发明名称 (-)-cis-2,8-Dimethyl-2,3,4,4a,5,9b-hexahydro-1H-pyrido-(4,3-b)indo le, its preparation and pharmaceutical compositions, in particular antiarrhythmics
摘要 The invention relates to (-)-cis-2,8-dimethyl- 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole of the formula I <IMAGE> its salts, its preparation and appropriate pharmaceutical compositions, in particular having antiarrhythmic and subsidiary action in myocardial hypoxia. The compounds according to the invention also have a hypotensive, local anaesthetic, spasmolytic, x-adrenolytic and central sedative action. The compositions can be present in a liquid, semi-liquid and solid administration form. The compounds according to the invention are prepared from (+/-)-cis-2,8-dimethyl- 2,3,4,4a,5,9b-hexahydro-1H-pyrido[4,3-b]indole via the salt with an optically active acid, advantageously (+)-O,O'-dibenzoyl-D-tartaric acid, from which the (-)-cis-isomer is liberated by rendering it alkaline and optionally converting it into a pharmaceutically suitable salt, preferably the dihydrochloride (m.p. 270-274 DEG C, with decomposition) or the dipalmitate (m.p. 55-56 DEG C). The active substances according to the invention eliminate cardiac arrhythmias in doses which are lower than the agents used hitherto and at the same time have relatively low acute toxicity and the ability to protect the cardiac muscle during oxygen deficiency. Central effects such as neuroleptic and thymoleptic effects are additionally present.
申请公布号 DE3231088(A1) 申请公布日期 1983.03.10
申请号 DE19823231088 申请日期 1982.08.20
申请人 CESKOSLOVENSKA AKADEMIE VED 发明人 STOLC,SVORAD,DR.;BAUER,VIKTOR,DR.;BENES,LUDEK,DR.;TICHY,MILOS,DIPL.-ING.
分类号 A61K31/435;A61P9/06;C07D471/04;(IPC1-7):C07D471/04;A61K31/43 主分类号 A61K31/435
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