Abstract: The invention is concerned with novel compounds of the formula the pharmaceutically acceptable acid addition salts thereof and the stereochemically isomeric forms thereof, wherein X is oxygen or sulphur; R1 is hydrogen or halo; R2 is hydrogen, C1-4alkyl, phenylmethyl or halophenylmethyl; Alk is C1-4alkanediyl; —Z—A— is a bivalent radical selected from the group consisting of —S—CH2—CH2, —S—CH2—CH2—CH2—, —S—CH═CH—, —CH═CH—CH═CH—, —C(═CHR3)—CH2—CH2—CH2—, —CH═CH—O—, —CHR4—CH2—CH2—, —CHR4—CH2—CH2—CH2—, —CHR4—CH2—CH2—CH2—CH2—; in said bivalent radicals one hydrogen may be replaced by C1-4alkyl; R3 is phenyl or halophenyl; each R4 independently represents hydrogen, hydroxy, phenylmethyl or halophenylmethyl.

Abstract: There is disclosed a process for preparing an enantiomeric form of the compound having the formula: or a pharmaceutically acceptable acid addition salt thereof, wherein said process comprises the steps of: (a) reacting a racemic mixture of said compound with a chiral acid or acid chloride selected from the group consisting of tartaric acid, malic acid, mandelic acid, camphor sulfonic acid, 4,5-dihydro-1H-2-benzopyran-2-carboxylic acid, and the acid chlorides thereof, to form a mixture of diastereomeric salts or esters; (b) physically separating said mixture of diastereomeric salts or esters by selective crystallization or chromatography; and (c) converting said separated diastereomeric salts or esters into the corresponding enantiomeric forms of said compound by hydrolysis in an acidic or basic aqueous medium.

Abstract: The present invention concerns the compounds of formula ##STR1## the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dashed line designates an optional bond; R.sup.1 and R.sup.2 are each independently hydrogen, halogen, C.sub.1-6 alkyl or C.sub.1-6 alkyloxy; R.sup.3 and R.sup.4 are each independently hydrogen, C.sub.1-6 alkyl, phenyl or phenyl substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, trifluoromethyl, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, mercapto, amino, mono- and di(C.sub.1-6 alkyl)-amino, carboxyl, C.sub.1-6 alkyloxycarbonyl and C.sub.1-6 alkylcarbonyl; Alk is C.sub.1-4 alkanediyl; D is a pyrimidinone, piperidone or a benzimidozolidinone; having antipsychotic activity; their preparation, compositions containing them and their use as a medicine.

Abstract: The present invention is concerned with novel compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof and the stereochemically isomeric forms thereof, whereinAlk represents C.sub.1-4 alkanediyl;D is a bicyclic heterocycle of formula ##STR2## wherein each R.sup.1 independently is C.sub.2-6 alkenyl; C.sub.2-6 alkynyl; C.sub.3-6 cycloalkyl optionally substituted with C.sub.1-4 alkyl; C.sub.1-19 alkyl optionally substituted with C.sub.3-6 cycloalkyl, halo, C.sub.1-6 alkyloxy or cyano; and each R.sup.2 independently is hydrogen or C.sub.1-4 alkyl. Novel compounds; compositions; processes for preparing novel compounds and intermediates are described.

Abstract: Novel 2,9-disubstituted-4H-pyrido[1,2-a]pyrimidin-4-ones having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, whereinAlk represents C.sub.1-4 alkanediyl,D is a bicyclic heterocycle of formula ##STR2## wherein R.sup.1 represents C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl, carboxaldehyde, carboxyl, C.sub.1-10 alkylcarbonyloxyC.sub.1-4 alkyl; each R.sup.2 represents hydrogen or C.sub.1-4 alkyl; R.sup.3 represents C.sub.1-4 alkyl, hydroxyC.sub.1-4 alkyl or methyl substituted with phenyl, 5-methyl-2-furanyl or 3-pyridinyl; and R.sup.4 represents C.sub.1-3 alkyl, phenyl, 5-methyl-2-furanyl or 3-pyridinyl.

Abstract: 3-Piperidinyl-indazole derivatives and their pharmaceutically acceptable acid addition salts being useful antagonists of neurotransmitters; pharmaceutical compositions containing the same and a method of treating warm-blooded animals suffering from diseases associated with the release of said neutrotransmitters.

Abstract: 2-Amino-pyrimidininone derivatives possessing serotonin-antagonistic and anti-histaminic properties. Compositions containing these compounds as the active ingredient. Method of treating subjects suffering from diseases and/or disorders associated with the release of neurotransmitters, in particular, a method of treating subjects suffering form sleep disorders with 2-aminopyrimidinone derivatives substituted with a 4-bis(aryl)methylene-1-piperidinyl group; and a method of treating subjects suffering from psychotic diseases and/or disorders with 2-aminopyrimidinone derivatives substituted with a 4-arylcarbonyl-1-piperidinyl, 4-benzazolyl-1-piperidinyl, 4-benzazolyl-1-piperazinyl or 4-indolyl-1-piperidinyl, 4-benzo[b]furanyl-1-piperidinyl or 4-benzo[b]thienyl-1-piperidinyl group.

