Invention Grant
- Patent Title: Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use
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Application No.: US15749895Application Date: 2016-08-04
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Publication No.: US10246429B2Publication Date: 2019-04-02
- Inventor: Jennifer R. Allen , Albert Amegadzie , Matthew P. Bourbeau , James A. Brown , Ning Chen , Michael J. Frohn , Longbin Liu , Qingyian Liu , Liping H. Pettus , Wenyuan Qian , Corey M. Reeves , Aaron C. Siegmund
- Applicant: AMGEN INC.
- Applicant Address: US CA Thousand Oaks
- Assignee: AMGEN INC.
- Current Assignee: AMGEN INC.
- Current Assignee Address: US CA Thousand Oaks
- Agent Markus Bergauer
- International Application: PCT/US2016/045650 WO 20160804
- International Announcement: WO2017/024180 WO 20170209
- Main IPC: C07D417/10
- IPC: C07D417/10 ; C07D279/08 ; C07D417/14 ; C07D471/04 ; C07D491/056 ; A61P25/28 ; A61P25/00 ; A61P25/16 ; C07D491/08 ; C07D491/107 ; C07D498/10 ; C07F7/08

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, A7, and each of Ra, Rb, R1, R2, R3, R8 R9 and R10 of Formula I, independently, are defined herein. The invention also provides pharmaceutical compositions comprising the compounds, and uses of the compounds and compositions for treatment of disorders and/or conditions related to Aβ 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.
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