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    C5-C6-Oxacyclic Fused Iminothiadiazine Dioxide Compounds Bearing an Ether Linker as BACE Inhibitors, Compositions, and Their Use
    13.
    发明申请
    C5-C6-Oxacyclic Fused Iminothiadiazine Dioxide Compounds Bearing an Ether Linker as BACE Inhibitors, Compositions, and Their Use 审中-公开

    公开(公告)号：US20190040081A1

    公开(公告)日：2019-02-07

    申请号：US16076441

    申请日：2017-02-06

    Applicant: Merck Sharp & Dohme Corp.

    Inventor： Shawn P. Walsh ,  Jared N. Cumming ,  Xing Dai

    IPC: C07D513/04 ,  A61P25/28

    Abstract: 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 RN, R1, R2, RA, 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.

    C5-C6-oxacyclic fused iminopyrimidinone compounds as bace inhibitors, compositions, and their use
    14.
    发明授权
    C5-C6-oxacyclic fused iminopyrimidinone compounds as bace inhibitors, compositions, and their use 有权

    公开(公告)号：US10047098B2

    公开(公告)日：2018-08-14

    申请号：US15527975

    申请日：2015-11-20

    Applicant: Merck Sharp & Dohme Corp.

    Inventor： Xing Dai ,  Jared N. Cumming ,  Hong Liu ,  Jack D. Scott

    IPC: A61K31/519 ,  C07D491/048 ,  C07D491/052

    Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminopyrimidinone compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1, RA, ring A, m, n, -L1-, ring B, RB, 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.

    C5-C6-OXACYCLIC FUSED IMINOPYRIMIDINONE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    15.
    发明申请
    C5-C6-OXACYCLIC FUSED IMINOPYRIMIDINONE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开

    公开(公告)号：US20170362248A1

    公开(公告)日：2017-12-21

    申请号：US15527975

    申请日：2015-11-20

    Applicant: MERCK SHARP & DOHME CORP.

    Inventor： Xing Dai ,  Jared N. Cumming ,  Hong Liu ,  Jack D. Scott

    IPC: C07D491/052

    CPC classification number: C07D491/052 ,  A61P25/16 ,  A61P25/28

    Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminopyrimidinone compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein RN, R1, RA, ring A, m, n, -L1-, ring B, RB, 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.

    COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY
    16.
    发明申请
    COMPOUNDS INHIBITING LEUCINE-RICH REPEAT KINASE ENZYME ACTIVITY 有权
    化合物抑制富含重复激素激酶活性

    公开(公告)号：US20160289207A1

    公开(公告)日：2016-10-06

    申请号：US15035255

    申请日：2014-11-10

    Applicant: MERCK SHARP & DOHME CORP.

    Inventor： Duane DeMong ,  Michael Miller ,  Hong Liu ,  Xing Dai ,  Thomas Greshock ,  Andrew Stamford ,  Ravi Nargund

    IPC: C07D401/04 ,  C07D401/14

    CPC classification number: C07D401/04 ,  C07D231/56 ,  C07D401/14

    Abstract: 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.

    Abstract translation: 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涉及LRRK-2激酶的疾病中的用途。

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