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公开(公告)号：EP3176176A1
公开(公告)日：2017-06-07
申请号：EP17151891.3
申请日：2013-11-27
申请人： INSERM (Institut National de la Santé et de la Recherche Médicale) , SC BELENOS , UNIVERSITE DE BORDEAUX
发明人： PIAZZA, Pier Vincenzo , VALLEE, Monique , FELPIN, François-Xavier , REVEST, Jean-Michel , FABRE, Sandy
CPC分类号： C07J7/0045 , C07J7/002 , C07J41/005 , C07J41/0094
摘要： The invention relates to a compound of Formula I or a pharmaceutically acceptable salt thereof:
wherein R1 is C1-8 alkyl, C1-8 alkoxy, CN, NO 2 , amino, COOH, COOCH 3 , OH, N 3 , or halogen and R2 is H, OH, C1-8 alkyl, C1-8 alkoxy, C2-C6 alkenyl, halogen, Bn-O-, Bn-optionally substituted, or Ph- optionally substituted.摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐：其中R 1为C 1-8烷基，C 1-8烷氧基，CN，NO 2，氨基，COOH，COOCH 3，OH，N 3或卤素且R 2为H， OH，C 1-8烷基，C 1-8烷氧基，C 2 -C 6链烯基，卤素，Bn-O-，Bn-任选取代或Ph-任选取代。
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公开(公告)号：EP1841778A1
公开(公告)日：2007-10-10
申请号：EP06700710.4
申请日：2006-01-17
发明人： MOUTOU, Jean-luc , RONDOT, Benoît , LAFAY, Jean , MAILLOS, Philippe, c/o Solvay Pharmaceuticals GmbH
IPC分类号： C07J7/00
CPC分类号： C07J7/0045
摘要： A method for the preparation of medrogestone by heterogeneously palladium- catalysed isomerisation from 17-methyl-6-methylenepregn-4-ene-3,20-dione is described.
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公开(公告)号：EP0941361A1
公开(公告)日：1999-09-15
申请号：EP97910556.0
申请日：1997-10-31
发明人： ROBERTS, Stanley, Michael , EDDOLLS, Jonathan, Paul , WILLETTS, Andrew, John , ATKINSON, Anthony , MURPHY, Jonathan, Paul
CPC分类号： C12P33/02 , C07J5/0053 , C07J7/0045 , C07J7/0085
摘要： Disclosed is a method for the production of an adrenocorticoid steroid represented by general formula (I), wherein R1 and R3 may be H, alkyl, substituted alkyl, silyl, acyl, acyloxy or carbamoyl (and wherein R1 need not be the same as R3), and wherein R2 may be methyl, mono- or disubstituted methyl, substituted alkyl, methyl or substituted alkylhydroxy, silyloxy, alkyloxy, acyl, acyloxy or carbamoyl; the method comprising treatment of a precursor thereof so as to effect the following steps: hydroxylation at the 11β position; formation of a double bond between positions 1 and 2; and hydroxylation at position 21.
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公开(公告)号：EP0886645A1
公开(公告)日：1998-12-30
申请号：EP97902235
申请日：1997-01-17
申请人： THERAMEX
发明人： PIASCO ALAIN , LAFAY JEAN , DELANSORNE REMI , PARIS JACQUES , PASCAL JEAN-CLAUDE
IPC分类号： A61K31/57 , A61K31/00 , A61P5/24 , C07J5/00 , C07J7/00 , C07J21/00 , C07J41/00 , C07J53/00 , C07J71/00
CPC分类号： C07J7/0045 , C07J21/006 , C07J41/0016 , C07J53/004 , C07J71/001
摘要： The invention relates to compounds of formula (I), in which R1, R2, R3, R4, R5, R6, n and X are as defined in the specification, and to pharmaceutical compositions containing them. These compounds are excellent progestogens which are devoid of residual androgenic activity.
