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    Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol and applications thereof
    1.
    发明授权
    Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol and applications thereof 失效
    14.15-二氢20.21-二烧烤蛋白-14-醇的衍生物及其应用

    公开(公告)号：US07354918B2

    公开(公告)日：2008-04-08

    申请号：US11581950

    申请日：2006-10-13

    申请人： Paola Ciapetti ,  Laurence Deyon ,  Camille-Georges Wermuth ,  Jean-François Pujol ,  Dinah Weissmann

    发明人： Paola Ciapetti ,  Laurence Deyon ,  Camille-Georges Wermuth ,  Jean-François Pujol ,  Dinah Weissmann

    IPC分类号： A61K31/5377 ,  A61K31/4375 ,  C07D413/14 ,  C07D471/22

    CPC分类号： C07D461/00

    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 C1-C6 alkyl radicals, C2-C6 alkenyls, C2-C6 alkynyls, arylalkyls; esters comprising the formula —R1— CO—O—R2; amides comprising the formula —R3—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.

    摘要翻译： 本发明涉及具有式（I）的式14所示的衍生物，其中R表示自由基-AR'，其中A表示杂原子，R'表示选自 包括直链或支链C 1 -C 6烷基，C 2 -C 6亚烷基，C 2 -C 6亚烷基， C 2 -C 6炔基，芳基烷基; 包含式-R 1 -CO-O-R 2的酯; 酰胺，其包含式-NR 3 -CO-NZY，其中Y和Z一起可以形成任选被一个或多个烷基取代的环烷基或杂环基; 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，对映体和非对映异构体及其混合物。 本发明还涉及新型衍生物用于制备药物组合物的用途，其特别用于治疗和/或预防人类中认知成分中的抑郁症，睡眠 - 苏醒循环障碍和症状性前额症。