发明公开
EP2547686A1 AMINO -DIHYDROOXAZINE AND AMINO - DIHYDROTHIAZINE SPIRO COMPOUNDS AS BETA - SECRETASE MODULATORS AND THEIR MEDICAL USE
有权
氨基 - 二氢恶嗪及氨基酸以β-分泌酶调节剂dihydrothiazine螺化合物及其医药用途
- 专利标题： AMINO -DIHYDROOXAZINE AND AMINO - DIHYDROTHIAZINE SPIRO COMPOUNDS AS BETA - SECRETASE MODULATORS AND THEIR MEDICAL USE
- 专利标题（中）： 氨基 - 二氢恶嗪及氨基酸以β-分泌酶调节剂dihydrothiazine螺化合物及其医药用途
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申请号： EP11714873.4申请日： 2011-03-14
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公开(公告)号： EP2547686A1公开(公告)日： 2013-01-23
- 发明人: CHEN, Jian, J. , ZHONG, Wenge , YANG, Bryant , QIAN, Wenyuan , LOPEZ, Patricia , WHITE, Ryan , WEISS, Matthew , JUDD, Ted , POWERS, Timothy , CHENG, Yuan , DINEEN, Thomas , EPSTEIN, Oleg , LOW, Jonathan , MARX, Isaac , MINATTI, Ana Elena , PARAS, Nick, A. , POTASHMAN, Michele
- 申请人： Amgen Inc.
- 申请人地址： One Amgen Center Drive Thousand Oaks, California 91320-1799 US
- 专利权人： Amgen Inc.
- 当前专利权人： Amgen Inc.
- 当前专利权人地址： One Amgen Center Drive Thousand Oaks, California 91320-1799 US
- 代理机构： Grünecker, Kinkeldey, Stockmair & Schwanhäusser
- 优先权： US314024P 20100315
- 国际公布： WO2011115928 20110922
- 主分类号： C07D498/10
- IPC分类号： C07D498/10 ; C07D498/20 ; C07D513/10 ; C07D513/20 ; A61K31/537 ; A61K31/5386 ; A61K31/547 ; A61P25/28
摘要：
The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula (I): wherein A
1 , A
2 , A
3 , A
4 , A
5 , A
6 , R
2 , R
7 , X, Y and Z of Formula (I) are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).
1 , A
2 , A
3 , A
4 , A
5 , A
6 , R
2 , R
7 , X, Y and Z of Formula (I) are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula (I), intermediates and processes useful for the preparation of compounds of Formula (I).
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