3-CYANO-4-(4-PHENYL-PIPERIDIN-1-YL)-PYRIDIN-2-ONE DERIVATIVES

摘要

Disclosed is a 3-cyano-1-alkyl-4-(-4-phenyl-piperidin-1-yl)-pyridine-2(1H)-one compound of formula (I) including any stereo chemically isomeric form thereof, wherein R1 is alkyl; R2 is hydrogen; hydroxyl; fluoro; alkyl substituted with hydroxyl; alkyl with fluoro; or alkyloxy substituted with fluoro; R3 is hydrogen or halo; or a pharmaceutically acceptable salt thereof or a solvate thereof; for treating or preventing a central nervous system disorder selected from the group of anxiety disorders, psychotic disorders, personality disorders, substance-related disorders, eating disorders, mood disorders, migraine, epilepsy or convulsive disorders, childhood disorders, cognitive disorders, neurodegeneration, neurotoxicity and ischemia. Also disclosed is a process for preparing a compound as claimed in claim 1, characterized by a) reacting an 3-cyano-pyridin-2(1H)-one intermediate of formula (II) wherein Y represents a suitable leaving group, with an 4-piperidine intermediate of formula (III) in a suitable reaction-inert solvent, in the presence of a suitable base, under heating conditions or reacting an intermediate of formula (II) with an intermediate of formula (III) in a suitable reaction-inert solvent, in the presence of a suitable base, a suitable catalyst, under heating conditions; reacting a compound of formula (I-b) with a suitable fluorinating agent in a suitable reaction-inert solvent, under a moderately low temperature; c) reacting an intermediate of formula (IV) with a suitable fluorinating agent in a suitable reaction-inert solvent, under a moderately low temperature; d) hydrogenating an intermediate of formula (XIV) in a suitable solvent and in the presence of a suitable catalyst and a suitable base.