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, WENYU
申请号:
PH12015502001
公开号:
PH12015502001A1
申请日:
2015.09.08
申请国别(地区):
PH
年份:
2016
代理人:
摘要:
PERFLUORINATED CYCLOPROPYL FUSED 1,3-OXAZIN-2-AMINE COMPOUNDS AS BETA-SECRETASE INHIBITORS AND METHODS OF USE ABSTRACT OF THE DISCLOSURE 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: {INSERT STRUCTURE HERE} 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, Alzheimers 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.