首页> 外国专利> heilmittel besonders mit antiarrhythmischer und subsidiarer wirkung bei der hypoxie des myokards und sein herstellungsverfahren

heilmittel besonders mit antiarrhythmischer und subsidiarer wirkung bei der hypoxie des myokards und sein herstellungsverfahren

机译:心肌缺氧及其制造过程的治疗方法,尤其是具有抗心律失常和辅助作用的治疗方法

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.
机译:本发明涉及式I的(-)-顺式-2,8-二甲基-2,3,4,4a,5,9b-六氢-1H-吡啶并[4,3-b]吲哚及其盐,其制剂和合适的药物组合物,特别是在心肌缺氧中具有抗心律不齐和辅助作用。本发明的化合物还具有降压,局部麻醉,解痉,x-肾上腺溶解和中枢镇静作用。该组合物可以以液体,半液体和固体给药形式存在。根据本发明的化合物由(+/-)-顺-2,8-二甲基-2,3,4,4a,5,9b-六氢-1H-吡啶并[4,3-b]吲哚制备。盐与旋光酸,最好是(+)-O,O'-二苯甲酰基-D-酒石酸形成盐,通过将其呈碱性并将其转化为可药用的盐,从中释放出(-)-顺式异构体,优选二盐酸盐(熔点为270-274℃,有分解)或二棕榈酸酯(熔点为55-56℃)。本发明的活性物质以低于迄今使用的药剂的剂量消除了心律不齐,同时具有相对低的急性毒性和在缺氧时保护心肌的能力。另外还存在诸如神经镇痛药和胸腺药的中枢作用。

著录项

  • 公开/公告号SE8204693D0

    专利类型

  • 公开/公告日1982-08-13

    原文格式PDF

  • 申请/专利权人 CESKOSLOVENSKA AKADEMIE VED;

    申请/专利号SE19820004693

  • 发明设计人 S * STOLC;L * BENES;V * BAUER;M * TICHY;

    申请日1982-08-13

  • 分类号A61K31/435;A61P9/06;C07D471/04;

  • 国家 SE

  • 入库时间 2022-08-22 13:31:00

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