Invention Grant
US09556135B2 Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
有权
氨基二氢噻嗪和氨基二氧化二氢噻嗪化合物作为β-分泌酶拮抗剂和使用方法
- Patent Title: Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use
- Patent Title (中): 氨基二氢噻嗪和氨基二氧化二氢噻嗪化合物作为β-分泌酶拮抗剂和使用方法
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Application No.: US14433769Application Date: 2013-10-10
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Publication No.: US09556135B2Publication Date: 2017-01-31
- Inventor: 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
- Applicant: Amgen Inc.
- Applicant Address: US CA Thousand Oaks
- Assignee: Amgen, Inc.
- Current Assignee: Amgen, Inc.
- Current Assignee Address: US CA Thousand Oaks
- Agent Bernard P. Friedrichsen; Markus Bergauer
- International Application: PCT/US2013/064400 WO 20131010
- International Announcement: WO2014/059185 WO 20140417
- Main IPC: C07D279/12
- IPC: C07D279/12 ; C07D417/04 ; C07D471/04 ; C07D239/74 ; C07D495/04 ; C07D213/79 ; C07D241/44 ; C07D417/12 ; C07D417/14 ; C07D513/04 ; C07D498/04 ; C07D513/10 ; C07D279/14 ; C07D519/00

Abstract:
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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