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    TIGECYCLINE AND METHODS OF PREPARING INTERMEDIATES
    2.
    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。

    Synthesis and characterization of polymorph form III 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile
    3.
    发明申请
    Synthesis and characterization of polymorph form III 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile 审中-公开
    多晶型III 4-（2-（4,4-二甲基-2-氧代恶唑烷-3-基）噻唑-4-基）苄腈的合成和表征

    公开(公告)号：US20080249148A1

    公开(公告)日：2008-10-09

    申请号：US12075248

    申请日：2008-03-10

    申请人： Mahmoud Mirmehrabi ,  Abdolsamad Tadayon ,  Subodh Deshmukh

    发明人： Mahmoud Mirmehrabi ,  Abdolsamad Tadayon ,  Subodh Deshmukh

    IPC分类号： A61K31/422 ,  C07D417/04 ,  A61P15/18 ,  A61P35/00

    CPC分类号： C07D417/04

    摘要： A polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form III are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.Also provided are methods for preparing polymorph Form I of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile from polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.

    摘要翻译： 描述了4-（2-（4,4-二甲基-2-氧代恶唑烷-3-基）噻唑-4-基）苄腈的多晶型物III和制备形式III的方法。 还提供了避孕，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，多囊卵巢综合征和激素依赖性癌症的方法，提供激素替代疗法，刺激食物摄入和同步发情，包括使用4- （2-（4,4-二甲基-2-氧代恶唑烷-3-基）噻唑-4-基）苄腈。 还提供了制备4-（2-（4,4-二甲基-2-氧代恶唑烷-3-基）噻唑-4-基）苄腈的多晶型物I的方法， 4-二甲基-2-氧代恶唑烷-3-基）噻唑-4-基）苄腈。

    Synthesis and characterization of polymorph form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-YL)thiazol-4-YL)benzonitrile
    4.
    发明申请
    Synthesis and characterization of polymorph form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-YL)thiazol-4-YL)benzonitrile 审中-公开
    4-（2-（4,4-二甲基-2-氧代恶唑烷-3-基）噻唑-4-基）苄腈的多晶型II的合成和表征

    公开(公告)号：US20080234340A1

    公开(公告)日：2008-09-25

    申请号：US12075228

    申请日：2008-03-10

    申请人： Mahmoud Mirmehrabi ,  Yuping Niu ,  Abdolsamad Tadayon ,  Subodh Deshmukh ,  Mannching Sherry Ku

    发明人： Mahmoud Mirmehrabi ,  Yuping Niu ,  Abdolsamad Tadayon ,  Subodh Deshmukh ,  Mannching Sherry Ku

    IPC分类号： A61K31/427 ,  C07D413/02 ,  A61P35/00 ,  A61P5/24

    CPC分类号： C07D417/04

    摘要： A polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form II are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.Further provided are methods for preparing polymorph Form I of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile from polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile.

    摘要翻译： 描述了4-（2-（4,4-二甲基-2-氧代恶唑烷-3-基）噻唑-4-基）苄腈的多晶型II和制备形式II的方法。 还提供了避孕，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，多囊卵巢综合征和激素依赖性癌症的方法，提供激素替代疗法，刺激食物摄入和同步发情，包括使用4- （2-（4,4-二甲基-2-氧代恶唑烷-3-基）噻唑-4-基）苄腈。 进一步提供的是由4-（2-（4,4-二甲基-2-氧代恶唑烷-3-基）噻唑-4-基）苄腈的多晶型II制备多晶型物I的方法， 4-二甲基-2-氧代恶唑烷-3-基）噻唑-4-基）苄腈。

    CRYSTALLINE FORMS AND POLYMORPHS OF N-(3-(DIMETHYLAMINO)PROPYL)-4-(4-(3-FLUORO-4-METHOXYPHENYL) PYRIMIDIN-2-YLAMINO) BENZENESULFONAMIDE AS SUCCINATE SALTS
    10.
    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。