml) were reacted and treated to obtain the title compound (Intermediate 60,1. 96 g).

Synthesis of methyl 3- [4-hydroxy-3- (naphthalen-2-yl)-5-nitrophenyl] propionate (Intermediate 51) According to the procedure described in the synthesis method of Intermediate 10 provided that the reaction was carried out for 3 hours, pyridine (10 ml), concentrated hydrochloric acid (10 ml), and Intermediate 50 (1.00 g) were reacted and treated to obtain crude powder substance. This substance was reacted with thionyl chloride (282 u 1) in methanol and treated according to the procedure described in the synthesis method of Intermediate 1 to obtain the title compound (Intermediate 51,306 mg).

Synthesis of methyl 3- [4-cyclopentyloxy-3- (naphthalen-2-yl)-5- nitrophenyl] propionate (Compound No. Q-1) According to the procedure described in the synthesis method of Compound No. A-6 with the modifications that the reaction was carried out for 15.5 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 19: 1), Intermediate 51 (84 mg), Ph3P (125 mg), cyclopentanol (50 u 1) and 40% DIAD (224, u l) were reacted and treated to obtain the title compound (Compound No. Q-1, 90 mg).

[Example Q-2] Synthesis of methyl 3- [3-amino-4-cyclopentyloxy-5-(naphthalen-2- yl) phenyl] propionate (Compound No. Q-2) A solution of Compound No. Q-1 (59.1 mg) in methanol (5 ml) was added with platinum oxide (5 mg, Ald), and stirred at room temperature for 30 minutes under hydrogen atmosphere. The reaction mixture was filtered, and the solvent of the filtrate was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 4 : 1) to obtain the title compound (Compound No. Q-2, 49 mg).

[Example Q-3] Synthesis of 3- [3-amino-4-cyclopentyloxy-5- (naphthalen-2-yl) phenyl] propionic acid (Compound No. Q-3) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 2 hours, Compound No. Q-2 (40 mg) and 2 N aqueous sodium hydroxide (150 u 1) were reacted and treated to obtain the title compound (Compound No. Q-3, 38 mg).

[Example Q-4] Synthesis of methyl 3- [4-cyclopentyloxy-3-(lH-indol-5-yl)-5-nitrophenyl] propionate (Compound No. Q-4) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out at 80°C for 16 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 4 : 1), Compound No. A-28 (187 mg), 5-indoleboronic acid (143 mg), 2 M aqueous sodium carbonate (400, u 1) and (PhsP) 4Pd (51 mg) were reacted and treated to obtain the title compound (Compound No. Q-4,192 mg).

[Example Q-5] Synthesis of methyl 3-13-amino-4-cyclop entyloxy-5- (lH-indol-5-yl) phenyl] propionate (Compound No. Q-5) According to the procedure described in the synthesis method of Compound No. Q-2 with the modification that the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 2 : 1), Compound No. Q-4 (59.1 mg) and platinum oxide (5 mg) were reacted and treated to obtain the title compound (Compound No. Q-5,49. 3 mg).

[Example Q-6] Synthesis of 3- [3-amino-4-cyclopentyloxy-5- (lH-indol-5-yl) phenyl] propionic acid (Compound No. Q-6) According to the procedure described in the synthesis method of Intermediate 9, Compound No. Q-5 (44 mg) and 2 N aqueous sodium hydroxide (150 iL 1) were reacted and treated to obtain the title compound (Compound No. Q-6, 41 mg).

[Example Q-8] Synthesis of methyl 3- [4-cyclopentyloxy-3- (l-methyl-lH-indazol-5-yl)-5- nitrophenyl] propionate (Compound No. Q-8) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out at 80°C for 16 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 3:1), Compound No. A-28 (182 mg), 1-methyl-5- indazoleboronic acid (152 mg), 2 M aqueous sodium carbonate (400, u 1) and (Ph3P) 4Pd (58.9 mg) were reacted and treated to obtain the title compound (Compound No. Q-8, 181 mg).

[Example Q-9] Synthesis of methyl 3- [3-amino-4-cyclopentyloxy-5- (1-methyl-lH-indazol-5- yl) phenyl] propionic acid (Compound No. Q-9) A solution of Compound No. Q-8 (578 mg) in a mixture of ethyl acetate (2 ml) and methanol (5 ml) was added with Raney 2800 nickel (230 mg) and stirred at room temperature for 6 hours under hydrogen atmosphere. The reaction mixture was filtered, and the solvent of the filtrate was evaporated under reduced pressure.

The residue was purified by column chromatography (Quad, hexane : ethyl acetate 2 : 1) to obtain the title compound (Compound No. Q-9, 484 mg).

[Example Q-10] Synthesis of 3- [3-amino-4-cyclopentyloxy-5- (lH-indazol-5-yl) phenyl] propionic acid (Compound No. Q-10) According to the procedure described in the synthesis method of Intermediate 9, Compound No. Q-9 (56 mg) and 2 N aqueous sodium hydroxide (200 , u 1) were reacted and treated to obtain the title compound (Compound No. Q-10, 50 mg).

[Example Q-47] Synthesis of methyl 3- [4-benzyloxy-3- (naphthalen-2-yl)-5-nitrophenyl] propionate (Compound No. Q-47) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out at 80°C for 12 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 8: 1), Compound No. B-95 (6.00 g), 2-naphthaleneboronic acid (4.11 g), 2 M aqueous sodium carbonate (13.5 ml) and (Ph3P) 4Pd (1.36 g) were reacted and treated to obtain the title compound (Compound No. Q-47, 5.81 g).

[Example Q-48] Synthesis of methyl 3- [3-amino-4-benzyloxy-5- (naphthalen-2-yl) phenyl] propionate (Compound No. Q-48) According to the procedure described in the synthesis method of Compound No. Q-9 with the modifications that the reaction was carried out for 20 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 2: 1), Compound No. Q-47 (5.04 g) and Raney 2800 nickel (2.50 g) were reacted and treated to obtain the title compound (Compound No. Q-48, 4.21 g).

