A 3-substituted tetrahydropyridopyrimidione derivative of the formula shown as a therapeutic composition having a high affinity for 5-HT1B, 5-HT1D and 5-HT1A serotonin receptors. The compounds are suitable for treating pathological states in which the serotonin concentration is reduced such as depression, mood disturbances with central nervous causation (dysthymia), anxiety such as panic attacks, sociophobia, obsessive-compulsive neuroses and post-traumatic stress symptoms, memory disturbances such as dementia, amnesias and age-related loss of memory and psychogenic eating disorders such as anorexia nervosa and bulimia nervosa. Wherein; one of the two radicals X and Y is CH2 and the other is NR1, R1 is hydrogen, C1-6alkyl branched or unbranched, CO-C1-4alkyl, CO2tBu, CO-phenyl and a phenylalkyl-C1-4 radical which in turn may be substituted on the aromatic system by F, Cl, Br, I, C1-4alkyl, C1-4alkoxy, trifluoromethyl, hydroxyl, amino, cyano or nitro, A is branched or unbranched C1-10alkylene or straight-chain or branched C2-10alkylene which comprises at least one group Z which is selected from O, S, NR2, cyclopropyl, CO2, CHOH, a double or triple bond, R2 is hydrogen and C1-4alkyl, B is 4-piperidine, 4-tetrahydro-1,2,3,6 pyridine, 4-piperazine or the corresponding cyclic compounds enlarged by one methylene group, with the linkage to A being via an N atom of B, and Ar is phenyl which is unsubstituted or substituted by C1-6alkyl branched or unbranched, O-C1-6alkyl branched or unbranched, OH, F, Cl, Br, I, trifluoromethyl, NR22, CO2R2, cyano or phenyl, or is tetralin, indan, naphthalene which is unsubstituted or substituted by C1-4alkyl or O-C1-4alkyl, anthracene or 5- or 6-membered aromatic heterocycles having 1 or 2 heteroatoms which are selected, independently of one another, from O and N.
Serotonin antagonists 3-substituted tetrahydropyridopyrimidinone derivatives for treating 5HT, depression and related disorders