发明公开
EP0920441A1 7ALPHA-(EPSILON-AMINOALKYL)-ESTRATRIENE, VERFAHREN ZU DEREN HERSTELLUNG, PHARMAZEUTISCHE PRÄPARATE, DIE DIESE 7ALPHA-(EPSILON-AMINOALKYL)-ESTRATRIENE ENTHALTEN SOWIE DEREN VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN
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7ALPHA-(ε-己氨基烷基) - 雌三烯,PROCESS FOR PRODUCING药物制剂THAT THIS 7ALPHA-(ε-己氨基烷基) - 雌三烯容纳和它们在药物的生产
- 专利标题: 7ALPHA-(EPSILON-AMINOALKYL)-ESTRATRIENE, VERFAHREN ZU DEREN HERSTELLUNG, PHARMAZEUTISCHE PRÄPARATE, DIE DIESE 7ALPHA-(EPSILON-AMINOALKYL)-ESTRATRIENE ENTHALTEN SOWIE DEREN VERWENDUNG ZUR HERSTELLUNG VON ARZNEIMITTELN
- 专利标题(英): 7alpha-(epsilon-aminoalkyl)-estratrienes, process for preparing the same, pharmaceutical preparations containing said 7alpha-(epsilon-aminoalkyl)-estratrienes and their use for preparing medicament
- 专利标题(中): 7ALPHA-(ε-己氨基烷基) - 雌三烯,PROCESS FOR PRODUCING药物制剂THAT THIS 7ALPHA-(ε-己氨基烷基) - 雌三烯容纳和它们在药物的生产
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申请号: EP97943814.0申请日: 1997-08-20
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公开(公告)号: EP0920441A1公开(公告)日: 1999-06-09
- 发明人: BOHLMANN, Rolf , BITTLER, Dieter , HEINDI, Josef , HEINRICH, Nikolaus , HOFMEISTER, Helmut , KÜNZER, Hermann , SAUER, Gerhard , HEGELEHARTUNG, Christa , LICHTNER, Rosemarie , NISHINO, Yukishige , PARCZYK, Karsten , SCHNEIDER, Martin
- 申请人: SCHERING AKTIENGESELLSCHAFT
- 申请人地址: Müllerstrasse 170/178 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 170/178 13353 Berlin DE
- 优先权: DE19961035525 19960820
- 国际公布: WO1998007740 19980226
- 主分类号: A61K31
- IPC分类号: A61K31 ; A61P5 ; C07J41 ; C07J43 ; C07J53
摘要:
The present invention describes new substituted 7α-(κ-aminoalkyl)-estratrienes of general formula (I), in which the side chain SK is a radical of partial formula (II), where m equals 4, 5 or 6; n equals 0, 1 or 2; x equals 0, 1 or 2; A is a hydrogen atom or a C1-5-alkyl group; B and D represent each a hydrogen atom, or A and B represent together an alkylene group -(CH2)p- where p = 2, 3, 4 or 5 and D is a hydrogen atom, or A and D form together an alkylene group -(CH2)q- where q = 2, 3 or 4 and B is a hydrogen atom; and E is a non-substituted ethyl radical or an ethyl radical fluorinated one to five times; or the terminal substituent -(CH2)3-E in the side chain is substituted by an optionally substituted aryl or heteroaryl radical bonded to the sulphur atom directly or by a mono-, di- or trimethylene group; R3 is a hydrogen atom, a hydrocarbon radical with up to 8 carbon atoms or a radical of partial formula R3'-C(O)-, where R3' is a hydrogen atom or a hydrocarbon radical with up to 8 carbon atoms or a phenyl radical; R11 is a hydrogen atom, a halogen atom or a nitrooxy group -O-NO¿2?, R?14, R15α, R15β, R16α and R16β¿ represent each a hydrogen atom or R?14 and R15α¿ are an additional bond or a methylene bridge, or R15β is a methyl group and R15α is a hydrogen atom, R?15α and R15β¿ represent each a methyl group, or R?15β and R16β¿ form together a methylene bridge, or R?16α or R16β¿ are a halogen atom or R?16α and R16β¿ form together a methylidene group, and the remaining substitutents R?14, R15α, R15β, R16α and R16β¿ represent each a hydrogen atom, R17' at the α- or β-position is a hydrogen atom, a C¿1-5? alkyl, C2-5 alkenyl or C2-5 alkinyl group or a trifluoromethyl group; and R?17'¿ is a hydrogen atom or a radical of partial formula R17'''-C(O)-, where R17''' is a hydrogen atom or a hydrocarbon radical with up to 8 carbon atoms, or when R17' is at the α-position, R17' forms together with R14 an ethano bridge, provided that when A and B do not stand together for -(CH¿2?)p- or A and D stand together for -(CH2)q-, at least one of the substituents R?11, R14, R15α, R15β, R16α and R16b¿ be not a hydrogen atom. Also disclosed are the physiologically tolerable addition salts of these compounds with organic and inorganic acids. These new compounds have a very strong anti-estrogenic activity. Some of them are pure anti-estrogenes, others are anti-estrogenes with a partial estrogenic effect. Because of their spectrum of activity, these new compounds are most suitable for preparing medicaments for tumor therapy and hormone substitution therapy.
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