N-oxides of diazabicyclononyl pyrimidine derivatives and...

C - Chemistry – Metallurgy – 07 – D

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C07D 471/08 (2006.01) A61K 31/53 (2006.01) A61P 25/28 (2006.01)

Patent

CA 2750447

This invention relates to novel N-oxides of certain diazabicyclononyl pyrimidine derivatives and their use in the manufacture of pharmaceutical compositions. The compounds of the invention are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

La présente invention concerne de nouveaux N-oxydes de certains dérivés diazabicyclononyle pyrimidine et leur utilisation dans la fabrication de compositions pharmaceutiques. On a découvert que les composés de l'invention sont des ligands cholinergiques sur les récepteurs nicotiniques d'acétylcholine et des modulateurs de transporteurs et de récepteurs de monoamine. En raison de leur profil pharmacologique, les composés de l'invention peuvent être utiles dans le traitement de maladies et de troubles aussi divers que ceux liés au système cholinergique du système nerveux central (SNC), le système nerveux périphérique (SNP), aux maladies ou troubles liés à la contraction des muscles mous, aux maladies ou troubles endocriniens, aux maladies ou troubles liés à la neuro-dégénérescence, aux maladies ou troubles liés à l'inflammation, à la douleur, et aux symptômes de sevrage liés à l'arrêt de l'abus de substances chimiques.

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