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5,6-Dihydro-imidazo [1,2-a] pyrazin-8-ylamine derivatives useful as beta-secretase inhibitors (BACE)
专利权人:
Janssen Pharmaceutica NV
发明人:
TRABANCO-SUAREZ, Andrés,DELGADO-JIMENEZ, Francisca,VEGA RAMIRO, Juan,TRESADERN, Gary,GIJSEN, Henricus,OEHLRICH, Daniel
申请号:
ES11804561
公开号:
ES2648143T3
申请日:
2011.12.21
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 and R2 are independently selected from the group consisting of hydrogen, halo, cyano, C1-3 alkyl, mono- and polyhalo-C 1-3 alkyl and C 3-6 cycloalkyl; wherein halo is fluorine, chlorine or bromine, R3 is selected from the group consisting of hydrogen, C1-3 alkyl, C3-6 cycloalkyl, mono- and polyhalo-C1-3 alkyl, homoaryl and heteroaryl; X1, X2, X3, X4 are independently C (R4) or N, provided that no more than two of them represent N; each R4 is selected from the group consisting of hydrogen, halo, C1-3 alkyl, mono- and C1-3 polyhaloalkyl, cyano, C1-3 alkyloxy, mono- and C1-3 polyhaloalkyloxy; L is a bond or -N (R5) CO-, wherein R5 is hydrogen or C1-3 alkyl; 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 alkyloxy, mono- and C1-3 polyhaloalkyl; The heteroaryl is selected from the group consisting of pyridyl, pyrimidyl, pyrazyl, pyridazyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, triazolyl, thiazolyl, isothiazolyl, thiadiazolyl, oxazolyl and oxadiazolyl, each optionally substituted with one, two or three substituents selected from the group consisting of halo, cyano, C1-3 alkyl, C1-3 alkyloxy, mono- and C1-3 polyhaloalkyl or an addition salt or a solvate thereof.Un compuesto de Fórmula (I)**Fórmula** o un tautómero o una forma estereoisómera del mismo, en el que: R1 y R2 se seleccionan independientemente del grupo que consiste en hidrógeno, halo, ciano, alquilo C1-3, mono- y polihalo-alquilo C1-3 y cicloalquilo C3-6; en el que halo es flúor, cloro o bromo, R3 se selecciona del grupo que consiste en hidrógeno, alquilo C1-3, cicloalquilo C3-6, mono- y polihalo-alquilo C1-3, homoarilo y heteroarilo; X1, X2, X3, X4 son independientemente C(R4) o N, siempre que no más de dos de los mismos representen N; cada R4 se selecciona del grupo q
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