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    FUSED AMINODIHYDROTHIAZINE DERIVATIVES
    1.
    发明申请
    FUSED AMINODIHYDROTHIAZINE DERIVATIVES 有权
    熔融氨基二氢卟吩衍生物

    公开(公告)号：US20120190672A1

    公开(公告)日：2012-07-26

    申请号：US13354716

    申请日：2012-01-20

    申请人： Adrian Hall ,  Christopher Neil Farthing ,  Jose Luis Castro Pineiro

    发明人： Adrian Hall ,  Christopher Neil Farthing ,  Jose Luis Castro Pineiro

    IPC分类号： A61K31/542 ,  A61P25/28 ,  A61P3/10 ,  C07D513/04

    CPC分类号： C07D513/04

    摘要： The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C≡N; and pharmaceutically acceptable salts thereof; which compound has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

    摘要翻译： 本发明涉及式（I）的稠合氨基二氢噻嗪衍生物：其中X是氢或氟; A是CH或N; Y是甲基，乙基，一氟甲基，二氟甲基，三氟甲基，二氟乙基，甲氧基，乙氧基，甲氧基甲基或-C≡N; 及其药学上可接受的盐; 该化合物具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

    FUSED AMINODIHYDRO-OXAZINE DERIVATIVES
    2.
    发明申请
    FUSED AMINODIHYDRO-OXAZINE DERIVATIVES 有权
    熔融氨基二氧杂环丁烷衍生物

    公开(公告)号：US20120202804A1

    公开(公告)日：2012-08-09

    申请号：US13386092

    申请日：2010-07-21

    申请人： John Mark Ellard ,  Christopher Neil Farthing ,  Adrian Hall

    发明人： John Mark Ellard ,  Christopher Neil Farthing ,  Adrian Hall

    IPC分类号： A61K31/5365 ,  A61P25/28 ,  C07D498/04

    CPC分类号： C07D498/04

    摘要： A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

    摘要翻译： 由通式（I）表示的化合物或其药学上可接受的盐或其溶剂合物，其中环A为C 6-14芳基等，L为-NReCO-等（其中Re为氢原子 等），环B为C 6-14芳基等，X为C 1-3亚烷基等，Y为单键等，Z为C1-3亚烷基等 R 1和R 2各自独立地为氢原子等，R 3，R 4，R 5和R 6独立地为氢原子，卤素原子等，具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

    Fused aminodihydro-oxazine derivatives
    3.
    发明授权
    Fused aminodihydro-oxazine derivatives 有权
    熔融氨基二氢恶嗪衍生物

    公开(公告)号：US09079914B2

    公开(公告)日：2015-07-14

    申请号：US13386092

    申请日：2010-07-21

    申请人： John Mark Ellard ,  Christopher Neil Farthing ,  Adrian Hall

    发明人： John Mark Ellard ,  Christopher Neil Farthing ,  Adrian Hall

    IPC分类号： C07D498/04 ,  A61K31/5365

    CPC分类号： C07D498/04

    摘要： A compound represented by the general formula: or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1 and R2 are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

    摘要翻译： 由通式表示的化合物或其药学上可接受的盐或其溶剂化物，其中环A是C 6-14芳基等，L是-NReCO-等（其中Re是氢原子或 环）B是C 6-14芳基等，X是C 1-3亚烷基等，Y是单键等，Z是C 1-3亚烷基等，R 1 和R 2各自独立地为氢原子等，R 3，R 4，R 5和R 6独立地为氢原子，卤素原子等，具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

    Fused aminodihydrothiazine derivatives
    4.
    发明授权
    Fused aminodihydrothiazine derivatives 有权
    融合氨基二氢噻嗪衍生物

    公开(公告)号：US08338407B2

    公开(公告)日：2012-12-25

    申请号：US13354716

    申请日：2012-01-20

    申请人： Adrian Hall ,  Christopher Neil Farthing

    发明人： Adrian Hall ,  Christopher Neil Farthing

    IPC分类号： C07D513/04 ,  A61K31/542

    CPC分类号： C07D513/04

    摘要： The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; A is CH or N; Y is methyl, ethyl, monofluoromethyl, difluoromethyl, trifluoromethyl, difluoroethyl, methoxy, ethoxy, methoxymethyl or —C≡N; and pharmaceutically acceptable salts thereof; which compound has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

    摘要翻译： 本发明涉及式（I）的稠合氨基二氢噻嗪衍生物：其中X是氢或氟; A是CH或N; Y是甲基，乙基，一氟甲基，二氟甲基，三氟甲基，二氟乙基，甲氧基，乙氧基，甲氧基甲基或-C≡N; 及其药学上可接受的盐; 该化合物具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。

    FUSED AMINODIHYDROPYRIMIDONE DERIVATIVES
    5.
    发明申请
    FUSED AMINODIHYDROPYRIMIDONE DERIVATIVES 有权
    熔融的氨基二氢咪唑啉酮衍生物

    公开(公告)号：US20120202828A1

    公开(公告)日：2012-08-09

    申请号：US13386199

    申请日：2010-07-21

    申请人： Jose Luis Castro Pineiro ,  Adrian Hall ,  Andrew Madin ,  Ngoc-Tri Vo

    发明人： Jose Luis Castro Pineiro ,  Adrian Hall ,  Andrew Madin ,  Ngoc-Tri Vo

    IPC分类号： A61K31/519 ,  A61P25/28 ,  C07D491/048

    CPC分类号： C07D491/048

    摘要： A compound represented by the general formula (I) or a pharmaceutically acceptable salt thereof or a solvate thereof, wherein Ring A is a C6-14 aryl group or the like, L is —NReCO— or the like (wherein Re is a hydrogen atom or the like), Ring B is a C6-14 aryl group or the like, X is a C1-3 alkylene group or the like, Y is a single bond or the like, Z is a C1-3 alkylene group or the like, R1, R2 and Rx are each independently a hydrogen atom or the like, and R3, R4, R5 and R6 are independently a hydrogen atom, a halogen atom or the like, has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.

    摘要翻译： 由通式（I）表示的化合物或其药学上可接受的盐或其溶剂合物，其中环A为C 6-14芳基等，L为-NReCO-等（其中Re为氢原子 等），环B为C 6-14芳基等，X为C 1-3亚烷基等，Y为单键等，Z为C1-3亚烷基等 R 1，R 2和R 3各自独立地为氢原子等，R 3，R 4，R 5和R 6独立地为氢原子，卤素原子等，具有A＆bgr; 产生抑制作用或BACE1抑制作用，可用作由A＆Bgr引起的神经变性疾病的预防或治疗剂; 并以阿尔茨海默氏型痴呆为代表。