[Example Q-1 to Q-52] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-Q-1. zx Rx-\//0-Y ex Table-Q-1 AR Exp. RxO Y Zx AR Syn LCMS"" method Mass Q-1 cPenO 2-Nap Q-1 Q-2 cPenO Me NH2 2-Nap Q-2 Q-3 cPenO H NH2 2-Nap Q-3 A 4. 78 376 Q-4 cPenO Me N02 5-Ind Q-4 Q-5 cPenO Me NH2 5-Ind Q-6 cPenO H NH2 5-land Q-6 A 3. 75 365 (M++1) Q-7 cPenO H NH2 1 Me-5-Ind Q-6 A 4. 19 379 (M++1) Q-8 cPenO Me N02 1 Q-8 Q-9 cPenO. Me NH2 1 Q-10 cPenO H NH2 1 Q-11 H NH2 5-1 Q-12 H NH2 5-Bzt Q-8, Q-9, Q-10 Q-13 cPenO H NH2 5-2ABzt Q-8, Q-9, Q-10 Q-14 cPenO H NH2 2Me-5-Bzt Q-15 cHexO H NH2 2-Nap Q-1, Q-2, Q-3 A 5. 66 404 (M++1) Q-16 cHexO H NH2 1 Me-5-Ind Q-6 Q-17 cHexO H NH2 1 Q-18 H NH2 2-Nap Q-1, Q-2, Q-3 Q-19 H NH2 5-Ind Q-6 A 4. 26 381 (M++1) Q-20 2EtBuO H NH2 1 Me-5-Ind Q-6 Q-21 2EtBuO H NH2 5-1 Q-8, Q-9, Q-10 Q-22 2EtBuO H NH2 1 Q-23 2EtBuO H NH2 5-Bzt Q-8 Q-9. Q-10 Q-24 2EtBuO H NH2 5-2ABzt Q-8, Q-9. Q-10 Q-25 2EtBuO H NH2 2Me-5-Bzt Q-8 Q-9 Q-10 Q-26 iBuO H NH2 2-Nap Q-1, Q-2, Q-3 A 4. 82 364 (M++1) Q-27 iBuO H NH2 1 Me-5-Ind Q-6 Q-28 iBuO H NH2 1 A 3. 66 368 (M++1) Q-29 (S) 1 H NH2 2-Nap Q-1, Q-2, Q-3 A 4. 87 412 (M++1) Q-30 (S) 1 H NH2 1 Me-5-Ind Q-6 A 4. 31 415 (M++1) Q-31 (S) 1 H NH2 1 Q-10 A 3. 76 416 Q-32 4CF3BnO H NH2 2-Nap Q-1, Q-2, Q-3 A 5. 26 466 (M++1) Q-33 4CF3BnO H NH2 1 Q-6 A 4. 20 455 (M++1) Q-34 4CF3BnO H NH2 l Q-35 2-IndanO H NH2 2-Nap Q-1, Q-2, Q-3 A 5. 10 424 (M++1) Q-36 2-IndanO H NH2 1 Q-6 A 4. 63 Q-37 2-IndanO H NH2 1 A 4. 14 428 Q-38 5OMe-2-IndanO H NH2 2-Nap Q-1, Q-2, Q-3 Q-39 5, 6 (OMe)-2-lndano H NH2 1 Q-6 Q-40 5F-2-IndanO H NH2 1 Q-41 2 (4FPh) EtO H NH2 2-Nap Q-1, Q-2, Q-3 Q-42 2 (4FPh) EtO H NH2 1 Q-43 2 (4FPh) EtO H NH2 1 A 4. 48 448 (M++1) Q-44 2 (4DMAPh) EtO H NH2 2-Nap Q-1, Q-2, Q-3 A 4. 28 455 Q-45 2 (4DMAPh) EtO H NH2 1 Q-46 2 (4DMAPh) EtO H NH2 1 A 3. 12 459 (M++1) Q-47 Me N02 2-Nap Q-47 Q-48 BnO Me NH2 2-Nap Q-48 Q-49 BnO H NH2 2-Nap Q-3 Q-50 BnO Me N02 1 Q-47 a Me NH2 1 Q-52 [Example S-1] Synthesis of methyl 3- {4-benzyloxy-3- (naphthalen-2-yl) -5- [N- (2, 2,2- trifluoroacetyl) amino] phenyl} propionate (Intermediate 52) According to the procedure described in the synthesis method of Compound No. B-103 with the modifications that the reaction was carried out for 1.5 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 4: 1), Compound No. Q-48 (4. 18 g), triethylamine (4.65 ml) and trifluoroacetic anhydride (7.40 ml) were reacted and treated to obtain the title compound (Intermediate 52,4. 72 g).

Synthesis of methyl 3- {4-hydroxy-3- (naphthalen-2-yl)-5- [N- (2, 2,2- trifluoroacetyl) amino] phenyl} propionate (Intermediate 53) A solution of Intermediate 52 (3.20 g) in a mixture of ethyl acetate (50 ml) and methanol (25 ml) was added with 10% palladium/carbon (98 mg), and stirred at room temperature for 2 hours under hydrogen atmosphere. The reaction mixture was filtered, and the solvent of the filtrate was evaporated under reduced pressure to obtain the title compound (Intermediate 53, 2. 39 g).

Synthesis of methyl 3- {4-cyclopentyloxy-3- (naphthalen-2-yl)-5- [N- (2, 2,2- trifluoroacetyl) amino] phenyl} propionate (Intermediate 54) According to the procedure described in the synthesis method of Compound No. A-6 with the modifications that the reaction was carried out for 15.5 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 19 : 1), Intermediate 53 (84 mg), PhsP (125 mg), cyclopentanol (50 u 1) and 40% DIAD (224, u 1) were reacted and treated to obtain the title compound (Intermediate 54,90 mg).

Synthesis of methyl 3- {4-cyclopentyloxy-3- [N-methyl-N- (2, 2,2- trifluoroacetyl) amino]-5- (naphthalen-2-yl) phenyl} propionate (Intermediate 55) A solution of Intermediate 54 (208 mg) in DMF (5 ml) was added with 60% sodium hydride (21 mg) under ice cooling, and stirred for 20 minutes. This reaction mixture was added dropwise with methyl iodide (150, u 1), stirred for 10 minutes, then warmed to room temperature, and further stirred for 1 hour. The reaction mixture was poured into ice water, and ethyl acetate (100 ml) was added for extraction. The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure.

The residue was purified by column chromatography (Quad, hexane : ethyl acetate = 5 : 1) to obtain the title compound (Intermediate 55,200 mg).

Synthesis of 3- [4-cyclopentyloxy-3-(N-methylamino)-5- (naphthalen-2- yl) phenyl] propionic acid (Compound No. S-1) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 6 hours, Intermediate 55 (198 mg) and 2 N aqueous sodium hydroxide (800 u 1) were reacted and treated to obtain the title compound (Compound No. S-1, 38 mg).

[Example S-3] Synthesis of methyl 3- [3-acetylamino-4-cyclopentyloxy-5- (naphthalen-2- yl) phenyl] propionate (Compound No. S-3) A solution of Compound No. Q-2 (81 mg) in methylene chloride (2 ml) was added with N-methylmorpholine (33, u l, WAKO), and added with acetyl chloride (22, u 1) under ice cooling. The reaction mixture was stirred for 10 minutes, then warmed to room temperature, and further stirred for 18 hours. The reaction mixture was poured into aqueous sodium hydrogencarbonate (100 ml), and added with ethyl acetate (150 ml) for extraction. The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 6: 1) to obtain the title compound (Compound No. S-3,85 mg).

[Example S-4] Synthesis of 3- [3-acetylamino-4-cyclopentylmethyloxy-5- (naphthalen-2- yl) phenyl] propionic acid (Compound No. S-4) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 15 hours, Compound No. S-3 (80 mg) and 2 N aqueous sodium hydroxide (400 t 1) were reacted and treated to obtain the title compound (Compound No. S-4, 75 mg).

[Example S-5] Synthesis of 3- [4-cyclopentyloxy-3-formylamino-5- (naphthalen-2- yl) phenyl] propionic acid (Compound No. S-5) A solution of Compound No. Q-2 (90 mg) in DMF (5 ml) was added with a mixture of formic acid (200 u 1) and acetic anhydride (100, u 1) under ice cooling.

The reaction mixture was stirred 10 minutes, then warmed to room temperature, and further stirred for 18 hours. The reaction mixture was poured into aqueous sodium hydrogencarbonate (100 ml), and added with ethyl acetate (150 ml) for extraction. The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure.

The residue was purified by column chromatography (Quad, hexane : ethyl acetate = 5: 1). The obtained substance was reacted and treated with 2N aqueous sodium hydroxide (400 u 1) according to the procedure described in the synthesis method of Intermediate 9 to obtain the title compound (Compound No. S-5,65 mg).

[Example S-6] Synthesis of methyl 3- [3- (2-acetoxyacetylamino)-4-cyclopentyloxy-5- (naphthalen-2- yl) phenyl] propionate (Compound No. S-6) According to the procedure described in the synthesis method of Intermediate 70, Compound No. Q-2 (88 mg), N-methylmorpholine (36 A 1) and acetoxyacetyl chloride (35 u 1, Ald) were reacted and treated to obtain the title compound (Compound No. S-6, 75 mg).

