Iracil derivatives as enzyme inhibitors

Details Iracil derivatives as enzyme inhibitors Iracil derivatives as enzyme inhibitors

C - Chemistry, Metallurgy

07

D

C07D 239/54 (2006.01) A61K 31/505 (2006.01) A61K 31/675 (2006.01) C07D 239/56 (2006.01) C07F 9/6506 (2006.01)

Patent

CA 2139836

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 select- ed 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,CH2OCH2CH20H 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 composi- tions containing them, their uses in medicine and the preparation of such compounds are disclosed.

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