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    SUBSTITUTED ESTRATRIENES AS SELECTIVELY ACTIVE ESTROGENS
    1.
    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
    2.
    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。

    11β-long-chain-substituted 19-nor-17α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring
    7.
    发明授权
    11β-long-chain-substituted 19-nor-17α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring 失效
    具有21,16α-内酯环的11β-长链取代的19-去甲-17α-前 - 1,3,5（10） - 三烯-17β-

    公开(公告)号：US07119082B2

    公开(公告)日：2006-10-10

    申请号：US10397854

    申请日：2003-03-27

    申请人： Gerd Mueller ,  Jens Hoffmann ,  Karl-Heinrich Fritzemeier ,  Alexander Hillisch

    发明人： Gerd Mueller ,  Jens Hoffmann ,  Karl-Heinrich Fritzemeier ,  Alexander Hillisch

    IPC分类号： A61K31/58 ,  C07J71/00

    CPC分类号： C07J17/00

    摘要： This invention relates to new 19-nor-17α-pregna-1,3,5(10)-trien-17β-ols with a 21,16α-lactone ring with a long-chain substituent in 11β-position of general formula II in which R11 means a straight-chain alkyl radical with 6 to 17 carbon atoms, and R3 and R13 have the meanings that are explained in more detail in the description. The compounds act in a tissue-selective manner as pure antiestrogens and are suitable for the production of pharmaceutical agents because of these properties.

    摘要翻译： 本发明涉及具有21,16α-内酯环的新的19-nor-17α-前 - 1,3,5（10） - 三烯-17β-环，其通式II在11b位具有长链取代基 其中R 11表示具有6至17个碳原子的直链烷基，R 3和R 13和R 13具有所述的含义 在描述中更详细。 化合物以组织选择性的方式作为纯抗雌激素起作用，并且由于这些性质而适用于制药。

    Prodrugs of ERbeta-selective substances, processes for their preparation and pharmaceutical compositions comprising these compounds
    8.
    发明申请
    Prodrugs of ERbeta-selective substances, processes for their preparation and pharmaceutical compositions comprising these compounds 审中-公开
    ERbeta选择性物质的前体药物，其制备方法和包含这些化合物的药物组合物

    公开(公告)号：US20070123500A1

    公开(公告)日：2007-05-31

    申请号：US11604891

    申请日：2006-11-28

    申请人： Gerd Mueller ,  Dirk Kosemund ,  Ralf Wyrwa

    发明人： Gerd Mueller ,  Dirk Kosemund ,  Ralf Wyrwa

    IPC分类号： A61K31/56 ,  C07J1/00

    CPC分类号： C07J1/00

    摘要： The present invention makes available prodrugs of 9α-substituted oestratrienes of the general formula (I) in which the group Z is bonded to the steroid, processes for their preparation, pharmaceutical compositions which comprise these compounds and use thereof. The compounds of the general formula I according to the invention do not bind to the oestrogen receptor a and/or β. They bind to carboanhydrases and inhibit these enzymes.

    摘要翻译： 本发明提供了通式（I）的9α-取代的邻三烯的前药，其中基团Z与类固醇结合，其制备方法，包含这些化合物的药物组合物及其用途。 根据本发明的通式I的化合物不结合雌激素受体a和/或β。 它们与碳水解酶结合并抑制这些酶。