Capsaicin receptor ligands

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 213/74 (2006.01) A61K 31/44 (2006.01) A61K 31/4402 (2006.01) A61K 31/444 (2006.01) A61K 31/4725 (2006.01) A61K 31/495 (2006.01) A61K 31/496 (2006.01) A61P 19/02 (2006.01) A61P 25/02 (2006.01) A61P 25/06 (2006.01) A61P 29/00 (2006.01) C07D 213/75 (2006.01) C07D 217/22 (2006.01) C07D 241/20 (2006.01) C07D 295/192 (2006.01) C07D 295/21 (2006.01) C07D 295/215 (2006.01) C07D 401/04 (2006.01) C07D 403/04 (2006.01) C07D 405/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2415606

Disclosed are diaryl piperazines and related compounds. These compounds are selective modulators of capsaicin receptors, including human capsaicin receptors, that are, therefore, useful in the treatment of a chronic and acute pain conditions, itch and urinary incontinence. Methods of treatment of such disorders and well as packaged pharmaceutical compositions are also provided. Compounds of the invention are also useful as probes for the localization of capsaicin receptors and as standards in assays for capsaicin receptor binding and capsaicin receptor mediated cation conductance. Methods of using the compounds in receptor localization studies are given.

L'invention concerne des diaryl pipérazines et des composés correspondants. Ces composés sont des modulateurs sélectifs des récepteurs de la capsicine, notamment des récepteurs de la capsicine humaine, qui sont, pour ces motifs utiles dans le traitement d'états de douleurs aiguës et chroniques, du prurit et de l'incontinence d'urine. L'invention concerne également des méthodes de traitement de ces troubles et des compositions pharmaceutiques emballées. Des composés de l'invention sont aussi utiles en tant que sondes destinées à la localisation des récepteurs de la capsicine et en tant que normes dans les tests de liaison des récepteurs de la capsicine et dans la conductance cationique induite par les récepteurs de la capsicine. L'invention concerne enfin l'utilisation des composés analysés dans les études de localisation des récepteurs.

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