PROCESS FOR PREPARING NOVEL CRYSTALLINE FORMS OF PELIGLITAZAR, NOVEL STABLE FORMS PRODUCED THEREIN AND FORMULATIONS
    3.
    发明申请
    PROCESS FOR PREPARING NOVEL CRYSTALLINE FORMS OF PELIGLITAZAR, NOVEL STABLE FORMS PRODUCED THEREIN AND FORMULATIONS 审中-公开
    制备新型结晶形式的方法,生产的新型稳定形式和配方

    公开(公告)号:US20070238770A1

    公开(公告)日:2007-10-11

    申请号:US11695124

    申请日:2007-04-02

    IPC分类号: A61K31/421 C07D263/34

    CPC分类号: C07D263/32

    摘要: A process is provided for selectively preparing novel stable crystalline forms, namely selectively and consistently preparing Form N-1 of the free acid peliglitazar, Form N-2 of the free acid peliglitazar and Form P-1 of the L-lysine salt of the free acid peliglitazar. The process preferably employs solvent systems which produce crystals having suitable flow properties and desired particle size.Novel Form N-1 crystals of the free acid, Form N-2 crystals of the free acid, Form P-1 crystals of the L-lysine salt of the free acid, pharmaceutical compositions containing such novel forms and a method of treating diabetes, dyslipidemia and atherosclerosis employing such novel forms are also provided.

    摘要翻译: 提供了一种选择性制备新的稳定结晶形式的方法,即选择性且一致地制备游离酸百日preparing唑形式的N-1,游离酸百日lit嗪的N-2型和游离酸性赖氨酸盐的L-赖氨酸盐形式P-1 酸苦瓜 该方法优选使用产生具有合适流动性和所需粒度的晶体的溶剂体系。 游离酸的新型N-1晶型,游离酸形式的N-2晶体,游离酸的L-赖氨酸盐的形式P-1晶体,含有这种新形式的药物组合物和治疗糖尿病的方法, 还提供了使用这种新型形式的血脂异常和动脉粥样硬化。

    PROCESS FOR PREPARING ATAZANAVIR BISULFATE AND NOVEL FORMS
    6.
    发明申请
    PROCESS FOR PREPARING ATAZANAVIR BISULFATE AND NOVEL FORMS 有权
    制备ATAZANAVIR BISULFATE和新型的方法

    公开(公告)号:US20110124689A1

    公开(公告)日:2011-05-26

    申请号:US12900588

    申请日:2010-10-08

    CPC分类号: C07D213/42

    摘要: A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate.A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.

    摘要翻译: 提供了一种制备HIV蛋白酶抑制剂阿扎那韦硫酸氢盐的方法,其中阿扎那韦游离碱的溶液与浓硫酸反应的量与小于约15重量%的游离碱反应,阿扎那韦的A型晶体种子 将硫酸氢盐加入到反应混合物中,并且以硫酸氢盐形式的结晶,按照立方式以增加的速率以多个阶段多次加入另外的浓硫酸,以实现阿扎那韦硫酸氢盐的形式A晶体的形成。 还提供了制备作为图案C材料的阿扎那韦硫酸氢盐的方法。 还提供了一种新型形式的阿扎那韦硫酸氢盐,其为E3型,其是来自乙醇的硫酸氢盐的高度结晶的三乙醇盐溶剂合物。