发明申请
US20150259308A1 AMINO-DIHYDROTHIAZINE AND AMINO-DIOXIDO DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE ANTAGONISTS AND METHODS OF USE
有权
氨基二苯并恶嗪和氨基二氧化二硅杂环化合物作为β-分泌酶拮抗剂及其使用方法
- 专利标题: AMINO-DIHYDROTHIAZINE AND AMINO-DIOXIDO DIHYDROTHIAZINE COMPOUNDS AS BETA-SECRETASE ANTAGONISTS AND METHODS OF USE
- 专利标题(中): 氨基二苯并恶嗪和氨基二氧化二硅杂环化合物作为β-分泌酶拮抗剂及其使用方法
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申请号: US14433769申请日: 2013-10-10
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公开(公告)号: US20150259308A1公开(公告)日: 2015-09-17
- 发明人: Richard T. Lewis , Jennifer R. Allen , Yuan Cheng , Deborah Choquette , Oleg Epstein , Angel Guzman-Perez , Paul E. Harrington , Zihao Hua , Randall W. Hungate , Jason Brooks Human , Ted Judd , Qingyian Liu , Patricia Lopez , Ana Elena Minatti , Philip Olivieri , Karina Romero , Shannon Rumfelt , Robert M. Rzasa , Laurie Schenkel , John Stellwagen , Ryan White , Qiufen Xue , Xiao Mei Zheng , Wenge Zhong
- 申请人: AMGEN INC.
- 申请人地址: US CA Thousand Oaks
- 专利权人: AMGEN INC.
- 当前专利权人: AMGEN INC.
- 当前专利权人地址: US CA Thousand Oaks
- 国际申请: PCT/US2013/064400 WO 20131010
- 主分类号: C07D279/12
- IPC分类号: C07D279/12 ; C07D471/04 ; C07D239/74 ; C07D495/04 ; C07D213/79 ; C07D513/10 ; C07D417/12 ; C07D417/14 ; C07D513/04 ; C07D498/04 ; C07D279/14 ; C07D417/04 ; C07D241/44
摘要:
The present invention provides a new class of compounds useful for the modulation of beta-secretase enzyme (BACE) activity. The compounds have a general Formula I: wherein variables A4, A5, A6, A8, R1, R2, R3, R7 and n of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and corresponding uses of the compounds and compositions for treatment of disorders and/or conditions related to A-beta plaque formation and deposition, resulting from the biological activity of BACE. Such BACE mediated disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairments, schizophrenia and other central nervous system conditions. The invention further provides compounds of Formula II and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-II.
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