PROCESS FOR FEBUXOSTAT
    3.
    发明申请
    PROCESS FOR FEBUXOSTAT 审中-公开
    FEBUXOSTAT的过程

    公开(公告)号:US20140112992A1

    公开(公告)日:2014-04-24

    申请号:US14123875

    申请日:2012-05-21

    IPC分类号: C07D277/56 A61K31/426

    CPC分类号: C07D277/56 A61K31/426

    摘要: The present invention provides a process for the preparation of 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester. The present invention also provides a process for the preparation of 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester. The present invention further provides novel crystalline Forms of febuxostat, processes for their preparation and pharmaceutical compositions comprising them. The present invention further provides febuxostat crystalline particles having a mean particle size of less than about 25 μm, the methods for the manufacture of said crystalline particles, and pharmaceutical compositions comprising said crystalline particles.

    摘要翻译: 本发明提供了制备2-(4-羟基苯基)-4-甲基噻唑-5-羧酸乙酯的方法。 本发明还提供了制备2-(3-甲酰基-4-羟基苯基)-4-甲基噻唑-5-甲酸乙酯的方法。 本发明进一步提供了新型的布氏抑菌素的结晶形式,其制备方法和包含它们的药物组合物。 本发明还提供平均粒度小于约25μm的Febustostat结晶颗粒,制备所述结晶颗粒的方法和包含所述结晶颗粒的药物组合物。