Invention Grant
US09296734B2 Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
有权
全氟化的5,6-二氢-4H-1,3-恶嗪-2-胺化合物作为β-分泌酶抑制剂和使用方法
- Patent Title: Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
- Patent Title (中): 全氟化的5,6-二氢-4H-1,3-恶嗪-2-胺化合物作为β-分泌酶抑制剂和使用方法
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Application No.: US14192710Application Date: 2014-02-27
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Publication No.: US09296734B2Publication Date: 2016-03-29
- Inventor: Ana Elena Minatti , Jonathan D. Low , Jennifer R. Allen , Jian Chen , Ning Chen , Yuan Cheng , Ted Judd , Qingyian Liu , Patricia Lopez , Wenyuan Qian , Shannon Rumfelt , Robert M. Rzasa , Nuria A. Tamayo , Qiufen Xue , Bryant Yang , 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 G. Prabhaker Reddy; Bernard P. Friedrichsen; Markus Bergauer
- Main IPC: C07D413/14
- IPC: C07D413/14 ; C07D413/12 ; C07D471/04 ; C07D513/04 ; C07F7/08 ; C07D413/04 ; C07D413/10 ; C07D265/08 ; C07D498/04

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, each of R1 and R2, R3 and R7 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 Formulas II and III, and sub-formula embodiments thereof, intermediates and processes and methods useful for the preparation of compounds of Formulas I-III.
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