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    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
    1.
    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。

    PROCESS FOR THE SYNTHESIS OF PROGESTERONE RECEPTOR MODULATORS
    2.
    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。

    Composition and method for forming a sprayable materials cover
    8.
    发明授权
    Composition and method for forming a sprayable materials cover 失效
    用于形成可喷涂材料盖的组合物和方法

    公开(公告)号：US07284930B2

    公开(公告)日：2007-10-23

    申请号：US10689415

    申请日：2003-10-20

    申请人： Caijun Shi ,  Yanzhong Wu

    发明人： Caijun Shi ,  Yanzhong Wu

    IPC分类号： B09B5/00

    CPC分类号： B09B1/004 ,  E02B3/122 ,  Y02W30/32

    摘要： An alternative cover for landfill may be formed from a slurry mixture of water, cementitious binder, adhesion enhancing admixture and fiber. These constituents may be mixed and applied to cover landfilled wastes, granular material piles or for soil erosion control. The cover will harden to minimize water infiltration, wind blown dust, odor and affinity to birds, flies and other insects. The water may include tap water, landfill leachate and wastewater. The binder may include Portland cement, blended cement, cement kiln dust, class C fly ash, and/or calcium sulphate hemihydrate. The adhesion enhancing admixture includes water-dispersible polymers. The fibers may comprise shredded paper or wood or plastic fibers.

    摘要翻译： 可以由水，水泥粘合剂，粘合增强混合物和纤维的浆料混合物形成用于填埋的备选盖。 这些成分可以混合并用于覆盖填埋废物，颗粒物料堆或用于土壤侵蚀控制。 盖子将硬化以尽量减少水分渗入，风吹灰尘，气味和亲和力，鸟类，苍蝇和其他昆虫。 水可能包括自来水，垃圾渗滤液和废水。 粘合剂可以包括波特兰水泥，混合水泥，水泥窑灰，C类飞灰和/或硫酸钙半水合物。 粘合增强混合物包括水分散性聚合物。 纤维可以包括切碎的纸或木材或塑料纤维。

    Advanced route for the synthesis of cPLA2 inhibitors
    9.
    发明授权
    Advanced route for the synthesis of cPLA2 inhibitors 失效
    用于合成cPLA2抑制剂的先进途径

    公开(公告)号：US07259277B2

    公开(公告)日：2007-08-21

    申请号：US11076117

    申请日：2005-03-08

    申请人： Yanzhong Wu ,  Panolil Raveendrath

    发明人： Yanzhong Wu ,  Panolil Raveendrath

    IPC分类号： C07C311/03 ,  C07C255/58

    CPC分类号： C07C303/38 ,  C07C303/40 ,  C07C311/13 ,  C07D209/14

    摘要： A process for making a compound of formula (I) in which process the compound HC≡C—(CH2)n—NH2 is reacted with the compound R1—SO2Cl to produce an intermediate compound, which intermediate compound is then reacted with the compound of formula to produce the compound of formula (I), and compounds produced by the process of this invention. The terms R1, R2, R3, R4 and n have the definitions set forth in the specification.

    摘要翻译： 制备式（I）化合物的方法，其中化合物HC≡C-（CH 2 CH 2）n -NH 2 N 2是 与化合物R 1 -SO 2 Cl反应以产生中间体化合物，然后将该中间体化合物与下式化合物反应以制备式（I）化合物： ，以及通过本发明的方法制备的化合物。 术语R 1，R 2，R 3，R 4和n具有如下的定义： 规范。