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Aza-heterociclos bicíclicos sustituidos y análogos como moduladores de sirtuina
专利权人:
GlaxoSmithKline LLC
发明人:
CASAUBON, Rebecca,NARAYAN, Radha,OALMANN, Christopher,VU, Chi
申请号:
ES12842273
公开号:
ES2627347T3
申请日:
2012.10.19
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound represented by the structural formula (I): Formula ** ** wherein E is N and D is C and B is N and A is CR or a pharmaceutically acceptable salt thereof, wherein: each R is independently hydrogen, halogen, OH, C> = N selected, C1-C4 alkyl, C2-C4 alkyl substituted with halogen, C1-C4 alkoxy-substituted alkyl C1- C4, C1-C8 alkyl substituted with hydroxy, OR3, O- (C1-C4) - OR3, S- (C1-C2) -, S- (C1-C4 alkyl substituted with halogen) -, N (C1 C4 substituted with hydroxy) 2, N (C1-C4 alkyl substituted with methoxy) 2, N (C1-C4) (C1-C4 substituted by hydroxy) -, N (C1-C4) (C1-C4 10 substituted with methoxy) -, N (C1-C4 alkyl substituted with hydroxy) (C1-C4 substituted with methoxy) -, cycloalkyl C5- C7, and nonaromatic 4- to 8-membered, methyl substituted with halogen and C3 C4 R1 is selected from: ** Formula ** wherein R1 is optionally substituted with one or more substituents independently selected from halogen, C> = N, C1-C4 alkyl, C1-C4 alkyl substituted with halogen, C1-C4 alkyl substituted with C1-C4 alkoxy, C1-C8 alkyl substituted with hydroxy, O-R3, O- (C1-C4) -OR3,> = O, C3-C7cycloalkyl, SO2R3, S-R3, (C1-C4) - N (R3) (R3), N (R3) (R3), O- (C1-C4 alkyl) -N (R3) (R3), O- (C0-C4 alkyl) -CR3R3 (C0-C4 alkyl) - , (C1-C4) -O- (C1-C4 alkyl) -N (R3) (R3), C (O) -N (R3) (R3), (C1-C4) -C (> = O ) -N (R3) (R3), O- (C0-C4 alkyl) -CRxRx- (C0-C4 alkyl) -, CRxRx, phenyl, O-phenyl, heterocycle, O- (heterocycle), 3,4-methylenedioxy , 3,4-methylenedioxy substituted with halogen, 3,4-ethylenedioxy, 3,4-ethylenedioxy and substituted by halogen, wherein any phenyl substituent R1 or heterocycle is optionally substituted with one or more substituents independently selected from halogen, C≡ N, C1-C4 alkyl, C1-C4 alkyl substituted with hal geno, O- (C1-C4 alkyl substituted with halogen) -, O- (C1-C4) -, S- (C1-C4) - and S- (C1-C4 substituted by halogen) R2 is a carbocycle or heterocycle, wherein R2 is optionally substituted with one or more substituents independently selected f
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