abstract |
Azetidinone Compounds of Formula (I) - Z-R1 XCR4R $ ¿X¿Y wherein R 1 and R 2, which are the same or different, are each selected from hydrogen, halogen, or C (C 1-6 alkyl; R 4 and R 5, which are the same or different, each selected from hydrogen, C 1-6 alkyl, C 2-6 alkenyl, aryl, arylC 1-6 alkyl and heteroarylC 1-4 alkyl each optionally substituted, or R 4 and R 5 may be linked to form the remainder of a cycloalkyl ring; X is a linker group; Y is an optionally substituted aryl group; Z is oxygen and R 3 is C 1 -C 8 alkyl, C 1-4 cycloalkyl, heteroaryl, heteroarylC 1-4 alkyl, aryl or arylC 1-4 alkyl, each of which is optionally or Z is S (O) n wherein n is O, 1 or 2 and R 3, C 1-8 cycloalkyl, C (3-8) CycloalkylC (1-) alkyl, aryl, arylC 1-4 alkyl, heteroaryl or heteroarylC 1-6 alkyl, each of which is optionally substituted, the compounds are inhibitors of the enzyme Lp-PLA2 and are useful in the therapy, especially in the treatment of atherosclerosis. |