[Example S-7] Synthesis of 3- [4-cyclopentyloxy-3- (2-hydroxyacetylamino) -5- (naphthalen-2- yl) phenyl] propionic acid (Compound No. S-7) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 15.5 hours, Compound No. S-6 (102 mg) and 2 N aqueous sodium hydroxide (500 u 1) were reacted and treated to obtain the title compound (Compound No. S-7,80 mg).

[Example S-8] Synthesis of 3- [3-carbamoylamino-4-cyclopentyloxy-5- (naphthalen-2- yl) phenyllpropionic acid (Compound No. S-8) A solution of Compound No. Q-2 (100 mg) in a mixture of acetic acid (2 ml) and purified water (0.4 ml) was added with potassium cyanate (45 mg, Wako Pure Chemical Industries), and stirred at room temperature for 1 hour. The reaction mixture was poured into water (50 ml) containing ice, and extracted with isopropyl ether (150 ml x 2). The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The obtained substance was reacted with 2 N aqueous sodium hydroxide (300, jeu 1) and treated according to the procedure described in the synthesis method of Intermediate 9 to obtain the title compound (Compound No. S-8, 70 mg).

[Example S-9] Synthesis of methyl 3- [4-cyclopentyloxy-3-methylsulfonylamino-5- (naphthalen-2- yl) phenyl] propionate (Compound No. S-9) A solution of Compound No. Q-2 (81 mg) in methylene chloride (2 ml) was added with pyridine (300 u 1), and then added with methanesulfonyl chloride (40 u 1) under ice cooling. The reaction mixture was stirred for 10 minutes, then warmed to room temperature, and further stirred for 2 hours. The reaction mixture was poured into 1 N hydrochloric acid, and added with ethyl acetate (150 ml) for extraction. The organic layer was washed successively with saturated aqueous sodium hydrogencarbonate, and saturated brine, and dried, and then the solvent of the organic layer was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane : ethyl acetate = 13: 2) to obtain the title compound (Compound No. S-9, 96 mg).

Synthesis of 3- [4-cyclopentyloxy-3-methylsulfonylamino-5- (naphthalen-2- yl) phenyl] propionic acid (Compound No. S-10) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out at room temperature for 17.5 hours and at 60°C for 3 hours, Compound No. S-9 (81 mg) and 2 N aqueous sodium hydroxide (400 u 1) were reacted and treated to obtain the title compound (Compound No. S-10,80 mg).

[Example S-11] Synthesis of 3- [4-cyclopentyloxy-3- (N, N-dimethylsulfamoylamino)-5- (naphthalen-2- yl) phenyl] propionic acid (Compound No. S-11) A solution of Compound No. Q-2 (163 mg) in pyridine (5 ml) was successively added with 4-dimethylaminopyridine (104 mg, TCI) and dimethylsulfamoyl chloride (520 g 1, TCI), and stirred for 5 days. The reaction mixture was added with water (30 ml) and ethyl acetate (90 ml) for extraction.

The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane : ethyl acetate = 6: 1). The obtained substance was reacted with 2 N aqueous sodium hydroxide (300 u 1) and treated according to the procedure described in the synthesis method of Intermediate 9 to obtain the title compound (Compound No. S-11, 105 mg).

[Example S-12] Synthesis of 3- [4-cyclop entyloxy-3- (N, N-dimethylamino)-5- (nap hthalen-2- yl) phenyl] propionic acid (Compound No. S-12) A solution of Compound No. Q-2 (60 mg) in DMF (3 ml) was added with 60% sodium hydride (26 mg) under ice cooling, and stirred for 10 minutes. The reaction mixture was added with methyl iodide (100 je 1), stirred for 10 minutes, then warmed to 60°C, and further stirred for 2 hours. The reaction mixture was poured into water (20 ml), and ethyl acetate (50 ml) was added for extraction. The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 8: 1). The obtained substance was reacted with 2 N aqueous sodium hydroxide (150, A 1) and treated according to the procedure described in the synthesis method of Intermediate 9 to obtain the title compound (Compound No. S-12,46 mg).

Synthesis of methyl 3- {4-benzyloxy-3- (l-methyl-lH-indazol-5-yl)-5- [N- (2,2, 2- trifluoroacetyl) amino] phenyl} propionate (Intermediate 56) According to the procedure described in the synthesis method of Compound No. B-103 with the modifications that the reaction was carried out for 1.5 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 3: 1), Compound No. Q-51 (2.09 g), triethylamine (3.70 ml) and trifluoroacetic anhydride (2.35 ml) were reacted and treated to obtain the title compound (Intermediate 56,2. 36 g).

Synthesis of methyl 3- {4-hydroxy-3- (l-methyl-lH-indazol-5-yl)-5- [N- (2,2, 2- trifluoroacetyl) amino] phenyl} propionate (Intermediate 57) A solution of Intermediate 56 (1.62 g) in a mixture of ethyl acetate (10 ml) and methanol (3 ml) was added with 10% palladium/carbon (29 mg), and stirred at room temperature for 17 hours under hydrogen atmosphere. The reaction mixture was filtered, and the solvent of the filtrate was evaporated under reduced pressure to obtain the title compound (Intermediate 57,1. 19 g).

