发明名称 TRI-SUBSTITUTED PHENYL DERIVATIVES USEFUL AS PDE IV INHIBITORS
摘要 Compounds of general formula (1) are described, formula 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) wherein Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; Z1 is 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-, -CC-, -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.
申请公布号 CA2192645(A1) 申请公布日期 1995.12.28
申请号 CA19952192645 申请日期 1995.06.21
申请人 CELLTECH THERAPEUTICS LIMITED 发明人 WARRELLOW, GRAHAM JOHN;BOYD, EWAN CAMPBELL;ALEXANDER, RIKKI PETER
分类号 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;C07D213/30;C07D213/89;C07D401/00;C07D405/00;C07D409/00;C07D409/12;C07D411/00;C07D413/00;C07D417/00;C07D471/04;C07D521/00;(IPC1-7):C07D213/30 主分类号 A61K31/395
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