Azepine derivatives and their anti-thrombotic compositions and methods
    4.
    发明授权
    Azepine derivatives and their anti-thrombotic compositions and methods 失效
    Azepine衍生物及其抗血栓形成和方法

    公开(公告)号:US4414225A

    公开(公告)日:1983-11-08

    申请号:US348496

    申请日:1982-02-12

    摘要: Compounds of the formula ##STR1## wherein n and m are each 1, 2 or 3, and the sum of n+m is 4;R.sub.1 is alkyl; alkenyl; unsubstituted, mono- or di-substituted aralkyl; unsubstituted, mono- or di-substituted benzoyl; alkoxycarbonyl; aralkoxycarbonyl; or, when m and n are each 2 and/or R.sub.2 and R.sub.3 are other than both hydrogen at the same time, also hydrogen;one of R.sub.2 and R.sub.3 is hydrogen or amino, and the other is carboxyl or alkoxycarbonyl; or, when R.sub.3 is hydrogen,R.sub.2 is hydrogen; amino; alkoxycarbonyl-amino; (unsubstituted or mono-substituted phenyl)-aminocarbonyl-; (unsubstituted or mono-substituted phenyl)ethylaminocarbonyl; azidocarbonyl; or hydrazinocarbonyl;X is oxygen, sulfur or ##STR2## where R.sub.4 is hydrogen; alkyl; phenyl-alkyl; or phenyl; non-toxic, pharmacologically acceptable acid addition salts thereof; and, when R.sub.2 or R.sub.3 is carboxyl, non-toxic, pharmacologically acceptable salts thereof formed with inorganic or organic bases. The compounds as well as their salts are useful as antithrombotics.

    摘要翻译: 其中n和m各自为1,2或3,并且n + m的和为4; R1是烷基; 烯基; 未取代的,单或二取代的芳烷基; 未取代的,单或二取代的苯甲酰基; 烷氧基羰基 芳烷氧羰基; 或者当m和n各自为2和/或R 2和R 3不同时为氢时,也为氢; R2和R3之一是氢或氨基,另一个是羧基或烷氧基羰基; 或当R3为氢时,R2为氢; 氨基; 烷氧基羰基 - 氨基; (未取代或单取代的苯基) - 氨基羰基 - ; (未取代或单取代的苯基)乙基氨基羰基; 叠氮羰基; 或肼基羰基; X是氧,硫或者其中R 4是氢; 烷基; 苯基 - 烷基; 或苯基; 无毒,药理学上可接受的酸加成盐; 并且当R 2或R 3为羧基时,与无机或有机碱形成的无毒的药学上可接受的盐。 化合物及其盐可用作抗血栓形成剂。