N-oxides of pyridylmethylpiperazine and -piperidine derivatives

摘要

The invention concerns N-oxides of certain pyridylmethylpiperazine and -piperidine derivativesas alternatives or as `prodrugs' of their respective parent compounds,to pharmaceutical compositions containing these N-oxides, to methods for preparingthem, and methods for preparing compositions. The invention relates to N-oxidesof compounds having formula (a), wherein the symbols have the meanings givenin the description, and wherein the oxidized nitrogen atom may be the nitrogen atomin the pyridyl ring of R, or the nitrogen atom in the piperidine ring(when Z is carbon) or either one of the nitrogen atoms in the piperazine ring (whenZ is nitrogen), or bóth the nitrogen atom connected to R via amethylene group, ánd the nitrogen atom in the pyridyl ring of R, andtautomers, stereoisomers, pharmacologically acceptable salts, hydrates andsolvates thereof. The invention also relates to the uses of such N-oxides andcompositions, particularly for the manufacture of a medicament useful in thetreatment of affections or diseases of the central nervous system caused by disturbancesin either the dopaminergic or serotinergic systems, for example Parkinson'sdisease, aggression, anxiety disorders, autism, vertigo, depression, disturbancesof cognition or memory and in particular schizophrenia and other psychotic disorders.