[Examples S-1 to S-73] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-S-1 and Table-S-2. Zx Rx-O air Table-S-1 _. -., LCMS method S-1 cPenO H S-1 S-2 cPenO H NHEt 2-Nap S-1 S-3 cPenO Me NHAc 2-Nap S-3 S-4 cPenO H NHAc 2-Nap S-4 C S-5 cPenO H NHCHO 2-Nap S-5 C S-6 S-8 S-7 cPenO H NHCOCH2OH 2-Nap S-7 C 437 (M++1) S-8 cPenO H NHCONHa 2-Nap S-8 C 422 (M++1) S-9 cPenO Me NHSO2Me 2-Nap S-9 S-10 cPenO H NHSO2Me 2-Nap S-10 C S-11 cPenO H NHSO2NMe2 2-Nap S-11 C483 S-12 cPenO H NMe2 2-Nap S-12 S-13 cPenO H NHMe 1 Me-5-Ind S-1 S-14 cPenO H NMe2 1 S-12 C S-15 cPenO H NHMe 1 S-16 cPenO H NMe2 1 S-12 S-17 cPenO H NHMe 5-Bzt S-1 S-18 cPenO H NMe2 5-Bzt S-12 S-19 cPenO H NHMe 5-2ABzt S-1 S-20 cPenO H NMe2 5-2ABzt S-12 S-21 cPenO H NHMe 2Me-5-Bzt S-1 S-22 cPenO H NMe2 2Me-5-Bzt S-12 S-23 cPenMeO H S-1 S-24 cPenMeO H NMe2 S-12 S-25 cPenMeO H NHME S-26 cPenMeO H NMe2 1 S-27 cHexO H NHMe 2-Nap S-1 S-28 cHexO H NMe2 2-Nap S-12 S-29 cHexO H NHMe 1 S-1 C S-30 cHexO H NMe2 1 S-12 S-31 cHexO H NHMe 1 S-1 S-32 cHexO H NMe2 1 Me-5-1 Hldz S-33 2EtBuO H NHMe 2-Nap S-1 C S-34 2EtBuO H NHMe 6-OMe-2-Nap S-1 S-35 2EtBuO H NHMe 1 S-1 S-36 2EtBuO H NHMe 5-Bzt S-1 S-37 2EtBuO H NHMe 1 S-1 S-38 iBuO H NHMe 2-Nap S-1 S-39 iBuO H NMe2 2-Nap S-12 C 392 (M++1) S-40 H NHMe 1 S-1 C S-41 iBuO H NMe 1 Me-5-Ind S-12 S-42 iBuO H NHMe 1 S-43 iBuO H NMez S-12 S-44 lPhEtO S-45'1 X fYTable-S-2 S-46 1 H NHMe 1 S-1 S-47 1 S-48 1 H NHMe 1 S-1 C S-49 H NMea 1 S-12 S-50 4CF3BnO H NHMe 2-Nap S-1 S-51 40FsBnO 2-Nap S-12 S-52 4CF3BnO H NHMe 1 S-53 4CF3BnO H NMe2 1 S-12 C S-54 4CF3BnO H NHMe 1Me-5-1HIdz S-55 4CF3BnO H NMe2 1 S-12 S-56 2-IndanO H NHMe S-1 S-57 2-IndanO H NMe2 2-Nap S-12 S-58 2-IndanO H NHMe 1 S-1 C441 +1) S-59 2-IndanO H NMe2 1 S-12 S-60 2-IndanO H NHMe 1 A 4. 16 442 (M++1) S-61 2-IndanO H NMe2 1 S-12 A 4. 18 456 (M++1) S-62 2 (4FPh) EtO H NHMe 2-Nap S-1 S-63 2 (4FPh) EtO H NMe2 2-Nap S-12 C S-64 2 (4FPh) EtO H NHMe 1 S-1 C S-65 2 (4FPh) EtO H NMe2 1Me-5-Ind S-66 2 (4FPh) EtO H NHMe 1 S-67 2 (4FPh) EtO H NMe2 1 S-12 S-68 2 (4DMAPh) EtO H NHMe 2-Nap S-1 C S-69 2 (4DMAPh) EtO H NMe2 2-Nap S-12 S-70 2 (4DMAPh) H NHMe 1 S-1 S-71 2 (4DMAPh) EtO H NMe2 1 S-72 2 (4DMAPh) EtO H NHMe t S-73 2 (4DMAPh) EtO H NMe2 1 Me-5-1 [Example T-1] Synthesis of 3- [4-cyclopentylmethyloxy-3-hydroxy-5- (naphthalen-2- yl) phenyl) propionic acid (Compound No. T-1) A solution of Compound No. Q-2 (403 mg) in acetic acid (1.5 ml) was added with 20% sulfuric acid (1.0 ml). This reaction mixture was added dropwise with an aqueous solution (0.5 ml) of sodium nitrite (76 mg) over 10 minutes while keeping the temperature of the reaction mixture below 10°C, and further stirred for 5 minutes. This reaction solution was added to a solution of sodium acetate (328 mg) in acetic acid (3.5 ml) heated and stirred at 100°C beforehand, and further stirred for 10 minutes with heating. The reaction solution was poured into ice water (50 ml), and extracted with isopropyl ether (100 ml x 2). The organic layer was washed successively with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 10 : 1). The obtained substance was reacted with 2 N aqueous sodium hydroxide (500 u 1) and treated according to the procedure described in the synthesis method of Intermediate 9 to obtain the title compound (Compound No. T-1, 78 mg).

Example T-2] Synthesis of ethyl 3- [3-acetoxy-4-cyclopentyloxy-5- (naphthalen-2- yl) phenyl] propionate (Intermediate 58) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 13 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 9: 1), Compound No. B-114 (160 mg), 2-naphthaleneboronic acid (382 mg, Ald), 2 M aqueous sodium carbonate (0.7 ml) and (Ph3P) 4Pd (105 mg) were reacted and treated to obtain the title compound (Intermediate 58,152 mg).

Synthesis of 3- [4-cyclopentyloxy-3-hydroxy-5- (naphthalen-2-yl) phenyl] propionic acid (Compound No. T-2) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 2 hours, Intermediate 58 (146 mg) and 2 N aqueous sodium hydroxide (0.35 ml) were reacted and treated to obtain the title compound (Compound No. T-2,135 mg).

[Example T-31] Synthesis of ethyl 3- [4-cyclopentyloxy-3-methoxy-5- (naphthalen-2- yl) phenyl] propionate (Compound No. T-31) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 14 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 9 : 1), Compound No. A-25 (210 mg), 2-naphthaleneboronic acid (184 mg), 2 M aqueous sodium carbonate (0.5 ml) and (Ph3P) 4Pd (65.3 mg) were reacted and treated to obtain the title compound (Compound No. T-31, 181 mg).

[Example T-32] Synthesis of 3- [4-cyclopentyloxy-3-methoxy-5- (naphthalen-2-yl) phenyl] propionic acid (Compound No. T-32) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 2 hours, Compound No. T-31 (166 mg) and 2 N aqueous sodium hydroxide (0.45 ml) were reacted and treated to obtain the title compound (Compound No. T-32,135 mg).

[Example T-33] Synthesis of 4- (t-butyldimethylsilyloxy) -3- (lH-indol-5-yl)-5-methoxybenzaldehyde (Intermediate 59) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 12.5 hours, and the purification was performed by flash column chromatography (hexane: ethyl acetate = 7: 1), 5-indoleboronic acid (1.29 g), Intermediate 16 (1.75 g), 2 M aqueous sodium carbonate (4.8 ml) and (Ph3P) 4Pd (400 mg) were reacted and treated to obtain the title compound (Intermediate 59,910 mg).

Synthesis of ethyl 3- [4- (t-butyldimethylsilyloxy)-3- (lH-indol-5-yl)-5- methoxyphenyl] aerylate (Intermediate 60) According to the procedure described in the synthesis method of Intermediate 7 with the modifications that the reaction was carried out for 1.5 hours, and the purification was performed by flash column chromatography (hexane: ethyl acetate = 3: 1), Intermediate 59 (910 mg), ethyl diethylphosphonoacetate (500, l) and 60% sodium hydride (100 mg) were reacted and treated to obtain the title compound (Intermediate 60,945 mg).

Synthesis of ethyl 3- [4- (t-butyldimethylsilyloxy)-3-(lH-indol-5-yl)-5- methoxyphenyl] propionate (Intermediate 61) According to the procedure described in the synthesis method of Intermediate 8, Intermediate 60 (945 mg) and 10% palladium/carbon (95 mg) were reacted and treated under hydrogen gas atmosphere to obtain the title compound (Intermediate 61,940 mg).

Synthesis of ethyl 3-L4-hydroxy-3- (lH-indol-5-yl)-5-methoxyphenyl] propionate (Intermediate 62) According to the procedure described in the synthesis method of Intermediate 19 with the modifications that the reaction was carried out for 1.5 hours, and the purification was performed by flash column chromatography (hexane : ethyl acetate = 2: 1), Intermediate 61 (750 mg) and a 1 M solution of tetrabutylammonium fluoride in THF (5.0 ml) were reacted and treated to obtain the title compound (Intermediate 62,555 mg).

Synthesis of ethyl 3- [4-cyclopentyloxy-3- (lH-indol-5-yl)-5- methoxyphenyl] propionate (Compound No. T-33) According to the procedure described in the synthesis method of Compound No. A-6 with the modifications that the reaction was carried out for 16 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 7: 1), Intermediate 62 (340 mg), PhsP (1.31 g), cyclopentanol (450 A 1) and TMAD (860 mg) were reacted and treated to obtain the title compound (Compound No. T-33,376 mg).

[Example T-34] Synthesis of 3- [4-cyclopentyloxy-3- (lH-indol-5-yl)-5-methoxyphenyl] propionic acid (Compound No. T-34) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 2 hours, Compound No. T-33 (99 mg) and 2 N aqueous sodium hydroxide (500, u 1) were reacted and treated to obtain the title compound (Compound No. T-34, 76 mg).

