发明授权
EP1272505B1 8BETA-SUBSTITUIERTE-11BETA-PENTYL-UND 11BETA-HEXYL-ESTRA-1,3,5(10)-TRIENDERIVATE
有权
8BETA-SUBSTITUIERTE-11BETA-PENTYL-UND 11BETA-HEXYL-ESTRA-1,3,5(10)-TRIENDERIVATE
- 专利标题: 8BETA-SUBSTITUIERTE-11BETA-PENTYL-UND 11BETA-HEXYL-ESTRA-1,3,5(10)-TRIENDERIVATE
- 专利标题(英): 8beta-substituted-11beta-pentyl- and 11beta-hexyl-estra-1,3,5(10)-triene derivatives
- 专利标题(中): 8BETA-SUBSTITUIERTE-11BETA-PENTYL-UND 11BETA-HEXYL-ESTRA-1,3,5(10)-TRIENDERIVATE
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申请号: EP01940331.0申请日: 2001-04-12
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公开(公告)号: EP1272505B1公开(公告)日: 2005-08-24
- 发明人: PETERS, Olaf , BRAEUER, Nico , HILLISCH, Alexander , HEGELE-HARTUNG, Christa , 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: DE10019167 20000412; US207370P 20000526
- 国际公布: WO2001077138 20011018
- 主分类号: C07J1/00
- IPC分类号: C07J1/00 ; A61K31/565 ; C07J41/00 ; A61P5/30
摘要:
The present invention relates to the novel 8β-substituted estradienes of general formula (I), wherein R?2, R3, R6, R6", R7, R7", R14, R15, R15", R16, R16", R17 and R17"¿ have the meanings given in the description, R8 means a straight-chain or branched-chain, optionally partially or entirely halogenated alkyl or alkenyl radical having up to 5 carbon atoms, an ethynyl or prop-1-inyl radical and R11 means an n-pentyl- or n-hexyl radical. Said estradienes are used as pharmaceutical active agents which, in vitro, are provided with a higher affinity of estrogen receptor preparations of rat prostate than of estrogen receptor preparations of rat uterus and, in vivo, preferably act in a preferential contraceptive manner on the ovary without stimulating the uterus. The invention also relates to the production thereof, the therapeutic use thereof and pharmaceutical administration forms which contain the novel compounds. The invention further relates to the use of said compounds for male contraception and to the use of non-malignant or malignant proliferate diseases of the ovary, such as ovarian carcinoma or granulosa cell tumours for instance.
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