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    4,6-DIARYLAMINOTHIAZINES AS BACE1 INHIBITORS AND THEIR USE FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION
    5.
    发明申请
    4,6-DIARYLAMINOTHIAZINES AS BACE1 INHIBITORS AND THEIR USE FOR THE REDUCTION OF BETA-AMYLOID PRODUCTION 有权
    4-DIARYLAMINOTHIAZINES作为BACE1抑制剂及其用于减少β-淀粉样生成的用途

    公开(公告)号：US20150329506A1

    公开(公告)日：2015-11-19

    申请号：US14653025

    申请日：2012-12-19

    申请人： BRISTOL-MYERS SQUIBB COMPANY

    发明人： Yong-Jin Wu ,  Jason M. Guernon

    IPC分类号： C07D279/06 ,  C07D417/14 ,  C07D417/10

    CPC分类号： C07D279/06 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14

    摘要： Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: (I) wherein R1 and R2 are independently hydrogen, or —CH3; or R1 and R2 can join together in a ring by adding —(CH2)4—; R3 is hydrogen or C1-C3 alkyl; Y and Z are independently a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4 dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, —C═OC1-4 alkyl, —SO2C1-4 alkyl, and C2-C4 alkynyl; A is selected from the group of phenyl, benzyl, oxazolyl, thiazolyl, isoxazolyl, imidazolyl, pyrazolyl, pyridyl, pyrimidinyl, and pyrazinyl groups which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4 dialkylamino, haloC1-4 alkyl, hydroxyC1-6 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is —NHCO—, or is a single bond; and L and Z together can be absent.

    摘要翻译： 包括其药学上可接受的盐的式（I）化合物在本文中阐述：（I）其中R 1和R 2独立地是氢或-CH 3; 或者R 1和R 2可以通过加入 - （CH 2）4 - R3是氢或C1-C3烷基; Y和Z独立地是C 6 -C 10 - 芳基或5-10元杂环基，其可以进一步被0-3个选自以下的取代基取代：卤素，羟基，氨基，C 1-4烷基氨基，C 1-4二烷基氨基 卤代C 1-4烷基，CN，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基，-C 1 -C 1-4烷基，-SO 2 C 1-4烷基和C 2 -C 4炔基; A选自苯基，苄基，恶唑基，噻唑基，异恶唑基，咪唑基，吡唑基，吡啶基，嘧啶基和吡嗪基，其可以进一步被0-3个选自以下的取代基取代：卤素，羟基，氨基， C 1-4烷基氨基，C 1-4二烷基氨基，卤代C 1-4烷基，羟基C 1-6烷基，CN，C 1 -C 6烷基或环烷基，C 1 -C 6烷氧基和C 2 -C 4炔基; L是-NHCO-，或是单键; 可以不存在L和Z。

    4,6-diarylaminothiazines as BACE1 inhibitors and their use for the reduction of beta-amyloid production
    10.
    发明授权
    4,6-diarylaminothiazines as BACE1 inhibitors and their use for the reduction of beta-amyloid production 有权
    4,6-二芳基氨基噻嗪作为BACE1抑制剂及其用于减少β-淀粉样蛋白产生的用途

    公开(公告)号：US09475784B2

    公开(公告)日：2016-10-25

    申请号：US14653025

    申请日：2012-12-19

    申请人： BRISTOL-MYERS SQUIBB COMPANY

    发明人： Yong-Jin Wu ,  Jason M. Guernon

    IPC分类号： C07D279/06 ,  C07D417/10 ,  C07D417/14 ,  C07D417/04 ,  C07D417/12

    CPC分类号： C07D279/06 ,  C07D417/04 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14

    摘要： Compounds of formula (I), including pharmaceutically acceptable salts thereof, are set forth herein: wherein R1 and R2 are independently hydrogen, or —CH3; or R1 and R2 can join together in a ring by adding —(CH2)4—; R3 is hydrogen or C1-C3 alkyl; Y and Z are independently a C6-C10-aryl group or a 5-10 membered heterocyclic group which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, —C═OC1-4alkyl, —SO2C1-4alkyl, and C2-C4 alkynyl; A is selected from the group of phenyl, benzyl, oxazolyl, thiazolyl, isoxazolyl, imidazolyl, pyrazolyl, pyridyl, pyrimidinyl, and pyrazinyl groups which can be further substituted with from 0-3 substituents selected from the group of halogen, hydroxy, amino, C1-4alkylamino, C1-4dialkylamino, haloC1-4 alkyl, hydroxyC1-6 alkyl, CN, C1-C6 alkyl or cycloalkyl, C1-C6 alkoxy, and C2-C4 alkynyl; L is —NHCO— or is a single bond; and L and Z together can be absent.