(+)-norcisapride useful for 5-ht3 and 5-ht4 mediated disorders

A - Human Necessities – 61 – K

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A61K 31/445 (2006.01)

Patent

CA 2292480

The present invention concerns (+)-norcisapride of formula (I) and compounds (V), and its pharmaceutically acceptable acid additions salts, a process for preparing said compound, and its use for the manufacture of a medicament for treating gastro-intestinal disorders while avoiding central nervous system effects. Also provided are method of treating gastro-intestinal disorders. Compounds of formula (V) wherein the piperidine ring has the absolute configuration (3S, 4R) and PG is methyloxycarbonyl, ethyloxycarbonyl, tert- butyloxycarbonyl or phenylmethyl.

L'invention concerne le (+)-norcisapride de formule (I) et composés (V) et ses sels d'addition acides pharmaceutiquement acceptables, un procédé pour préparer ce composés ainsi que l'utilisation de ce composé pour la préparation d'un médicament destiné à traiter les troubles gastro-intestinaux tout en évitant les effets secondaires sur le système nerveux central. L'invention concerne en outre un traitement des troubles gastro-intestinaux. Dans les composés de formule (V) l'anneau pipéridine possède la configuration absolue (3S, 4R) et PG est méthyloxycarbonyle, éthyloxycarbonyle, tert-butyloxycarbonyle ou phénylméthyle.

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