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1. 发明授权

US4474701A Process for the separation of 4-androsten-3,17-dione and 1,4-androstadien-3,17-dione 失效
标题翻译：分离4-雄甾-3,17-二酮和1,4-雄甾烯-3,17-二酮的方法
公开(公告)号：US4474701A
公开(公告)日：1984-10-02
申请号：US474314
申请日：1983-03-10
申请人： Gerhard Teichmuller , Joachim Rabe , Harry Henkel
发明人： Gerhard Teichmuller , Joachim Rabe , Harry Henkel
IPC分类号： C07J1/00 , C07J41/00
CPC分类号： C07J1/0011 , C07J41/0094
摘要： A process is disclosed for the separation of 4-androsten-3,17-dione/1,4-androstadien-3,17-dione mixtures, which are produced, e.g., upon microbiological sterol-side chain decomposition, through conversion of said mixture into a mixture of 17.beta.-cyano-17.alpha.-hydroxy-4-androsten-3-one/17.beta.-cyano-17.alpha.-hydroxy-1,4-androstadien-3-one, from which the difficultly soluble 17.beta.-cyano-17.alpha.-hydroxy-4-androsten-3-one is separated in crystalline form through filtration, and the 17.beta.-cyano-17.alpha.-hydroxy-1,4-androstadiene remaining in the mother liquor is re-split, directly or after extraction with organic solvent, by treatment in alkaline medium, into 1,4-androstadien-3,17-dione, and isolated as such. The separation of the products follows in high yields, and in sufficient purity for further working-up in the synthesis of androstane and pregnane derivatives, as well as estratrienes.
摘要翻译：公开了用于分离4-雄甾-3,17-二酮/ 1,4-雄甾烯-3,17-二酮混合物的方法，其通过例如微生物甾醇侧链分解产生，通过所述混合物的转化转化为17β-氰基-17α-羟基-4-雄甾-3-酮/17β-氰基-17α-羟基-1,4-雄甾烯-3-酮的混合物，难溶于17β- 通过过滤将氰基-17α-羟基-4-雄甾-3-酮以结晶形式分离，并将残留在母液中的17β-氰基-17α-羟基-1,4-雄甾二烯直接再分裂或者用有机溶剂萃取后，通过在碱性介质中处理，形成1,4-雄甾二烯-3,17-二酮，并将其分离。产物的分离遵循高产率，并且具有足够的纯度用于进一步处理雄甾烷和孕烷衍生物以及雌三烯的合成。

2. 发明授权

US5866559A 17.alpha.-cyanomethylestra-4,9-dien derivatives and pharmaceutical compositions containing same 失效
标题翻译： 17α-氰基甲基雌-4,9-二烯衍生物和含有它们的药物组合物
公开(公告)号：US5866559A
公开(公告)日：1999-02-02
申请号：US771805
申请日：1996-12-20
申请人： Gerhard Teichmuller , Gerd Muller , Sigfrid Schwarz , Bernd Undeutsch , Harry Henkel , Ronald Gebuhr , Gunter Kaufmann , Doris Hubler , Michael Oettel
发明人： Gerhard Teichmuller , Gerd Muller , Sigfrid Schwarz , Bernd Undeutsch , Harry Henkel , Ronald Gebuhr , Gunter Kaufmann , Doris Hubler , Michael Oettel
IPC分类号： A61K31/565 , A61P13/02 , A61P15/00 , A61P35/00 , A61P43/00 , C07J41/00 , C07J75/00 , A61K31/57 , C07J7/00
CPC分类号： C07J41/0016 , C07J41/0094
摘要： The 17.alpha.-cyanomethylestra-4,9-diene derivative compounds are of formula I: ##STR1## wherein R.sub.1 is an alkyl group having from 1 to 2 carbon atoms; R.sub.2 is an alkyl group with 1 to 10 carbon atoms, an acyl group with 1 to 10 carbon atoms or a trialkylsilyl group; and R.sub.3 is an oxygen atom or a R--O--N group, wherein R is a hydrogen atom, an acyl group with 1 to 10 carbon atoms, an alkyl group with 1 to 10 carbon atoms, a sulfamoyl group, an alkylsilyl group or a trialkylsilyl group. These compounds, particularly in combination with at least one suitable estrogen, are suitable for treatment of endometrioses or gestagen-dependent tumors and for hormonal contraception and climacteric hormone replacement therapy (HRT). Processes for making the new steroids are described as well as methods of making the pharmaceutical compositions containing them.
摘要翻译： 17α-氰基甲基雌甾-4,9-二烯衍生物化合物具有式I：其中R 1是具有1至2个碳原子的烷基; R2是碳原子数为1〜10的烷基，碳原子数1〜10的酰基或三烷基甲硅烷基; R3为氧原子或R-O-N基，其中R为氢原子，具有1-10个碳原子的酰基，具有1-10个碳原子的烷基，氨磺酰基，烷基甲硅烷基或三烷基甲硅烷基。这些化合物，特别是与至少一种合适的雌激素组合，适用于治疗子宫内膜异位症或孕激素依赖性肿瘤以及激素避孕和更年期激素替代疗法（HRT）。描述了制备新类固醇的方法以及制备含有它们的药物组合物的方法。

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