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    AMINOPYRAZINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES
    2.
    发明公开
    AMINOPYRAZINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES 审中-公开
    具有A2A拮抗剂性质的氨基嘧啶化合物

    公开(公告)号：EP3220910A1

    公开(公告)日：2017-09-27

    申请号：EP15861650.8

    申请日：2015-11-13

    申请人： Merck Sharp & Dohme Corp.

    发明人： KUANG, Rongze ,  TING, Pauline ,  ALI, Amjad ,  WU, Heping ,  BERLIN, Michael ,  STAMFORD, Andrew ,  WANG, Hongwu ,  ZHOU, Gang ,  KIM, David ,  DENG, Qiaolin ,  LIM, Yeon-Hee ,  YU, Younong

    IPC分类号： A61K31/497 ,  C07D241/26 ,  C07D413/04

    摘要： Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein "R1", "RA-1", "R2", "R3", and "Het" are defined herein above, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.

    摘要翻译： 公开了式A和式A-1的化合物或其盐，以及包含这些化合物或其盐的药物制剂（药物组合物） 其中“R1”，“RA-1”，“R2”，“R3”和“Het”如上文所定义，认为该化合物适用于选择性拮抗A2a受体，例如以高密度 在基底神经节。 据信这样的化合物和药物制剂可用于治疗或控制神经退行性疾病，例如帕金森病，或由于使用用于治疗或控制帕金森病的某些药物引起的运动障碍。