Heterocyclic compounds

Details Heterocyclic compounds Heterocyclic compounds

C - Chemistry, Metallurgy

07

D

C07D 453/02 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01)

Patent

CA 2111895

A B S T R A C T HETEROCYCLIC COMPOUNDS Compounds of formula I and their pharmaceutically acceptable Image salts in which R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 are joined together so that CR1-CR2 is a double bond; is selected from -CH2CH2-, -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 medicine.

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