Derivatives of phenoxyethylamine having a high affinity for...

C - Chemistry – Metallurgy – 07 – C

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C07C 233/78 (2006.01) A61K 31/16 (2006.01) A61K 31/275 (2006.01) A61K 31/44 (2006.01) A61K 31/47 (2006.01) C07C 217/20 (2006.01) C07C 233/25 (2006.01) C07C 233/36 (2006.01) C07C 233/37 (2006.01) C07C 233/62 (2006.01) C07C 235/40 (2006.01) C07C 235/50 (2006.01) C07C 235/60 (2006.01) C07C 237/42 (2006.01) C07C 255/54 (2006.01) C07C 259/10 (2006.01) C07C 271/28 (2006.01) C07C 275/24 (2006.01) C07C 275/34 (2006.01) C07C 323/20 (2006.01) C07D 209/48 (2006.01) C07D 213/81 (2006.01) C07D 217/26 (2006.01)

Patent

CA 2217479

Phenoxyethylamine derivatives of general formula (I) having high affinity for the 5-HT1A receptor, methods for preparing same, pharmaceutical compositions containing said derivatives, and their use, in particular as gastric acid secretion inhibitors or as antiemetics, are disclosed. In general formula(I), Ar is phenyl substituted by one or more substituents; and R is a C1-1- hydrocarbon radical selected from straight or branched alkyl, alkenyl or alkynyl radicals, saturated or unsaturated mono- or polycyclic cycloalkyl, cycloalkylalkyl or alkylcycloalkyl radicals; a pyridyl or isoquinolyl radical, phenyl optionally substituted by one or more substituent, and salts thereof.

La présente invention concerne des dérivés de phénoxyéthylamine de formule générale (I) possédant une haute affinité pour le récepteur 5-HT1A, des procédés pour leur préparation, des compositions pharmaceutiques les contenant et leur utilisation notamment en tant qu'inhibiteurs de sécrétion d'acide gastrique ou en tant qu'anti-émétiques. Dans ladite formule Ar représente un phényle substitué par un ou plusieurs substituants; R représente un radical hydrocarboné contenant de 1 à 10 atomes de carbone choisi parmi les radicaux alkyle, alkényle, alkynyle linéaires ou ramifiés, les radicaux cycloalkyle, cycloalkylalkyle ou alkylcycloalkyle, monocycliques ou polycycliques, saturés ou insaturés; le radical pyridyl ou isoquinolyl, un phényle, éventuellement substitué par un ou plusieurs substituants; ainsi que les sels de ces produits.

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