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公开(公告)号：EP0754701B1
公开(公告)日：1998-08-12
申请号：EP95913412.3
申请日：1995-04-03
发明人： HIBINO, Satoshi , SUGINO, Eiichi , KOHNO, Tetsuya , FUJIMORI, Shiho , NEMOTO, Hideo , ICHIHARA, Yoshitatsu , SATO, Yoshio
IPC分类号： C07J5/00 , A61K31/57 , A61K31/575
CPC分类号： C07J7/0045 , C07J21/006 , C07J71/001
摘要： A progesterone compound represented by general formula (1) and a neovascularization inhibitor containing the same as the active ingredient (wherein R represents a C1-C23 hydrocarbon group). It has a potent neovascularization inhibitory effect and is hence useful as a remedy for malignant tumor, diabetic retinitis and rheumatism.
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6.发明公开
公开(公告)号：EP0785211A1
公开(公告)日：1997-07-23
申请号：EP96400145.7
申请日：1996-01-22
申请人： LABORATOIRE THERAMEX
发明人： Maillos, Philippe , Verdan, Christina , Delansorne, Rémi , Paris, Jacques , Pascal, Jean-Claude
CPC分类号： C07J13/007 , C07J7/0045 , C07J17/00 , C07J41/0016 , C07J53/004
摘要： The invention relates to compounds of the formula :
wherein :
each of R 1 and R 2 is hydrogen or a (C 1 -C 6 )alkyl, R 1 and R 2 being not simultaneously hydrogen ;
R 3 is hydrogen, a (C 1 -C 6 )alkyl or a (C 1 -C 6 )alkoxy ;
R 4 is hydrogen, a (C 1 -C 6 )alkyl or a group -COR 6 where R 6 is a (C 1 -C 6 )alkyl ;
R 5 is hydrogen or a (C 1 -C 6 )alkyl ;
n is zero or one ;
X is oxygen or an hydroxyimino group ; and
the dotted line may represent a double bond ; provided that when n = 0, R 3 is hydrogen only if both R 1 and R 2 are a (C 1 -C 6 )alkyl,
and to pharmaceutical compositions containing them.
These compounds are potent progestogens which are devoid of residual androgenic activity.摘要翻译： 本发明涉及下式的化合物：其中：R1和R2各自为氢或（C1-C6）烷基，R1和R2不同时为氢; R3是氢，（C1-C6）烷基或（C1-C6）烷氧基; R4是氢，（C1-C6）烷基或基团-COR6，其中R6是（C1-C6）烷基; R5是氢或（C1-C6）烷基; n为零或一; X是氧或羟基亚氨基; 虚线可以表示双键; 条件是当n = 0时，只有当R1和R2都是（C1-C6）烷基时，R3是氢，以及含有它们的药物组合物。 这些化合物是没有残留雄激素活性的有效的孕激素。
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公开(公告)号：EP0680970A3
公开(公告)日：1997-05-02
申请号：EP95302934.5
申请日：1995-04-28
CPC分类号： C07J53/002 , C07J7/0045
摘要： A process for the production of medrogestone, in which, in an intermediate step, the solvate 3β,5α,6β-trihydroxy-6α,17α-dimethylpregnan-20-one monomethanolate is obtained as a solid, stable compound by displacing the organic solvent from a solution of of 3β,5α,6β-trihydroxy-6α,17α-dimethylpregnan-20-one with a lower alkanol, and a Diels-Alder adduct of 6-methylene-17α-methylpregn-4-ene-3,20-dione with maleic anhydride is used as an intermediate for production of the corresponding dicarboxylic acid salt for removal of 6-methylene-17α-methylpregn-4-ene-3,20-dione contamination of the desired product. Another intermediate, 6β-hydroxy-6α,17α-dimethylpregn-4-ene-3,20-dione, has been found to prevent smooth muscle proliferation and is useful in the treatment of atherosclerosis and restinosis.
