发明公开
- 专利标题: 18-NOR-STEROIDE ALS SELEKTIV WIRKSAME ESTROGENE
- 专利标题(英): 18-nor-steroids as selectively active estrogens
- 专利标题(中): 18-NOR类固醇AS选择性有效的雌激素
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申请号: EP00981233.0申请日: 2000-11-02
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公开(公告)号: EP1226155A2公开(公告)日: 2002-07-31
- 发明人: HILLISCH, Alexander , BOIDOL, Werner , SCHWEDE, Wolfgang , ESPERLING, Peter , SAUER, Gerhard , HEGELE-HARTUNG, Christa , KOLLENKIRCHEN, Uwe , FRITZEMEIER, Karl-Heinrich
- 申请人: Schering Aktiengesellschaft
- 申请人地址: Müllerstrasse 178 13353 Berlin DE
- 专利权人: Schering Aktiengesellschaft
- 当前专利权人: Schering Aktiengesellschaft
- 当前专利权人地址: Müllerstrasse 178 13353 Berlin DE
- 优先权: DE19954105 19991102; US188197P 20000310
- 国际公布: WO0132680 20010510
- 主分类号: C07J1/00
- IPC分类号: C07J1/00 ; A61K31/565
摘要:
The invention relates to novel 18-norsteroids (gonatrienes) of general formula (I), wherein R?1, R2, R3, R6, R7, R8, R9, R11, R11", R14, R15, R15", R16, R17 and R17"¿ have the meaning cited in the description, and to the use of said compounds as pharmaceutical active ingredients. Said compounds exhibit a high affinity in vitro for estrogen receptor preparations of rat prostate and in an estrogen receptor preparation of rat uterus. Said compounds exhibit in vivo preferential activity on bones as compared to the uterus and/or significant activity with regard to stimulating the expression of 5HT2a-receptors and transporter molecules. The invention also relates to the production of said compounds, therapeutic use and galenic form of said compounds contained in the novel compounds of invention. The invention also relates to utilization of steroids based on the gonatriene molecular skeleton in order to treat estrogen deficiency-induced diseases and disorders, in addition to the use of said gonatriene structural component in the total structure of compounds which dissociate to produce enhanced estrogen activity in bone as compared to the uterus.
公开/授权文献
- EP1226155B1 18-NOR-STEROIDE ALS SELEKTIV WIRKSAME ESTROGENE 公开/授权日:2007-05-02
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