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    • 1. 发明授权
    • 3-Cyano-indoles as cardioselective agents
    • 3-氰基 - 吲哚作为心脏选择剂
    • US4468520A
    • 1984-08-28
    • US288075
    • 1981-07-29
    • Helmut MichelWolfgang KampeRoland OfenlochKarl DietmannGisbert Sponer
    • Helmut MichelWolfgang KampeRoland OfenlochKarl DietmannGisbert Sponer
    • C07D209/12A61K31/40A61K31/403A61K31/404A61P9/00C07D209/08C07D209/42C07D209/43C07D209/04
    • C07D209/08
    • The present invention provides aminopropanol derivatives of the general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a lower alkanoyl or an aroyl radical, R.sub.2 is a lower alkyl radical or a radical of the general formula: ##STR2## wherein X is a valency bond, a methylene group or an oxygen or sulphur atom, Ar is a monocyclic, carbo- or heterocyclic aryl radical, R.sub.6 and R.sub.7, which can be the same or different, are hydrogen atoms or lower alkyl radicals, R.sub.8 and R.sub.9, which can be the same or different, are hydrogen or halogen atoms, hydroxyl groups, lower alkanoyl radicals, alkenyl radicals, alkynyl radicals, alkyl radicals, lower alkoxy radicals, aralkoxy radicals, alkenyloxy radicals, alkynyloxy radicals, lower alkylthio radicals, aminocarbonyl radicals, aminosulphonyl radicals or acylamino radicals; or R.sub.2 is a 1,4-benzodioxan-2-ylmethyl radical, R'.sub.2 is a hydrogen atom or a benzyl radical, R.sub.3 is a carboxyl group or a lower alkoxycarbonyl, aminocarbonyl, cyano, oximinomethyl, formyl, hydroxymethyl or lower alkoxycarbimidoyl radical, R.sub.4 is a hydrogen atom or a lower alkyl radical or a --CH.sub.2 --O--R.sub.1 radical, R.sub.1 having the same meaning as above, and R.sub.5 is a hydrogen atom or a lower alkyl radical; the optionally-active forms and racemates thereof and the pharmacologically acceptable salts thereof. The present invention also provides processes for the preparation of these compounds and pharmaceutical compositions containing them. Furthermore, the present invention is concerned with the use of these compounds for the prophylaxis and treatment of heart and circulatory diseases.
    • 本发明提供以下通式的氨基丙醇衍生物:其中R1是氢原子或低级烷酰基或芳酰基,R2是低级烷基或通式如下的基团:其中 X是价键,亚甲基或氧或硫原子,Ar是单环,碳或杂环芳基,R6和R7可以相同或不同,是氢原子或低级烷基,R8和 R9可相同或不同,为氢或卤原子,羟基,低级烷酰基,烯基,炔基,烷基,低级烷氧基,芳烷氧基,烯氧基,炔氧基,低级烷硫基,氨基羰基 自由基,氨基磺酰基或酰氨基; 或R 2为1,4-苯并二恶烷-2-基甲基,R'2为氢原子或苄基,R 3为羧基或低级烷氧基羰基,氨基羰基,氰基,肟基甲基,甲酰基,羟甲基或低级烷氧基甲脒基 R4是氢原子或低级烷基或-CH2-O-R1基,R1具有与上述相同的含义,R 5是氢原子或低级烷基; 其任选活性形式和外消旋物及其药理学上可接受的盐。 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组合物。 此外,本发明涉及这些化合物用于预防和治疗心脏和循环系统疾病的用途。