- 专利标题： PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE
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申请号： EP14717004.7申请日： 2014-03-06
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公开(公告)号： EP2964644B1公开(公告)日： 2018-12-26
- 发明人: MINATTI, Ana Elena , LOW, Jonathan, D. , ALLEN, Jennifer, R. , AMEGADZIE, Albert , BROWN, James , FROHN, Michael, J. , GUZMAN-PEREZ, Angel , HARRINGTON, Paul, E. , LOPEZ, Patricia , MA, Vu Van , NISHIMURA, Nobuko , QIAN, Wenyuan , RUMFELT, Shannon , RZASA, Robert, M. , SHAM, Kelvin , SMITH, Adrian, L. , WHITE, Ryan , XUE, Qiufen
- 申请人： AMGEN, INC.
- 申请人地址： One Amgen Center Drive Thousand Oaks, CA 91320 US
- 专利权人： AMGEN, INC.
- 当前专利权人： AMGEN, INC.
- 当前专利权人地址： One Amgen Center Drive Thousand Oaks, CA 91320 US
- 代理机构： Hoffmann Eitle
- 优先权： US201361775380P 20130308; US201461939580P 20140213
- 国际公布： WO2014138484 20140912
- 主分类号： C07D413/14
- IPC分类号： C07D413/14 ; C07D413/10 ; C07D413/12 ; C07D417/12 ; C07D417/14 ; C07D471/04 ; C07D265/12 ; C07D491/048 ; A61P25/00 ; A61K31/536
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, 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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