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    Non-steroidal progesting
    4.
    发明授权
    Non-steroidal progesting 失效
    非甾体类孕酮

    公开(公告)号：US07388006B2

    公开(公告)日：2008-06-17

    申请号：US10384775

    申请日：2003-03-11

    申请人： Norbert Schmees ,  Manfred Lehmann ,  Ulrike Fuhrmann ,  Peter Muhn ,  Christa Hegele-Hartung ,  Michael Klotzbuecher

    发明人： Norbert Schmees ,  Manfred Lehmann ,  Ulrike Fuhrmann ,  Peter Muhn ,  Christa Hegele-Hartung ,  Michael Klotzbuecher

    IPC分类号： A61K31/502 ,  A61K31/536 ,  C07D237/32 ,  C07D265/02

    CPC分类号： C07D307/88 ,  A61K31/365 ,  A61K31/535 ,  A61K31/565 ,  C07D265/02 ,  A61K2300/00

    摘要： The present invention relates to non-steroidal progestins of the general formula (I) wherein R1 and R2 are independently of each other —H or —F, R3 is —CH3 or —CF3, and Ar is or a pharmaceutically acceptable derivative or analogue thereof. These progestins are suitable for selectively modulating progesterone receptor mediated effects in different target tissues, particularly in uterine tissue versus breast tissue. Therefore, the progestins of the present invention, optionally in combination with estrogens, may be used for contraception (in particular in estrogen-free oral contraceptives), hormone replacement therapy and the treatment of gynecological disorders. The present invention furthermore relates to methods for selectively modulating progesterone receptor mediated effects in different target tissues or organs.

    摘要翻译： 本发明涉及通式（I）的非甾体孕激素，其中R 1和R 2各自独立地为-H或-F，R SUB > 3是-CH 3或-CF 3 N，Ar是其药学上可接受的衍生物或类似物。 这些孕激素适合于在不同的靶组织中，特别是在子宫组织与乳腺组织中选择性调节孕激素受体介导的作用。 因此，本发明的孕激素，任选地与雌激素组合，可用于避孕（特别是无雌激素的口服避孕药），激素替代疗法和妇科疾病的治疗。 本发明还涉及用于在不同靶组织或器官中选择性调节孕酮受体介导的作用的方法。

    SUBSTITUTED ESTRATRIENES AS SELECTIVELY ACTIVE ESTROGENS
    5.
    发明申请
    SUBSTITUTED ESTRATRIENES AS SELECTIVELY ACTIVE ESTROGENS 审中-公开
    取代的ESTRATRIRIES作为选择性活动的ESTROGENS

    公开(公告)号：US20080132476A1

    公开(公告)日：2008-06-05

    申请号：US12027618

    申请日：2008-02-07

    申请人： Dirk KOSEMUND ,  Gerd Mueller ,  Alexander Hillisch ,  Karl-Heinrich Fritzemeier ,  Peter Muhn

    发明人： Dirk KOSEMUND ,  Gerd Mueller ,  Alexander Hillisch ,  Karl-Heinrich Fritzemeier ,  Peter Muhn

    IPC分类号： A61K31/56 ,  A61P19/08 ,  A61P15/08 ,  A61P5/24 ,  A61P15/02 ,  A61P19/02 ,  A61P17/06 ,  A61P9/00 ,  A61P9/12 ,  A61P25/28

    CPC分类号： C07J41/00 ,  Y10S514/825 ,  Y10S514/843

    摘要： This invention describes the new 9α-substituted estratrienes of general formula I in which R3, R7, R7′, R13, R16 as well as R17 and R17′ have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds.The invention also describes the use of these compounds for treating estrogen-deficiency-induced diseases and conditions.

    摘要翻译： 本发明描述了通式I的新的9α-取代的雌三烯，其中R 3，R 7，R 7'，R“ 13，R 16以及R 17和R 17'具有在说明书中指出的含义， 是指直链或支链，任选部分或完全卤化的具有2-6个碳原子的烯基，乙炔基或丙-1-炔基，作为在体外表现出的药物活性成分 对来自大鼠前列腺的雌激素受体制剂的亲和力高于来自大鼠子宫内和体内的雌激素受体制剂的亲和力，优选与子宫相比优于子宫，其生产，其治疗用途和含有新化合物的药物分配形式的优选作用。 本发明还描述了这些化合物用于治疗雌激素缺乏诱导的疾病和病症的用途。

    9-α-substituted estratrienes as selectively active estrogens
    7.
    发明授权
    9-α-substituted estratrienes as selectively active estrogens 失效
    9-α-取代的雌三醇作为选择性活性雌激素

    公开(公告)号：US07414043B2

    公开(公告)日：2008-08-19

    申请号：US10458735

    申请日：2003-06-11

    申请人： Dirk Kosemund ,  Gerd Mueller ,  Alexander Hillisch ,  Karl-Heinrich Fritzemeier ,  Peter Muhn

    发明人： Dirk Kosemund ,  Gerd Mueller ,  Alexander Hillisch ,  Karl-Heinrich Fritzemeier ,  Peter Muhn

    IPC分类号： A61K31/56 ,  C07J1/00

    CPC分类号： C07J41/00 ,  Y10S514/825 ,  Y10S514/843

    摘要： This invention describes the new 9α-substituted estratrienes of general formula I in which R3, R7, R7′, R13, R16 as well as R17 and R17′ have the meanings that are indicated in the description and R9 means a straight-chain or branched-chain, optionally partially or completely halogenated alkenyl radical with 2 to 6 carbon atoms, an ethinyl or prop-1-inyl radical, as pharmaceutical active ingredients that exhibit in vitro a higher affinity to estrogen receptor preparations from rat prostates than to estrogen receptor preparations from rat uteri and in vivo preferably a preferential action on the ovary in comparison to the uterus, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treating estrogen-deficiency-induced diseases and conditions.

    摘要翻译： 本发明描述了通式I的新的9α-取代的雌三烯，其中R 3，R 7，R 7'，R“ 13，R 16以及R 17和R 17'具有在说明书中指出的含义， 是指具有2-6个碳原子的直链或支链，任选部分或完全卤化的烯基，乙炔基或丙-1-茚基，作为在体外表现出的药物活性成分 对来自大鼠前列腺的雌激素受体制剂的亲和力高于来自大鼠子宫内和体内的雌激素受体制剂的亲和力，优选与子宫相比优于子宫，其生产，其治疗用途和含有新化合物的药物分配形式的优选作用。 本发明还描述了这些化合物用于治疗雌激素缺乏诱导的疾病和病症的用途。