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    Crystalline Solid Forms of N--N'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, Processes for Making, and Methods of Use
    5.
    发明申请
    Crystalline Solid Forms of N--N'-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide, Processes for Making, and Methods of Use 审中-公开
    N-N' - （4-氟苯基）环丙烷-1,1-二甲酰胺的结晶固体形式，制备方法和使用方法

    公开(公告)号：US20170044106A1

    公开(公告)日：2017-02-16

    申请号：US15118738

    申请日：2015-02-16

    申请人： Exelixis, Inc.

    发明人： Dana T. Aftab ,  Nathan Guz ,  Stephen Lau ,  Noel Hamill ,  Tracy Walker ,  Jana Galbraith ,  Simon Yau ,  Khalid Shah

    IPC分类号： C07D215/233

    CPC分类号： C07D215/233 ,  C07B2200/13 ,  C07D215/22

    摘要： The invention relates to novel crystalline solid forms of the chemical compound N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N′-(4-fluorophenyl) cyclopropane-1,1-dicarboxamide (Compound 1), and solvates thereof, including hydrates, that are useful for the treatment of cancer. Also disclosed are pharmaceutical compositions comprising the crystalline solid forms and processes for making the crystalline solid forms, as well as methods of using them for the treatment of cancer, particularly thyroid cancer, prostate cancer, hepatocellular cancer, renal cancer, and non-small cell lung carcinoma. The crystalline solid forms can be used to make the L-malate salt of cabozantinib.

    摘要翻译： 本发明涉及化合物N- {4 - [（6,7-二甲氧基喹啉-4-基）氧基]苯基} -N' - （4-氟苯基）环丙烷-1,1-二甲酰胺（ 化合物1）及其溶剂化物，包括水合物，其可用于治疗癌症。 还公开了包含结晶固体形式和用于制备结晶固体形式的方法的药物组合物，以及其用于治疗癌症，特别是甲状腺癌，前列腺癌，肝细胞癌，肾癌和非小细胞的方法 肺癌。 结晶固体形式可用于制备卡泊沙坦的L-苹果酸盐。