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5,6-Dihydro-2H- [1,4] oxazin-3-ylamine derivatives useful as beta-secretase inhibitors (BACE)
专利权人:
Janssen Pharmaceutica; N.V.
发明人:
TRABANCO-SUAREZ, Andrés,ROMBOUTS, Frederik,TRESADERN, Gary,VAN GOOL, Michiel,MACDONALD, Gregor,MARTINEZ LAMENCA, Carolina,GIJSEN, Henricus
申请号:
ES11723974
公开号:
ES2607083T3
申请日:
2011.06.08
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of Formula (I) ** Formula ** or a tautomer or stereoisomeric form thereof, in which R1, R2 and R3 are independently selected from the group consisting of hydrogen, fluoro, cyano, C1-3 alkyl, mono- and polyhalo-C1-3 alkyl, and C3-6 cycloalkyl; R4 is fluoro or trifluoromethyl; or R1 and R2, or R3 and R4, taken together with the carbon atom to which they are attached, can form a C3-6-diyl cycloalkane ring; R5 is selected from the group consisting of hydrogen, C1-3 alkyl, cyclopropyl, mono- and polyhalo-C1-3 alkyl, homoaryl and heteroaryl; X1, X2, X3, X4 are independently C (R6) or N, with the proviso that no more than two of them represent N; each R6 is selected from the group consisting of hydrogen, halo, C1-3 alkyl, mono- and polyhalo-C1-3 alkyl, cyano, C1-3-oxy alkyl, mono- and polyhalo-C1-3-oxy alkyl ; L is a bond or -N (R7) CO-, wherein R7 is hydrogen or C1-3 alkyl; Ar is homoaryl or heteroaryl; Homoaryl is phenyl or phenyl substituted with one, two or three substituents selected from the group consisting of halo, cyano, C1-3alkyl, C1-3alkyl-oxy, mono- and polyhalo-C1-3alkyl, mono- and polyhalo-C1-3-alkyl alkyl; 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 with or three substituents selected from the group consisting of halo, cyano, C1-3 alkyl, C2-3 alkynyl, C1-3 alkyl, mono- and polyhalo-C1-3 alkyl, mono- and polyhalo-C1 alkyl -3-oxy, and C 1-3 alkyl-oxy-C 1-3 alkyl oxy; or an addition salt or solvate thereof.Un compuesto de Fórmula (I)**Fórmula** o un tautómero o una forma estereoisomérica del mismo, en la que R1, R2 y R3 se seleccionan independientemente del grupo que consiste en hidrógeno, fluoro, ciano, alquilo de C1-3, mono- y polihalo-alquilo de C1-3, y cicloalquilo de C3-6; R4 es fluoro o trifluorometilo; o R1 y R2, o R3 y
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