[Examples T-1 to T-61] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-T-1 and Table T-2. Zx 0 Table-T-1 _ Exp. RxO Y Zx AR Syn method T-1 cPenMeO H OH 2-Nap T-1 5. 03 382 (M++1) T-2 cPenO H OH T-3 cPenO H OH 5-Ind T-2 C 366 (M'+1) T-4 cPenO H OH 1 Me-5-Ind Int73, T-2 T-5 cPenO H OH 5-1 T-2 T-6 cPenO H OH 1 T-2 C T-7 cHexO H OH 2-Nap T-1 T-8 cHexO H OH 1 Me-5-Ind T-1 T-9 cHexO H OH 1 T-10 2EtBuO H OH 2-Nap T-1 _ T-11 OH I Me-5-Ind T-1 T-12 2EtBuO H OH 1 T-1 T-13 iBuO H OH 2-Nap T-1 T-14 iBuO H OH 1 Me-5-Ind T-15 iBuO H OH 1 Me-5-ldz T-1 T-16 H OH 2-Nap T-1 T-17 1 H OH 1 Me-5-Ind T-1 C T-18 1 H OH 1 T-1 T-19 4CF3BnO H OH 2-Nap T-1 T-20 4CF3BnO H OH 1 Me-5-Ind T-1 T-21 4CF3BnO H OH T-22 2-IndanO H OH 2-Nap T-1 T-23 2-IndanO H OH 1 Me-5-Ind T-1 T-24 2-IndanO H OH T-1 A 3. 91 429 (M++l) T-25 2 (4FPh) EtO H OH 2-Nap T-1 T-26 2 (4FPh) EtO H OH 1Me-5-Ind T-27 2 (4FPh) EtO H OH 1Me-5-Idz T-1 T-28 2 H OH 2-Nap T-1 T-29 2 (4DMAPh) EtO H OH I T-30 2 H OH T-1 T-31 cPenO Et OMe 2-Nap T-31 T-32 cPenO H OMe 2-Nap T-32 T-33 cPenO Et OMe 5-Ind T-34 cPenO H OMe 5-Ind T-34 T-35 cPenO H OMe 1 Me-5-Ind T-33, 4. 72 394 (M++1) T-36 cPenO H OMe 5-1 T-32 T-37 cPenO H OMe 1 T-38 cHexO H OMe 2-Nap T-31, T-32 C T-39 cHexO H OMe 1 Me-5-Ind T-33, T-34 T-40 cHexO H OMe 1Me-5-Idz T-32 T-41 2EtBuO H OMe 2-Nap T-31, T-32 T-42 2EtBuO H OMe 1 Me-5-Ind T-33, T-34 T-43 2EtBuO H OMe 1 ARTable-T-2 T-44 iBuO H OMe 2-Nap T-31, T-32 T-45 iBuO H OMe 1 T-34 C 382 (M++1) T-46 iBuO H OMe 1 T-47 I H OMe 2-Nap T-31. T-48 1 H OMe 1 T-49 1 H OMe 1 T-32 C T-50 4CF3BnO H OMe 2-Nap T-31, T-32 T-51 4CF3BnO H OMe 1 T-34 T-52 4CF3BnO H OMe T-32 T-53 2-IndanO H OMe 2-Nap T-31, T-32 T-54 2-IndanO H OMe 1 T-34 T-55 2-IndanO H OMe T-32 C T-56 2 (4FPh) EtO H OMe 2-Nap T-31, T-57 2 (4FPh) EtO H OMe 1 T-34 C T-58 2 (4FPh) EtO H OMe 1Me-5-1H T-59 2 (4DMAPh) EtO H OMe 2-Nap T-31, T-32 C T-60 2 (4DMAPh) EtO H OMe 1Me-5-Ind T-61 2 H OMe 1 T-32 [Example tJ-1] Synthesis of 4-cyclohexylmethyloxy-3- (naphthalen-2-yl) phenylacetonitrile (Intermediate 63) A solution of Compound No. C-1 (172 mg) in dehydrated THF (5 ml) was added successively with trimethylsilylnitrile (133 u 1, TCI) under ice cooling and zinc iodide (16 mg, WAKO) under argon gas atmosphere, stirred for 15 minutes, then warmed to room temperature, and further stirred for 27 hours. The reaction mixture was added with ethyl acetate (90 ml), and washed successively with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride and saturated brine. The organic layer was dried, and then the solvent was evaporated under reduced pressure. A solution of the residue in anhydrous methylene chloride (5 ml) was added with triethylsilane (240/ 1, TCI) under ice cooling and boron trifluoride diethyl ether complex (366 1, TCI) under argon gas atmosphere, warmed to room temperature, and stirred for 3.5 hours. The reaction mixture was poured into ice water (50 ml), and extracted with ethyl acetate (90 MI).

The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 10: 1) to obtain the title compound (Intermediate 63,116 mg).

Synthesis of 4-cyclohexylmethyloxy-3- (naphthalen-2-yl) phenylacetic acid (Compound No. U-1) According to the procedure described in the synthesis method of Intermediate 9 with the modifications that the reaction was carried out for 24 hours under reflux by heating, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 2: 1), Intermediate 63 (110 mg) and 5 N aqueous sodium hydroxide (900, it 1) were reacted and treated to obtain the title compound (Compound No. U-1, 62 mg).

[Example U-10] Synthesis of methyl 4- [4-cyclopentylmethyloxy-3- (nap hthalen-2-yl) phenyl] butyrate (Compound No. U-10) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 18 hours, and the purification was performed by column chromatography (Quad, hexane : isopropyl ether = 8: 1), Compound No. F-1 (355 mg), 2-naphthaleneboronic acid (344 mg), 2 M aqueous sodium carbonate (2.1 ml) and (Ph3P) 4Pd (115 mg) were reacted and treated to obtain the title compound (Compound No. U-10, 392 mg).

[Example U-11] Synthesis of 4- [4-cyclopentylmethyloxy-3- (naphthalen-2-yl) phenyl] butyric acid (Compound No. U-11) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 3.5 hours, Compound No. U-10 (380 mg) and 2 N aqueous sodium hydroxide (1.0 ml) were reacted and treated to obtain the title compound (Compound No. U-11, 342 mg).

Examples U-1 to U-18] Typical examples of the compounds of the present invention that can be obtained by reacting and treating corresponding starting compounds using any of the methods described in the present specification including the examples described above are shown in Table-U-1. Z Rx-O< srs Table _ Exp. RxO Y Zx n AR Syn LCMS method Mass U-1 cHexMeO H H 1 2-Nap U-1 C U-2 cHexMeO H H U-1 U-3 cHexMeO H H 1 iMe-5-ldz U-4 cPenMeO H H 2-Nap Int63, U-1 C U-5 cPenMeO H H 1 U-1 U-6 cPenO H H 1 2-Nap Int63, U-1 U-7 cPenO H H 1 1 U-1 C U-8 2 (4FPh) EtO H H 1 2-Nap Int63. U-1 U-9 2 (4FPh) EtO H H 1 1 U-1 U-10 cPenMeO Me H 3 2-Nap U-10 C U-11 H 3 2-Nap U-11 U-12 H H 3 1 U-13 cPenO H 3 2-Na U-14 H H 3 1Me-5-Ind U-10, U-15 cHexO H H 3 2-Nap U-10, U-11 U-16 cHexO H H 3 1 U-17 2 (4FPh) EtO H H U-18 2 (4FPh) Et0 (CH2kCOOYExample V-1] Synthesis of ethyl 3- [4-cyclohexylmethyloxy-3-(naphthalen-1-yl) phenyl] acrylate (Intermediate 64) According to the procedure described in the synthesis method of Intermediate 7 provided that the reaction was carried out for 1 hour, Compound No.

