发明授权
US4710510A Pyrrolobenzimidazoles, pharmaceutical compositions containing them, and
use of 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,以及它们用于治疗某些心脏和循环系统疾病
- 专利标题: Pyrrolobenzimidazoles, pharmaceutical compositions containing them, and use of 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,以及它们用于治疗某些心脏和循环系统疾病
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申请号: US807260申请日: 1985-12-10
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公开(公告)号: US4710510A公开(公告)日: 1987-12-01
- 发明人: Alfred Mertens , Jens-Peter Holck , Wolfgang Kampe , Bernd Muller-Beckmann , Klaus Strein , Wolfgang Schaumann
- 申请人: Alfred Mertens , Jens-Peter Holck , Wolfgang Kampe , Bernd Muller-Beckmann , Klaus Strein , Wolfgang Schaumann
- 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: DEX3445669 19841214
- 主分类号: A61K31/415
- IPC分类号: A61K31/415 ; A61K31/4184 ; A61P9/00 ; A61P9/04 ; C07D209/34 ; C07D209/42 ; C07D487/04 ; A61K31/55
摘要:
The present invention provides new pyrrolobenzimidazoles of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or an alkyl, alkenyl or cycloalkyl radical; R.sub.2 is a hydrogen atom, cyano group or alkyl or alkenyl radical or a carbonyl group substituted by hydroxyl, alkyl, alkoxy, amino, alkylamino, dialkylamino or hydrazino or together with R.sub.1 forms a cycloalkylene radical or R.sub.1 and R.sub.2 together form an alkylidene or cycloalkylidene radical; R.sub.3, R.sub.4 and R.sub.5, which can be the same or different, each represent a hydrogen atom or an alkanesulphonyloxy, trifluoromethanesulphonyloxy, alkanesulphonylamino, trifluoromethanesulphonylamino, N-alkyl-alkanesulphonylamino, N-alkyl-trifluoromethanesulphonylamino, alkylsulphenylmethyl, alkylsulphinylmethyl or alkylsulphonylmethyl radical, a carbonyl group substituted by hydroxyl, alkoxy, amino, alkylamino or dialkylamino, a sulphonyl group substituted by amino, alkylamino, dialkylamino or cyclic imino, whereby a methylene group in the 4-position can be replaced by a sulphur or oxygen atom, an alkylcarbonylamino, aminocarbonylamino or alkylaminocarbonylamino radical, an alkylthio, alkylsulphinyl or alkylsulphonyl radical, a nitro, halogen, amino, hydroxyl, alkyl, trifluoromethyl, alkoxy, alkenyloxy, alkynyloxy, cyanoalkoxy, carboxyalkoxy, alkoxycarbonylalkoxy, dialkylamino, 1-imidazolyl or cyano group; X is a valency bond, a C.sub.1 -C.sub.4 alkylene radical or a vinyl radical; and T is an oxygen or sulphur atom; the tautomers thereof and the physiologically acceptable salts thereof with inorganic and organic acids.The present invention also provides processes for the preparation of these compounds and pharmaceuticals containing them for the prophylaxis and treatment of heart and circulatory diseases.
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