Prolinamide-tetrazole derivatives as nk3 receptor antagonists

C - Chemistry – Metallurgy – 07 – D

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C07D 403/12 (2006.01) A61K 31/496 (2006.01) A61P 25/00 (2006.01)

Patent

CA 2690292

The present invention relates to a compound of formula (I) : wherein R is cycloalkyl or is phenyl unsubstituted or substituted by one or two halogen atoms; R2 is hydrogen or halogen; R3 is hydrogen, CN, lower alkoxy, lower alkyl or halogen; n is 0, 1 or 2; or to a pharmaceutically suitable acid addition salt thereof. It has been found that the present compounds are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).

La présente invention concerne un composé représenté par la formule (I) ou l'un de ses acides d'addition pharmaceutiquement admis. Dans cette formule, R1 est cycloalkyle. R1 peut également être phényle non substitué ou phényle substitué par un ou deux atomes halogènes. R2 est hydrogène ou halogène. R3 est hydrogène, CN, alcoxy inférieur ou halogène. Enfin, n vaut 0, 1 ou 2. Il s'est avéré que les composés de l'invention sont des antagonistes à fort potentiel du récepteur NK-3 convenant au traitement de la dépression, de la douleur, de la psychose, de la maladie de Parkinson, de la schizophrénie, de l'anxiété et du syndrome d'hyperactivité avec déficit d'attention.

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