Novel benzamide derivatives and process for the preparation...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 211/62 (2006.01) A61K 31/165 (2006.01) A61K 31/445 (2006.01) A61P 1/00 (2006.01) A61P 1/06 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 417/12 (2006.01)

Patent

CA 2679260

The present invention provides a novel benzamide derivative represented by formula 1 and an isomer, a pharmaceutically acceptable salt or hydrate thereof, and a composition for activating a 5-HT4 receptor comprising the same, as an active ingredient. Benzamide derivatives of the present invention has superior affinity for 5-HT4 receptors, capability to reduce the gastric evacuation time, capability to alleviate ventricular tachycardia, ventricular fibrillation, torsades de pointes and QT prolongation, and low toxicity. Therefore, benzamide derivatives of the present invention are therapeutically effective for digestive system diseases.

La présente invention concerne un nouveau dérivé de benzamide représenté par la formule 1 et un isomère, un sel pharmaceutiquement acceptable ou un hydrate de celui-ci ainsi qu'une composition pour activer un récepteur de 5-HT4 le comprenant en tant qu'ingrédient actif. Les nouveaux dérivés de benzamide de la présente invention ont une affinité supérieure vis-à-vis des récepteurs de 5-HT4 et une capacité de réduire le temps d'évacuation gastrique, une capacité d'atténuer la tachycardie ventriculaire, la fibrillation ventriculaire, les torsades de pointes et la prolongation de QT; ils ont en outre une toxicité réduite. De cette manière, les dérivés de benzamide de la présente invention sont thérapeutiquement efficaces pour les maladies du système digestif.

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