Quinoline derivatives, their production and use

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 215/56 (2006.01) A61K 31/47 (2006.01) C07D 401/06 (2006.01)

Patent

CA 2229201

The present quinoline derivatives of formula (I), wherein R1 is a group of formula (a) in which R5 is an aralkyl group, R6 is an alkyl group, X is an alkylene group, or an alkyl group which may optionally be substituted by halogen, R2 is an acylaminoaryl group, R3 is a halogenoaralkyl group, R4 is a carboxyl group which may optionally be esterified or amidated, or a salt thereof, have gronadotropin-releasing hormone antagonistic activity and are useful as propylactics or therapeutic agent for the prevention or treatment of several hormone dependent diseases.

La présente invention concerne les dérivés de la quinoléine de formule (I), dans laquelle R?1¿ est un groupement ayant pour formule (a), dans laquelle R?5¿ est un groupe aralkyle, R?6¿ un groupe alkyle, X est un groupe alkylène ou un groupe alkyle qui peut être facultativement substitué par un halogène, R?2¿ est un groupe acylaminoaryle, R?3¿ est un groupe halogénoaralkyle, R?4¿ est un groupe carboxyle qui peut facultativement être estérifié ou amidé, ou un sel de ces substances. Ces composés ont un effet antagoniste de la gonadolibérine et ils sont utiles comme agent prophylactique ou thérapeutique, pour la prévention ou le traitement de plusieurs maladies sur lesquelles influent les hormones.

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