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    PROCESS FOR THE SYNTHESIS OF PROGESTERONE RECEPTOR MODULATORS
    1.
    发明申请
    PROCESS FOR THE SYNTHESIS OF PROGESTERONE RECEPTOR MODULATORS 审中-公开
    合成前列腺素受体调节剂的方法

    公开(公告)号：US20080319204A1

    公开(公告)日：2008-12-25

    申请号：US12120959

    申请日：2008-05-15

    申请人： Yanzhong Wu ,  Karen Sutherland ,  John Leo Considine ,  Bogdan Kazimierz Wilk ,  Pierre Giguere ,  Michael MacEwan ,  Archana Sharma ,  Alexander Gontcharov

    发明人： Yanzhong Wu ,  Karen Sutherland ,  John Leo Considine ,  Bogdan Kazimierz Wilk ,  Pierre Giguere ,  Michael MacEwan ,  Archana Sharma ,  Alexander Gontcharov

    IPC分类号： C07D209/96

    CPC分类号： C07D209/96 ,  C07D403/04

    摘要： Processes for preparing substituted oxindole-2-ones, and specifically the following, are described, wherein R1-R4, R6, and n are defined herein. The processes include reacting a first alkali metal hydroxide, a tetraalkyl ammonium salt, a benzonitrile, and R6X or XCH2(CH2)nX′, wherein R6 is C1 to C6 alkyl, substituted C1 to C6 alkyl, C3 to C8 cycloalkyl, substituted C3 to C8 cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic, or substituted heterocyclic, X and X′ are, independently, leaving groups, and n is 1 to 5; (ii) reacting the product of step (i) with a second alkali metal hydroxide at a temperature of at least about 60° C.; (iii) reacting the product of step (ii) with an alkali alkoxide at a temperature of at least about 140° C. to form an oxindol-2-one; (iv) brominating the oxindol-2-one; and (v) coupling the brominated oxindol-2-one with a coupling reagent.

    摘要翻译： 描述了制备取代羟吲哚-2-酮的方法，具体如下，其中R1-R4，R6和n如本文所定义。 所述方法包括使第一碱金属氢氧化物，四烷基铵盐，苄腈和R6X或XCH2（CH2）nX'反应，其中R6为C1至C6烷基，取代的C1至C6烷基，C3至C8环烷基，取代C3至 C8环烷基，芳基，取代的芳基，杂芳基，取代的杂芳基，杂环或取代的杂环，X和X'独立地为离去基团，n为1至5; （ii）使步骤（i）的产物与至少约60℃的温度下的第二碱金属氢氧化物反应; （iii）使步骤（ii）的产物与碱金属醇盐在至少约140℃的温度下反应，形成羟吲哚-2-酮; （iv）溴化羟吲哚-2-酮; 和（v）将溴代羟吲哚-2-酮与偶联剂偶联。

    POLYMORPHS, SOLVATES, AND HYDRATE OF 5-(4'-FLUORO-2'-OXO-1',2'-DIHYDROSPIRO[CYCLOPROPANE-1,3'-INDOL]-5'-YL)-1-METHYL-1H-PYRROLE-2-CARBONITRILE
    2.
    发明申请
    POLYMORPHS, SOLVATES, AND HYDRATE OF 5-(4'-FLUORO-2'-OXO-1',2'-DIHYDROSPIRO[CYCLOPROPANE-1,3'-INDOL]-5'-YL)-1-METHYL-1H-PYRROLE-2-CARBONITRILE 审中-公开
    5-（4'-氟-2'-OXO-1'，2'-二氢吡啶并[环丙烷-1,3'-吲哚] -5'-YL）-1-甲基-1H-咪唑并[ PYRROLE-2-CARBONITRILE

    公开(公告)号：US20080312306A1

    公开(公告)日：2008-12-18

    申请号：US12138852

    申请日：2008-06-13

    申请人： Mahmoud Mirmehrabi ,  John Leo Considine ,  Yuping Niu ,  Abdolsamad Tadayon ,  Subodh Deshmukh ,  Jennifer Q. Liang ,  Yanzhong Wu

    发明人： Mahmoud Mirmehrabi ,  John Leo Considine ,  Yuping Niu ,  Abdolsamad Tadayon ,  Subodh Deshmukh ,  Jennifer Q. Liang ,  Yanzhong Wu

    IPC分类号： A61K31/404 ,  C07D403/02 ,  A61P15/00 ,  A61P35/00

    CPC分类号： C07D207/34

    摘要： Novel polymorph Form II and III, solvate Forms I, II, III, and IV, and the hydrate of 5-(4′-fluoro-2′-oxo-1′,2′-dihydrospiro[cyclopropane-1,3′-indol]-5′-yl)-1-methyl-1H-pyrrole-2-carbonitrile are provided, as are methods for preparing the same. Pharmaceutical compositions and kits containing these novel polymorphs, solvates, and hydrate, and combinations thereof are further provided, as are methods of contraception; treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, hormone-dependent carcinomas; treating symptoms of premenstrual syndrome and premenstrual dysphoric disorder; providing hormone replacement therapy; stimulating food intake; synchronizing estrus; or treating symptoms of premenstrual syndrome using one or more of these polymorphs, solvates, or hydrate.

    摘要翻译： 新型多晶型II型和III型，溶剂合物形式I，II，III和IV，以及5-（4'-氟-2'-氧代-1'，2'-二氢螺[环丙烷-1,3'- 吲哚] -5'-基）-1-甲基-1H-吡咯-2-甲腈，其制备方法也是如此。 还提供了含有这些新型多晶型物，溶剂化物和水合物的药物组合物和试剂盒及其组合，以及避孕方法; 治疗或预防子宫肌瘤，子宫平滑肌瘤，子宫内膜异位症，功能障碍性出血，多囊卵巢综合征，激素依赖性癌症; 治疗经前期综合征和经前期焦虑症的症状; 提供激素替代疗法; 刺激食物摄入; 同步发情 或使用这些多晶型物，溶剂化物或水合物中的一种或多种来治疗经前综合征的症状。

    Preparation and purification of 4-(indazol-3-yl)phenols
    9.
    发明授权
    Preparation and purification of 4-(indazol-3-yl)phenols 失效
    制备和纯化4-（吲唑-3-基）苯酚

    公开(公告)号：US07601847B2

    公开(公告)日：2009-10-13

    申请号：US11257344

    申请日：2005-10-24

    申请人： John Leo Considine ,  Galina Vid ,  Zhixian Ding

    发明人： John Leo Considine ,  Galina Vid ,  Zhixian Ding

    IPC分类号： C07D231/56

    CPC分类号： C07D231/56

    摘要： The present invention concerns processes for the production and purification of compounds of the formula: where R1-R10 are as defined in the specification. Preferred processes of the invention utilize a lithium bis(trimethylsilyl)amide, lithium dicyclohexylamide, or potassium bis(trimethylsilyl)amide base and a R1—X alkylating agent where X is as described in the specification. An alcohol preferably is added to the product solution is used to promote crystallization of the desired product.

    摘要翻译： 本发明涉及生产和纯化下式化合物的方法：其中R1-R10如说明书中所定义。 本发明的优选方法使用双（三甲基甲硅烷基）氨基锂，二环己基氨基锂或二（三甲基甲硅烷基）氨基钾酰胺碱和R1为-X-烷基化剂，其中X如说明书中所述。 将优选加入到产物溶液中的醇用于促进所需产物的结晶。