Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol and applications thereof
    8.
    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

    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。

    Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol, and applications thereof
    9.
    发明申请
    Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol, and applications thereof 失效
    14.15-二氢20.21-二辛氨in -14-醇的衍生物及其应用

    公开(公告)号:US20070088046A1

    公开(公告)日:2007-04-19

    申请号:US11581950

    申请日:2006-10-13

    IPC分类号: A61K31/4745 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。