HETEROARYLSUBSTITUTED DERIVATIVES OF 1,3-DIOXOLAN-4-YLMETHOXYPHENYL-1-PIPERAZINYLPHENYL-2,4-DIHYDRO- 2-ALKYL-3H-1,2,4-TRIAZOL-3-ONE, METHOD AND INTERMEDIATES FOR THEIR PRODUCTION AND PHARMACEUTICAL PREPARATIONS

摘要

Heteroaryl-substituted 1,3-dioxolan-4-ylmethoxyphenyl-1-piperazinylphenyl-2,4-dihydro-2-alkyl-3H-1,2,4-triazol-3-one derivatives of formula (I) wherein A and B together represent a bivalent radical of formula -N = CH- (a), -CH = N- (b), -CH 2 -CH 2 - (c), -CH = CH- (d), -C (= O) -CH 2 (e) ) or -CH 2 -C (= O) - (f), wherein in the bivalent radical of formula (a) or (b) the hydrogen atom is optionally replaced by an alkyl group having 1 to 6 carbon atoms and in the bivalent radical of formula (c), (d) , (e) or (f) is optionally one or two hydrogen atoms replaced with C 1 -C 6 alkyl; R 1 is H, alkyl of 1 to 6 C or halogen; R 2 is H or halogen; R 3 is H, alkyl of 1 to 8 C, cycloalkyl of 3 to 6 C, or alkyl of 1 to 8 C substituted with hydroxyl, oxo, cycloalkyl of 3 to 6 C or aryl; Het is a heterocyclic radical as defined in the claims; and aryl is phenyl; optionally substituted with 1-6C alkyl or halogen; their N-oxides, stereochemically isomeric forms, and pharmaceutically acceptable acid addition salts thereof; intermediates of formula (III) wherein R 1, R 2 and Het are as defined above and W is a leaving group such as halogen or sulfonyloxy and their acid addition salts or stereochemically isomeric forms; a process for the preparation of compounds of formula (I) and pharmaceutical compositions thereof. The compounds of formula (I) are useful in the treatment of hyperlipidemia