5,6,8,9-Tetrahydro-7H-dibenz(d,f)azonine derivatives, the production thereof and compositions containing them
申请人:GÖDECKE AKTIENGESELLSCHAFT
公开号:EP0035360A2
公开(公告)日:1981-09-09
The present invention provides 5.6;8,9-tetrahydro-7H-di- benz(d,f)azonine derivatives of the formula:
wherein R1 and R2, which are the same or different, are hydrogen or halogen atoms or lower alkyl or lower alkoxy radicals, R3 is a hydrogen atom or a lower alkyl radical, R4 is a hydrogen atom or a lower alkyl or lower alkanoyl radical and n is 1 or 2; and the pharmaceutically acceptable salts thereof formed with inorganic and organic acids; but excluding 6-benzyl-2,12-dimethoxy-1-hydroxy-7-methyl-5,6;8,9-tetrahy- dro-7H-dibenz(d,f)azonine in which case R1, R2 and R4 are hydrogen, n is 1 and R3 is methyl. The lower alkyl, lower alkanoyl and lower alkoxy radicals are straight chain or branched radicals containing 1 to 5 carbon atoms.
The present invention also provides a process for the production of these compounds, as well as pharmaceutical compositions containing them.
The compounds are useful as antiarrhythmic agents and as local anaesthetics; they do not cause some of the unsatisfactory side effects associated with known agents.
本发明提供式 5.6;8,9-四氢-7H-二苯并(d,f)唑嗪衍生物:
其中 R1 和 R2(相同或不同)为氢原子或卤素原子或低级烷基或低级烷氧基,R3 为氢原子或低级烷基,R4 为氢原子或低级烷基或低级烷酰基,n 为 1 或 2;及其与无机酸和有机酸形成的药学上可接受的盐;但不包括 6-苄基-2,12-二甲氧基-1-羟基-7-甲基-5,6;8,9-四氢-7H-二苯并(d,f)唑嗪,在这种情况下,R1、R2 和 R4 为氢原子,n 为 1,R3 为甲基。低级烷基、低级烷酰基和低级烷氧基是含有 1 至 5 个碳原子的直链或支链基。
本发明还提供了生产这些化合物的工艺以及含有这些化合物的药物组合物。
这些化合物可用作抗心律失常药剂和局部麻醉剂;它们不会引起与已知药剂相关的某些令人不满意的副作用。