Invention Grant
US09085576B2 Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
有权
全氟化环丙基稠合的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 cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use
- Patent Title (中): 全氟化环丙基稠合的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.: US14199844Application Date: 2014-03-06
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Publication No.: US09085576B2Publication Date: 2015-07-21
- Inventor: Ana Elena Minatti , Jonathan D. Low , Jennifer R. Allen , Albert Amegadzie , James Brown , Michael J. Frohn , Angel Guzman-Perez , Paul E. Harrington , Patricia Lopez , Vu Van Ma , Nobuko Nishimura , Wenyuan Qian , Shannon Rumfelt , Robert M. Rzasa , Kelvin Sham , Adrian L. Smith , Ryan White , Qiufen Xue
- 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; G. Prabhakar Reddy
- Main IPC: C07D471/04
- IPC: C07D471/04 ; C07D265/12 ; C07D417/12 ; C07D417/14 ; C07D413/12 ; C07D413/14 ; A61K31/537 ; C07D413/10 ; C07D491/048

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 Ra, Rb, R1, R2, R3 and R7 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 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 methods for preparing compounds of the invention.
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