Abstract: 2-Amino-pyrimidininone derivatives possessing serotonin-antagonistic and antihistaminic properties. Compositions containing these compounds as the active ingredient. Method of treating subjects suffering from diseases and/or disorders associated with the release of neurotransmitters, in particular, a method of treating subjects suffering from sleep disorders with 2-aminopyrimidinone derivatives substituted with a 4-bis(aryl)methylene-1-piperidinyl group; and a method of treating subjects suffering from psychotic diseases and/or disorders with 2-aminopyrimidinone derivatives substituted with a 4-arylcarbonyl-1-piperidinyl, 4-benzazolyl-1-piperidinyl, 4-benzazolyl-1-piperazinyl or 4-indolyl-1-piperidinyl, 4-benzo[b]furanyl-1-piperidinyl or 4-benzo[b]thienyl-1-piperidinyl group.

Abstract: The invention relates to C.sub.2-20 alkanoic acid esters of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6, 7,8,9-tetrahydro-9-hydroxy-2 -methyl-4H-pyrido[1,2-a]pyrimidin-4-one, pharmaceutically acceptable acid addition salts thereof, and enantiomeric forms thereof, which are useful in the treatment of warm-blooded animals suffering from psychotic diseases.

Abstract: 3-Piperidinyl-indazole derivatives and their pharmaceutically acceptable acid addition salts being useful antagonists of neurotransmitters; pharmaceutical compositions containing the same and a method of treating warm-blooded animals suffering from diseases associated with the release of said neutrotransmitters.

Abstract: The present invention relates to novel 3-piperidinyl-1,2-benzisoxazoles having long-acting antipsychotic properties and which are useful in the treatment of warm-blooded animals suffering from psychotic diseases. Methods of preparing said compounds and compositions containing the same.

Abstract: 2-Amino-pyrimidininone derivatives possessing serotonin-antagonistic and antihistaminic properties. Compositions containing these compounds as the active ingredient. Method of treating subjects suffering from diseases and/or disorders associated with the release of neurotransmitters, in particular, a method of treating subjects suffering from sleep disorders with 2-aminopyrimidinone derivatives substituted with a 4-bis(aryl)methylene-1-piperidinyl group; and a method of treating subjects suffering from psychotic diseases and/or disorders with 2-aminopyrimidinone derivatives substituted with a 4-arylcarbonyl-1-piperidinyl, 4-benzazoyl-1-piperidinyl, 4-benzazolyl-1-piperazinyl or 4-indolyl-1-piperidinyl, 4-benzo[b]furanyl-1-piperidinyl or 4-benzo[b]thienyl-1-piperidinyl group.

Abstract: 3-Piperazinyl-1,2-benzazoles and their pharmaceutically acceptable acid addition salts having useful antipsychotic properties and being useful in the treatment of a variety of disorders in which serotonin and/or dopamine release is of predominant importance.

Abstract: 3-Piperazinyl-1,2-benzazoles and their pharmaceutically acceptable acid addition salts having useful antipsychotic properties and being useful in the treatment of a variety of disorders in which serotonin and/or dopamine release is of predominant importance.

Abstract: 3-Piperdinyl-1,2-benzisothiazoles and 3-piperidinyl-1,2-benzisoxazoles and their pharmaceutically acceptable acid addition salts having useful antipsychotic properties and being useful in the treatment of a variety of complaints in which serotonin release is of predominant importance.

Abstract: Novel derivatives of hydroxy- or amino-substituted (piperidinylalkyl)quinazolines which are useful agents in the treatment of warmblooded animals suffering from diseases according to the vascular bed in which excessive serotonin release occurs.

Abstract: Novel [[bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones, wherein the pyrimidinone-ring is embraced within a bicyclic system, being useful compounds in the treatment of psychosomatic disorders.

Abstract: 1H-Indol-3-yl containing 1,3-dimethyl-1H-purine-2,6-diones having psychotropic activity.

Abstract: Novel [[bis(aryl)methylene]-1-piperidinyl]alkyl-pyrimidinones, wherein the pyrimidinone-ring is embraced within a bicyclic system, being useful compounds in the treatment of psychosomatic disorders.

Abstract: Novel quinazoline derivatives, comprising in the heterocyclic part of their quinazoline nucleus at least one carbonyl or thiocarbonyl group and a particularly substituted piperidinyl-alkyl side chain, said compounds being potent serotonin-antagonists.