摘要翻译： 制备孕激素的方法，其中在中间步骤中，获得溶剂合物3β，5α，6β-三羟基-6α，17α-二甲基孕甾-20-酮单甲醇化物作为固体稳定化合物，通过 从3β，5α，6β-三羟基-6α，17α-二甲基孕烷-20-酮与低级链烷醇的溶液中取代有机溶剂，并将6-亚甲基-17α- 甲基孕-4-烯-3,20-二酮与马来酸酐用作生产相应二羧酸盐的中间体，用于除去6-亚甲基-17α-甲基孕-4-烯-3,20-二酮污染物 所需产品。 已经发现另一种中间体6β-羟基-6α，17α-二甲基孕-4-烯-3,20-二酮可以预防平滑肌增生，并且可用于治疗动脉粥样硬化和再狭窄。
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公开(公告)号：EP0573362B1
公开(公告)日：1996-10-23
申请号：EP93401419.2
申请日：1993-06-03
申请人： ROUSSEL UCLAF
CPC分类号： C07J5/0053 , C07J7/0045
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公开(公告)号：EP0680970A2
公开(公告)日：1995-11-08
申请号：EP95302934.5
申请日：1995-04-28
CPC分类号： C07J53/002 , C07J7/0045
摘要： A process for the production of medrogestone, in which, in an intermediate step, the solvate 3β,5α,6β-trihydroxy-6α,17α-dimethylpregnan-20-one monomethanolate is obtained as a solid, stable compound by displacing the organic solvent from a solution of of 3β,5α,6β-trihydroxy-6α,17α-dimethylpregnan-20-one with a lower alkanol, and a Diels-Alder adduct of 6-methylene-17α-methylpregn-4-ene-3,20-dione with maleic anhydride is used as an intermediate for production of the corresponding dicarboxylic acid salt for removal of 6-methylene-17α-methylpregn-4-ene-3,20-dione contamination of the desired product. Another intermediate, 6β-hydroxy-6α,17α-dimethylpregn-4-ene-3,20-dione, has been found to prevent smooth muscle proliferation and is useful in the treatment of atherosclerosis and restinosis.
摘要翻译： 在中间步骤中，通过置换有机溶剂从而获得作为固体，稳定的化合物的溶剂合物3β，5α，6β-三羟基-6α，17α-二甲基孕烷-20-酮单甲醇化物的孕二烯酮的制备方法 3β，5α，6β-三羟基-6α，17α-二甲基孕烷-20-酮与低级链烷醇的溶液，以及6-亚甲基-17α-甲基孕甾-4-烯-3,20-二酮的Diels-Alder加合物 与马来酸酐一起用作生产相应二羧酸盐的中间体，以除去所需产物的6-亚甲基-17α-甲基孕甾-4-烯-3,20-二酮污染物。 另一种中间体6β-羟基-6α，17α-二甲基孕烯-4-烯-3,20-二酮已经被发现可以预防平滑肌增殖并且可用于治疗动脉粥样硬化和再狭窄。
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10.发明授权
公开(公告)号：EP0510167B1
公开(公告)日：1995-08-23
申请号：EP92900237.6
申请日：1991-11-12
发明人： LANQUETIN, Michel
CPC分类号： C07J7/0045 , C07J1/0025 , C07J1/0074 , C07J1/0077 , C07J5/0053 , C07J11/00
摘要： A novel method is provided for crystallizing organic and particularly steroidal substances. In particular, a crystallization method is provided whereby a predeterminable and homogenous particle size class can be obtained non-mechanically, and wherein a substance is dissolved in a ternary mixture consisting of a lipophilic solvent, a hydrophilic solvent and a surface-active agent at a temperature close to boiling, whereafter the mixture is allowed to cool to a temperature at which crystallization is initiated and the crystals thereby formed are separated. The method can be used for producing pharmaceutical active principles.
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