申请人:Boehringer Mannheim GmbH
公开号:US04710510A1
公开(公告)日:1987-12-01
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.
本发明提供了一种新的吡咯并苯并咪唑通式如下:##STR1##其中,R.sub.1是氢原子或烷基,烯基或环烷基基团; R.sub.2是氢原子,氰基或烷基或烯基基团或羟基,烷氧基,氨基,烷基氨基,二烷基氨基或肼基取代的羰基基团或与R.sub.1形成环烷基基团或R.sub.1和R.sub.2共同形成烷基亚甲基或环烷基亚甲基基团; R.sub.3,R.sub.4和R.sub.5,可以相同也可以不同,每个代表氢原子或烷基磺酸酯氧基,三氟甲磺酸酯氧基,烷基磺酰氨基,三氟甲磺酰氨基,N-烷基烷基磺酰氨基,N-烷基三氟甲磺酰氨基,烷基磺酚甲基,烷基亚磺酰甲基或烷基磺酰甲基基团,羟基,烷氧基,氨基,烷基氨基或二烷基氨基取代的羰基基团,氨基,烷基氨基,二烷基氨基或环亚氨基取代的磺酰基基团,其中4-位的亚甲基基团可以被硫或氧原子取代,烷基羰基氨基,氨基羰基氨基或烷基氨基羰基氨基基团,烷基硫,烷基亚磺酰基或烷基磺酰基基团,硝基,卤素,氨基,羟基,烷基,三氟甲基,烷氧基,烯基氧基,炔基氧基,氰基烷氧基,羧基烷氧基,烷氧羰基烷氧基,二烷基氨基,1-咪唑基或氰基; X是价键,C.sub.1-C.sub.4烷基或乙烯基; T是氧原子或硫原子; 它们的互变异构体和与无机和有机酸的生理上可接受的盐。本发明还提供了制备这些化合物和包含它们的药物,用于预防和治疗心脏和循环系统疾病的方法。