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4-Amino-6-phenyl-5,6-dihydroimidazo [1,5-a] pyrazin-3 (2H) -one derivatives as beta-secretase inhibitors (BACE)
专利权人:
Janssen Pharmaceutica N.V.
发明人:
OEHLRICH, Daniel,GIJSEN, Henricus
申请号:
ES14732131
公开号:
ES2627633T3
申请日:
2014.06.12
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of Formula (I) ** Formula ** or a stereoisomeric form thereof, wherein R is selected from the C1-4 alkyl group optionally substituted with one or more substituents each independently selected from halo, -CN, C3 cycloalkyl -7 optionally substituted with one or more halo substituents, and C1-4 alkyloxy optionally substituted with one or more halo substituents; and C3-7 cycloalkyl optionally substituted with one or more substituents each independently selected from halo, -CN, and C1-4 alkyloxy optionally substituted with one or more halo substituents; R1 is selected from the group of hydrogen; halo; and C1-4 alkyl; R2 is selected from the C1-4 alkyl group optionally substituted with one or more substituents each independently selected from fluoro and C1-4 alkyloxy; and C3-7 cycloalkyl; R3 is in each case an independently selected halo substituent; n is an integer selected from 1 and 2; R4 is selected from (a) and (b): ** Formula ** wherein R5 and R6 are each independently selected from the aryl and heteroaryl group, each of which may be optionally substituted with one or more substituents each independently selected from the group of halo, -CN, C1-4 alkyl optionally substituted with one or more halo substituents, and C1-4 alkyloxy optionally substituted with one or more halo substituents; wherein the aryl is phenyl; wherein the heteroaryl is a 5-membered aromatic heterocycle selected from the group consisting of oxazole and pyrazole; or is a 6-membered aromatic heterocycle selected from the group consisting of pyridinyl, pyrimidinyl and pyrazinyl; or a pharmaceutically acceptable salt or solvate thereof.Un compuesto de Fórmula (I)**Fórmula** o una forma estereoisómera del mismo, en donde R se selecciona del grupo de alquilo C1-4 opcionalmente sustituido con uno o más sustituyentes cada uno seleccionado independientemente de halo, -CN, cicloalquilo C3-7 opcionalmente sustituido con uno o más sustituyentes halo, y alquiloxi C1-4 opcionalmente sustituido con un
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