N-oxides of pyridylmethylpiperazine and -piperidine derivatives

• Main Authors: VAN AAR, MARCEL P. M, VAN AMSTERDAM, PETER H, ZORGDRAGER, JAN, HERREMANS, ARNOLDUS H. J, DEN BESTEN, CATHALINE, BARF, GERRIT A, BAKKER, JOHAN ANTOINE
• Format: Patent
• Language: English
• Published: 29.07.2009
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The invention concerns N-oxides of certain pyridylmethylpiperazine and -piperidine derivatives as alternatives or as `prodrugs' of their respective parent compounds, to pharmaceutical compositions containing these N-oxides, to methods for preparing them, and methods for preparing compositions. The invention relates to N-oxides of compounds having formula (a), wherein the symbols have the meanings given in the description, and wherein the oxidized nitrogen atom may be the nitrogen atom in the pyridyl ring of R5, or the nitrogen atom in the piperidine ring (when Z is carbon) or either one of the nitrogen atoms in the piperazine ring (when Z is nitrogen), or bóth the nitrogen atom connected to R5 via a methylene group, ánd the nitrogen atom in the pyridyl ring of R5, and tautomers, stereoisomers, pharmacologically acceptable salts, hydrates and solvates thereof. The invention also relates to the uses of such N-oxides and compositions, particularly for the manufacture of a medicament useful in the treatment of affections or diseases of the central nervous system caused by disturbances in either the dopaminergic or serotinergic systems, for example Parkinson's disease, aggression, anxiety disorders, autism, vertigo, depression, disturbances of cognition or memory and in particular schizophrenia and other psychotic disorders.