C5-C6-OXACYLIC FUSED IMINOTHIAZINE DIOXIDE COMPOUNDS BEARING AN ETHER LINKER AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    12.
    发明申请
    C5-C6-OXACYLIC FUSED IMINOTHIAZINE DIOXIDE COMPOUNDS BEARING AN ETHER LINKER AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
    C5-C6-OXACYLIC稠合的亚硝基二硫化物化合物,带有一种醚键作为BACE抑制剂,组合物和它们的用途

    公开(公告)号:WO2017139209A1

    公开(公告)日:2017-08-17

    申请号:PCT/US2017/016634

    申请日:2017-02-06

    CPC classification number: C07D513/04 C07D513/10

    Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiazine 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 1 , R 2 , R 3 , R A , ring A, m, n, -L 1 -, ring B, R B , 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,本发明提供了带有醚接头的某些C5-C6-氧杂环稠合亚氨噻嗪二氧化物化合物,包括式(I)化合物或其互变异构体,以及所述化合物的药学上可接受的盐 和所述互变异构体,其中R 1,R 2,R 3,R A,环A,m, n,-L 1 - ,环B,R B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。

    C5-C6-OXACYCLIC FUSED IMINOPYRIMIDINONE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    13.
    发明申请
    C5-C6-OXACYCLIC FUSED IMINOPYRIMIDINONE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
    C5-C6-氧化丙烯酰胺嘧啶酮化合物作为BACE抑制剂,组合物及其使用

    公开(公告)号:WO2016085780A1

    公开(公告)日:2016-06-02

    申请号:PCT/US2015/061727

    申请日:2015-11-20

    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 R N , R 1 , R A , ring A, m, n, -L 1 -, ring B, R B , 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C5-C6-氧杂环稠合的亚氨基嘧啶酮化合物,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RN,R1,RA,环 A,m,n,-L1-,环B,RB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。

    C5-C6-FUSED TRICYCLIC IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    14.
    发明申请
    C5-C6-FUSED TRICYCLIC IMINOTHIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
    C5-C6-聚合三环十二烷基二氧化物作为BACE抑制剂,组合物及其使用

    公开(公告)号:WO2016053828A1

    公开(公告)日:2016-04-07

    申请号:PCT/US2015/052554

    申请日:2015-09-28

    Abstract: In its many embodiments, the present invention provides certain C5-C6 fused tricyclic iminothiadiazine compounds, including compounds Formula (I): or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R 1A , R 2 , R 3 , R A , 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/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C5-C6稠合的三环亚氨基二嗪化合物,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,R2,R3, 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。

    C6-AZASPIRO IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS
    16.
    发明申请
    C6-AZASPIRO IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS 审中-公开
    C6-AZASPIRO IMINOTHIADIAZINE DIOXIDES作为BACE抑制剂

    公开(公告)号:WO2014099768A1

    公开(公告)日:2014-06-26

    申请号:PCT/US2013/075369

    申请日:2013-12-16

    CPC classification number: C07D513/10

    Abstract: In its many embodiments, the present invention provides certain C2-ring-substituted thiadiazine compounds, including compounds Formula (I): (structure represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R 1 , R 4 , ring A, R A , m, -L 1 -, R L , and ring C 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C2环取代的噻二嗪化合物,包括式(I):(其结构)或其互变异构体的化合物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R1,R4,环 A,RA,m,-L1-,RL和环C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。

    TRICYCLIC SUBSTITUTED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE
    18.
    发明申请
    TRICYCLIC SUBSTITUTED THIADIAZINE DIOXIDE COMPOUNDS AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
    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:WO2014062549A1

    公开(公告)日:2014-04-24

    申请号:PCT/US2013/064795

    申请日:2013-10-14

    Abstract: In its many embodiments, the present invention provides 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 作为“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。

    PENTAFLUOROSULFUR IMINO HETEROCYCLIC COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE
    19.
    发明申请
    PENTAFLUOROSULFUR IMINO HETEROCYCLIC COMPOUNDS AS BACE-1 INHIBITORS, COMPOSITIONS, AND THEIR USE 审中-公开
    PENTAFLUOROSULFUR IMINO杂环化合物作为BACE-1抑制剂,组合物及其使用

    公开(公告)号:WO2011044185A2

    公开(公告)日:2011-04-14

    申请号:PCT/US2010051558

    申请日:2010-10-06

    CPC classification number: C07D239/22 C07D405/04

    Abstract: In its many embodiments, the present invention provides certain pentafluorosulfur imino heterocyclic compounds, including compounds Formula (a) and pharmaceutically acceptable salts thereof. Compounds of Formula(a) have the general structure: (a) wherein each variable is selected independently and as defined herein. 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 (Aß) protein, including Alzheimers Disease, are also disclosed.

    Abstract translation: 在其许多实施方案中,本发明提供某些五氟硫亚氨基杂环化合物,包括式(a)化合物及其药学上可接受的盐。 式(a)的化合物具有通式结构:(a)其中每个变量是独立选择的,如本文所定义。 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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