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    Heterocyclic Adenosine Receptor Antagonists
    3.
    发明申请
    Heterocyclic Adenosine Receptor Antagonists 有权

    公开(公告)号：US20210292332A1

    公开(公告)日：2021-09-23

    申请号：US17201380

    申请日：2021-03-15

    Applicant: Exelixis, Inc.

    Inventor： Sunghoon Ma ,  Yong Wang ,  Wei Xu

    IPC: C07D487/04 ,  C07D487/14 ,  C07D513/14

    Abstract: Heterocyclic compounds useful as antagonists of adenosine receptors, and methods of treatment of diseases using antagonists of adenosine receptors are disclosed herein. Also disclosed herein are pharmaceutical compositions and methods of administration of heterocyclic antagonists of adenosine receptors and processes for producing heterocyclic antagonists of adenosine receptors.

    RORGamma Modulators
    6.
    发明申请
    RORGamma Modulators 审中-公开
    RORGAMM调制器

    公开(公告)号：US20150266856A1

    公开(公告)日：2015-09-24

    申请号：US14436355

    申请日：2013-10-17

    Applicant: BRISTOL-MYERS SQUIBB COMPANY ,  EXELIXIS, INC.

    Inventor： Wei Xu ,  Yong Wang ,  Sunghoon Ma ,  Elena S. Koltun ,  Byung Gyu Kim ,  Joon Won Jeong ,  T.G. Muralii Dhar ,  Lynn Canne Bannen

    IPC: C07D403/04 ,  C07D405/14 ,  C07D413/14 ,  C07D403/14 ,  C07D417/14

    CPC classification number: C07D403/04 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

    Abstract: Described are RORy modulators of the formula (I), and N-oxides thereof, and pharmaceutically acceptable salts thereof, and solvates and hydrates thereof, wherein R1, R2, R3, R4, R5, R6, Ra, x, y, L, G, Z, the bond denoted by “q”, the ring system denoted by “A” and the ring system denoted by “B” are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for modulating RORy activity in a cell and methods for treating a subject suffering from a disease or disorder in which the subject would therapeutically benefit from modulation of RORy activity, for example, autoimmune and/or inflammatory disorders.

    Abstract translation: 描述了式（I）的RORY调节剂及其N-氧化物及其药学上可接受的盐及其溶剂化物和水合物，其中R1，R2，R3，R4，R5，R6，Ra，x，y，L， G，Z，由“q”表示的键，由“A”表示的环系统和由“B”表示的环系统在此定义。 还提供了包含其的药物组合物。 这样的化合物和组合物可用于调节细胞中的RORY活性的方法和用于治疗受试者治疗受益于RORY活性（例如自身免疫和/或炎症性疾病）的疾病或病症的受试者的方法。

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