发明名称 TRI-SUBSTITUTED PHENYL DERIVATIVES USEFUL AS PDE IV INHIBITORS
摘要 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 a -XR, ¢where R is and optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl group!, -C(R11)=C(R1)(R2) or or ¢-CH(R11)!nCH(R1)(R2) group where R11 is a hydrogen or a fluorine atom or a methyl group, and R1 and R2, which may be the same or different, is each a hydrogen or fluorine atom or an optionally substituted alkyl, alkenyl, alkynyl, alkoxy, alkylthio, -CO2R8, ¢where R8 is a hydrogen atom or an optionally substituted alkyl, aralkyl, or aryl group!, CONR9R10 ¢where R9 and R10, which may be the same or different are as defined for R8!, -CSNR9R10, -CN or -NO2 group, or R1 and R2 together with the C atom to which they are attached are linked to form an optionally substituted cycloalkyl or cycloalkenyl group and n is zero or the integer 1; Z is a group (A), or (B) wherein R3 is a hydrogen or a fluorine atom, an optionally substituted straight or branched alkyl group, or a hydroxyl group; R4 is a hydrogen atom or group -(CH2)tAr or -(CH2)t-Ar-(L1)n-Ar'; R5 is a -(CH2)tAr' or -(CH2)t-Ar-(L1)n-Ar' group; R6 is a hydrogen or a fluorine atom, or an optionally substituted alkyl group; R7 is a hydrogen or a fluorine atom, an optionally substituted straight or branched alkyl group or an ORc group where Rc is 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 desease such as asthma where an unwanted inflammatory response or muscular spasm is present.
申请公布号 CA2192643(A1) 申请公布日期 1995.12.28
申请号 CA19952192643 申请日期 1995.06.21
申请人 CELLTECH THERAPEUTICS LIMITED 发明人 WARRELLOW, GRAHAM JOHN;ALEXANDER, RIKKI PETER
分类号 A61K31/395;C07D213/24;C07D213/89;C07D401/00;C07D405/00;C07D409/00;C07D411/00;C07D413/00;C07D417/00;C07D471/04;(IPC1-7):C07D213/24 主分类号 A61K31/395
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