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Imidazo [4,5-c] quinolines as DNA inhibitors –- PK
专利权人:
MERCK PATENT GMBH
发明人:
FUCHSS, THOMAS,MEDERSKI, WERNER,ZENKE, FRANK
申请号:
ES11748260
公开号:
ES2536313T3
申请日:
2011.07.26
申请国别(地区):
ES
年份:
2015
代理人:
摘要:
Compounds of the formula (I) ** Formula ** wherein R1 is Y or - (CY2) n-Ar, R2 is Y, - (CY2) p- (C [YR6]) s-R7 or -Alk-R7 , R3 is Y or CN, R4 is Y, Hal, - (CY2) p-COOY or - (CY2) p-CO-NYY, R5 is A, Hal, - (CY2) p-OY, - (CY2) p -NYY, - (CY2) p-COOY, - (CY2) p-CO-NYY or - (CY2) p-NY-COY, R6 is Y, Hal, - (CY2) n-NYY, - (CY2) n -NY-COO- (CY2) n-SiA3, - (CY2) n-COOY, -CO-NYY, -CO-NY- (CY2) n-OY, - CO-NY- (CY2) n-NYY or SO2A , R7 is - (CY2) p-Ar or - (CY2) p-Het1, X is CH2, O, S or a single bond, Y is H or A, A is unbranched or branched alkyl with 1, 2, 3 , 4, 5, 6, 7, 8, 9 or 10 C atoms, where 1, 2, 3, 4, 5, 6 or 7 H atoms can be replaced, independently of each other, by Hal, Alk is alkylene with 1, 2, 3, 4, 5 or 6 C atoms, Ar is unsubstituted or mono-, di- or trisubstituted phenyl by Hal, A, CN, - (CY2) p-OY, - (CY2) p-NYY, - (CY2) p-COOY, - (CY2) p-CO-NYY or - (CY2) p-NY-COY, Het1 is an aromatic mono- or binuclear heterocycle with 2, 3, 4, 5, 6, 7, 8 or 9 atoms of C and 1, 2, 3 or 4 atoms of N, O and / or S, which p may not be substituted or may be mono-, di- or trisubstituted by Hal, A, CN, - (CY2) p-OY, - (CY2) p-NYY, - (CY2) p-COOY, - (CY2) p-CO-NYY, - (CY2) p-NY-COY or -SO2-Het², Het2 is a mononuclear saturated heterocycle with 2, 3, 4, 5, 6 or 7 C atoms and 1, 2, 3 or 4 atoms of N, O and / or S, which may not be substituted or which may be monosubstituted by A, Hal is F, Cl, Br or I, m is 0, 1, 2, 3 or 4, and n, p, s they are independently of each other, 0, 1, 2, 3, 4, 5 or 6, and / or their physiologically safe salts, tautomers and / or stereoisomers, including their mixtures in all proportions.Compuestos de la fórmula (I)**Fórmula** en donde R1 es Y o -(CY2)n-Ar, R2 es Y, -(CY2)p-(C[YR6])s-R7 o -Alk-R7, R3 es Y o CN, R4 es Y, Hal, -(CY2)p-COOY o -(CY2)p-CO-NYY, R5 es A, Hal, -(CY2)p-OY, -(CY2)p-NYY, -(CY2)p-COOY, -(CY2)p-CO-NYY o -(CY2)p-NY-COY, R6 es Y, Hal, -(CY2)n-NYY, -(CY2)n-NY-COO-(CY2)n-SiA3, -(CY2)n-COOY, -CO-NYY, -CO-NY-(CY2)n-OY, - CO-NY-(CY2)n-NYY o S
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