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    PYRIMIDINE DERIVATIVE
    2.
    发明申请
    PYRIMIDINE DERIVATIVE 审中-公开

    公开(公告)号：US20200172494A1

    公开(公告)日：2020-06-04

    申请号：US16473749

    申请日：2017-12-26

    申请人： Daiichi Sankyo Company, Limited

    发明人： Yasuyuki Takeda ,  Yamato Suzuki ,  Toshiharu Noji ,  Hidenobu Murafuji ,  Satoshi Muneoka ,  Hidekazu Inoue ,  Bitoku Takahashi ,  Rie Inaba

    IPC分类号： C07D239/34 ,  A61P11/12

    摘要： Cystic fibrosis is developed through mutation of Cystic Fibrosis Transmembrane conductance Regulator (CFTR), which is one type of chloride channel. An object of the present invention is to provide compounds effective in the treatment of cystic fibrosis that open a chloride channel different from CFTR, which is the cause of the disease, and do not depend on CFTR.Compounds of the present invention are compounds or pharmaceutically acceptable salts thereof that open calcium dependent chloride channels (CaCCs) via G-protein coupled receptor 39 (GPR39) agonism to have strong chloride ion-secretory action, and are represented by the following general formula (I):General formula (I): wherein, X represents a carboxyl group or a tetrazolyl group; Q represents a C1-C3 alkylene group, an oxygen atom, a sulfur atom, etc.; G represents a phenyl group where the phenyl group may have 1 to 3 substituents independently selected from the group consisting of a halogen atom, a cyano group, a C1-C6 alkyl group, etc.; R1 represents a C1-C6 alkyl group, etc.; R2 represents a C1-C6 alkyl group that may have 1 to 3 substituents independently selected from the following group A, or a group selected from the following group B: Group A: a phenyl group and a pyridyl group, wherein the phenyl group and the pyridyl group may have 1 to 3 substituents independently selected from the following group D; Group B: —OH, —O-M, —SH, —S-M, —NH2, —NH-M, and —N-M2, wherein M is a C1-C6 alkyl group that may have 1 or 2 substituents independently selected from the following group C, or a C3-C6 cycloalkyl group that may have 1 or 2 substituents independently selected from the following group C; Group C: a halogen atom, a cyano group, a phenyl group, a pyridyl group, etc., wherein the phenyl group and the pyridyl group may have 1 to 3 substituents independently selected from the following group D; and Group D: a halogen atom, a cyano group, a C1-C6 alkyl group, etc.

    Pyrimidine derivative
    5.
    发明授权
    Pyrimidine derivative 有权

    公开(公告)号：US11034659B2

    公开(公告)日：2021-06-15

    申请号：US16473749

    申请日：2017-12-26

    申请人： Daiichi Sankyo Company, Limited

    发明人： Yasuyuki Takeda ,  Yamato Suzuki ,  Toshiharu Noji ,  Hidenobu Murafuji ,  Satoshi Muneoka ,  Hidekazu Inoue ,  Bitoku Takahashi ,  Rie Inaba

    IPC分类号： A61K31/506 ,  A61K31/505 ,  C07D239/52 ,  C07D239/34 ,  A61P11/12

    摘要： Cystic fibrosis is developed through mutation of Cystic Fibrosis Transmembrane conductance Regulator (CFTR), which is one type of chloride channel. An object of the present invention is to provide compounds effective in the treatment of cystic fibrosis that open a chloride channel different from CFTR, which is the cause of the disease, and do not depend on CFTR.
    Compounds of the present invention are compounds or pharmaceutically acceptable salts thereof that open calcium dependent chloride channels (CaCCs) via G-protein coupled receptor 39 (GPR39) agonism to have strong chloride ion-secretory action, and are represented by the following general formula (I):
    General formula (I): wherein, X represents a carboxyl group or a tetrazolyl group; Q represents a C1-C3 alkylene group, an oxygen atom, a sulfur atom, etc.; G represents a phenyl group where the phenyl group may have 1 to 3 substituents independently selected from the group consisting of a halogen atom, a cyano group, a C1-C6 alkyl group, etc.; R1 represents a C1-C6 alkyl group, etc.; R2 represents a C1-C6 alkyl group that may have 1 to 3 substituents independently selected from the following group A, or a group selected from the following group B: Group A: a phenyl group and a pyridyl group, wherein the phenyl group and the pyridyl group may have 1 to 3 substituents independently selected from the following group D; Group B: —OH, —O-M, —SH, —S-M, —NH2, —NH-M, and —N-M2, wherein M is a C1-C6 alkyl group that may have 1 or 2 substituents independently selected from the following group C, or a C3-C6 cycloalkyl group that may have 1 or 2 substituents independently selected from the following group C; Group C: a halogen atom, a cyano group, a phenyl group, a pyridyl group, etc., wherein the phenyl group and the pyridyl group may have 1 to 3 substituents independently selected from the following group D; and Group D: a halogen atom, a cyano group, a C1-C6 alkyl group, etc.

    Thienopyrazole derivative having PDE7 inhibitory activity
    6.
    发明授权
    Thienopyrazole derivative having PDE7 inhibitory activity 有权
    具有PDE7抑制活性的噻吩衍生物

    公开(公告)号：US08901315B2

    公开(公告)日：2014-12-02

    申请号：US14013168

    申请日：2013-08-29

    申请人： Daiichi Sankyo Company, Limited

    发明人： Hidekazu Inoue ,  Hidenobu Murafuji ,  Yasuhiro Hayashi

    IPC分类号： C07D231/18 ,  C07D495/04

    CPC分类号： C07D231/18 ,  C07D495/04

    摘要： To provide thienopyrazole derivatives inhibiting PDE 7 selectively, and therefore, enhance cellular cAMP level. Consequently, the compound is useful for treating various kinds of disease such as allergic diseases, inflammatory diseases or immunologic diseases. The compound is thienopyrazole compound represented by the following formula (I): [wherein, especially, R1 is a cyclohexyl, a cycloheptyl group or a tetrahydropyranyl group; R2 is methyl; R3 is a hydrogen atom; and R4 is a group: —CONR5R6 (in which any one of R5 and R6 is a hydrogen atom)].

    摘要翻译： 提供抑制PDE 7的噻吩并吡唑衍生物，从而提高细胞cAMP水平。 因此，该化合物可用于治疗各种疾病如过敏性疾病，炎性疾病或免疫疾病。 该化合物是由下式（I）表示的噻吩并吡唑化合物：[其中，特别是R 1是环己基，环庚基或四氢吡喃基; R2是甲基; R3是氢原子; 和R 4是基团-CONR 5 R 6（其中R 5和R 6中的任一个是氢原子）]。