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    CRYSTALLINE FORMS AND POLYMORPHS OF N-(3-(DIMETHYLAMINO)PROPYL)-4-(4-(3-FLUORO-4-METHOXYPHENYL) PYRIMIDIN-2-YLAMINO) BENZENESULFONAMIDE AS SUCCINATE SALTS
    13.
    发明申请
    CRYSTALLINE FORMS AND POLYMORPHS OF N-(3-(DIMETHYLAMINO)PROPYL)-4-(4-(3-FLUORO-4-METHOXYPHENYL) PYRIMIDIN-2-YLAMINO) BENZENESULFONAMIDE AS SUCCINATE SALTS 审中-公开
    N-（3-（二甲基氨基）丙基）-4-（4-（3-氟-4-甲氧基苯基）嘧啶-2-基氨基）苯甲酰胺作为磺酸盐的结晶形式和聚合物

    公开(公告)号：US20080262008A1

    公开(公告)日：2008-10-23

    申请号：US12105443

    申请日：2008-04-18

    申请人： Mahmoud Mirmehrabi ,  Sreenivasulu Megati ,  Abdolsamad Tadayon ,  Subodh Deshmukh

    发明人： Mahmoud Mirmehrabi ,  Sreenivasulu Megati ,  Abdolsamad Tadayon ,  Subodh Deshmukh

    IPC分类号： A61K31/505 ,  C07D239/42 ,  A61P35/00

    CPC分类号： C07D239/42

    摘要： The present invention relates to methods for preparing and manufacturing a crystalline form or polymorph of a compound of formula I: in the form of pharmaceutically acceptable salts and polymorphs thereof. The present invention is directed to methods for preparing and manufacturing crystalline polymorphs or forms of specific anilino-pyrimidine benzenesulfonamide compounds. Methods for converting one crystalline form or polymorph of compounds of formula I as their pharmaceutically acceptable salt polymorph to other different crystalline polymorphs of compounds of formula I as their corresponding pharmaceutically acceptable salt are also disclosed.

    摘要翻译： 本发明涉及制备和制备式I化合物的结晶形式或多晶型物的方法：其药学上可接受的盐和多晶型物。 本发明涉及制备和制备结晶多晶型物或特定苯胺基嘧啶苯磺酰胺化合物形式的方法。 还公开了将式I化合物的一种结晶形式或多晶型物作为其药学上可接受的盐多晶型物转化为式I化合物的其它不同结晶多晶型物作为其相应的药学上可接受的盐的方法。

    TIGECYCLINE AND METHODS OF PREPARING INTERMEDIATES
    15.
    发明申请
    TIGECYCLINE AND METHODS OF PREPARING INTERMEDIATES 审中-公开
    TIGECYCLINE和制备中间体的方法

    公开(公告)号：US20090099376A1

    公开(公告)日：2009-04-16

    申请号：US12251488

    申请日：2008-10-15

    申请人： Michel Bernatchez ,  Warren Chew ,  Sylvain Daigneault ,  Ernest Palus ,  Mahmoud Mirmehrabi ,  Luc Bouchard

    发明人： Michel Bernatchez ,  Warren Chew ,  Sylvain Daigneault ,  Ernest Palus ,  Mahmoud Mirmehrabi ,  Luc Bouchard

    IPC分类号： C07C237/26

    CPC分类号： C07C237/26 ,  C07C231/10 ,  C07C2603/46

    摘要： Methods of preparing and purifying 9-nitrominocycline and 9-aminominocycline and salts thereof used in the process of making tigecycline, are disclosed. In one embodiment, the invention is directed to a method of preparing the compound of formula 1 or a pharmaceutically acceptable salt thereof, comprising: (a) reacting nitric acid with the compound of formula 2, or a salt thereof, to produce a reaction mixture comprising an intermediate; and (b) further reacting the intermediate to form the compound of formula 1, wherein the intermediate is isolated from the reaction mixture, the method further comprising sparging with an inert gas prior to step (a).

    摘要翻译： 公开了在制备替加环素的过程中制备和纯化9-硝基喹诺酮和9-氨基环霉素及其盐的方法。 在一个实施方案中，本发明涉及制备式1化合物或其药学上可接受的盐的方法，其包括：（a）使硝酸与式2化合物或其盐反应，以产生反应混合物 包括中间体; 和（b）使中间体进一步反应形成式1化合物，其中中间体与反应混合物分离，该方法还包括在步骤（a）之前用惰性气体喷雾。

    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
    16.
    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。