| 摘要 |
Novel uracil derivatives of formula (I) and esters and prodrugs thereof wherein R1 is H, C1-8 straight or branched-chain alkyl, C2-6 alkenyl, or (C1-3 alkyl-C3-6 cycloalkyl-C1-3 alkyl) optionally substituted by 1 or 2 substituents selected from -OR8 or -NR8R9 (wherein R8 and R9 are the same or different and are selected from H, C1-6 straight or branched-chain alkyl, and aralkyl); or a -CH2ZR10, -ZCH2R10, or CH2ZR10aZR10 group (wherein R10a is selected from C1-6 straight or branched-chain alkylene and R10 is selected from C1-6 straight or branched chain alkyl) each of R10a and R10 being optionally substituted by 1 or 2 substituents independently selected from -OR8 and -NR8R9 (wherein R8 and R9 are as defined above) and Z is selected from O, S, -CH2O-, or -CH2S-); R2 is selected from O or S; R3 is selected from O, S, -SO, -SO2, -NR8, C=O, or -C1-6 straight or branched-chain alkyl; R4 is selected from H, C1-4 straight or branched-chain alkyl, halogen, -OR11 (wherein R11 is C1-4 straight or branched-chain alkyl optionally substituted by halogen, aryl, C3-6 cycloalkyl, (C1-3 alkyl-C3-6 cycloalkyl), C2-6alkenyl or C2-6alkynyl), methylenedioxy, -CX3 (wherein X is halogen), NO2, or CN; R5 is selected from H, halogen or -OR11; R6 is selected from H, or Y-Ar-R7(m) (wherein Y is selected from O, S, -SO, -SO2, -NR8, C=O, or -C1-6 straight or branched-chain alkyl, Ar is phenyl or naphthyl, m is 1-3 and R7 is selected from R8, -CO2R8, -COR8, -CONR8R9, R8aOR8 (wherein R8a is selected from C1-6 straight or branched-chain alkyl, and aralkyl), -CN, -CX3 (wherein X is halogen), -OR8, OCX3 (wherein X is halogen), -SR8, -SO2R8, -OR8aO- (when m=1), -NO2, -NR8R9, -NHCOR8, -NHSO2R8, fluoro, chloro, bromo, or iodo, or a combination thereof); provided that when R1 is H, CH2OCH2CH2OH or CH2OCH(CH2OH)2, R2 is O, R3 is -CH2 then R4, R5 and R6 are other than -OCH3, -OCH2CH3, -OCH2Ph, or -O-iso-propyl, pharmaceutical compositions containing them, their uses in medicine and the preparation of such compounds are disclosed. |
