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4,7-dihydro-pyrazolo[1,5-a]pyrazin-6-ylamine derivatives useful as inhibitors of beta-secretase (bace)
专利权人:
JANSSEN PHARMACEUTICA NV
发明人:
TRABANCO-SUÁREZ ANDRÉS AVELINO,TRESADERN GARY JOHN,DELGADO-JIMÉNEZ FRANCISCA
申请号:
NZ60684811
公开号:
NZ606848A
申请日:
2011.09.20
申请国别(地区):
NZ
年份:
2015
代理人:
摘要:
Disclosed are N-{ 3-[6-amino-4-methyl-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5-a]pyrazin-4-yl]-phenyl} -benzamide derivatives as represented by the general formula (I), or a tautomer or a stereoisomeric form thereof, wherein R1 and R2 are independently selected from the group consisting of hydrogen, fluoro, cyano, alkyl, mono- and polyhalo-alkyl, and cycloalkyl or R1 and R2 taken together with the carbon atom to which they are attached may form a cycloalkanediyl ring R3 is selected from the group consisting of hydrogen, alkyl, cycloalkyl, mono- and polyhalo-alkyl, homoaryl and heteroaryl X1, X2, X3, X4 are independently C(R4) or N, provided that no more than two thereof represent N each R4 is selected from the group consisting of hydrogen, halo, alkyl, mono- and polyhalo-alkyl, cyano, alkyloxy, mono- and polyhalo-alkyloxy L is a bond or -N(R5)CO-, wherein R5 is hydrogen or alkyl R6 is hydrogen or trifluoromethyl 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, alkyl, alkyloxy, mono and polyhalo-alkyl and mono- and polyhalo-alkyloxy heteroaryl is selected from the group consisting of pyridyl, pyrimidyl, pyrazyl, pyridazyl, furanyl, thienyl, pyrrolyl, pyrazolyl, imidazolyl, triazolyl, thiazolyl, thiadiazolyl, oxazolyl, and oxadiazolyl, each optionally substituted with one, two or three substituents selected from the group consisting of halo, cyano, alkyl, alkyloxy, mono- and polyhalo-alkyl and mono- and polyhalo-alkyloxy or an addition salt or a solvate thereof. Representative compounds of formula (I) include N-{ 3-[6-amino-4-methyl-2-(trifluoromethyl)-4,7-dihydropyrazolo[1,5-a]pyrazin-4-yl]-4-fluorophenyl} -3,5-dichloropyridine-2-carboxamide, (R)-N-{ 3-[6-amino-4-cyclopropyl-4,7-dihydropyrazolo[1,5-a]pyrazin-4-yI]-4-fluorophenyl} -5-chloro-3-fluoropyridine-2-carboxamide, (R)-4-(3&rsquo-methoxybiphenyl-3-yl)-4-methyl-4,7-dihydropyrazolo[1,5-a]pyrazin-6-amine,
来源网站:
中国工程科技知识中心
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