发明授权
US4695567A Pyrrolobenzimidazoles, pharmaceutical compositions containing them and
method of using them to treat certain heart and circulatory diseases
失效
吡咯并苯并咪唑,含有它们的药物组合物和使用它们治疗某些心脏和循环系统疾病的方法
- 专利标题: Pyrrolobenzimidazoles, pharmaceutical compositions containing them and method of using them to treat certain heart and circulatory diseases
- 专利标题(中): 吡咯并苯并咪唑,含有它们的药物组合物和使用它们治疗某些心脏和循环系统疾病的方法
-
申请号: US820259申请日: 1986-01-17
-
公开(公告)号: US4695567A公开(公告)日: 1987-09-22
- 发明人: Alfred Mertens , Jens-Peter Holck , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein , Egon Roesch
- 申请人: Alfred Mertens , Jens-Peter Holck , Herbert Berger , Bernd Muller-Beckmann , Klaus Strein , Egon Roesch
- 申请人地址: DEX Mannheim
- 专利权人: Boehringer Mannheim GmbH
- 当前专利权人: Boehringer Mannheim GmbH
- 当前专利权人地址: DEX Mannheim
- 优先权: DEX3501497 19850118
- 主分类号: A61K31/415
- IPC分类号: A61K31/415 ; A61K31/4184 ; A61K31/42 ; A61K31/50 ; A61K31/505 ; A61P9/00 ; A61P9/04 ; C07D403/12 ; C07D405/12 ; C07D487/04 ; C07D403/06
摘要:
The present invention provided pyrrolobenzimidazoles or tautomer thereof, of the general formula: ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.3 -C.sub.7 cycloalkyl;R.sub.2 is hydrogen, cyano, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, or a carbonyl group substituted by hydroxyl, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkyoxy, amino, C.sub.1 -C.sub.6 alkylamino, C.sub.2 -C.sub.12 dialkylamino or hydrazino, orR.sub.2 and R.sub.1 together with the carbon to which they are attached form a C.sub.3 -C.sub.8 spirocycloalkyl ring, or R.sub.1 and R.sub.2 together form C.sub.3 -C.sub.7 alkylidene or C.sub.3 -C.sub.7 cycloalkylkidene,X is a valency bond, C.sub.1 -C.sub.4 alkylene or vinylene andT is oxygen or sulphur;and Het is furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, thiadiazolyl, pyrazinyl, pyrimidinyl or pyridazinyl wherein the heterocyclic five- and six-membered rings are unsubstituted or substituted by one or more C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, hydroxyl, oxo, nitro, amino, halo, carboxyl, C.sub.2 -C.sub.7 alkoxycarbonyl, aminocarbonyl or cyano groups; or a physiologically acceptable salt thereof with an inorganic or organic acid. These compounds are useful for treating heart or circulatory diseases, especially those which respond to a change of blood pressure, an increase in cardiac output and/or a change in micro-circulation.