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    (Heteroarylmethyl) Thiohydantoins as anticancer drugs
    4.
    发明申请
    (Heteroarylmethyl) Thiohydantoins as anticancer drugs 审中-公开
    （杂芳基甲基）硫代乙内酰脲作为抗癌药物

    公开(公告)号：US20120238533A1

    公开(公告)日：2012-09-20

    申请号：US13395087

    申请日：2010-09-03

    申请人： Arwed Cleve ,  Ulrich Lücking ,  Stefan Bäurle ,  Martin Fritsch ,  Jens Schröder ,  Bernd-Wolfgang Igl

    发明人： Arwed Cleve ,  Ulrich Lücking ,  Stefan Bäurle ,  Martin Fritsch ,  Jens Schröder ,  Bernd-Wolfgang Igl

    IPC分类号： A61K31/4166 ,  A61K31/4439 ,  A61K31/57 ,  A61K31/167 ,  A61K31/56 ,  A61K31/407 ,  A61P35/00 ,  A61K31/565 ,  A61K31/366 ,  A61K31/277 ,  A61K31/4704

    CPC分类号： A61K31/275 ,  A61K31/4439

    摘要： The invention refers to the use of androgen receptor antagonists for the treatment and/or prevention of fibroids, also known as uterine leiomyoma, leiomyomata. Particularly, the invention refers to the use of an androgen receptor antagonist being any one of the compounds according to the following list: cyproterone acetate, oxendolone, chlormadinone acetate, spironolactone, osaterone acetate, dienogest, flutamide, hydroxyflutamide, nilutamide, bicalutamide, RU 58841, LGD-2226, MDV3100, BMS-641988, BMS-779333, or 4-(3-{[6-(2-hydroxy-2-methylpropoxy)pyridin-3-yl]methyl}-4,4-dimethyl-5-oxo-2-thioxoimidazolidin-1-yl)-2-(trifluoromethyl)benzonitrile (thioxoimidazolidine derivative) for the treatment of fibroids.

    摘要翻译： 本发明涉及雄激素受体拮抗剂用于治疗和/或预防子宫肌瘤，也称为子宫平滑肌瘤，平滑肌瘤的用途。 特别地，本发明涉及使用根据以下列举的化合物中的任何一种的雄激素受体拮抗剂：醋酸环丙孕酮，羟考灵，乙酸氯地孕酮，螺内酯，醋酸奥托酮，依诺孕，氟他胺，羟基氟他胺，尼鲁替胺，比卡鲁胺，RU 58841 ，LGD-2226，MDV3100，BMS-641988，BMS-779333或4-（3 - {[6-（2-羟基-2-甲基丙氧基）吡啶-3-基]甲基} -4,4-二甲基-5 - 氧代-2-硫代咪唑烷-1-基）-2-（三氟甲基）苄腈（硫代咪唑烷衍生物）。

    Crystalline forms of 11β-(4-acetylphenyl)-20,20,21,21,21-pentafluoro-17-hydroxy-19-nor-17α-pregna-4,9-dien-3-one
    6.
    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

    IPC分类号： A01N29/12 ,  A61K31/03 ,  C07C49/00

    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。