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3-AMINO-5,6-DIHYDRO-1H-PYRAZIN-2-ONE DERIVATIVES USEFUL FOR THE TREATEMENT OF ALZHEIMERS DISEASE AND OTHER FORMS OF DEMENTIA
专利权人:
JANSSEN PHARMACEUTICA NV
发明人:
TRABANCO-SUAREZ, ANDRES AVELINO,DELGADO-JIMENEZ, FRANCISCA,TRESADERN, GARY, JOHN
申请号:
NZ60389611
公开号:
NZ603896A
申请日:
2011.06.27
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
Abstract - 603896 Disclosed are 3-amino-5-[3-(aryl / heteroaryl)-phenyl]-5,6-dihydro-1H-pyrazin-2-one derivatives as represented by the general Formula (I) or stereoisomeric forms thereof, wherein R1 is selected from the group consisting of hydrogen, alkyl, mono- and polyhalo-alkyl, aryl and heteroaryl R2 is selected from the group consisting of hydrogen, alkyl, mono- and polyhalo-alkyl, aryl and heteroaryl X1, X2, X3, X4 are independently C(R3) or N, provided that no more than two thereof represent N each R3 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(R4)CO-, wherein R4 is hydrogen or 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, alkyl, alkyloxy, mono and polyhalo-alkyl 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 or an addition salt or a solvate thereof. Representative compounds include 3-(6-amino-2,4-dimethyl-5-oxo-2,3,4,5-tetrahydropyrazin-2-yl)-biphenyl-3-carbonitrile, 3-amino-5-[3-(5-methoxy-pyridin-3-yl)-phenyl]-1,5-dimethyl-5,6-dihydro-1H-pyrazin-2-one, 5-chloro-pyridine-2-carboxylic acid [3-(6-amino-2,4-dimethyl-5-oxo-2,3,4,5-tetrahydro-pyrazin-2-yl)-phenyl]-amide, 5-chloro-pyridine-2-carboxylic acid [3-(6-amino-2,4-dimethyl-5-oxo-2,3,4,5-tetrahydro-pyrazin-2-yl)-phenyl]-amide, 5-amino-3-(2,4-difluoro-biphenyl-5-yl)-1,3-dimethyl-2H-pyrazin-6-one, 5-amino-3-[2,4-difluoro-5-(5-methoxy-3-pyridyl)phenyl]-1,3-dimethyl-2H-pyrazin-6-one, 5-amino-3-(2,4-difluoro-5-pyrimidin-5-yl-phenyl)-1,3-dimethyl-2H-pyrazin-6-one, 5-chlo
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