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    C5-C6-CARBOCYCLIC FUSED IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    31.
    发明申请
    C5-C6-CARBOCYCLIC FUSED IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
    C5-C6-碳环稠合的亚硝基二嗪二氧化物作为BACE抑制剂，组合物及其用途

    公开(公告)号：WO2017095759A1

    公开(公告)日：2017-06-08

    申请号：PCT/US2016/063892

    申请日：2016-11-29

    Applicant: MERCK SHARP & DOHME CORP. ,  SCOTT, Jack, D. ,  BLIZZARD, Timothy, A. ,  WALSH, Shawn, P. ,  CUMMING, Jared, N.

    Inventor： SCOTT, Jack, D. ,  BLIZZARD, Timothy, A. ,  WALSH, Shawn, P. ,  CUMMING, Jared, N.

    IPC: A61P25/28 ,  C07D471/04 ,  A61K31/541

    CPC classification number: C07D471/04 ,  C07D285/20 ,  C07D417/12

    Abstract: In its many embodiments, the present invention provides certain C5-C6-carbocyclic fused iminothiazine dioxide compounds, including compounds Formula (I): and tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R 1 , ring A, R A , m, -L 1 -, ring B, R B , n, q, ring C, R C , and p 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.

    Abstract translation: 在其许多实施方案中，本发明提供了某些C 5 -C 6 - 碳环稠合的亚氨噻嗪二氧化物化合物，包括式（I）化合物及其互变异构体，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R 1，环A，R A，m，-L 1 - ，环B，R B， ，n，q，环C，R c和p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。

    DIAZINE-FUSED AMIDINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    32.
    发明申请
    DIAZINE-FUSED AMIDINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
    二氮嗪化合物作为BACE抑制剂，组合物及其使用

    公开(公告)号：WO2016044120A1

    公开(公告)日：2016-03-24

    申请号：PCT/US2015/049882

    申请日：2015-09-14

    Applicant: MERCK SHARP & DOHME CORP. ,  LIU, Kun ,  HE, Shuwen ,  CUMMING, Jared, N. ,  STAMFORD, Andrew, W.

    Inventor： LIU, Kun ,  HE, Shuwen ,  CUMMING, Jared, N. ,  STAMFORD, Andrew, W.

    IPC: C07D471/04

    CPC classification number: C07D471/04 ,  A61K45/06 ,  A61P25/00

    Abstract: In its many embodiments, the present invention provides certain C-6 spirocarbocyclic iminothiadiazine compounds, including compounds Formula (I) or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R 1A , R 1B , R 2 , R A , ring A, R A , m, L 1 , R L , ring C, R C , and p 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.

    Abstract translation: 在其许多实施方案中，本发明提供某些C-6螺环羧基亚氨基二嗪化合物，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R1A，R1B，R2，RA，环A ，RA，m，L1，RL，环C，RC和p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。

    S-IMINO-S-OXO IMINOTHIAZINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    34.
    发明申请
    S-IMINO-S-OXO IMINOTHIAZINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
    S-IMINO-S-OXO三嗪化合物作为BACE抑制剂，组合物及其使用

    公开(公告)号：WO2014150331A1

    公开(公告)日：2014-09-25

    申请号：PCT/US2014/022974

    申请日：2014-03-11

    Applicant: MERCK SHARP & DOHME CORP. ,  KHAN, Tanweer, A. ,  SCOTT, Jack, D. ,  CUMMING, Jared, N.

    Inventor： KHAN, Tanweer, A. ,  SCOTT, Jack, D. ,  CUMMING, Jared, N.

    IPC: A61K31/55

    CPC classification number: C07D279/12 ,  C07D417/12

    Abstract: In its many embodiments, the present invention provides provides certain S-imino-S-oxo iminothiazine compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein R N , R 1A , R 1B , R 2 , R 3 , R 4 , ring A, R A , m, L 1 -, and R L 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.

