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TRICYCLIC AND TETRACYCLIC SYSTEMS WITH ACTIVITY ON THE CENTRAL-NERVOUS AND VASCULAR SYSTEMS

机译:对中枢神经和血管系统有活性的三环和四环系统

摘要

The present invention relates to chemistry and pharmacy and, in particular, to the production of novel molecular entities, tricyclic and tetracyclic derivatives of benzodiazepine, pyridodiazepine and pyrimidodiazepine type fused with 1,4-dihydropyridine derivatives, having an effect on the central-nervous and vascular systems. Derivatives containing a dihydropyridine ring are used, by means of reactions with compounds of the ortho-phenylenediamine, ortho-diaminopyridine and ortho-diaminopyrimidine type, and also subsequent conversions to some thereof, to obtain tricyclic and tetracyclic derivatives of general formula I-XII that contain a diazepine or diazepinone nucleus fused to a 1,4- dihydropyridine nucleus, in which the A ring is a substituted or unsubstituted benzene, pyridine or pyrimidine ring. Said molecular entities exhibit GABAergica and modulating action in the case of calcium channels which can be used in the treatment of cardiovascular, cerebrovascular, neurodegenerative, neuropsychiatric and neurological disorders.
机译:本发明涉及化学和药学,特别是涉及与1,4-二氢吡啶衍生物融合的新型分子实体,苯并二氮杂,、吡啶二氮杂and和嘧啶二氮杂type型的三环和四环衍生物,其对中枢神经和血管系统。通过与邻苯二胺,邻二氨基吡啶和邻二氨基嘧啶类型的化合物反应,使用含有二氢吡啶环的衍生物,以及随后的转化为其中的一些,以获得通式I-XII的三环和四环衍生物,其含有与1,4-二氢吡啶核稠合的二氮杂或二氮杂酮核,其中A环是取代或未取代的苯,吡啶或嘧啶环。所述分子实体在钙通道的情况下显示出GABAergica和调节作用,其可用于治疗心血管,脑血管,神经退行性疾病,神经精神病学和神经疾病。

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