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

    公开(公告)号：US20030229059A1

    公开(公告)日：2003-12-11

    申请号：US10397854

    申请日：2003-03-27

    申请人： Schering AG

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

    IPC分类号： A61K031/585 ,  C07J017/00

    CPC分类号： C07J17/00

    摘要： This invention relates to new 19-nor-17null-pregna-1,3,5(10)-trien-17null-ols with a 21,16null-lactone ring with a long-chain substituent in 11null-position of general formula II 1 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具有在说明书中更详细说明的含义。 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。

    9-alpha-substituted estratrienes as selectively active estrogens
    2.
    发明申请
    9-alpha-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：US20040087565A1

    公开(公告)日：2004-05-06

    申请号：US10458735

    申请日：2003-06-11

    申请人： Schering AG

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

    IPC分类号： A61K031/56 ,  C07J041/00

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

    摘要： This invention describes the new 9null-substituted estratrienes of general formula I 1 in which R3, R7, R7null, R13, R16 as well as R17 and R17null 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9-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， 17'具有在说明书中指出的含义，R 9表示具有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 作为药物活性成分，其在体外具有比来自大鼠前列腺素的雌激素受体制剂更高的亲和力，而不是雌激素受体制剂从大鼠子宫和体内表现出优于子宫与子宫，其生产，其治疗用途相比的优先作用， 含有新化合物的药物分配形式。 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。