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    Iminothiadiazepane Dioxide Compounds as BACE Inhibitors, Compositions, and Their Use
    26.
    发明申请
    Iminothiadiazepane Dioxide Compounds as BACE Inhibitors, Compositions, and Their Use 有权
    作为BACE抑制剂，组合物及其用途的伊马替西二酮二氧化物化合物

    公开(公告)号：US20170037056A1

    公开(公告)日：2017-02-09

    申请号：US15104257

    申请日：2014-12-16

    申请人： Xing DAI ,  Jared N. CUMMING ,  Jack D. SCOTT ,  Hong LIU ,  Anandan PALANI ,  MERCK SHARP & DOHME CORP.

    发明人： Xing Dai ,  Jared N. Cumming ,  Jack D. Scott ,  Hong Liu ,  Anandan Palani

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

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

    摘要： In its many embodiments, the present invention provides certain iminothiadiazepane dioxide compounds, including compounds Formula (I): 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： 或其互变异构体和所述化合物和所述互变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。

    S-IMINO-S-OXO-IMINOTHIADIAZINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    28.
    发明申请
    S-IMINO-S-OXO-IMINOTHIADIAZINE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权
    S-IMINO-S-OXO-IMINOTHIADIAZINE化合物作为BACE抑制剂，组合物及其使用

    公开(公告)号：US20160016923A1

    公开(公告)日：2016-01-21

    申请号：US14774200

    申请日：2014-03-11

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

    发明人： Tanweer A. Khan ,  Jack D. Scott ,  Jared N. Cumming

    IPC分类号： C07D285/18 ,  C07D417/12

    CPC分类号： C07D285/18 ,  C07D417/12 ,  C07D419/12

    摘要： In its many embodiments, the present invention provides certain S-imino-S-oxo iminothiadiazine 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 RN, R1, 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： 在其许多实施方案中，本发明提供某些S-亚氨基-3-氧亚氨基二嗪化合物，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，R1，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。

    Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use
    29.
    发明授权
    Iminothiadiazine dioxide compounds as bace inhibitors, compositions, and their use 有权
    二氢化二氮杂二恶烷化合物作为抑制剂，组合物及其用途

    公开(公告)号：US08563543B2

    公开(公告)日：2013-10-22

    申请号：US13392955

    申请日：2010-10-06

    申请人： Jack D. Scott ,  Andrew W. Stamford ,  Eric J. Gilbert ,  Jared N. Cumming ,  Ulrich Iserloh ,  Lingyan Wang ,  Wei Li

    发明人： Jack D. Scott ,  Andrew W. Stamford ,  Eric J. Gilbert ,  Jared N. Cumming ,  Ulrich Iserloh ,  Lingyan Wang ,  Wei Li

    IPC分类号： A61K31/54

    CPC分类号： C07D417/04 ,  C07D285/18 ,  C07D417/10

    摘要： In its many embodiments, the present invention 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 R1, R2, R3, R4, R5, R9, ring A, ring B, ring C, m, n, p, q, -L1-, -L2-, L3-, and L4- 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.

    摘要翻译： 在其许多实施方案中，本发明提供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，溶剂合物，前药，酯， 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- 独立选择和如本文所定义。 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用于治疗与包括阿尔茨海默病在内的淀粉样蛋白β（Abeta）蛋白相关的病理学的方法。

    PIPERIDINE DERIVATIVES USEFUL AS CCR5 ANTAGONISTS
    30.
    发明申请
    PIPERIDINE DERIVATIVES USEFUL AS CCR5 ANTAGONISTS 失效
    哌啶衍生物作为CCR5拮抗剂有用

    公开(公告)号：US20080214575A1

    公开(公告)日：2008-09-04

    申请号：US12104914

    申请日：2008-04-17

    申请人： Anandan Palani ,  Michael W. Miller ,  Jack D. Scott

    发明人： Anandan Palani ,  Michael W. Miller ,  Jack D. Scott

    IPC分类号： A61K31/506 ,  C07D401/14 ,  A61P31/12

    CPC分类号： C07D401/14

    摘要： The present invention provides a compound of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein R1, R2, R3, R9, R10, A and B are as defined in the specification. The present invention also provides pharmaceutical compositions containing the compound of this invention, and methods of treatment using the compound of this invention. The invention also relates to the use of a combination of a compound of this invention and one or more antiviral or other agents useful in the treatment of Human Immunodeficiency Virus (HIV). The invention further relates to the use of a compound of this invention, alone or in combination with another agent, in the treatment of solid organ transplant rejection, graft v. host disease, arthritis, rheumatoid arthritis, inflammatory bowel disease, atopic dermatitis, psoriasis, asthma, allergies or multiple sclerosis.

    摘要翻译： 本发明提供下式的化合物或其药学上可接受的盐或溶剂化物，其中R 1，R 2，R 3，R 3， A，B和B如本说明书中所定义。 本发明还提供含有本发明化合物的药物组合物和使用本发明化合物的治疗方法。 本发明还涉及本发明化合物与一种或多种可用于治疗人类免疫缺陷病毒（HIV）的抗病毒剂或其它药剂的组合的用途。 本发明还涉及本发明化合物单独或与另一种药剂组合用于治疗实体器官移植排斥，移植物抗宿主病，关节炎，类风湿性关节炎，炎症性肠病，特应性皮炎，牛皮癣 ，哮喘，过敏或多发性硬化。