首页> 外国专利> METHOD OF PRODUCING PYRROLOBENZIMIDAZOLS OR THEIR TAUTOMERS, OR THEIR PHYSIOLOGICALLY COMPATIBLE SALTS OF INORGANIC ACIDS

METHOD OF PRODUCING PYRROLOBENZIMIDAZOLS OR THEIR TAUTOMERS, OR THEIR PHYSIOLOGICALLY COMPATIBLE SALTS OF INORGANIC ACIDS

机译:制备吡咯并苯并咪唑或它们的生理相容性无机盐的方法

摘要

The present invention provided pyrrolobenzimidazoles or tautomer thereof, of the general formula: IMAGE (I) wherein R1 is hydrogen, C1-C6 alkyl, C2-C6 alkenyl or C3-C7 cycloalkyl; R2 is hydrogen, cyano, C1-C6 alkyl, C2-C6 alkenyl, or a carbonyl group substituted by hydroxyl, C1-C6 alkyl, C1-C6 alkyoxy, amino, C1-C6 alkylamino, C2-C12 dialkylamino or hydrazino, or R2 and R1 together with the carbon to which they are attached form a C3-C8 spirocycloalkyl ring, or R1 and R2 together form C3-C7 alkylidene or C3-C7 cycloalkylkidene, X is a valency bond, C1-C4 alkylene or vinylene and T 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 C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylthio, hydroxyl, oxo, nitro, amino, halo, carboxyl, C2-C7 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.
机译:本发明提供了具有以下通式的吡咯并苯并咪唑或其互变异构体:(I)其中R 1为氢,C 1 -C 6烷基,C 2 -C 6烯基或C 3 -C 7环烷基; R 2是氢,氰基,C 1 -C 6烷基,C 2 -C 6烯基或被羟基,C 1 -C 6烷基,C 1 -C 6烷氧基,氨基,C 1 -C 6烷基氨基,C 2 -C 12二烷基氨基或肼基取代的羰基,或R 2 R 1和与其连接的碳一起形成C 3 -C 8螺环烷基环,或R 1和R 2一起形成C 3 -C 7亚烷基或C 3 -C 7环烷基亚基,X为价键,C 1 -C 4亚烷基或亚乙烯基,并且T为氧气或硫磺;并且Het为呋喃基,噻吩基,吡咯基,吡唑基,咪唑基,恶唑基,噻唑基,三唑基,恶二唑基,噻二唑基,吡嗪基,嘧啶基或哒嗪基,其中杂环的五元和六元环未被取代或被一个或多个C1-C6取代,C 1 -C 6烷氧基,C 1 -C 6烷硫基,羟基,氧代,硝基,氨基,卤素,羧基,C 2 -C 7烷氧羰基,氨基羰基或氰基;或其生理学上可接受的与无机或有机酸形成的盐。这些化合物可用于治疗心脏或循环系统疾病,尤其是那些对血压变化,心输出量增加和/或微循环变化有反应的疾病。

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