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AssigneeDainippon Pharmaceutical Co., Ltd.
InventorsShiro Kato, Hiroshi Yamazaki, Yoshimi Hirokawa, Yoko Kan, Naoyuki Yoshida, Kazuo Morikage, Yukiko Morikage
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(S)-4-Amino-5-chloro-2-methoxy-N-[-[1 -(2-tetrahydrofurylcarbonyl)-4-piperidinylmethyl]-4-piperidinyl]benzamide of the following formula (I): 1 or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, and a process for preparing the same, a pharmaceutical composition containing the same, and intermediate therefor. The compound of the present invention 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.
An (S)-4-amino-5-chloro-2-methoxy-N-[1-[1-(2-tetrahydrofurylcarbonyl)-4-piperidinylmethyl]-4-piperidinyl]benzamide of the following formula (I):
An (S)-4-amino-5-chloro-2-methoxy-N [1-[1-(2-tetrahydrofurylcarbonyl)-4-piperidinylmethyl]-4-piperidinyl]benzamide or a hydrate thereof.
An (S)-4-amino-5-chloro-2-methoxy-N-[1-[1-(2-tetrahydrofurylcarbonyl)-4-piperidinylmethyl]-4-piperidinyl]benzamide.fumarate or a hydrate thereof.
An (S)-4-amino-5-chloro-2-methoxy-N-[1-[1-(2-tetrahydrofurylcarbonyl)-4-piperidinylmethyl]-4-piperidinyl]benzamide maleate, or a hydrate thereof.
A pharmaceutical composition, which comprises as an active ingredient an (S)-4-amino-5-chloro-2-methoxy-N-[1-[1-(2-tetrahydrofurylcarbonyl)-4-piperidinylmethyl]-4-piperidinyl]benzamide, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof in admixture with a conventional pharmaceutically acceptable carrier or diluent.
A process for preparing an (S)-4-amino-5-chloro-2-methoxy-N-[1-[1-(2-tetrahydrofurylcarbonyl)-4-piperidinylmethyl]-4-piperidinyl]benzamide of the following formula (I):
An (S)-4-amino-1-[1-(2-tetrahydrofurylcarbonyl)-4-piperidinylmethyl]piperidine of the following formula (V):
Dependencies are inferred from the claim text.