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New derivatives of (6-oxo-1,6-dihydro-pyrimidin-2-yl) -amide, its preparation and its pharmaceutical use as phosphorylation inhibitors of AKT
专利权人:
SANOFI;SANOFI
发明人:
CARRY, JEAN-CHRISTOPHE,CERTAL, VICTOR,HALLEY, FRANK,KARLSSON, KARL ANDREAS,SCHIO, LAURENT,THOMPSON, FABIENNE
申请号:
ES10742014
公开号:
ES2464125T3
申请日:
2010.07.01
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
Products of formula (I): ** Formula ** in which: R 1 represents an aryl or heteroaryl radical optionally substituted with one or more identical or different radicals chosen from halogen atoms and hydroxyl radicals, CN, nitro, -COOH , -COOalk, -NRxRy, -CONRxRy, -NRxCORy, -CORy, -NRxCO2Rz, alkoxy, phenoxy, alkylthio, alkyl, alkenyl, alkynyl, cycloalkyl, O-cycloalkyl, heterocycloalkyl, aryl and heteroaryl; the latter being alkoxy, phenoxy, alkylthio, alkyl, alkenyl, alkynyl, heterocycloalkyl, aryl and heteroaryl radicals themselves optionally substituted with one or more identical or different radicals chosen from the halogen atoms and the hydroxyl, alkoxy, NRvRw, heterocycloalkyl radicals or heteroaryl; the aryl and heteroaryl radicals being optionally substituted with one or more alkyl and alkoxy radicals themselves optionally substituted with one or more halogen atoms; the heterocycloalkyl and heteroaryl radicals may also contain an oxo radical, R represents a hydrogen atom or forms with R1 a cycle of 5 or 6 saturated or partially or totally unsaturated links fused to an aryl or heteroaryl moiety and optionally containing one or more different heteroatoms chosen from O, S, N, NH and Nalk, this bicyclic radical being optionally substituted with one or several identical or different radicals chosen from halogen atoms and CO-NH2, hydroxyl, alkyl and alkoxy radicals; said latter radical being itself optionally substituted with a hydroxyl, alkoxy, NH2, NHAlk or N (alk) 2 radical; R2, R3, identical or different, independently represent a hydrogen atom, a halogen atom or an alkyl radical optionally substituted with one or more halogen atoms; R4 represents a hydrogen atom; R5 represents a hydrogen atom or an alkyl radical optionally substituted with one or more halogen atoms; NRxRy being such that Rx represents a hydrogen atom or an alkyl radical and Ry represents a hydrogen atom, a cycloalkyl radical or an alkyl radical optionally substituted with one or more identical or
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