Title:
置換8-アリールキノリン系ホスホジエステラーゼ-4阻害薬
Document Type and Number:
Japanese Patent JP3782011
Kind Code:
B2
Abstract:
Novel substituted 8-arylquinolines represented by Formula (I), or a pharmaceutically acceptable salt thereof, wherein S1, S2 and S3 are independently H, -OH; halogen, -C1-C6alkyl, -NO2, -CN, or -C1-C6alkoxy, wherein the alkyl and alkoxy groups are optionally substituted with 1-5 substituents; wherein each substituent is independently a halogen or OH; R1 is a H, OH, halogen, carbonyl, or -C1-C6alkyl, -cycloC3-C6alkyl, -C1-C6alkenyl, -C1-C6alkoxy, aryl, heteroaryl, -CN, -heterocycloC3-C6alkyl, -amino, -C1-C6alkylamino, -(C1-C6alkyl)(C1-C6alkyl)amino, -C1-C6alkyl(oxy)C1-C6alkyl, -C(O)NH(aryl), -C(O)NH(heteroaryl), -SOnNH(aryl), -SOnNH(heteroaryl), -SOnNH(C1-C6alkyl), -C(O)N(C0-C6alkyl) (C0-C6alkyl), -NH-SOn-(C1-C6alkyl), -SOn-(C1-C6alkyl), -(C1-C6alkyl)-O-C(CN)-dialkylamino, or -(C1-C6alkyl)-SOn-(C1-C6alkal) group, wherein any of the groups is optionally substituted with 1-5 substituents; wherein each substituent is independently a halogen, -OH, -CN, -C1-C6alkyl, -cycloC3-C6alkyl, -C(O)(heterocycloC3-C6alkyl), -C(O)-O-(C0-C6alkyl), -C(O)-aryloxy, -C1-C6alkoxy, -(C0-C6alkyl)(C0-C6alkyl)amino, cycloalkyloxy, acyl, acyloxy, -cycloC3-C6alkyl, heterocycloC3-C6alkyl, aryl, heteroaryl, carbonyl, carbamoyl, or -SOn-(C1-C6alkyl); A is CH, C-ester, or C-R4; R2 and R3 independently is an aryl, heteroaryl, H, halogen, -CN, -C1-C6alkyl, heterocycloC3-6alkyl, -C1-C6alkoxy, carbonyl, carbamoyl, -C(O)OH, -C1-C6alkyl)-SOn-(C1-C6alkyl), -C(O)N(C0-C6alkyl)(C0-C6alkyl), or -C1-C6alkylacylamino group, wherein any of the groups is optionally substituted with 1-5 substituents, wherein each substituent is independently an aryl, heteroaryl, halogen, -NO2, -C(O)OH, carbonyl, -CN, -C1-C6alkyl, -SOn-(C1-C6alkyl), -SOn-(aryl), aryloxy, -heteroaryloxy, C1-C6alkoxy, N-oxide, -C(O)-heterocycloC3-C6alkyl, -NH-cycloC3-C6alkyl, amino, -OH, or -(C0-C6alkyl)(C0-C6alkyl)amino, -C(O)-N(C0-C6alkyl)(C0-C6alkyl) substituent group, wherein each substituent group independently is optionally substituted with -OH, C1-C6alkoxy, -C1-C6alkyl, -cycloC3-C6alkyl, aryloxy, -C(O)OH, -C(O)O(C1-C6alkyl), halogen, -NO2, -CN, -SOn-(C1-C6alkyl), or -C(O)-N(C0-C6alkyl)(C0-C6alkyl); one of R2 and R3 must be an aryl or heteroaryl, optionally substituted; when R2 and R3 are both an aryl or heteroaryl, then R2 and R3 may be optionally connected by a thio, oxy, or (C1-C4alkyl) bridge to form a fused three ring system; are PDE4 inhibitors.
Inventors:
Decienne, Douni
Doyub, Daniel
Gear Run, Michel
Girard, Eve
Racombe, Patrick
McDonald's, Dwight
Masturbation, Anthony
Perrier, Helene
Doyub, Daniel
Gear Run, Michel
Girard, Eve
Racombe, Patrick
McDonald's, Dwight
Masturbation, Anthony
Perrier, Helene
Application Number:
JP2001547062A
Publication Date:
June 07, 2006
Filing Date:
December 20, 2000
Export Citation:
Assignee:
Merck Frost Canada and Company
International Classes:
C07D215/12; A61K31/47; A61K31/4709; A61K45/00; A61P1/04; A61P7/12; A61P9/00; A61P11/00; A61P11/06; A61P11/16; A61P13/12; A61P17/00; A61P17/04; A61P17/06; A61P19/02; A61P19/10; A61P37/08; C07D215/14; C07D401/10; C07D401/14; C07D405/12; C07D409/10; C07D413/10; C07D413/14; C07D417/10; C07D417/12; C07D417/14
Domestic Patent References:
| JP8511238A |
Foreign References:
| WO1999037622A1 |
Other References:
松本光雄,薬剤学マニュアル,株式会社 南山堂,1989年,p.118
Attorney, Agent or Firm:
Yoshio Kawaguchi
Mitsuru Inoue
Akio Ichiiri
Katsuma Osaki
Takamasa Soma
Mitsuru Inoue
Akio Ichiiri
Katsuma Osaki
Takamasa Soma