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    PYRAZOLE DERIVATIVE, OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF
    1.
    发明公开
    PYRAZOLE DERIVATIVE, OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF 审中-公开
    吡唑衍生物，或药物可接受的盐

    公开(公告)号：EP3315492A1

    公开(公告)日：2018-05-02

    申请号：EP16814372.5

    申请日：2016-06-22

    申请人： Kissei Pharmaceutical Co., Ltd.

    发明人： HIRASAWA, Hideaki ,  TANADA, Fumiya ,  MUTAI, Yousuke ,  FUSHIMI, Nobuhiko ,  KOBAYASHI, Junichi ,  KIJIMA, Yoshiro

    IPC分类号： C07D231/12 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/427 ,  A61K31/436 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61P11/02

    摘要： [Problem]
    The present invention is to provide a novel pyrazole derivative, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and a pharmaceutical use thereof.
    [Solution]
    The present invention provides a compound represented by the formula (I) or a pharmaceutically acceptable salt thereof, which has TRPM8 inhibitory effects:

    wherein ring A is C 6-10 aryl or the like; X is CR 4a or the like; R 1 and R 2 are a hydrogen atom or the like; R 3 is a hydrogen atom or the like; R 4 is a hydrogen atom or the like; ring B is C 6-10 aryl or the like; R 5 is a hydrogen atom or the like; R 6a is a hydrogen atom or the like; R 7a is a hydrogen atom or the like; R 7b is a hydrogen atom or the like; R 6b is a hydrogen atom or the like; R 8 is a hydrogen atom or the like; n is 0, 1 or 2. Therefore, the compound represented by the formula (I) of the present invention or a pharmaceutically acceptable salt thereof is useful as an agent for treating or preventing diseases or symptoms caused by hyperexcitability or disorder of afferent neurons.

    摘要翻译： 本发明提供新的吡唑衍生物或其药学上可接受的盐，含有其的药物组合物及其药物用途。 本发明提供具有TRPM8抑制效果的式（I）所示的化合物或其药学上可接受的盐，其中环A为C 6-10芳基等; X是CR4a等; R1和R2是氢原子等; R3是氢原子等; R4是氢原子等; 环B是C 6-10芳基等; R5是氢原子等; R6a是氢原子等; R7a是氢原子等; R7b是氢原子等; R6b是氢原子等; R8是氢原子等; n为0,1或2.因此，由本发明的式（I）表示的化合物或其药学上可接受的盐可用作用于治疗或预防由传入神经元的兴奋过度或病症引起的疾病或症状的药剂。

    CRYSTAL OF IMIDAZOPYRIDINONE COMPOUND OR SALT THEREOF
    2.
    发明公开
    CRYSTAL OF IMIDAZOPYRIDINONE COMPOUND OR SALT THEREOF 审中-公开

    公开(公告)号：EP4091670A1

    公开(公告)日：2022-11-23

    申请号：EP21767151.0

    申请日：2021-03-10

    申请人： KISSEI PHARMACEUTICAL CO., LTD.

    发明人： TAKEUCHI, Hideki ,  KIJIMA, Yoshiro ,  MORIYAMA, Akihiro

    IPC分类号： A61P1/04 ,  C07D471/04 ,  A61K31/4188

    摘要： As a drug substance, a crystal having good physical properties is preferable. However, the crystal form that is most excellent as a drug substance may vary with the compound. In general, it is difficult to predict a crystal form of a drug substance having good physical properties, and it is required to variously examine each compound. Therefore, an object of the present invention is to provide a crystal having good physical properties as a drug substance for a novel compound or a salt thereof.
    The present invention relates to a crystal of the compound represented by the following formula (I) or a salt thereof useful for the treatment of an inflammatory bowel disease.