发明公开
EP0095875A2 Novel tri-phenyl alkane and alkene derivatives and their preparation and use
失效
三苯基烷烃 -alkenderivate，ihre Herstellung und Verwendung。
- 专利标题： Novel tri-phenyl alkane and alkene derivatives and their preparation and use
- 专利标题（中）： 三苯基烷烃 -alkenderivate，ihre Herstellung und Verwendung。
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申请号： EP83302912.7申请日： 1983-05-20
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公开(公告)号： EP0095875A2公开(公告)日： 1983-12-07
- 发明人: Toivola, Reijo Juhani , Karjalainen, Ario Johannes , Kurkela, Kauko Oiva Antero , Soderwall, Marja-Liisa , Kangas, Lauri Veikko Matti , Blanco, Guillermo Luis , Sundquist, Hannu Kalervo
- 申请人： Farmos Group Ltd.
- 申请人地址： Tengströminkatu 6 P.O. Box 425 SF-20101 Turku 10 FI
- 专利权人： Farmos Group Ltd.
- 当前专利权人： Farmos Group Ltd.
- 当前专利权人地址： Tengströminkatu 6 P.O. Box 425 SF-20101 Turku 10 FI
- 代理机构： Collier, Jeremy Austin Grey (GB)
- 优先权： FI821879 19820527; GB8218414 19820625
- 主分类号： C07C33/26
- IPC分类号： C07C33/26 ; C07C33/28 ; C07C39/14 ; C07C39/15 ; A61K31/34 ; C07C39/17 ; C07C43/23 ; C07C69/157 ; C07C69/78 ; C07C93/06 ; C07C143/68
摘要：
The invention provides novel compounds of the formula:
and
wherein m is 1 or 2, R 6 and R 7 , which can be the same or different are H or an alkyl group of 1 to 4 carbon atoms, or
wherein n is 0 to 4, R 1 and R 2 , which can be the same or different are H, OH, alkoxy of 1 to 4 carbon atoms, benzyloxy or methoxymethoxy; R 3 is H, OH, halogen, alkoxy of 1 to 4 carbon atoms, benzyloxy, methoxymethoxy, 2,3-dihydroxypropoxy or
can form an N-containing three-, four-, five- or six-membered heterocyclic ring; R 4 is OH, F, Cl, Br, I, mesyloxy, tosyloxy, formyloxy, alkylcarbonyloxy of 1 to 4 carbon atoms or CH 2 R 4 is replaced by CHO; R 5 is H or OH; or R 4 and R 5 together form an -0- bridge between the carbon atoms to which they are attached, and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof. Processes for the preparation of these compounds are described, and also novel pharmaceutical compositions containing them. These compounds exhibit valuable pharmacological properties as estrogenic, anti-estrogenic, and progestanic agents. They are also effective against oestrogen-dependent tumours. Certain compounds are useful as chemical intermediates for the preparation of pharmacologically active compounds of the invention.
and
wherein m is 1 or 2, R 6 and R 7 , which can be the same or different are H or an alkyl group of 1 to 4 carbon atoms, or
wherein n is 0 to 4, R 1 and R 2 , which can be the same or different are H, OH, alkoxy of 1 to 4 carbon atoms, benzyloxy or methoxymethoxy; R 3 is H, OH, halogen, alkoxy of 1 to 4 carbon atoms, benzyloxy, methoxymethoxy, 2,3-dihydroxypropoxy or
can form an N-containing three-, four-, five- or six-membered heterocyclic ring; R 4 is OH, F, Cl, Br, I, mesyloxy, tosyloxy, formyloxy, alkylcarbonyloxy of 1 to 4 carbon atoms or CH 2 R 4 is replaced by CHO; R 5 is H or OH; or R 4 and R 5 together form an -0- bridge between the carbon atoms to which they are attached, and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof. Processes for the preparation of these compounds are described, and also novel pharmaceutical compositions containing them. These compounds exhibit valuable pharmacological properties as estrogenic, anti-estrogenic, and progestanic agents. They are also effective against oestrogen-dependent tumours. Certain compounds are useful as chemical intermediates for the preparation of pharmacologically active compounds of the invention.
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