Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol, and applications thereof
    1.
    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。

    Derivatives of 14.15-dihydro 20.21-dinoreburnamenin-14-ol and applications thereof
    2.
    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。

    Imidazo [1,2-c] quinazoline compounds
    10.
    发明授权
    Imidazo [1,2-c] quinazoline compounds 失效
    咪唑(1,2-C)喹唑啉化合物

    公开(公告)号:US5128338A

    公开(公告)日:1992-07-07

    申请号:US666802

    申请日:1991-03-08

    CPC分类号: C07D487/04

    摘要: New imidazo [1,2-c] quinazoline compounds useful as coronary smooth muscle relaxants and corresponding to the formula: ##STR1## in which: Y is oxygen or sulfur;R.sub.1 is (C.sub.1 -C.sub.6) alkyl optionally substituted by a phenyl itself optionally substituted, a (C.sub.3 -C.sub.6) cycloalkyl, optionally substituted phenyl, furyl, thienyl or acyl;R.sub.2 is hydrogen, a halogen or a (C.sub.1 -C.sub.6) alkyl optionally substituted by amino or dialkylamino;R.sub.3 is hydrogen, (C.sub.1 -C.sub.6) alkyl optionally substituted by an aryl, or R--CO--(CH.sub.2).sub.n -- [n being 1, 2 or 3, and R being (C.sub.1 -C.sub.6) alkoxy, amino, (alkyl or dialkyl)amino, morpholino or methylpiperazinyl]; andX is hydrogen or a halogen.These compounds and their physiologically tolerated salts can be used in medical treatment of coronary smooth-muscle dysfunctions.

    摘要翻译: 新的咪唑并[1,2-c]喹唑啉化合物,可用作冠状平滑肌松弛剂,对应于下式:其中:Y为氧或硫; R 1是任选被苯基本身任选取代的(C 1 -C 6)烷基,(C 3 -C 6)环烷基,任选取代的苯基,呋喃基,噻吩基或酰基; R 2是氢,卤素或任选被氨基或二烷基氨基取代的(C 1 -C 6)烷基; R 3是氢,任选被芳基取代的(C 1 -C 6)烷基,或R-CO-(CH 2)n - [n是1,2或3,并且R是(C 1 -C 6)烷氧基,氨基,(烷基或 二烷基)氨基,吗啉代或甲基哌嗪基]; X是氢或卤素。 这些化合物及其生理耐受盐可用于治疗冠状动脉平滑肌功能障碍。