abstract |
Compounds of formula (I) and their pharmaceutically acceptable salts in which R1 is hydrogen or hydroxy; R2 is hydrogen; or R?1 and R2¿ are joined together so that CR1-CR2 is a double bond; X is selected from -CH¿2?CH2-, -CH = CH-, -C C-, -CH2O-, -OCH2-, -CH2NH-, -NHCH2-, -CH2CO-, -COCH2-, -N = CH-, -CH = N-, -CH2S- and -SCH2- (wherein the sulphur atom in the latter two groups may optionally bear one or two oxygen atoms); Ar is a heterocyclic moiety containing up to three heteroatoms independently selected from nitrogen, oxygen and sulphur; and wherein Ar may optionally be unsubstituted or may bear one or more substituents independently selected from halogeno, hydroxy, amino, nitro, cyano, carboxy, carbamoyl, alkyl, alkenyl, alkynyl, alkoxy, alkylamino, di-alkylamino, N-alkylcarbamoyl, di-N,N-alkylcarbamoyl, alkoxycarbonyl, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl, alkanoylamino, ureido, N'-alkylureido, alkanoyl and oxime derivatives thereof and O-alkyl ethers of said oxime derivatives; are inhibitors of squalene synthase and hence useful in treating medical conditions in which a lowering of cholesterol is beneficial. Processes preparing these derivatives, pharmaceutical compositions containing them are also described together with their use in medecine. |