Benzazepine derivatives, their pharmaceutical compositions and method of
use
    10.
    发明授权
    Benzazepine derivatives, their pharmaceutical compositions and method of use 失效
    苯扎西平衍生物,其药物组合物和使用方法

    公开(公告)号:US4490369A

    公开(公告)日:1984-12-25

    申请号:US547940

    申请日:1983-11-02

    Abstract: Compounds of the formula ##STR1## wherein A is --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --NH--CO--, --CH.sub.2 --CO-- or ##STR2## where R.sub.7 is alkyl of 1 to 3 carbon atoms, andB is methylene, carbonyl or thiocarbonyl, orA is --CO--CO--, --N.dbd.CH--, ##STR3## where R.sub.8 is hydrogen or alkyl of 1 to 3 carbon atoms substituted by a phenyl, methoxyphenyl or dimethoxyphenyl, andB is methylene;E is n-alkylene of 2 to 4 carbon atoms optionally substituted by an alkyl of 1 to 3 carbon atoms, 2-hydroxy-n-propylene, 2-hydroxy-n-butylene or 3-hydroxy-n-butylene;G is n-alkylene of 1 to 5 carbon atoms optionally substituted by an alkyl of 1 to 3 carbon atoms, wherein one methylene group of an n-alkylene of 2 to 5 carbon atoms can be replaced by a carbonyl group, with the proviso that B represents a methylene or carbonyl group, or methylene-n-hydroxy-alkylene of 1 to 4 carbon atoms, where the methylene group is attached to the nitrogen atom; andR.sub.1 to R.sub.5 are simple substituents of various types;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.

    Abstract translation: 其中A是-CH 2 -CH 2 - , - CH = CH - , - NH-CO-, - CH 2 -CO-或者其中R 7是1至3个碳原子的烷基,和B 是亚甲基,羰基或硫代羰基,或A是-CO-CO-,-N = CH-,其中R 8是氢或被苯基,甲氧基苯基或二甲氧基苯基取代的1至3个碳原子的烷基,和 B是亚甲基; E是任选被1至3个碳原子的烷基取代的2至4个碳原子的正亚烷基,2-羟基 - 正丙烯,2-羟基 - 正丁烯或3-羟基 - 正丁烯; G是任选被1至3个碳原子的烷基取代的1至5个碳原子的正亚烷基,其中2至5个碳原子的正亚烷基的一个亚甲基可被羰基取代,条件是 B表示亚甲基或羰基,或亚甲基与氮原子连接的1至4个碳原子的亚甲基 - 正 - 羟基 - 亚烷基; 而R1至R5是各种简单的取代基; 和无毒的,药学上可接受的酸加成盐。 化合物及其盐可用作心动过缓。

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