(s)-4-amino-5-chloro-2-methoxy-n-¬1-¬1-(2-tetrahydrofurylcar...

Details (s)-4-amino-5-chloro-2-methoxy-n-¬1-¬1-(2-tetrahydrofurylcar... (s)-4-amino-5-chloro-2-methoxy-n-¬1-¬1-(2-tetrahydrofurylcar...

C - Chemistry, Metallurgy

07

D

C07D 405/14 (2006.01) A61K 31/4545 (2006.01) A61P 1/00 (2006.01) A61P 1/04 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2483368

The compound (S)-4-Amino-5-chloro-2-methoxy-N-~1-~1-(2-tetrahydrofuryl- carbonyl)-4-piperidinylmethyl~-4-piperidinyl~benzamide of the following formula (I): ,or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, is useful as a gastrointestinal motility enhancer or a gastrointestinal prokinetic agent, which shows a potent affinity for 5-HT4 receptor, and shows few effects on the heart, and further shows few side effects on the central nervous system based on the dopamine D2 receptor. A process for preparing the compound, a pharmaceutical composition containing it and an intermediate therefor are also described.

Le composé (S)-4-amino-5-chloro-2-méthoxy-N-Ý1-Ý1-(2-tétrahydrofuryl-carbonyl)-4-pipéridinylméthyl¨-4-pipéridinyl¨benzamide de formule (I), ou un sel d'addition d'acide de celui, acceptable au plan pharmaceutique, ou un hydrate de celui-ci, est utile en tant qu'activateur de la motilité gastro-intestinale ou en tant qu'agent pro-cinétique, qui présente une affinité vis-à-vis du récepteur 5-HT¿4?, et agit sur le coeur. Il possède également peu d'effets secondaires sur le système nerveux central pour ce qui concerne le récepteur de la dopamine D¿2?. Un procédé de préparation dudit composé, une composition pharmaceutique le contenant et un intermédiaire pour la préparation dudit composé sont également décrits.

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