Amides as npy5 receptor antagonists

C - Chemistry – Metallurgy – 07 – C

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C07C 235/24 (2006.01) A61K 31/16 (2006.01) A61K 31/167 (2006.01) A61K 31/196 (2006.01) A61K 31/33 (2006.01) A61K 31/341 (2006.01) A61K 31/41 (2006.01) A61K 31/4164 (2006.01) A61K 31/4184 (2006.01) A61K 31/4196 (2006.01) A61K 31/422 (2006.01) A61K 31/423 (2006.01) A61K 31/4245 (2006.01) A61K 31/426 (2006.01) A61K 31/428 (2006.01) A61K 31/433 (2006.01) A61K 31/44 (2006.01) A61K 31/4412 (2006.01) A61K 31/445 (2006.01) A61K 31/47 (2006.01) A61K 31/495 (2006.01) A61K 31/505 (2006.01) A61K 31/517 (2006.01) A61K 3

Patent

CA 2251580

.alpha.-alkoxy and .alpha.-thioalkoxyamide compounds of formula (I) and methods of administering the compositions to mammals to treat disorders such as obesity that are mediated by NPY and especially those mediated by NPY via the Y5 receptor, or pharmaceutically acceptable salts thereof wherein R1-R5 are each individually selected from the group of substituents including hydrogen, halogen, hydroxyl, thiol, lower alkyl, substituted lower alkyl, alkenyl, alkynyl, alkylalkenyl, alkyl alkynyl, alkoxy, alkylthio, acyl, aryloxy, amino, amido, carboxyl, aryl, substituted aryl, heterocycle, heteroaryl, substituted heterocycle, heteroalkyl, cycloalkyl, substituted cycloalkyl, alkylcycloalkyl, alkylcycloheteroalkyl, phenyl, substituted phenyl, benzothiophene, furan, fluoride, nitro, cyano, naphthyl, substituted naphthyl, fluorene, substituted fluorene and dibenzofuran, and wherein X is oxygen or sulfur.

L'invention concerne des compositions à base d'.alpha.-alcoxy et de .alpha.-thioalcoxyamide de formule (I) ou des sels pharmaceutiquement acceptables de celles-ci, ainsi que des procédés d'administration desdites compositions à des mammifères pour le traitement de troubles tels que l'obésité, troubles liés au neuropeptide NPY par le truchement du récepteur de Y5. Dans la formule (I), R¿1?-R¿5? sont choisis séparément dans le groupe de substituants comprenant hydrogène, halogène, hydroxyle, thiol, alkyle inférieur, alkyle inférieur substitué, alcényle, alcynyle, alkylalcényle, alkylalcynyle, alcoxy, alkylthio, acyle, aryloxy, amino, amido, carboxyle, aryle, aryle substitué, hétérocycle, hétéroaryle, hétérocycle substitué, hétéroalkyle, cycloalkyle, cycloalkyle substitué, alkylcycloalkyle, alkylcyclohétéroalkyle, phényle, phényle substitué, benzothiophène, furan, fluorure, nitro, cyano, naphtyle, naphtyle substitué, fluorène, fluorène substitué et dibenzofuran, X représentant oxygène ou soufre.

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