发明名称 PYRAZOLONAPHTHYRIDINONE DERIVATIVES AS METAP2 INHIBITORS (METHIONINE AMINOPEPTIDASE TYPE-2)
摘要 The invention related to pyrazolonaphthyridinone derivatives of formula (I) to their preparation and to their therapeutic use as selective inhibitors of type 2 methionine aminopeptidase (hMETAP2).;
申请公布号 US2016060265(A1) 申请公布日期 2016.03.03
申请号 US201414778948 申请日期 2014.03.21
申请人 SANOFI 发明人 GUILLO Nathalie;MARTIN Valérie
分类号 C07D471/14;C07F5/04;C07D405/14 主分类号 C07D471/14
代理机构 代理人
主权项 1. Compound of the Formula (I)in which: X represents CH or a nitrogen atom, Y represents CH or a nitrogen atom, where X or Y is a nitrogen atom, R1 represents a (C1-C4)alkyl non substituted or substituted with one or more halogen atoms, R2 represents an aryl or a heteroaryl group, non substituted or substituted with one or more substituents independently selected from: a halogen atoma (C1-C4)alkyl group, where the alkyl group is non-substituted or substituted with one or more substituents independently selected from a halogen atom, a heterocyclyl, (C1-C4)alkoxy or hydroxy group or NHR3 O—R4 (CO)NR5R5.a heterocyclyl group, non substituted or substituted with one or more (C1-C4)alkyl groupa cycloalkyl groupa cyano groupNR6R6′SO2NR6R6′NHSO2R7 NH(CO)R7 (CO)R8 anda heteroaryl group R3 represents a (C1-C4)alkyl or a cycloalkyl group, R4 represents a hydrogen atom or a (C1-C4)alkyl group, where the alkyl group is non substituted or substituted with one or more halogen atom or heterocyclyl group, R5 and R5′ represent independently a hydrogen atom, a (C1-C4)alkyl or aryl group, R6 and R6′ represent independently a hydrogen atom or a (C1-C4)alkyl group, R7 represents a (C1-C4)alkyl group, and R8 represents a (C1-C4)alkyl, (C1-C4)alkoxy, cycloalkyl or hydroxy group, in the form of a base, enantiomers, diastereoisomers, tautomers including racemic mixture, and addition salt with an acid.
地址 Paris FR