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126 条记录 (耗时 0.061 秒)

    Cyanopyrroles
    17.
    发明申请
    Cyanopyrroles 有权
    青色

    公开(公告)号：US20050256110A1

    公开(公告)日：2005-11-17

    申请号：US11184313

    申请日：2005-07-19

    申请人： Mark Collins ,  Valerie Mackner ,  Jay Wrobel ,  Lin Zhi ,  Todd Jones ,  James Edwards ,  Christopher Tegley

    发明人： Mark Collins ,  Valerie Mackner ,  Jay Wrobel ,  Lin Zhi ,  Todd Jones ,  James Edwards ,  Christopher Tegley

    IPC分类号： C07D403/04 ,  A61K31/40 ,  A61K31/403 ,  A61K31/404 ,  A61K31/405 ,  A61K31/536 ,  A61K31/5415 ,  A61P5/34 ,  A61P13/08 ,  A61P15/00 ,  A61P15/14 ,  A61P15/16 ,  A61P15/18 ,  A61P35/00 ,  A61P43/00 ,  C07D413/04

    CPC分类号： C07D403/04 ,  A61K31/405 ,  A61K31/5415 ,  C07D413/04

    摘要： This invention provides a progesterone receptor antagonist of formula 1 having the structure wherein, T is O, S, or absent; R1, and R2 are each, independently, hydrogen, alkyl, substituted alkyl; or R1 and R2 are taken together form a ring and together contain —CH2(CH2)nCH2—, —CH2CH2CMe2CH2CH2—, —O(CH2)pCH2—, —O(CH2)qO—, —CH2CH2OCH2CH2—, or —CH2CH2NR7CH2CH2—; n=1-5; p=1-4; q=1-4; R3 is hydrogen, OH, NH2, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, or CORA; RA is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R4 is hydrogen, halogen, CN, NH2, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R5 is hydrogen, alkyl, or substituted alkyl; R6 is hydrogen, alkyl, substituted alkyl, or CORB; RB is hydrogen, alkyl, substituted alkyl, alkoxy, substituted alkoxy, aminoalkyl, or substituted aminoalkyl; R7 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof.

    摘要翻译： 本发明提供具有以下结构的式1的孕酮受体拮抗剂，其中T为O，S或不存在; R 1，R 2和R 2各自独立地为氢，烷基，取代的烷基; 或R 1和R 2一起形成环，并且一起含有-CH 2（CH 2）2 CH 2 CH 2 - ， - CH 2 CH 2 CH 2 CH 2 N 2 CH 2 2 CH 2 - ， - O（CH 2）2 CH 2 - ， - （CH 2 CH 2） O（CH 2 CH 2）q O - ， - CH 2 CH 2 OCH 2 - / SUB CH 2，或CH 2 CH 2，NR 7，CH 2，CH 2， CH 2 - ; n = 1-5; p = 1-4; q = 1-4; R 3是氢，OH，NH 2，烷基，取代的烷基，烯基，取代的烯基，炔基，取代的炔基或COR A。 R A是氢，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的氨基烷基; R 4是氢，卤素，CN，NH 2，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的氨基烷基; R 5是氢，烷基或取代的烷基; R 6是氢，烷基，取代的烷基或COR B; R B是氢，烷基，取代的烷基，烷氧基，取代的烷氧基，氨基烷基或取代的氨基烷基; R 7是氢或烷基; 或其药学上可接受的盐。

    Combination regimens using progesterone receptor modulators
    18.
    发明授权
    Combination regimens using progesterone receptor modulators 失效
    使用孕酮受体调节剂的联合治疗方案

    公开(公告)号：US06759408B2

    公开(公告)日：2004-07-06

    申请号：US10141792

    申请日：2002-05-09

    申请人： Gary S. Grubb ,  Puwen Zhang ,  Eugene A. Terefenko ,  Andrew Fensome ,  Jay E. Wrobel ,  Horace Fletcher, III ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

    发明人： Gary S. Grubb ,  Puwen Zhang ,  Eugene A. Terefenko ,  Andrew Fensome ,  Jay E. Wrobel ,  Horace Fletcher, III ,  James P. Edwards ,  Todd K. Jones ,  Christopher M. Tegley ,  Lin Zhi

    IPC分类号： A61K31535

    CPC分类号： A61K31/535 ,  A61K31/56 ,  Y10S514/843 ,  A61K2300/00

    摘要： This invention relates to cyclic combination therapies and regimens utilizing substituted indoline derivative compounds which are antagonists of the progesterone receptor having the general structure: wherein R1 and R2 may be single substituents or fused; R3 is H, OH, NH2, C1 to C6 alkyl, CORC, or optionally substituted C1 to C6 alkyl, C3 to C6 alkenyl, or alkynyl; RC is H, or optionally substituted C1 to C3 alkyl, aryl, C1 to C3 alkoxy, or C1 to C3 aminoalkyl; R4 is H, halogen, CN, NO2, or optionally substituted C1 to C6 alkyl, alkynyl, C1 to C6 alkoxy, amino, or C1 to C6 aminoalkyl; and R5 is a benzene ring, a five or six membered heterocyclic ring; or pharmaceutically acceptable salt thereof. Methods of treatment include contraception, secondary amenorrhea, dysfunctional bleeding, uterine leiomyomata, endometriosis, polycystic ovary syndrome, carcinomas, adenocarcinomas minimization of side effects, or food intake stimulation.

    摘要翻译： 本发明涉及使用具有通式结构的孕酮受体的拮抗剂的取代的二氢吲哚衍生物化合物的环状组合疗法和方案：其中R 1和R 2可以是单个取代基或稠合的; R 3是H，OH，NH 2，C 1 -C 6烷基，COR C或任选取代的C 1 -C 6烷基，C 3至C 6烯基或炔基; R C是H或任选取代的C 1至C 3烷基，芳基，C 1至C 3烷氧基或C 1至C 3氨基烷基; R 4是H，卤素，CN，NO 2或任选取代的C 1至C 6烷基，炔基，C 1至C 6烷氧基，氨基或C 1至C 6氨基烷基; 和R 5为苯环，五或六元杂环; 或其药学上可接受的盐。 治疗方法包括避孕，继发性闭经，功能障碍性出血，子宫平滑肌瘤，子宫内膜异位症，多囊卵巢综合征，癌，腺癌最小化副作用或食物摄取刺激。