C-2 (361 mg), ethyl diethylphosphonoacetate (240, u 1), 60% sodium hydride (69 mg) were reacted and treated to obtain the title compound (Intermediate 64,377 mg).

Synthesis of ethyl 3- [4-cyclohexylmethyloxy-3-(naphthalen-l-yl) phenyl] propionate (Compound No. V-1) According to the procedure described in the synthesis method of Intermediate 8 with the modifications that the reaction was carried out for 1.5 hours, and the purification was performed by flash column chromatography (hexane : ethyl acetate = 10 : 1), Intermediate 64 (361 mg) and 10% palladium/carbon (49 mg) were reacted under hydrogen atmosphere and treated to obtain the title compound (Compound No. V-1, 344 mg).

[Example V-2] Synthesis of 3- [4-cyclohexylmethyloxy- 3- (naphthalen-I-yl) p henyllp rop ionic acid (Compound No. V-2) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 1.5 hours, Compound No. V-1 (332 mg) and 2 N aqueous sodium hydroxide (900 A 1) were reacted and treated to obtain the title compound (Compound No. V-2, 295 mg).

[Example V-3] Synthesis of methyl 3- [4-cyclopentylmethyloxy-3- (6-hydroxynaphthalen-2- yl) phenyl] propionate (Compound No. V-3) A solution of 2-bromo-6-hydroxynaphthalene (243 mg, TCI) in anhydrous THF (10 ml) was cooled to-78°C, added dropwise with a 1.6 M solution of n- butyllithium in hexane (1.18 ml) over 20 minutes under argon gas atmosphere, and stirred for 30 minutes. The reaction mixture was added dropwise with (iPrO) 3B (1.73 ml) over 10 minutes, stirred for 30 minutes, then warmed to room temperature, and further stirred for 2 hours. The reaction mixture was added with 0.5 M aqueous sulfuric acid (2 ml), and extracted with diethyl ether (40 ml x 3).

The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure to obtain crude 6-hydroxy-2- naphthaleneboronic acid (378 mg). A solution of this substance in ethanol (1 ml), Compound No. A-1 (230 mg), and 2 M aqueous sodium carbonate (2.4 ml) were added with toluene (3 ml) and (Ph3P) 4Pd (115 mg) and stirred at 100°C for 13 hours.

The reaction mixture was added with ethyl acetate (100 ml), and washed successively with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride and saturated brine. The organic layer was dried, and then the solvent was evaporated under reduced pressure. The residue was purified by flash column chromatography (hexane : ethyl acetate = 6: 1) to obtain the title compound (Compound No. V-3, 270 mg).

[Example V-41 Synthesis of 3- [4-cyclopentylmethyloxy-3- (6-hydroxynaphthalen-2- yl) phenyl] propionic acid (Compound No. V-4) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 14 hours, Compound No. V-3 (149 mg) and 2 N aqueous sodium hydroxide (370 u 1) were reacted and treated to obtain the title compound (Compound No. V 4, 117 mg).

[Example V-5] Synthesis of methyl 3- [4-cyclopentylmethyloxy-3- (5-hydroxynaphthalen-2- yl) phenyl] propionate (Compound No. V-5) 2-Amino-5-hydroxynaphthalene (4.80 g, TCI) was dissolved in 6 N hydrochloric acid (300 ml), added dropwise with an aqueous solution (22.5 ml) of sodium nitrite (2.25 g) over 30 minutes under ice cooling, and stirred for 30 minutes. The reaction mixture was added dropwise with an aqueous solution (75 ml) of potassium iodide (9.90 g, WAKO), stirred for 30 minutes, then warmed to room temperature, and further stirred for 3.5 hours. The reaction mixture was neutralized with aqueous ammonia, and then filtered through a Celite layer. The filtrate was added with ethyl acetate (90 ml x 2) for extraction. The organic layer was washed successively with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride and saturated brine, and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 10 : 1) to obtain l-hydroxy-6- iodonaphthalene (1.48 g). A solution of this substance (539 mg) in anhydrous THF (10 ml) was added with 60% sodium hydride (171 mg) under ice cooling, and stirred for 1 hour. The reaction mixture was cooled to-78°C under argon gas atmosphere, added dropwise with a 1.6 M solution of n-butyllithium in hexane (3.75 ml) over 10 minutes, and stirred for 30 minutes. The reaction mixture was added dropwise with (iPrO) 3B (1.16 ml) over 10 minutes, stirred for 30 minutes, then warmed to room temperature, and further stirred for 3 hours. The reaction mixture was added with water (3 ml) and 0.5 M aqueous sulfuric acid (7 ml), and extracted with diethyl ether (100 ml x 3). The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure to obtain crude 7-hydroxy-2-naphthaleneboronic acid. A solution of this substance in ethanol (1 ml), Compound No. A-1 (350 mg), 2 M aqueous sodium carbonate (2.4 ml) and (Ph3P) 4Pd (116 mg) were reacted and treated according to the procedure described in the synthesis method of Compound No. V-3 with the modifications that the reaction was carried out for 14 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 6: 1) to obtain the title compound (Compound No. V 5, 388 mg).

[Example V-6] Synthesis of 3-14-cyclopentylmethyloxy-3- (5-hydroxynaphthalen-2- yl) phenyl] propionic acid (Compound No. V-6) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 12 hours, Compound No. V-5 (355 mg) and 2 N aqueous sodium hydroxide (1. 75 ml) were reacted and treated to obtain the title compound (Compound No. V-6, 158 mg).

[Example V-7] Synthesis of methyl 3- [4-cyclopentylmethyloxy-3- (7-hydroxynaphthalen-2- yl) phenyl] propionate (Compound No. V-7) According to the procedure described in the synthesis method of Compound No. V-5 with the modifications that the reaction was carried out for 4 hours, and the purification was performed by flash column chromatography (hexane : ethyl acetate = 6 : 1), crude 7-hydroxy-2-naphthaleneboronic acid prepared from 2-bromo- 7-hydroxynaphthalene (559 mg, MAYB), a 1.6M solution of n-butyllithium in hexane (3.91 ml) and (iPrO) sB (1.16 ml), Compound No. A-1 (386 mg), 2 M aqueous sodium carbonate (4.0 ml) and (Ph3P) 4Pd (195 mg) were reacted and treated to obtain the title compound (Compound No. V-7,460 mg).

[Example V-8] Synthesis of 3- [4-cyclopentylmethyloxy-3- (7-hydroxynaphthalen-2- yl) phenyl] propionic acid (Compound No. V-8) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 27 hours, Compound No. V-7 (176 mg) and 2 N aqueous sodium hydroxide (436, u 1) were reacted and treated to obtain the title compound (Compound No. V-8, 109 mg).

[Example V-11] Synthesis of methyl 3- 4-cyclohexylmethyloxy-3- [6- (N, N- dimethylcarbamoylmethyloxy) naphthalen-2-yl] phenyllpropionate (Compound No. V- 11) A solution of Compound No. V-3 (185 mg) in DMF (5 ml) was added with potassium carbonate (274 mg), and 2-chloro-N, N-dimethylacetamide (411 1, KANTO), and stirred at 50°C for 18 hours. The reaction mixture was added with ethyl acetate (90 ml), and washed with saturated brine. The organic layer was dried, and then the solvent was evaporated under reduced pressure. The residue was purified by PTLC (chloroform : methanol = 10: 1) to obtain the title compound (Compound No. V-11, 213 mg).

