发明公开
EP2167525A2 17ß-CYANO-19-ANDROST-4-EN-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL
审中-公开
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基本信息:
- 专利标题: 17ß-CYANO-19-ANDROST-4-EN-DERIVAT, DESSEN VERWENDUNG UND DAS DERIVAT ENTHALTENDE ARZNEIMITTEL
- 专利标题(英):17ß-CYANO-19-ANDROST-4-ENE DERIVATIVE, USE THEREOF AND MEDICAMENTS CONTAINING SAID DERIVATIVE
- 专利标题(中):17-氰基-19-雄甾-4-烯衍生物,其用途及药物含有该衍生物的
- 申请号:EP08760962.4 申请日:2008-06-12
- 公开(公告)号:EP2167525A2 公开(公告)日:2010-03-31
- 发明人: KUHNKE, Joachim , HUEBNER, Jan , BOHLMANN, Rolf , FRENZEL, Thomas , KLAR, Ulrich , MENGES, Frederik , RING, Sven , BORDEN, Steffen , MUHN, Hans-Peter , PRELLE, Katja
- 申请人: Bayer Schering Pharma Aktiengesellschaft
- 申请人地址: Müllerstrasse 178 13353 Berlin DE
- 专利权人: Bayer Schering Pharma Aktiengesellschaft
- 当前专利权人: Bayer Schering Pharma Aktiengesellschaft
- 当前专利权人地址: Müllerstrasse 178 13353 Berlin DE
- 优先权: DE102007027635 20070612; US943651P 20070613
- 国际公布: WO2008152112 20081218
- 主分类号: C07J53/00
- IPC分类号: C07J53/00 ; C07J41/00
摘要:
The 17ß-cyano-19-androst-4-ene derivatives of the present invention have gestagenic activity. They have the general chemical formula (1), in which Z is selected from the group comprising O, two hydrogen atoms, NOR and NNHSO2R, wherein R is hydrogen or C1-C4 alkyl, R1 and R2 independently of one another are hydrogen or methyl, or R1 and R2 together form methylene, or are omitted, whereby a double bond is formed between C1 and C2, R4 is hydrogen or halogen and in addition either: R6a, R6b together form methylene or 1,2 ethanediyl or R6a is hydrogen and R6b is selected from the group comprising hydrogen, methyl and hydroxymethylene, and R7 is selected from the group comprising hydrogen, C1-C4 alkyl, C2-C3 alkenyl and cyclopropyl, or: R6a is hydrogen and R6b and R7 together form methylene, or are omitted, whereby a double bond is formed between C6 and C7, or: R6a is methyl and R6b and R7 are omitted, whereby a double bond is formed between C6 and C7, R15 and R16 are hydrogen, or together form methylene and R17 is selected from the group comprising hydrogen, C1-C4- alkyl and aIIyI. The derivatives also comprise the solvates, hydrates, stereoisomers, diastereomers, enantiomers and salts of the aforementioned substances, with the proviso that certain compounds are excluded.