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    C2-azaspiro iminothiazine dioxides as BACE inhibitors, compositions, and their use
    1.
    发明授权
    C2-azaspiro iminothiazine dioxides as BACE inhibitors, compositions, and their use 有权
    C2-azaspiro亚氨基噻嗪二氧化物作为BACE抑制剂，组合物及其用途

    公开(公告)号：US09453034B2

    公开(公告)日：2016-09-27

    申请号：US14774204

    申请日：2014-03-11

    Applicant: Merck Sharp & Dohme Corp.

    Inventor： Eric J. Gilbert ,  Jared N. Cumming ,  Jack D. Scott ,  Wen-Lian Wu ,  Duane A. Burnett ,  Andrew W. Stamford

    IPC: C07D513/10

    CPC classification number: C07D513/10

    Abstract: In its many embodiments, the present invention provides certain C2-azaspirosubstituted iminothiazine dioxide compounds. 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C2-氮杂二取代的亚氨基噻嗪二氧化物化合物。 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。

    Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
    2.
    发明授权
    Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use 有权
    三环取代噻二嗪二氧化物作为BACE抑制剂，组合物及其应用

    公开(公告)号：US09416129B2

    公开(公告)日：2016-08-16

    申请号：US14433298

    申请日：2013-10-14

    Applicant: Merck Sharp & Dohme Corp.

    Inventor： Eric J. Gilbert ,  Jared N. Cumming ,  Andrew W. Stamford ,  Younong Yu ,  Jack D. Scott ,  Ulrich Iserloh ,  Lingyan Wang ,  John P. Caldwell

    IPC: C07D417/14 ,  C07D417/10 ,  C07D417/04 ,  A61K31/549 ,  A61K45/06 ,  C07D495/04

    CPC classification number: C07D417/14 ,  A61K31/549 ,  A61K45/06 ,  C07D417/10 ,  C07D495/04

    Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 6-membered ring, and each of the remaining variables shown in the formula 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 Alzheimer's disease, are also disclosed.

    Abstract translation: 在其许多实施方案中，本发明提供了某些亚氨基噻嗪二氧化物化合物，包括式（I）化合物：（I）及其互变异构体和立体异构体，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，其中中环 在本文中作为“环B”）是三环取代基是任选取代的6元环，并且式中所示的各个残基如本文所定义。 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，包括阿尔茨海默氏病。

    TRICYCLIC SUBSTITUTED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS AND THEIR USE
    3.
    发明申请
    TRICYCLIC SUBSTITUTED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS AND THEIR USE 有权
    三环取代的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：US20150284379A1

    公开(公告)日：2015-10-08

    申请号：US14433298

    申请日：2013-10-14

    Applicant: MERCK SHARP & DOHME CORP.

    Inventor： Eric J. Gilbert ,  Jared N. Cumming ,  Andrew W. Stamford ,  Younong Yu ,  Jack D. Scott ,  Ulrich Iserloh ,  Lingyan Wang ,  John P. Caldwell

    IPC: C07D417/14 ,  A61K45/06 ,  C07D495/04 ,  A61K31/549 ,  C07D417/10

    CPC classification number: C07D417/14 ,  A61K31/549 ,  A61K45/06 ,  C07D417/10 ,  C07D495/04

    Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): (I) and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 6-membered ring, and each of the remaining variables shown in the formula 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 Alzheimer's disease, are also disclosed.

    Abstract translation: 在其许多实施方案中，本发明提供了某些亚氨基噻嗪二氧化物化合物，包括式（I）化合物：（I）及其互变异构体和立体异构体，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，其中中环 在本文中作为“环B”）是三环取代基是任选取代的6元环，并且式中所示的各个残基如本文所定义。 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，包括阿尔茨海默氏病。

    Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use
    7.
    发明授权
    Tricyclic substituted thiadiazine dioxide compounds as BACE inhibitors, compositions and their use 有权
    三环取代噻二嗪二氧化物作为BACE抑制剂，组合物及其应用

    公开(公告)号：US09422277B2

    公开(公告)日：2016-08-23

    申请号：US14433296

    申请日：2013-10-14

    Applicant: Merck Sharp & Dohme Corp.

    Inventor： Eric J. Gilbert ,  Jared N. Cumming ,  Andrew W. Stamford ,  Younong Yu ,  Jack D. Scott ,  Ulrich Iserloh

    IPC: C07D417/14 ,  C07D417/10 ,  C07D417/04 ,  A61K31/549 ,  A61K45/06 ,  C07D471/04

    CPC classification number: C07D417/14 ,  A61K31/549 ,  A61K45/06 ,  C07D417/10 ,  C07D471/04

    Abstract: In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomeros and said stereoisomers, wherein the middle ring (referred to herein as “ring B”) of the tricyclic substituent is an optionally substituted 5-membered ring, and each of the remaining variables shown in the formula 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 Alzheimer's disease, are also disclosed.

    Abstract translation: 在其许多实施方案中，本发明提供了某些亚氨基噻嗪二氧化物化合物，包括式（I）化合物及其互变异构体和立体异构体，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，其中中环（本文称为 三环取代基的“环B”是任选取代的5元环，并且式中所示的各个残基如本文所定义。 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，包括阿尔茨海默氏病。

    Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use
    8.
    发明授权
    Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use 有权
    作为BACE抑制剂，组合物及其用途的二氢化二氮杂二恶烷化合物

    公开(公告)号：US08940748B2

    公开(公告)日：2015-01-27

    申请号：US14221644

    申请日：2014-03-21

    Applicant: Merck Sharp & Dohme Corp.

    Inventor： Jack D. Scott ,  Andrew W. Stamford ,  Eric J. Gilbert ,  Jared N. Cumming ,  Ulrich Iserloh

    IPC: A01N43/54 ,  C07D239/42 ,  C07D417/12 ,  C07C309/30 ,  A61K31/495 ,  C07D239/14

    CPC classification number: A61K31/549 ,  A61K31/00 ,  A61K31/495 ,  A61K31/54 ,  A61K45/06 ,  C07C309/30 ,  C07D213/26 ,  C07D213/89 ,  C07D239/14 ,  C07D285/18 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  A61K2300/00

    Abstract: In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to β-amyloid (“Aβ”) production. 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 Alzheimer's disease, are also disclosed.

    Abstract translation: 在其许多实施方案中，本发明提供了某些亚氨基二嗪二氧化物化合物，包括式（I）化合物：并包括其立体异构体，以及所述化合物立体异构体的药学上可接受的盐，其中R1，R2，R3，R4，R5，R9， 环A，环B，m，n，p，-L 1 - ， - 2 - 和-L 3 - 独立地如本文所定义。 令人惊讶地发现本发明的新型亚氨基二嗪二氧化物化合物表现出预期使其作为BACE抑制剂和/或用于治疗和预防与“淀粉样蛋白”（“A”）生产有关的各种病理学的优点的性质。 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淀粉样蛋白β（Aβ）蛋白（包括阿尔茨海默氏病）相关的病理学的方法。

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