Title:
PDE IV インヒビターとして有用なトリ置換フェニル誘導体
Document Type and Number:
Japanese Patent JP3898757
Kind Code:
B2
Abstract:
Compounds of general formula (1) are described:wherein=W- is (1) =C(Y)- where Y is a halogen atom, or an alkyl or -XRa group where X is -O-, -S(O)m- [where m is zero or an integer of value 1 or 2], or -N(Rb)- [where Rb is a hydrogen atom or an optionally substituted alkyl group] and Ra is a hydrogen atom or an optionally substituted alkyl group or, (2) =N-;L is (1) a -C(R)=C(R1)(R2) or [-CH(R)]nCH(R1)(R2) group; is (2) a -(Xa)nAlk'Ar', or Alk'XaAr' group; or is (3) XaR1;Z is a group (A), (B), (C) or (D): whereinAr is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms;Z1is a group -NR12C(O)- [where R12 is a hydrogen atom or an optionally substituted alkyl or (Alk)tAr group], -C(O)NR12-, -NR12C(S)-, -C(S)NR12-, -C=C-, -NR12SO2-, or -SO2NR12-;Alk is an optionally substituted straight or branched alkyl chain optionally interrupted by an atom or group X;t is zero or an integer of value 1, 2 or 3;R3 is a hydrogen or a fluorine atom or an optionally substituted straight or branched alkyl group or an OR11 group [where R11 is a hydrogen atom or an optionally substituted alkyl, alkenyl, alkoxyalkyl, alkanoyl, formyl, carboxamido or thiocarboxamido group];R4 is a hydrogen atom or an optionally substituted alkyl, -CO2R8, -CSNR9R10, -CN, -CH2CN, or -(CH2)tAr group where t is zero or an integer of value 1, 2 or 3 and Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; provided that when L is a group of type (2) or (3) above then Z is a group of type (A) or type (B) in which R4 is a -(CH2)tAr group;R5 is a group -(CH2)tAr;R6 is a hydrogen or a fluorine atom, or an optionally substituted alkyl or -CO2R8, -CONR9R10, -CSNR9R10, -CN or -CH2CN group;R7 is a hydrogen or a fluorine atom, an optionally substituted straight or branched alkyl group, or an ORc group where Rc is a hydrogen atom or an optionally substituted alkyl or alkenyl group, alkoxyalkyl, alkanoyl, formyl, carboxamido or thiocarboxamido group; and the salts, solvates, hydrates, prodrugs and N-oxides thereof.Compounds according to the invention are phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of disease such as asthma where unwanted inflammatory response or muscular spasm is present.
Inventors:
Valero, Graham, John
Boyd, Ewan, Campbell
Alexander, Ricky, Peter
Boyd, Ewan, Campbell
Alexander, Ricky, Peter
Application Number:
JP50184596A
Publication Date:
March 28, 2007
Filing Date:
June 21, 1995
Export Citation:
Assignee:
Celtec Therapeutics Limited
International Classes:
C07D213/30; A61K31/395; A61K31/44; A61K31/4433; A61P43/00; C07C1/26; C07C1/32; C07C15/02; C07C15/12; C07C17/263; C07C25/02; C07C25/18; C07C43/20; C07C49/753; C07C57/30; C07C59/64; C07C69/76; C07C291/04; C07C311/15; C07D213/89; C07D401/00; C07D405/00; C07D409/00; C07D409/12; C07D411/00; C07D413/00; C07D417/00; C07D471/04; C07D521/00
Domestic Patent References:
| JP7504687A | ||||
| JP9506893A | ||||
| JP7504442A | ||||
| JP9510691A |
Foreign References:
| WO1994012461A1 | ||||
| WO1994010118A1 |
Other References:
T.Ramalingam, A.A.Deshmukh, P.B.Sattur, Synthesis and Pharmacology of 2,5-Disubstituted 1,3,4-Oxadiazoles, J.Indian Chem.Soc., 1981年3月,vol.LVIII, p.269-271
Attorney, Agent or Firm:
Shunichiro Suzuki