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    • 8. 发明授权
    • Pyrrolobenzimidazoles and pharmaceutical compositions containing them
    • 吡咯并苯并咪唑和含有它们的药物组合物
    • US4863945A
    • 1989-09-05
    • US131367
    • 1987-12-10
    • Walter-Gunar FriebeAlfred MertensKlaus StreinErwin Boehm
    • Walter-Gunar FriebeAlfred MertensKlaus StreinErwin Boehm
    • A61K31/40A61P7/02A61P9/04A61P9/12C07D487/04
    • C07D487/04
    • Pyrrolobenzimidazoles of the formula: ##STR1## are useful for treatment of heart and circulatory diseases. R.sub.1 is substituted phenyl; or optionally substituted naphthyl or a five- or six-membered heterocyclic group which can be condensed with a phenyl ring to form a bicyclic radical. R.sub.2 is hydrogen, alkyl, alkenyl or cycloalkenyl; R.sub.3 is alkyl, alkenyl or hydroxyalkyl or with R.sub.2 together forms cycloakylene; or R.sub.2 and R.sub.3 together form alkylidene or cycloalkylidene. R.sub.4 is hydrogen or lower alkanoyl. X is a valency bond, alkylene, vinylene, imino or carbonylamino. T stands for two hydrogen atoms. When X is a valency bond, R.sub.1 can also be hydrogen, hydrocarbyl which may also contain oxygen, amino, sulfur, carbonyl and sulfonyl groups. When X is imino or carbonylamino or when R.sub.1 is a bicyclic radical, T can also be oxygen. The compounds also include the tautomers and physiologically acceptable salts with inorganic and organic acids.
    • 下式的吡咯并苯并咪唑:可用于治疗心脏和循环系统疾病。 R1是取代的苯基; 或任选取代的萘基或可与苯环缩合形成双环基团的五元或六元杂环基。 R2是氢,烷基,烯基或环烯基; R3是烷基,烯基或羟基烷基或与R2一起形成亚环烷基; 或者R 2和R 3一起形成亚烷基或亚环烷基。 R4是氢或低级烷酰基。 X是价键,亚烷基,亚乙烯基,亚氨基或羰基氨基。 T代表两个氢原子。 当X是价键时,R 1也可以是氢,也可以含有氧,氨基,硫,羰基和磺酰基的烃基。 当X是亚氨基或羰基氨基时,或当R1是双环基时,T也可以是氧。 化合物还包括与无机和有机酸形成的互变异构体和生理上可接受的盐。