Substituted phenylpiperidine derivatives as melanocortin-4...

C - Chemistry – Metallurgy – 07 – D

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C07D 211/22 (2006.01) A61K 31/451 (2006.01) A61K 31/4523 (2006.01) A61P 3/00 (2006.01) C07D 211/26 (2006.01) C07D 401/10 (2006.01) C07D 401/12 (2006.01)

Patent

CA 2648335

The present invention relates to substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.

La présente invention concerne des dérivés de phénylpipéridine substitués en tant que modulateurs des récepteurs de la mélanocortine-4. En fonction de la structure et de la stéréochimie, les composés de l'invention sont soit des agonistes sélectifs, soit des antagonistes sélectifs du récepteur humain de la mélanocortine-4 (MC-4R). Les agonistes peuvent être utilisés pour le traitement de troubles et de maladies tels que l'obésité, le diabète et une dysfonction sexuelle, alors que les antagonistes sont utiles pour le traitement de troubles et de maladies tels que le cancer, l'émaciation, l'atrophie musculaire, l'anorexie, l'anxiété et la dépression. Généralement, toutes les maladies et tous les troubles associés à la régulation du MC-4R peuvent être traités avec les composés de l'invention.

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