公开(公告)号：US20090269301A1

公开(公告)日：2009-10-29

申请号：US11937149

申请日：2007-11-08

申请人： Michael Thormann ,  Michael Altmstetter ,  Andreas Treml ,  Ulrich Heiser ,  Mirko Buchholz ,  Andre J. Niestroj

发明人： Michael Thormann ,  Michael Altmstetter ,  Andreas Treml ,  Ulrich Heiser ,  Mirko Buchholz ,  Andre J. Niestroj

IPC分类号： A61K38/20 ,  C07D403/06 ,  A61K31/4178 ,  A61K31/4439 ,  C07D401/14 ,  A61P25/28 ,  A61K31/4709

CPC分类号： C07D403/06 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/04

摘要： The present invention relates to compounds of formula (I), combinations and uses thereof for disease therapy, R1 represents heteroaryl, -carbocyclyl-heteroaryl, -alkenylheteroaryl or -alkylheteroaryl; R2 represents hydrogen; halogen; alkenyl; alkynyl; -alkenylaryl; -alkenylheteroaryl; alkyl, which may optionally be substituted by one or more groups selected from halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; carbocyclyl, which may optionally be substituted by one or more groups selected from alkyl, halogen, hydroxyl, alkoxy-, -thioalkyl, —C(O)OH and —C(O)O-alkyl; -alkylcarbocyclyl; -alkylheterocyclyl; aryl; heteroaryl; heterocyclyl; -alkylaryl; -alkyl(aryl)2, -alkylheteroaryl; -aryl-heteroaryl; -heterocyclyl-aryl; -aryl-aryl; -heteroaryl-aryl; -heteroaryl-heteroaryl, and —C(O)R4; R3 represents halogen; alkyl optionally substituted by one or more groups selected from halogen, hydroxyl, alkoxy, thioalkyl, —C(O)OH and —C(O)O-alkyl; aryl; heteroaryl; —C(O)R5; R4 and R5 independently represent alkyl, aryl, heteroaryl, -alkylaryl, -alkylheteroaryl, carbocyclyl, heterocyclyl, -alkylcarbocyclyl and -alkylheterocyclyl, with the proviso that, when R1 is imidazolyl, -carbocyclyl-imidazolyl, -alkenyl-imidazolyl or -alkyl-imidazolyl, then R3 may not be —C(O)R5.

摘要翻译： 本发明涉及式（I）化合物，其用于疾病治疗的组合和用途，R 1表示杂芳基， - 碳环基 - 杂芳基， - 烯基杂芳基或 - 烷基杂芳基; R2表示氢; 卤素; 烯基; 炔基; - 烯基芳基; 烯基杂芳基 烷基，其可任选被一个或多个选自卤素，羟基，烷氧基 - ， - 硫代烷基，-C（O）OH和-C（O）O-烷基的基团取代; 碳环基，其可任选被一个或多个选自烷基，卤素，羟基，烷氧基 - ， - 硫代烷基，-C（O）OH和-C（O）O-烷基的基团取代; - 烷基羧基 - 烷基杂环基 芳基; 杂芳基; 杂环基; - 烷基芳基; - 烷基（芳基）2， - 烷基杂芳基; 芳基 - 杂芳基; - 杂环基 - 芳基; 芳芳基 - 杂芳基 - 芳基; - 杂芳基 - 杂芳基和-C（O）R 4; R3表示卤素; 任选被一个或多个选自卤素，羟基，烷氧基，硫代烷基，-C（O）OH和-C（O）O-烷基的基团取代的烷基; 芳基; 杂芳基; -C（O）R 5; R 4和R 5独立地表示烷基，芳基，杂芳基， - 烷基芳基， - 烷基杂芳基，碳环基，杂环基， - 烷基碳环基和 - 烷基杂环基，条件是当R 1是咪唑基， - 环保基 - 咪唑基， - 烯基 - 咪唑基或 - 咪唑基，那么R 3可以不是-C（O）R 5。