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31 条记录 (耗时 0.029 秒)

    C5-C6-OXACYLIC FUSED IMINOTHIADIAZINE DIOXIDE COMPOUNDS BEARING AN ETHER LINKER AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    1.
    发明申请
    C5-C6-OXACYLIC FUSED IMINOTHIADIAZINE DIOXIDE COMPOUNDS BEARING AN ETHER LINKER AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
    C 5 -C 6 - 氧杂环丙烷稠合的亚硝基二氮嗪二氧化物化合物，其带有作为BACE抑制剂，组合物及其用途的醚键

    公开(公告)号：WO2017139210A1

    公开(公告)日：2017-08-17

    申请号：PCT/US2017/016636

    申请日：2017-02-06

    申请人： MERCK SHARP & DOHME CORP. ,  WALSH, Shawn, P. ,  CUMMING, Jared, N. ,  DAI, Xing

    发明人： WALSH, Shawn, P. ,  CUMMING, Jared, N. ,  DAI, Xing

    IPC分类号： A61K31/549 ,  C07D513/04 ,  A61P25/28

    CPC分类号： C07D513/04

    摘要： In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiadiazine dioxide compounds bearing an ether linker, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R N , R 1 , R 2 , R A , ring A, ring C, and m are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or 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： 在其许多实施方案中，本发明提供了带有醚接头的某些C5-C6-氧杂环稠合的亚氨基噻二嗪二氧化物化合物，包括式（I）的化合物或其互变异构体，以及所述 化合物和所述互变异构体，其中R 1，R 2，R 1，R 2，R A，环A，环 C和m如本文所定义。 本发明的新化合物可用作BACE抑制剂和/或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的方法。

    IMINOTHIADIAZINE DIOXIDES BEARING AN AMINE-LINKED SUBSTITUENT AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    2.
    发明申请
    IMINOTHIADIAZINE DIOXIDES BEARING AN AMINE-LINKED SUBSTITUENT AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
    作为BACE抑制剂，组合物及其使用的支链胺取代基的三嗪二氧化物

    公开(公告)号：WO2016118404A1

    公开(公告)日：2016-07-28

    申请号：PCT/US2016/013509

    申请日：2016-01-15

    申请人： MERCK SHARP & DOHME CORP. ,  WU, Wen-Lian ,  HE, Shuwen ,  WALSH, Shawn, P. ,  CUMMING, Jared, N.

    发明人： WU, Wen-Lian ,  HE, Shuwen ,  WALSH, Shawn, P. ,  CUMMING, Jared, N.

    IPC分类号： A01N43/42

    CPC分类号： C07D417/14 ,  A61P3/10 ,  A61P9/04 ,  A61P25/16 ,  A61P25/28 ,  A61P27/06 ,  C07D417/12

    摘要： In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R 1 , R 2 , ring A, R A , m, ring B, R B , and n are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or 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： 在其许多实施方案中，本发明提供了某些亚氨基噻嗪二氧化物化合物，包括式（I）化合物或其互变异构体以及所述化合物和所述互变异构体的药学上可接受的盐，其中R1，R2，环A，RA，m，环B ，RB和n如本文所定义。 本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。 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它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物。