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    COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY
    8.
    发明公开
    COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY 有权
    VERBINDUNGEN ZUR HEMMUNG DER WIEDERHOLUNGSAKTIVITT EINES LEUKINREICHEN KINASEENZYMS

    公开(公告)号：EP3068389A4

    公开(公告)日：2017-06-21

    申请号：EP14861985

    申请日：2014-11-10

    申请人： MERCK SHARP & DOHME

    发明人： DEMONG DUANE ,  MILLER MICHAEL ,  LIU HONG ,  DAI XING ,  GRESHOCK THOMAS J ,  STAMFORD ANDREW ,  NARGUND RAVI

    IPC分类号： C07D231/56 ,  A61K31/415

    CPC分类号： C07D401/04 ,  C07D231/56 ,  C07D401/14

    摘要： The present invention is directed to substituted indazole compounds which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which LRRK-2 kinase is involved.

    摘要翻译： 本发明涉及取代的吲唑化合物，其是LRRK2激酶的有效抑制剂并且可用于治疗或预防其中涉及LRRK2激酶的疾病，例如帕金森病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗其中涉及LRRK-2激酶的疾病中的用途。

    IMINOTHIADIAZEPANE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    9.
    发明公开
    IMINOTHIADIAZEPANE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
    IMINOTHIADIAZINDIOXIDVERBINDUNGEN ALS BACE-HEMMER，ZUSAMMENSETZUNGEN DAMIT UND DEREN VERWENDUNG

    公开(公告)号：EP3082823A4

    公开(公告)日：2017-06-07

    申请号：EP14871886

    申请日：2014-12-16

    申请人： MERCK SHARP & DOHME

    发明人： DAI XING ,  CUMMING JARED N ,  SCOTT JACK D ,  LIU HONG ,  PALANI ANANDAN

    IPC分类号： A61K31/547 ,  A61P25/28 ,  C07D285/36 ,  C07D471/04 ,  C07D513/04

    CPC分类号： C07D513/04 ,  C07D285/36 ,  C07D417/12 ,  C07D471/04

    摘要： or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1A, R1B, R2, R3, R4, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and may be useful for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.

    摘要翻译： 其中R 1，R 2，R 3，R 4，环A，RA，m，-L 1 - 和RL如本文所定义。 本发明的新化合物可用作BACE抑制剂，并可用于治疗和预防与其有关的各种病症。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其他活性剂组合）的药物组合物，以及它们的制备和使用方法，包括用于可能治疗阿尔茨海默氏病。