Process for the preparation of form a of tegaserod

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 209/14 (2006.01) A61K 31/404 (2006.01) A61P 1/00 (2006.01)

Patent

CA 2687209

The present invention relates to a process for preparing polymorphic form A of 2-[(5-5 methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide maleate (tegaserod maleate). The invention further relates to tegaserod maleate form A substantially free of other polymorphic forms and chemicalimpurities, to compositions comprising tegaserod maleate form A and to the use of said compositions in the treatment of gastrointestinal disorders such as irritable bowel syndrome and heartburn.

L'invention concerne un procédé de préparation de la forme polymorphique A du 2-[(5-5 methoxy-1H-indol-3-yl)méthylène]-N-pentylhydrazinecarboximidamide maléate (tégasérode maléate). L'invention se rapporte également à une forme A de tégasérode maléate sensiblement dépourvue d'autres formes polymorphes et d'impuretés chimiques, à des compositions comprenant la forme A du tégasérode maléate et à l'utilisation desdites compositions dans le traitement de troubles gastrointestinaux tels que le le syndrome du côlon irritable et le pyrosis.

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