发明名称 Amide derivatives of thiazolyl-, oxazolyl-, pyrrolyl- and imidazolyl carboxylic acids useful as PDE4isozyme inhibitors
摘要 <p>This application is directed to 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 Y is =C(R1a)- or -[Nsquare(O)k]- where k is 0 or 1;G1 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 G1 is not a discontinuous or restricted biaryl moiety as defined under G2; 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; -G2 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; or that is a 7- to 18-membered discontinuous or restricted biaryl moiety; wherein for each of the carbon ring systems recited, optionally one carbon atom of said carbon ring system 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; E is selected from:and all other substituents shown above are as defined in the specification.</p>
申请公布号 CZ20031903(A3) 申请公布日期 2004.07.14
申请号 CZ20030001903 申请日期 2001.12.24
申请人 PFIZER PRODUCTS INC. 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):C07D417/12 主分类号 C07D277/20
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