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14,15-DIHYDRO-20,21-DINOREBURNAMENINE-14-OL DERIVATIVES AND THEIR USE

机译:14,15-二氢-20,21-丁诺丁宁-14-OL衍生物及其用途

摘要

The invention relates to novel derivatives of 14,15-dihydro 20,21-dinoreburnamenin-14-ol, having formula (I) in which R represents a radical -AR' wherein A represents a heteroatom and R' represents a group selected from the group comprising linear or branched CSUB1/SUB-CSUB6 /SUBalkyl radicals, CSUB2/SUB-CSUB6 /SUBalkenyls, CSUB2/SUB-CSUB6 /SUBalkynyls, arylalkyls; esters comprising the formula -RSUB1/SUB- CO-O-RSUB2/SUB; amides comprising the formula -RSUB3/SUB-CO-NZY, wherein Y and Z together can form a cycloalkyl radical or a heterocyclic radical, optionally substituted by one or more alkyl radicals; a radical selected from the group comprising alkyl radicals, alkenyls or alkynyls, substituted by at least one amine with formula -NZY; or one of the pharmaceutically-acceptable salts thereof, including the isomers, enantiomers and diastereoisomers thereof and mixtures thereof. The invention also relates to the use of the novel derivatives for the preparation of a pharmaceutical composition which is intended, in particular, for the treatment and/or prevention of depression, sleep-wake cycle disorders and symptomatic frontal disorders in cognitive components among humans.
机译:本发明涉及具有式(I)的14,15-二氢20,21-dinoreburnamenin-14-ol的新衍生物,其中R代表基团-AR′,其中A代表杂原子,R′代表选自下组的基团:包括直链或支链C 1 -C 6 烷基,C 2 -C 6 烯基,C < SUB> 2 -C 6 炔基,芳烷基;式-R 1 -CO-O-R 2 的酯;包含式-R 3 -CO-NZY的酰胺,其中Y和Z一起可以形成环烷基或杂环基,任选地被一个或多个烷基取代;选自由至少一个具有式-NZY的胺取代的烷基,烯基或炔基的基团;或其药学上可接受的盐之一,包括其异构体,对映异构体和非对映异构体及其混合物。本发明还涉及所述新型衍生物在制备药物组合物中的用途,所述药物组合物特别用于治疗和/或预防人的认知成分中的抑郁,睡眠-觉醒周期障碍和症状性额叶障碍。

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