4-substituted quinoline derivatives as nk-3 and/or gaba(a)...

Details 4-substituted quinoline derivatives as nk-3 and/or gaba(a)... 4-substituted quinoline derivatives as nk-3 and/or gaba(a)...

C - Chemistry, Metallurgy

07

D

C07D 401/04 (2006.01) A61K 31/47 (2006.01) A61P 43/00 (2006.01) C07D 209/00 (2006.01) C07D 235/00 (2006.01) C07D 401/14 (2006.01) C07D 413/04 (2006.01) C07D 487/04 (2006.01) G01N 33/94 (2006.01)

Patent

CA 2368455

The invention relates to certain novel compounds of general Formula (I) where R1, R2, R3, R4, X, Y1, and Y2 are defined herein. These compounds bind with high affinity to NK-3 receptors and/or GABAA receptors. Also provided are pharmaceutical compositions comprising them, and methods of treating patients suffering from certain central nervous system and peripheral diseases or disorders with these pharmaceutical compositions. This invention also relates to the use of such compounds in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. The compounds of this invention are also useful as probes for the localization of NK-3 receptors and GABAA receptors.

L'invention concerne de nouveaux composés représentés par la formule générale (I), R¿1?, R¿2?, R¿3?, R¿4?, X, Y¿1? et Y¿2? étant définis ici. Ces composés se lient avec une grande affinité aux récepteurs de NK-3 et/ou aux récepteurs de GABA¿A?. L'invention concerne également des compositions pharmaceutiques les contenant, ainsi que des méthodes de traitement, avec ces compositions pharmaceutiques, de patients souffrant de certaines affections du système nerveux central et d'affections ou de troubles périphériques. L'invention concerne en outre l'utilisation de ces composés en combinaison avec un ou plusieurs autres agents agissant sur le système nerveux central pour potentialiser l'effet des autres agents agissant sur le système nerveux central. Les composés selon la présente invention s'utilisent également comme sondes de localisation des récepteurs de NK-3 et de GABA¿A?.

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