abstract |
Certain novel imidazole derivatives N-substituted by a vinyl group itself carrying a mevalonic acid derivative or corresponding lactone are inhibitors of HMG-CoA reductase and are useful for lowering blood plasma cholesterol levels. n The compounds are of general formula (I): ##STR1## in which one of the groups R 1 and R 2 represents a C 1-6 alkyl group optionally substituted by one to three halogen atoms and the other represents a phenyl ring optionally substituted by one to five substituents selected from halogen atoms and hydroxyl, C 1-3 alkyl, C 1-3 alkoxy, S(O) n C 1-3 alkyl, (CH 2 ) m NR a R b , (CH 2 ) m NR c COR d and trifluoromethyl groups; n R 3 represents a phenyl ring optionally substituted by one to five substituents selected from halogen atoms and hydroxyl, C 1-3 alkyl, C 1-3 alkoxy, S(O) n C 1-3 alkyl, (CH 2 ) m NR a R b , (CH 2 ) m NR c COR d and trifluoromethyl groups; with the proviso that at least one of the groups R 1 , R 2 and R 3 contains an S(O) n C 1-3 alkyl, (CH 2 ) m NR a R b or (CH 2 ) m NR c COR d substituent; n X represents --CH═CH--; n Z represents ##STR2## and physiologically acceptable solvates, physiologically acceptable acid addition salts thereof when R 4 represents hydrogen or a physiologically acceptable and metabolically labile carboxyl protecting group when Z is (a), and quaternary ammonium derivatives thereof. |