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5- (3-Aminophenyl) -5-alkyl-5,6-dihydro-2H- [1,4] oxazin-3-amine derivatives for the treatment of disorders in which beta-secretase is involved
专利权人:
Janssen Pharmaceutica; N.V.
发明人:
GIJSEN, Henricus Jacobus Maria,VAN BRANDT, Sven Franciscus Anna
申请号:
ES12794730
公开号:
ES2582473T3
申请日:
2012.12.04
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of Formula (I) ** Formula ** or a tautomer or stereoisomeric form thereof, wherein R 1 is fluoro, fluoromethyl, difluoromethyl or trifluoromethyl; R2 is hydrogen or trifluoromethyl; or R1 and R2 form a divalent radical>; = CF2; R3 is hydrogen, C1-3 alkyl, cyclopropyl, mono- or C1-3 polyhaloalkyl; R4 is hydrogen or fluoro; Ar is homoaryl or heteroaryl; wherein homoaryl is phenyl or phenyl substituted with one, two or three substituents selected from the group consisting of halo, cyano, C1-3 alkyl, C1-3 alkyl-oxy, mono- and C1-3 polyhaloalkyl, mono- and polyhaloalkyl C1-3-oxy; heteroaryl is selected from the group consisting of pyridyl, pyrimidyl, pyrazyl, pyridazyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, triazolyl, tetrazolyl, thiazolyl, isothiazolyl, thiadiazolyl, oxazolyl, isoxazolyl, and oxadiazolyl, each optionally substituted two or three substituents selected from the group consisting of halo, cyano, C1-3 alkyl, C2-3 alkynyl, C1-3 alkyl, mono- and C1-3 polyhaloalkyl, mono- and C1-3-oxy polyhaloalkyl, and C 1-3 alkyl-C 1-3 alkyl oxy; or an addition salt thereof.Un compuesto de Fórmula (I)**Fórmula** o un tautómero o una forma estereoisomérica del mismo, en el que R1 es fluoro, fluorometilo, difluorometilo o trifluorometilo; R2 es hidrógeno o trifluorometilo; o R1 y R2 forman un radical divalente >;=CF2; R3 es hidrógeno, alquilo C1-3, ciclopropilo, mono- o polihaloalquilo C1-3; R4 es hidrógeno o fluoro; Ar es homoarilo o heteroarilo; en el que homoarilo es fenilo o fenilo sustituido con uno, dos o tres sustituyentes seleccionados del grupo que consiste en halo, ciano, alquilo C1-3, alquil C1-3-oxi, mono- y polihaloalquilo C1-3, mono- y polihaloalquil C1-3-oxi; heteroarilo se selecciona del grupo que consiste en piridilo, pirimidilo, pirazilo, piridazilo, furanilo, tienilo, pirrolilo, pirazolilo, imidazolilo, triazolilo, tetrazolilo, tiazolilo, isotiazolilo, tiadiazolilo, oxazolilo, isoxazolilo, y oxadiazolilo, cada uno opcionalmente sus
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