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Pyrrolo-benzimidazoles, medicaments containing these compounds and process for their preparation

机译:吡咯并苯并咪唑,含有这些化合物的药物及其制备方法

摘要

Pyrrolobenzimidazoles of the formula IMAGE in which A and B together with the two intermediate carbon atoms represent an imidazo group of the formula IMAGE in which R1 represents a hydrogen atom or an alkyl group which is optionally substituted by a phenyl group and R2 represents a hydrogen atom, an alkyl group which is optionally substituted by a phenyl, pyridyl or thienyl group, a vinylene group which is substituted at the end by a phenyl or pyridyl group, a phenyl group which is optionally substituted by a halogen atom, or a hydroxyl, alkoxy, mercapto, alkylmercapto, alkylsulphinyl, alkylsulphonyl, cyano, amino, alkylamino, dialkylamino, alkanoylamino or nitro group, it being possible for a hydroxyphenyl group to be substituted additionally by one or two alkyl groups or an aminophenyl group to be substituted by one or two halogen atoms, a phenyl group disubstituted by halogen atoms, or hydroxyl, alkoxy, mercapto, alkylmercapto, alkylsulphinyl or alkylsulphonyl groups, it being possible for the substituents of the phenyl ring to be identical or different, a 5- or 6-membered heteroaromatic ring bonded via a carbon atom and which contains an oxygen, sulphur or nitrogen atom, two or three nitrogen atoms or a nitrogen atom and an oxygen or sulphur atom, to which one or two 1,4-butadienyl groups can be additionally bonded via two adjacent carbon atoms, where in this case the bonding can also take place via a fused-on phenyl ring and in the case of the pyridines these can additionally be substituted by an amino, alkylamino, dialkylamino, alkanoylamino or morpholino group or by two halogen atoms or by a halogen atom and an amino or morpholino group and in the case of the quinolines can be additionally mono- or disubstituted by a halogen atom, or an alkoxy or phenyl group, it being possible for the substituents to be identical or different, a 5- to 7-membered saturated imino-, N-alkylimino- or N-alkanoylimino-alkylene ring bonded via a carbon atom, or a 1,2,3,4-tetrahydroquinolyl or 5,6,7,8-tetrahydroquinolyl group, R3 represents an alkyl group which is optionally substituted by a phenyl group, an alkyl group or an alkyl group which is substituted from position 2 by a hydroxyl, alkoxy or pyridinium group, R4 and R5, which can be identical or different, represent hydrogen atoms, alkyl groups or cycloalkyl groups, and their acid addition salts, for pharmaceutical use in particular their physiologically tolerable acid addition salts with inorganic or organic acids, which have useful pharmacological properties, in particular a slight influence on the blood pressure, a positive inotropic effect and an antithrombotic effect. The novel compounds can be prepared by methods known per se.
机译:的吡咯并苯并咪唑类,其中A和B与两个中间碳原子一起表示式的咪唑基,其中R1代表氢原子或可被苯基和R2取代的烷基代表氢原子,任选被苯基,吡啶基或噻吩基取代的烷基,末端被苯基或吡啶基取代的亚乙烯基,任选被卤素原子取代的苯基或羟基,烷氧基,巯基,烷基巯基,烷基亚磺酰基,烷基磺酰基,氰基,氨基,烷基氨基,二烷基氨基,链烷酰基氨基或硝基,羟基苯基还可以被一个或两个烷基或氨基苯基取代被一个或两个卤素原子,被卤素原子二取代的苯基或羟基,烷氧基,巯基,烷基巯基,烷基亚磺酰基或烷基磺酰基,苯环的取代基可以相同或不同,可以是通过碳原子键合的,含有氧,硫或氮原子,两个或三个氮原子或氮原子和氧或硫原子,一个或两个1,4-丁二烯基可以通过两个相邻的碳原子另外键合到该原子上,在这种情况下,键合也可以通过稠合的苯环发生,在吡啶的情况下这些可以另外被氨基,烷基氨基,二烷基氨基,烷酰基氨基或吗啉代基团取代,或者被两个卤素原子或被卤素原子和氨基或吗啉代基团取代,并且在喹啉的情况下,可以另外被卤素单或二取代。取代基可以相同或不同,也可以是经由碳原子键合的5至7元饱和亚氨基,N-烷基亚氨基-或N-烷氨基亚氨基-亚烷基环,或1,2,3,4-四氢喹啉基或5,6,7,8-四氢喹啉基,R3代表烷基,其任选地被苯基,烷基或从2位被羟基,烷氧基或吡啶鎓基取代的烷基取代,R4 R 5和R 5可以相同或不同,代表氢原子,烷基或环烷基及其酸加成盐,特别是对于药学用途而言,其与无机或有机酸的生理上可耐受的酸加成盐具有药学上的有用的药理学特性。特别是对血压有轻微影响,正性肌力作用和抗血栓形成作用。新化合物可以通过本身已知的方法制备。

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