    Abstract translation: 在其许多实施方案中，本发明提供了某些S-亚氨基-S-氧亚氨基噻嗪化合物，包括式（I）化合物或其互变异构体和/或立体异构体，以及所述化合物，所述互变异构体和所述立体异构体的药学上可接受的盐 其中RN，R1A，R1B，R2，R3，R4，环A，RA，m，L1-和RL如本文所定义。 本发明的新化合物可用作BACE抑制剂，并且可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。

    C5, C6 OXACYCLIC-FUSED IMINOTHIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS
    35.
    发明申请
    C5, C6 OXACYCLIC-FUSED IMINOTHIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS 审中-公开
    C5，C6氧化丙烯酰胺二氧化硫化合物作为BACE抑制剂

    公开(公告)号：WO2014099794A1

    公开(公告)日：2014-06-26

    申请号：PCT/US2013/075411

    申请日：2013-12-16

    Applicant: MERCK SHARP & DOHME CORP. ,  CUMMING, Jared, N. ,  KAELIN, David Earl, Jr. ,  SCOTT, Jack, D. ,  WU, Wen-Lian ,  BURNETT, Duane, A.

    Inventor： CUMMING, Jared, N. ,  KAELIN, David Earl, Jr. ,  SCOTT, Jack, D. ,  WU, Wen-Lian ,  BURNETT, Duane, A.

    IPC: A61K31/54 ,  C07D279/12

    CPC classification number: C07D513/04

    Abstract: In its many embodiments, the present invention provides certain C2-ring-substituted iminothiazine compounds, including compounds Formula (I): (structurally represented) or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and, wherein R1, R2, R3, R4, X, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention ofvarious 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.

    Abstract translation: 在其许多实施方案中，本发明提供了某些C2-环取代的亚氨基噻嗪化合物，包括式（I）化合物：（结构上被表示）或其互变异构体，以及所述化合物的药学上可接受的盐，其中R1，R2，R3， R4，X，环A，RA，m，-L1-和RL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理学。 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。

    IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    38.
    发明申请
    IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
    三氮嗪二氧化物作为BACE抑制剂，组合物及其使用

    公开(公告)号：WO2011044187A1

    公开(公告)日：2011-04-14

    申请号：PCT/US2010/051560

    申请日：2010-10-06

    Applicant: SCHERING CORPORATION ,  SCOTT, Jack, D. ,  STAMFORD, Andrew, W. ,  GILBERT, Eric, J. ,  CUMMING, Jared, N. ,  ISERLOH, Ulrich ,  WANG, Lingyan ,  LI, Wei

    Inventor： SCOTT, Jack, D. ,  STAMFORD, Andrew, W. ,  GILBERT, Eric, J. ,  CUMMING, Jared, N. ,  ISERLOH, Ulrich ,  WANG, Lingyan ,  LI, Wei

    IPC: A01N43/54 ,  A61K31/505

    CPC classification number: C07D417/04 ,  C07D285/18 ,  C07D417/10

    Abstract: In its many embodiments, the present invention provides provides certain iminothiadiazine dioxide compounds, including compounds Formula (a) and include tautomers, solvates, prodrugs, esters, and deuterates thereof, and pharmaceutically acceptable salts of said compounds, tautomers, solvates, prodrugs, esters, and deuterates, wherein each of R 1 , R 2 , R 3 , R 4 , R 5 , R 9 , ring A, ring B, ring C, m, n, p, q, -L 1 -, -L 2 -,L 3 -, and L 4 - is selected independently and as defined herein. The compounds of the invention have, surprisingly and advantageously, improved solution stability. 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 in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers Disease, are also disclosed.

    Abstract translation: 在其许多实施方案中，本发明提供了某些亚氨基二嗪二氧化物化合物，包括式（a）化合物，并且包括其互变异构体，溶剂化物，前药，酯和氘代，以及所述化合物，互变异构体，溶剂化物，前药，酯的药学上可接受的盐 和氘代，其中R1，R2，R3，R4，R5，R9，环A，环B，环C，m，n，p，q，-L1-，-L2-，L3-和L4- 独立选择并如本文所定义。 本发明的化合物令人惊奇地和有利地提高了溶液的稳定性。 还公开了包含一种或多种这样的化合物（单独并与一种或多种其它活性剂组合）的药物组合物及其制备和用于治疗与包括阿尔茨海默病（amzheimers disease）在内的淀粉样蛋白β（Aβ）蛋白相关的病理学的方法。

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