[Example V-12] Synthesis of 3-{4-cyclohexylmethyloxy-3- [6- (N, N- dimethylcarbamoylmethyloxy) naphthalen-2-yl] phenyl} propionic acid (Compound No.

V-10) According to the procedure described in the synthesis method of Intermediate 9 with the modifications that the reaction was carried out at room temperature for 18 hours and at 60°C for 8 hours, and the purification was performed by PTLC (chloroform : methanol = 10: 1), Compound No. V-11 (213 mg) and 2 N aqueous sodium hydroxide (420, u l) were reacted and treated to obtain the title compound (Compound No. V 12, 115 mg).

[Example V-13] Synthesis of methyl 3- [3- (6-aminonaphthalen-2-yl)-4- cyclopentylmethyloxyphenyl] propionate (Compound No. V-13) According to a known method described in a publication (Anderson, L. C. et al. , J. Am. Chem. Soc, 1943, vol. 65, p. 241), a solution of 2-amino-6- bromonaphthalene (223 mg) obtainable from commercially available 2-brom-6- hydroxynaphthalene (TCI) in anhydrous THF (10 ml) was added with 30% potassium hydride (191 mg, Ald) under ice cooling, and stirred for 1 hour. The reaction mixture was cooled to'78°C under argon gas atmosphere, added dropwise with a 1.7 M solution of t-butyllithium in pentane (1.88 ml) over 10 minutes, and stirred for 30 minutes. This reaction mixture was added dropwise with (iPrO) 3B (0.92 ml) over 10 minutes, stirred for 30 minutes, then warmed to room temperature, and further stirred for 3 hours. The reaction mixture was added with water (3 ml) and 0.5 M aqueous sulfuric acid (4 ml), and extracted with diethyl ether (100 ml x 3). The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure to obtain crude 6- amino-2-naphthaleneboronic acid (402 mg). A solution of this substance in ethanol (0.5 ml), Compound No. A-1 (119 mg), 2 M aqueous sodium carbonate (1.5 ml) and (Ph3P) 4Pd (61 mg) were reacted and treated according to the procedure described in the synthesis method of Compound No. V 3 with the modifications that the reaction was carried out for 13 hours, and the purification was performed by flash column chromatography (hexane : ethyl acetate = 4: 1) to obtain the title compound (Compound No. V-13,129 mg).

Example V-14] Synthesis of 3- [3- (6-aminonaphthalen-2-yl)-4-cyclopentylmethyloxyphenyl] propionic acid (Compound No. V-14) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 14 hours, Compound No. V-13 (120 mg) and 2 N aqueous sodium hydroxide (1.75 ml) were reacted and treated to obtain the title compound (Compound No. V-14, 89 mg).

[Example V-16] Synthesis of methyl 3- [3- ({6- [2- (acetyloxy) acetylamino) naphthalen-2-yl}-4- cyclopentylmethyloxyphenyl) propionate (Intermediate 65) A solution of Compound No. V-13 (151 mg) in dichloromethane (4 ml) was added with N-methylmorpholine (50 g 1), and then added with acetyloxyacetyl chloride (48.3 u 1) under ice cooling. The reaction mixture was stirred for 10 minutes, then warmed to room temperature, and further stirred for 4 hours. The reaction mixture was poured into aqueous sodium hydrogencarbonate (100 ml), and ethyl acetate (150 ml) was added for extraction. The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by PTLC (hexane : ethyl acetate = 1: 1) to obtain the title compound (Intermediate 88,136 mg).

Synthesis of 3- (4-cyclopentylmethyloxy-3-{6- [2- (hydroxyacetyl) amino] naphthalen-2- yl} phenyl) propionic acid (Compound No. V-16) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out at room temperature for 5 hours and at 60°C for 1 hour, Intermediate 65 (135 mg) and 2 N aqueous sodium hydroxide (1.12 ml) were reacted and treated to obtain the title compound (Compound No. V-16,102 mg).

(Example V-18] Synthesis of methyl 3- [4-cyclopentylmethyloxy-3- (6- methylsulfonylaminonaphthalen-2-yl) phenyl] propionate (Compound No. V-18) A solution of Compound No. V-13 (149.1 mg) in 1,2-dichloroethane (5 ml) was added successively with pyridine (500, u 1) and methanesulfonyl chloride (62 , u 1) under ice cooling, stirred for 1.5 hours, then warmed to room temperature, and stirred for 12 hours. The reaction mixture was added with water (30 ml) and ethyl acetate (90 ml) for extraction. The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by PTLC (hexane : ethyl acetate = 2: 1) to obtain the title compound (Compound No. V-18, 126 mg).

[Example V-19] Synthesis of 3- [4-cyclopentylmethyloxy-3- (6-methylsulfonylaminonaphthalen-2- yl) phenyl] propionic acid (Compound No. V-19) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out at room temperature for 3 hours and at 60°C for 1 hour, Compound No. V-18 (129 mg) and 2 N aqueous sodium hydroxide (535 A 1) were reacted and treated to obtain the title compound (Compound No. V-19,98 mg).

[Example V-20] Synthesis of methyl 3- {4-cyclopentylmethyloxy-3- [6- (N, N- dimethylsulfamoylamino) naphthalen-2-yl] phenyl} propionate (Compound No. V-20) A solution of Compound No. V-13 (165 mg) in pyridine (5 ml) was added successively with 4-dimethylaminopyridine (104 mg, TCI) and dimethylsulfamoyl chloride (520 u 1, TCI), stirred for 5 days, and then further stirred at 50°C for 4 hours. The reaction mixture was added with water (30 ml) and ethyl acetate (90 ml) ) for extraction. The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane : ethyl acetate = 6 : 1) to obtain the title compound (Compound No. V-20, 125 mg).

[Example V-21] Synthesis of 3-f4-cyclopentylmethyloxy-3- [6- (N, N- dimethylsulfamoylamino) naphthalen-2-yl] phenyl} propionic acid (Compound No. V- 21) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 1.5 hours, Compound No. V-20 (118 mg) and 2 N aqueous sodium hydroxide (460 u 1) were reacted and treated to obtain the title compound (Compound No. V 21, 87 mg).

[Example V-22] Synthesis of 2-bromo-6-sulfamoylaminonaphthalene (Intermediate 66) A solution of chlorosulfonyl isoeyanate (870, u 1, WAKO) in benzene (10 ml) was added dropwise with formic acid (377 u 1, WAKO) under ice cooling, warmed to room temperature, stirred and for 19. 5 hours, then warmed to 40°C, and further stirred for 4 hours. The reaction mixture was added dropwise with a solution of 2- amino-6-bromonaphthalene (443 mg) in benzene (5 ml) under ice cooling, warmed to room temperature, and stirred 21.5 hours. The reaction mixture was filtered to obtain solid, and the solid was added with ethyl acetate, mixed and filtered again.

The solvent of the filtrate was evaporated under reduced pressure. The residue was purified by column chromatography (Quad, hexane: ethyl acetate = 2 : 1) to obtain the title compound (Intermediate 66,158 mg).

