发明名称 8 Beta-hydrocarbyl-substituted estratrienes for use as selective estrogens
摘要 This invention describes the new 8beta-substituted estratrienes of general formula I in which R2, R3, R6, R6', R7, R7', R9, R11, R11', R12, R14, R15, R15', R16, R16', R17 and R17' have the meanings that are indicated in the description, and R8 means a straight-chain or branched-chain, optionally partially or completely halogenated alkyl or alkenyl radical with up to 5 carbon atoms, an ethinyl- or prop-1-inyl radical, as pharmaceutical active ingredients that have in vitro a higher affinity to estrogen receptor preparations of rat prostates than to estrogen receptor preparations of rat uteri and in vivo preferably a preferential action on bone rather than the uterus and/or a pronounced action with respect to stimulation of the expression of 5HT2a-receptors and 5HT2a-transporters, their production, their therapeutic use and pharmaceutical dispensing forms that contain the new compounds. The invention also describes the use of these compounds for treatment of estrogen-deficiency-induced diseases and conditions as well as the use of an 8beta-substituted estratriene structural part in the total structures of compounds that have a dissociation in favor of their estrogenic action on bones rather than the uterus.
申请公布号 US2003176405(A1) 申请公布日期 2003.09.18
申请号 US20030257288 申请日期 2003.04.01
申请人 PETERS OLAF;HILLISCH ALEXANDER;THIEME INA;ELGER WALTER;HEGELE-HARTUNG CHRISTA;KOLLENKIRCHEN UWE;FRITZEMEIER KARL-HEINRICH;PATCHEV VLADIMIR 发明人 PETERS OLAF;HILLISCH ALEXANDER;THIEME INA;ELGER WALTER;HEGELE-HARTUNG CHRISTA;KOLLENKIRCHEN UWE;FRITZEMEIER KARL-HEINRICH;PATCHEV VLADIMIR
分类号 A61K31/565;A61K31/566;A61K31/567;A61P1/04;A61P5/00;A61P5/24;A61P5/30;A61P5/32;A61P7/04;A61P9/00;A61P9/10;A61P9/12;A61P9/14;A61P13/00;A61P13/08;A61P15/00;A61P15/02;A61P15/08;A61P15/12;A61P15/16;A61P15/18;A61P19/08;A61P19/10;A61P25/00;A61P25/18;A61P25/20;A61P25/28;A61P29/00;A61P35/00;A61P37/00;A61P39/00;A61P43/00;C07J1/00;C07J41/00;(IPC1-7):A61K31/58;A61K31/56;C07J43/00;C07J31/00 主分类号 A61K31/565
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