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3,4-Dihydro-pyrrolo [1,2-a] pyrazin-1-ylamine derivatives useful as beta-secretase inhibitors (BACE)
专利权人:
JANSSEN PHARMACEUTICA N.V.
发明人:
TRABANCO-SUAREZ, ANDRÉS,DELGADO-JIMENEZ, FRANCISCA
申请号:
ES12707319
公开号:
ES2534973T3
申请日:
2012.03.07
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
A compound of Formula (I) ** Formula ** or a tautomer or stereoisomeric form thereof, wherein R1, R2, R3 are independently selected from the group consisting of hydrogen, halo, cyano, C1-3alkyl, mono and polyhalo-C1-3alkyl, and C3-6 cycloalkyl; R4 is selected from the group consisting of hydrogen, C1-3 alkyl, methoxymethyl, C3-6 cycloalkyl, mono and polyhalo-C1-3 alkyl, homoaryl, and heteroaryl; X1, X2, X3, X4 are independently C (R5) or N, with the proviso that no more than two of them represent N; R5 is selected from the group consisting of hydrogen, halo, cyano, C1-3 alkyl, mono and polyhalo-C1-3 alkyl, and C3-6 cycloalkyl; L is a bond or -NHCO-; 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 polyhalo-C1-3 alkyl, and mono and polyhalo -C1-3alkyloxy; heteroaryl is selected from the group consisting of pyridyl, pyrimidyl, pyrazinyl, pyridazyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, triazolyl, thiazolyl, thiadiazolyl, oxazolyl, and oxadiazolyl, each optionally substituted with one, two or three substituents selected among the group consisting of halo, cyano, C1-3 alkyl, C1-3 alkyloxy, mono and polyhalo-C1-3 alkyl, and mono and polyhalo-C1-3 alkyloxy; 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, R3 se seleccionan independientemente entre el grupo que consiste en hidrógeno, halo, ciano, alquilo C1-3, mono y polihalo-alquilo C1-3, y cicloalquilo C3-6; R4 se selecciona entre el grupo que consiste en hidrógeno, alquilo C1-3, metoximetilo, cicloalquilo C3-6, mono y polihalo-alquilo C1-3, homoarilo, y heteroarilo; X1, X2, X3, X4 son independientemente C(R5) o N, con la condición de que no más de dos de los mismos representan N; R5 se selecciona entre el grupo que consiste en hidrógeno, halo, ciano, alquil
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