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Pyrazolyl quinoxaline kinase inhibitors
专利权人:
ASTEX THERAPEUTICS LIMITED
发明人:
SAXTY GORDON,MURRAY CHRISTOPHER WILLIAM,BERDINI VALERIO,BESONG GILBERT EBAI,HAMLETT CHRISTOPHER CHARLES FREDERICK,JOHNSON CHRISTOPHER NORBERT,WOODHEAD STEVEN JOHN,READER MICHAEL,REES DAVID CHARLES,MEV
申请号:
NZ60272611
公开号:
NZ602726A
申请日:
2011.04.28
申请国别(地区):
NZ
年份:
2014
代理人:
摘要:
Disclosed are 3-(1-methylpyrazole-4-yl)-6-([phenyl]-alkyl-amino)-quinoxaline derivatives as represented by the general formula (I) including any tautomeric or stereochemically isomeric form thereof, a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof, wherein n represents an integer equal to 0, 1, 2, 3 or 4 R1 represents hydrogen, alkyl, alkenyl, hydroxyalkyl, haloalkyl, hydroxyhaloalkyl, cyanoalkyl, alkoxyalkyl wherein each alkyl may optionally be substituted each R1a is independently selected from hydrogen, alkyl, hydroxyalkyl, alkyl substituted with amino or mono- or di(alkyl)amino or -NH(cycloalkyl), cyanoalkyl, alkoxyalkyl, and alkyl substituted with one or more fluoro atoms R3 represents hydroxyl, alkoxy, hydroxyalkoxy, alkoxy substituted with -NR10R11, alkyl, alkenyl, alkynyl, haloalkyl optionally substituted with -O-C(=O)-alkyl, hydroxyalkyl optionally substituted with -O-C(=O)-alkyl, hydroxyalkenyl, hydroxyalkynyl, hydroxyhaloalkyl, cyanoalkyl, alkyl substituted with carboxyl, alkyl substituted with -C(=O)-alkyl, alkyl substituted with -C(=O)-O-alkyl, alkyl substituted with alkoxyalkyl-O-C(=O)-, alkyl substituted with alkoxyalkyl-C(=O)-, alkyl substituted with -O-C(=O)-alkyl, alkoxyalkyl wherein each alkyl may optionally be further substituted and wherein the remaining substituent are as defined herein. Representative compounds include 3-(1-methylpyrazol-4-yl)-6-([2-chloro-3,5-dimethoxy-phenyl]-ethyl-amino)-quinoxaline, 3-(1-methylpyrazol-4-yl)-6-([3,5-dimethoxy-phenyl]-(3-[S-2-hydroxymethyl-pyrrolindin-1-yl]propyl)-amino)-quinoxaline hydrochloride, 3-(pyrazol-4-yl)-6-([3,5-dimethoxy-phenyl]-([pyrrolindin-1-yl]propyl)-amino)-quinoxaline hydrochloride, 3-(1-(2-hydroxyethyl)-pyrazol-4-yl)-6-([3,5-dimethoxy-phenyl]-(3-aminopropyl)-amino)-quinoxaline, 3-(1-methyl-pyrazol-4-yl)-6-([3,5-dimethoxy-phenyl]-(2-hydroxy-3-methylbutyl)-amino)-quinoxaline and 3-(1-methylpyrazol-4-yl)-6-([3,5-dimethoxy-phenyl]-(3-(isopropylamino)-2-hydroxy-
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