| abstract |
"TETRALONE DERIVATIVES AS ANTITUMORAL AGENTS". The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, X and Y have the meanings defined below, process for the manufacture of such compounds and pharmaceuticals containing such a compound, which have HDAC inhibitory activity. R1 is selected from hydrogen, (1-4C) alkyl, COOH, COO (1-4C) alkyl, R2, R3, R4, R5 are independently selected from hydrogen, a halogen atom, one (1-4C) alkyl-, trifluoromethyl-, hydroxy-, (1-4C) alkoxy, aryloxy-, arylalkyloxy-, nitro-, amino- (1-4C) alkylamino-, di [(1-4C) alkyl] amino, piperidino, morpholine, pyrrolidino, (1-4C) alkanoylamino- or an aryl group, or a heteroaryl group, or R2 and R3 together or R3 and R4 together or R4 and R5 together, respectively, may form a (1-3C) alkylenedioxy ring, or R2 and R3 together or R3 and R4 together or R4 and R5 together, respectively, may form a (3-5C) alkylene chain. Y is CH ~ 2 ~ -CH ~ 2 ~ -, X is an alkylene chain of 4 to 10 carbon atoms which may be saturated or unsaturated with one or more double bonds or one or two triple bonds or one double and one triple bond, and which may be branched or unbranched or interrupted by a (3-7C) cycloalkyl ring. |