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PYRIDYL- AND PYRIMIDINYL-SUBSTITUTED PYRROLE-, THIOPHENE- AND FURANE-DERIVATIVES AS KINASE INHIBITORS
专利权人:
NERVIANO MEDICAL SCIENCES S.R.L.
发明人:
VANOTTI, ERMES,CALDARELLI, MARINA,CIRLA, ALESSANDRA,FORTE, BARBARA,ERMOLI, ANTONELLA,MENICHINCHERI, MARIA,PILLAN, ANTONIO,SCOLARO, ALESSANDRA
申请号:
NZ57220207
公开号:
NZ572202A
申请日:
2007.03.19
申请国别(地区):
NZ
年份:
2012
代理人:
摘要:
Disclosed are 5-(2-amino-pyrimidin-4-yl)-1H-pyrrole-3-carboxylic acid amide derivatives as represented by the general formula (I), wherein: wherein G is nitrogen atom W is NR1 R1 and R3? independently represent hydrogen or an optionally substituted group selected from alkyl, cycloalkyl, alkenyl, alkynyl, heterocyclyl, heterocyclylalkyl, aryl, arylalkyl, heterocyclyloxy-alkyl and alkoxycarbonyl group R2 is hydrogen or halogen atom, or an optionally substituted group selected from aryl, cycloalkyl and heterocyclyl group R4 is hydrogen or halogen atom, or an optionally substituted alkyl or alkenyl group R5 is hydrogen or halogen atom R6 is hydrogen atom or the amino group NHR7 R7 is hydrogen, an optionally substituted group selected from alkyl, aryl, cycloalkyl and heterocyclyl or -CO-R1 or a pharmaceutically acceptable salt thereof. Representative compounds include 5-(2-amino-pyrimidin-4-yl)-2-phenyl-1H-pyrrole-3-carboxylic acid amide, 5-(2-amino -pyrimidin-4-y1)-2-thiophen-3-yl-1H-pyrrole-3-carboxylic acid amide, 5-(2-amino -pyrimidin-4-yl)-2-(5-methyl-thiophen-2-yl)-1H-pyrrole-3-carboxylic acid amide and 5-(2-amino-5-chloro-pyrimidin-4-yl)-2-(2-fluoro-phenyl)-1H-pyrrole-3-carboxylic acid amide. Further disclosed is a pharmaceutical composition which comprises a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, as defined above, at least one pharmaceutically acceptable excipient, carrier and/or diluent and optionally one or more chemotherapeutic agents for treating cell proliferative disorders caused by and/or associated with an altered protein kinase activity or associated with an altered Cdc7 kinase, and particularly for the treatment of cancer, benign prostate hyperplasia, familial adenomatosis, polyposis, neuro-fibromatosis, psoriasis, vascular smooth cell proliferation associated with atherosclerosis, pulmonary fibrosis, arthritis glomerulonephritis and post-surgical stenosis and restenosis.
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