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    • 2. 发明授权
    • 9-α-substituted estratrienes as selectively active estrogens
    • 9-α-取代的雌三醇作为选择性活性雌激素
    • US07414043B2
    • 2008-08-19
    • US10458735
    • 2003-06-11
    • Dirk KosemundGerd MuellerAlexander HillischKarl-Heinrich FritzemeierPeter Muhn
    • Dirk KosemundGerd MuellerAlexander HillischKarl-Heinrich FritzemeierPeter Muhn
    • A61K31/56C07J1/00
    • C07J41/00Y10S514/825Y10S514/843
    • 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.
    • 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。