发明名称 Pyrrolyl- and imidazolyl-acid amide derivatives useful as inhibitors of PDE4 isozymes
摘要 Compounds useful as inhibitors of PDE4 in the treatment of diseases regulated by the activation and degranulation of eosinophils, especially asthma, chronic bronchitis, and chronic obstructuive pulmonary disease, of the formula: where j is 0 or 1 provided that when j is 0, n must be 2; k is 0 or 1; m is 0, 1, 2, or 3; n is 1 or 2; W<1 >is -O-; or -S(+O)t-, where t is 0, 1, or 2; or -N(R<3>)-; W<2 >is -O-CR<A>R<B>- or is absent; Y is =C(R<1>a, or -[N<custom-character file="US20030186974A1-20031002-P00900.TIF" wi="20" he="20" id="custom-character-00001"/>(O)k]- where k is 0 or 1; R<A >and R<B >are -H; -F; -CF3; -(C1-C4)alkyl; -(C3-C7)cycloalkyl; phenyl; or benzyl substituted with 0 to 3 substituents R<10>; or R<A >and R<B >are taken together, but only in the case where m is 1, to form a spiro moiety; R<C >and R<D >have the same meaning as R<A >and R<B >except that one of them must be -H, R<1 >and R<2 >are -H; -F; -Cl; -CN; -NO2; -(C1-C4)alkyl; -(C2-C4)alkynyl; fluorinated -(C1-C3)alkyl; -OR<16>; and -C(=O)NR<22>aR<22>b; R<3 >is -H; -(C1-C3)alkyl; phenyl; benzyl; or -OR<16>; R<4>, R<5 >and R<6 >in addition to other meanings may be taken together to form, e.g., G<1 >is a saturated or unsaturated carbon ring system that is a 3- to 7-membered monocyclic, or that is a 7- to 12-membered, fused polycyclic; provided that G<1 >is not a discontinuous or restricted biaryl moiety as defined under G<2>; where optionally one carbon atom may be replaced by a heteroatom selected from N, O, and S; where optionally a second carbon atom thereof, and further optionally a third carbon atom thereof may be replaced by N; -G<2 </superscript
申请公布号 US2003186974(A1) 申请公布日期 2003.10.02
申请号 US20020300950 申请日期 2002.11.20
申请人 MARFAT ANTHONY;MCKECHNEY MICHAEL WILLIAM 发明人 MARFAT ANTHONY;MCKECHNEY MICHAEL WILLIAM
分类号 C07D277/20;A61K;A61K31/357;A61K31/426;A61K31/427;A61K31/433;A61K31/4439;A61P;A61P1/00;A61P1/04;A61P1/16;A61P3/10;A61P7/00;A61P7/06;A61P9/00;A61P9/10;A61P9/12;A61P11/00;A61P11/02;A61P11/06;A61P11/08;A61P13/00;A61P13/02;A61P13/08;A61P13/12;A61P17/00;A61P17/04;A61P17/06;A61P19/02;A61P19/10;A61P21/04;A61P25/00;A61P25/14;A61P25/16;A61P25/24;A61P25/28;A61P27/02;A61P29/00;A61P29/02;A61P31/04;A61P31/10;A61P31/12;A61P31/16;A61P31/18;A61P31/22;A61P35/00;A61P35/02;A61P37/02;A61P37/04;A61P37/06;A61P37/08;A61P43/00;C07D;C07D277/56;C07D417/12;C07D417/14;(IPC1-7):A61K31/541;A61K31/537;A61K31/52;A61K31/501;C07D417/02 主分类号 C07D277/20
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