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1.发明授权Crystalline forms of 11β-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one 失效11β-（4-乙酰基苯基）-20,20,21,21,21-五氟-17-羟基-19-去甲-17α-孕甾-4,9-二烯-3-酮的结晶形式公开(公告)号：US07910573B2
公开(公告)日：2011-03-22
申请号：US11757118
申请日：2007-06-01
申请人： Wolfgang Beckmann , Gabriele Winter , Edda Kraemer , Thomas Ginko , Evelin Amoulong , Arwed Cleve
发明人： Wolfgang Beckmann , Gabriele Winter , Edda Kraemer , Thomas Ginko , Evelin Amoulong , Arwed Cleve
CPC分类号： C07J1/0081
摘要： The present invention relates to crystalline forms of 11β-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one. The invention relates in particular to two crystalline ansolvate/anhydrate forms of this compound, polymorphs I and II. However, the present invention also relates to crystalline solvates, for example methanol and ethanol solvates of 11β-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one as precursors for preparing these two polymorphs I and II. Processes for preparing polymorph I by displacement crystallization or by trituration are described. Selection of the last solvent before formation of the ansolvate can be based on the differences in the purification behaviour of the individual solvates of 11β-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one. Polymorph I according to the invention is particularly suitable for the manufacture of medicinal products.
摘要翻译： 本发明涉及11β-（4-乙酰基苯基）-20,20,21,21,21-五氟-17-羟基-19-去甲-17α-孕甾-4,9-二烯-3-酮的结晶形式 。 本发明特别涉及这种化合物的两种结晶固体/无水物形式，即多晶型物I和II。 然而，本发明还涉及结晶溶剂合物，例如11β-（4-乙酰基苯基）-20,20,21,21,21-五氟-17-羟基-19-去甲基-17α-前体的甲醇和乙醇溶剂合物 -4,9-二烯-3-酮作为制备这两种多晶型I和II的前体。 描述了通过置换结晶或研磨制备多晶型I的方法。 在形成溶剂化物之前，最后一种溶剂的选择可以基于11＆bgr-（4-乙酰基苯基）-20,20,21,21,21-五氟-17-羟基 - 19-nor-17α-前 - 4,9-二烯-3-酮。 根据本发明的多晶型I特别适用于制造药用产品。
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2.发明申请CRYSTALLINE FORMS OF 11SS-(4-ACETYLPHENYL)-20,20,21,21,21-PENTAFLUORO-17-HYDROXY-19-NOR-17A-PREGNA-4,9-DIEN-3-ONE 失效11SS-（4-乙酰苯基）-20,20,21,21,21-蓬多隆-17-羟基-19-诺-177-孕酮-4,9-二烯-3-酮的晶体形式公开(公告)号：US20080085875A1
公开(公告)日：2008-04-10
申请号：US11757118
申请日：2007-06-01
申请人： Wolfgang Beckmann , Gabriele Winter , Edda Kraemer , Thomas Ginko , Evelin Amoulong , Arwed Cleve
发明人： Wolfgang Beckmann , Gabriele Winter , Edda Kraemer , Thomas Ginko , Evelin Amoulong , Arwed Cleve
CPC分类号： C07J1/0081
摘要： The present invention relates to crystalline forms of 11β-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one. The invention relates in particular to two crystalline ansolvate/anhydrate forms of this compound, polymorphs I and II. However, the present invention also relates to crystalline solvates, for example methanol and ethanol solvates of 11β-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one as precursors for preparing these two polymorphs I and II. Processes for preparing polymorph I by displacement crystallization or by trituration are described. Selection of the last solvent before formation of the ansolvate can be based on the differences in the purification behaviour of the individual solvates of 11β-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one. Polymorph I according to the invention is particularly suitable for the manufacture of medicinal products.
摘要翻译： 本发明涉及11beta-（4-乙酰基苯基）-20,20,21,21,21-五氟-17-羟基-19-去甲-17α-孕甾-4,9-二烯-3-酮的结晶形式。 本发明特别涉及这种化合物的两种结晶固体/无水物形式，即多晶型物I和II。 然而，本发明还涉及结晶溶剂化物，例如11β-（4-乙酰基苯基）-20,20,21,21,21-五氟-17-羟基-19-去甲-17α-前 - 氨基甲酸的甲醇和乙醇溶剂合物， 4,9-二烯-3-酮作为制备这两种多晶型物I和II的前体。 描述了通过置换结晶或研磨制备多晶型I的方法。 在形成溶剂之前，最后一种溶剂的选择可以基于11beta-（4-乙酰基苯基）-20,20,21,21,21-五氟-17-羟基-199的各个溶剂化物的纯化行为的差异 -nor-17alpha-pregna-4,9-dien-3-one。 根据本发明的多晶型I特别适用于制造药用产品。
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