Synthesis of methyl 3- [4-cyclopentylmethyloxy-3- (6-sulfamoylaminonaphthalen-2- yl) phenyl propionate (Compound No. V-22) According to a procedure described in literature (Miyaura, N. et al., Tetrahedron. Lett. , 1997, p. 3447), Compound No. A-1 (209 mg), bis (pinacolate) diboron (177 mg, Ald), [1, 1'- bis (diphenylphosphono) ferrocene] palladium (II) dichloride (hereinafter abbreviated as"PdCl2 (dppf)", 28 mg, TCI) and potassium acetate (182.3 mg, Ald) were added to DMF (6 ml), and heated to 80°C with stirring under argon gas atmosphere for 5 hours. The reaction mixture was cooled to room temperature, then added with Intermediate 91 (130 mg), PdCl2 (dppf) (30 mg) and 2 M aqueous sodium carbonate (0.9 ml), and heated to 80°C for 21 hours with stirring under argon gas atmosphere.

The reaction mixture was added with ethyl acetate (100 ml), washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure.

The residue was purified by column chromatography (Quad, hexane : ethyl acetate = 3 : 1) to obtain the title compound (Compound No. V-22, 46 mg).

[Example V-23] Synthesis of 3- [4-cyclopentylmethyloxy-3- (6-sulfamoylaminonaphthalen-2- yl) phenyl] propionic acid (Compound No. V-23) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 24 hours, Compound No. V-22 (41 mg) and 2 N aqueous sodium hydroxide (340, u 1) were reacted and treated to obtain the title compound (Compound No. V-23, 22 mg).

[Example V-27] Synthesis of methyl 3- [4-cyclopentyloxy-3- (lH-indol-5-yl) phenyl] propionate (Compound No. V-27) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out at 80°C for 5 hours, and the purification was performed by flash column chromatography (hexane : ethyl acetate = 5 : 1), Compound No. A-5 (367 mg), 5-indoleboronic acid (310 mg, Frontier), 2 M aqueous sodium carbonate (0.9 ml) and (PhsP) 4Pd (132 mg) were reacted and treated to obtain the title compound (Compound No. V 27, 340 mg).

Example V-28] Synthesis of 3- [4-cyclopentyloxy-3- (lH-indol-5-yl) phenyl] propionic acid (Compound No. V-28) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 2 hours, Compound No. V-27 (330 mg) and 2 N aqueous sodium hydroxide (1.40 ml) were reacted and treated to obtain the title compound (Compound No. V-28, 310 mg).

[Example V-29] Synthesis of methyl 3- [4-cyclopentyloxy-3- (1-methyl-lH-indol-5- yl) phenyl] propionate (Compound No. V-29) A solution of Compound No. V-27 (123 mg) in DMF (5 ml) was added with 60% sodium hydride (19 mg) under ice cooling, and stirred for 10 minutes. The reaction mixture was added dropwise with methyl iodide (100 u 1), stirred for 10 minutes, then warmed to room temperature, and further stirred for 1 hour. The reaction mixture was poured into ice water, and ethyl acetate (100 ml) was added for extraction. The organic layer was successively washed with saturated aqueous sodium hydrogencarbonate, saturated aqueous ammonium chloride, and saturated brine and dried, and then the solvent was evaporated under reduced pressure.

The residue was purified by flash column chromatography (hexane : ethyl acetate = 8 : 1) to obtain the title compound (Compound No. V-29, 126 mg).

[Example V-30] Synthesis of 3- [4-cyclopentyloxy-3- (1-methyl-lH-indol-5-yl) phenyl] propionic acid (Compound No. V-30) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 1 hour, Compound No.

V-29 (123 mg) and 2 N aqueous sodium hydroxide (330 g 1) were reacted and treated to obtain the title compound (Compound No. V-30, 110 mg).

[Example V-31] Synthesis of methyl 3- [4-cyclopentylmethyloxy-3- (lH-indol-4-yl) phenyl propionate (Compound No. V-31) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 21 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 6: 1), Compound No. A-1 (200 mg), 4-indoleboronic acid (170 mg) obtainable from 4-bromoindole (TCI) according to a known method described in a publication (Doll, M. et al. , J. Org. Chem, 1999, vol. 64, p. 1372), 2 M aqueous sodium carbonate (550, u 1) and (Ph3P) 4Pd (60 mg) were reacted and treated to obtain the title compound (Compound No. V-31,214 mg).

[Example V-32] Synthesis of 3- [4-cyclopentylmethyloxy-3- (lH-indol-4-yl) phenyl] propionic acid (Compound No. V-32) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 1 hour, Compound No.

V-31 (210 mg) and 2 N aqueous sodium hydroxide (0.60 ml) were reacted and treated to obtain the title compound (Compound No. V 32, 173 mg).

[Example V-33] Synthesis of 4-bromo-1-methyl-lH-indole (Intermediate 67) According to the procedure described in the synthesis method of Compound No. V-29 with the modifications that the reaction was carried out for 30 minutes, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 10: 1), 4-bromoindole (5 g), 60% sodium hydride (1.14 g) and methyl iodide (3.18 ml, TCI) were reacted and treated to obtain the title compound (Intermediate 67,4. 95 g).

Synthesis of 1-methyl-lH-indole-4-boronic acid (Intermediate 68) A solution of Intermediate 67 (4.90 g) in anhydrous THF (30 ml) was cooled to-78°C under argon gas atmosphere, then added dropwise with a 1.62 M solution of t-butyllithium in pentane (28. 8 ml) over 30 minutes, and stirred for 30 minutes.

This reaction mixture was added dropwise with (iPrO) 3B (10.77 ml) over 10 minutes, stirred for 1 hour, then warmed to room temperature, and further stirred for 2.5 hours. The reaction mixture was poured into 1.2 N aqueous phosphoric acid (250 ml) containing ice, and extracted with diethyl ether (200 ml x 3). The organic layer was extracted with 0.4 N aqueous sodium hydroxide (150 ml x 3), and the aqueous layer was made acidic with 5 N hydrochloric acid under ice cooling, and extracted with diethyl ether (200 ml x 3) again. The organic layer was washed with saturated brine and dried, and then the solvent was evaporated under reduced pressure. The residue was washed with hexane to obtain the title compound (Intermediate 68,3. 17 g).

Synthesis of methyl 3- [4-cyclopentylmethyloxy-3- (1-methyl-lH-indol-4- yl) phenyl] propionate (Compound No. V-33) According to the procedure described in the synthesis method of Compound No. C-1 with the modifications that the reaction was carried out for 18 hours, and the purification was performed by column chromatography (Quad, hexane : ethyl acetate = 9: 1), Compound No. A-1 (200 mg), Intermediate 68 (185 mg), 2 M aqueous sodium carbonate (550, u 1) and (Ph3P) 4Pd (60 mg) were reacted and treated to obtain the title compound (Compound No. V-33, 208 mg).

[Example V-34] Synthesis of 3- [4-cyclopentylmethyloxy-3- (1-methyl-lH-indol-4-yl) pheny ] propionic acid (Compound No. V-34) According to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 3 hours, Compound No. V-33 (200 mg) and 2 N aqueous sodium hydroxide (0.60 ml) were reacted and treated to obtain the title compound (Compound No. V-34, 182 mg).

Example V-43] Synthesis of 3-{4-cyclopentylmethyloxy-3- [1-(2-hydroxyethyl)-lH-indol-5- yl] phenyl} propionic acid (Compound No. V-43) According to the procedure described in the synthesis method of Compound No. V-29 with the modifications that the reaction was carried out for 1.5 hours, and the purification was performed by column chromatography (Quad, hexane: ethyl acetate = 8 : 1), Compound No. V-27 (144mg), 60% sodium hydride (38 mg) and ethyl bromoacetate (160, u 1, TCI) were reacted and treated to obtain an oily substance.

This substance was reacted with 2 N aqueous sodium hydroxide (300 job 1) and treated according to the procedure described in the synthesis method of Intermediate 9 provided that the reaction was carried out for 1 hour to obtain the title c