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    • 6. 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。
    • 8. 发明授权
    • Pyrrolobenzimidazoles, pharmaceutical compositions containing them, and
use of them to treat certain heart and circulatory diseases
    • 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
    • US4710510A
    • 1987-12-01
    • US807260
    • 1985-12-10
    • Alfred MertensJens-Peter HolckWolfgang KampeBernd Muller-BeckmannKlaus StreinWolfgang Schaumann
    • Alfred MertensJens-Peter HolckWolfgang KampeBernd Muller-BeckmannKlaus StreinWolfgang Schaumann
    • A61K31/415A61K31/4184A61P9/00A61P9/04C07D209/34C07D209/42C07D487/04A61K31/55
    • C07D487/04C07D209/34C07D209/42
    • 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.
    • 本发明提供了以下通式的新的吡咯并苯并咪唑:其中R 1是氢原子或烷基,烯基或环烷基; R2是氢原子,氰基或烷基或烯基或被羟基,烷基,烷氧基,氨基,烷基氨基,二烷基氨基或肼基取代的羰基或与R1一起形成亚环烷基,或者R 1和R 2一起形成亚烷基或亚环烷基 激进; 可以相同或不同的R 3,R 4和R 5各自表示氢原子或烷磺酰氧基,三氟甲磺酰氧基,烷磺酰氨基,三氟甲磺酰氨基,N-烷基 - 烷磺酰氨基,N-烷基 - 三氟甲磺酰氨基,烷基亚磺酰基甲基,烷基亚磺酰基甲基或烷基磺酰基甲基,羰基 被羟基,烷氧基,氨基,烷基氨基或二烷基氨基取代的基团,被氨基,烷基氨基,二烷基氨基或环状亚氨基取代的磺酰基,其中4-位中的亚甲基可以被硫或氧原子,烷基羰基氨基,氨基羰基氨基 或烷基氨基羰基氨基,烷硫基,烷基亚磺酰基或烷基磺酰基,硝基,卤素,氨基,羟基,烷基,三氟甲基,烷氧基,烯氧基,炔氧基,氰基烷氧基,羧基烷氧基,烷氧基羰基烷氧基,二烷基氨基,1-咪唑基或氰基; X是价键,C1-C4亚烷基或乙烯基; 和T是氧或硫原子; 其互变异构体及其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的方法和含有它们的药物用于预防和治疗心脏和循环系统疾病。