发明授权
EP1140972B1 NEUE 7-ALPHA,17-ALPHA-BIS-ALKYLIERTE TESTOSTERONDERIVATE UND IHRE VERWENDUNG ZUR LANGZEITTHERAPIE VON ANDROGEN-ABHÄNGIGEN ERKRANKUNGEN
有权
NEW 7-α,17-α-二TO-烷基化睾酮衍生物及其使用雄激素依赖性疾病的长期治疗
- 专利标题: NEUE 7-ALPHA,17-ALPHA-BIS-ALKYLIERTE TESTOSTERONDERIVATE UND IHRE VERWENDUNG ZUR LANGZEITTHERAPIE VON ANDROGEN-ABHÄNGIGEN ERKRANKUNGEN
- 专利标题(英): New 7-alpha, 17-alpha-bis-alkylated testosterone derivatives and their use in long-term therapy of androgen-dependent diseases
- 专利标题(中): NEW 7-α,17-α-二TO-烷基化睾酮衍生物及其使用雄激素依赖性疾病的长期治疗
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申请号: EP99967003.7申请日: 1999-12-23
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公开(公告)号: EP1140972B1公开(公告)日: 2003-03-05
- 发明人: CLEVE, Arwed , SAUER, Gerhard , HUWE, Christoph , PARCZYK, Karsten , HOFFMANN, Jens , SCHNEIDER, Martin
- 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: DE19860719 19981223
- 国际公布: WO00039148 20000706
- 主分类号: C07J1/00
- IPC分类号: C07J1/00 ; A61K31/565 ; C07J31/00 ; C07J41/00 ; C07J43/00 ; C07J33/00 ; C07J51/00
摘要:
The invention relates to new 7 alpha , 17 alpha , 17 beta -substituted testosterone derivatives of general formula (I) and their use as pure antiandrogens for the long-term therapy of androgen-dependent diseases, notably for the long-term antiandrogen therapy of prostate carcinoma. In the general formula (I) A is an unbranched C6-C13-alkylene group; B is an oxygen atom, -S(O)p- group, in which p is 0, 1 or 2, an iminocarbonyl group -C(O)N(Y)-, an imino group -N(Y)-, a carbonylimino group -N(Y)C(O)-, a sulfonylimino group -NN(Y)S(O)2-, where Y is a hydrogen atom or a C1-C8-alkyl group, a sulfonyloxy group -OS(O)2-, a dimethylsilyloxy group -O--Si(CH3)2- or a carbonylsulfanyl group -SC(O)- or a bond between A and C or, together with C, a bond between A and D; C is a bond between B and D or, together with B, a bond between A and D or an unbranched C1-C6-alkylene group, a phenylene group, a substituted phenylene group, a five-membered ring or six-membered ring heteroarylene group, a substituted five-membered ring or six-membered ring heteroarylene group or a five-membered ring or six-membered ring heteroarylene group fused with a phenyl ring; and D is a hydrogen atom, a C1-C4-alkyl group, a vinyl group, a C1-C4-alkoxy group, a C1-C4-alkoxycarbonyl group, a bis(C1-C4-alkoxycarbonyl)methyl group, an acetyl(C1-C4-alkoxycarbonyl)methyl group, a cyan group, a carboxy group, an azide group, a hydroxy group, a halogen atom or a rest of the formula CnFmHo, in which n is 1, 2, 3 or 4, m > 1 and m+o = 2n+1.
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