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1. 发明申请

WO2007074089A1 ARYL-ISOXAZOL-4-YL-IMIDAZO[1, 5-A]PYRIDINE DERIVATIVES 审中-公开
标题翻译： ARYL-ISOXAZOL-4-YL-IMIDAZO [1,5-A]吡啶衍生物
公开(公告)号：WO2007074089A1
公开(公告)日：2007-07-05
申请号：PCT/EP2006/069792
申请日：2006-12-18
申请人： F. HOFFMANN-LA ROCHE AG , BUETTELMANN, Bernd , DONG, Jiaqiang , HAN, Bo , KNUST, Henner , THOMAS, Andrew
发明人： BUETTELMANN, Bernd , DONG, Jiaqiang , HAN, Bo , KNUST, Henner , THOMAS, Andrew
IPC分类号： C07D471/04 , A61K31/4188 , A61K31/437 , A61P25/28
CPC分类号： C07D471/04
摘要： The present invention is concerned with aryl-isoxazol-4-yl-imidazo[1,5-a]pyridine derivatives of formula (I) wherein: R 1 is hydrogen, halogen, hydroxy, lower alkyl, benzyloxy or -O-(CH 2 )-(CO)-5 or 6 membered heteroaryl optionally substituted by aryl and lower alkyl; R 2 is hydrogen, lower alkyl, or -(CO)-R a ; R 3 is hydrogen, halogen, cyano, lower alkyl, or -(CO)-R a ; R a is hydroxy, lower alkoxy, NR'R'', wherein R' and R'' are each independently hydrogen, cycloalkyl, 5 or 6-membered heterocycloalkyl or lower alkyl optionally substituted by cycloalkyl, cyano, 5 or 6-membered heterocycloalkyl or 5 or 6-membered heteroaryl; as well as pharmaceutically acceptable acid addition salts thereof. It has been found that this class of compounds show high affinity and selectivity for GABA A α5 receptor binding sites and might be useful as cognitive enhancer or for the treatment of cognitive disorders like Alzheimer's disease.
摘要翻译：本发明涉及式（I）的芳基 - 异恶唑-4-基 - 咪唑并[1,5-a]吡啶衍生物，其中：R 1是氢，卤素，羟基，低级烷基，任选被芳基和低级烷基取代的苄氧基或-O-（CH 2）2 - （CO）-5或6元杂芳基; R 2是氢，低级烷基或 - （CO）-R a; R 3是氢，卤素，氰基，低级烷基或 - （CO）-R a）。 R“是羟基，低级烷氧基，NR'R”，其中R'和R“各自独立地为氢，环烷基，5或6元杂环烷基或任选被环烷基取代的低级烷基，氰基，5或6元杂环烷基或5或6元杂芳基; 以及其药学上可接受的酸加成盐。已经发现，这类化合物显示出对GABA A a5受体结合位点的高亲和力和选择性，并且可用作认知增强剂或用于治疗认知障碍如阿尔茨海默氏病。

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