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Pyridonamides and their analogues demonstrating anticancer and antiproliferative activity
专利权人:
ДЕСИФЕРА ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи
发明人:
ФЛИНН Дэниел Л.,КАУФМАН Майкл Д.
申请号:
RU2014125230
公开号:
RU2014125230A
申请日:
2012.11.21
申请国别(地区):
RU
年份:
2015
代理人:
摘要:
1. The compound of formula I: Formula I or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer or tautomer thereof, wherein: X1 is halogen; X2 is halogen; Y is O, -NH; each R1 is individually and independently halogen, H, CC-alkyl, branched CC-alkyl, CC-cycloalkyl, CC-alkoxy, branched CC-alkoxy or cyano; each R2 individually and independently represents CC-alkyl, deutero-CC-alkyl, where the alkyl radical may be partially or fully deuterated, branched C -C-alkyl, branched deutero-CC-alkyl, where the alkyl residue may be partially or fully deuterated, CC-cycloalkyl, CC-alkoxy-CC-alkyl, branched CC-alkoxy-CC-alkyl or (R7) R6N-CC- alkyl; R3 is CC-alkyl, branched CC-alkyl, CC-cycloalkyl, -NR6 (R7), -R4, where each alkyl, branched alkyl or cycloalkyl may be optionally substituted with cyano, CC-alkoxy or hydroxy; each R4 is independently and individually selected from the group consisting of and where the symbol (##) represents the attachment point of residue R4; R5 represents oh CC-alkyl, branched CC-alkyl, CC-cycloalkyl or CC-alkoxy-CC-alkyl; each R6 and R7 is individually and independently H, CC-alkyl or branched CC-alkyl; each cycloalkyl and R4 are independently and optionally substituted - (R8); each R8 individually and independently represents CC-alkyl, branched CC-alkyl, halogen, - (CH) -CN, - (CH) -OR6, - (CH) -NR6 (R7), - ( CH) -SO-CC-alkyl, - (CH) -C (O) NR6 (R7), - (CH) -C (O) -CC-heterocyclyl or - (CH) -CC-heterocyclyl, where each alkyl or alkylene is optionally substituted with one or two CC alkyls; each m is individually and n1. Соединение формулы I:Формула Iили его фармацевтически приемлемая соль, гидрат, сольват, энантиомер, стереоизомер или таутомер, где:X1 представляет собой галоген;X2 представляет собой галоген;Y представляет собой O, -NH;каждый R1 индивидуально и независимо представляет собой галоген, H, C-C-алкил, разветвленный C-C-алкил, C-C-циклоалкил, C-C-алкокси, разветвленный C-C-алкокси или циано;каждый R2 индивидуальн
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