Crystalline anhydrous and monohydrate benzoate salts of...

Details Crystalline anhydrous and monohydrate benzoate salts of... Crystalline anhydrous and monohydrate benzoate salts of...

C - Chemistry, Metallurgy

07

D

C07D 207/12 (2006.01) A61K 31/401 (2006.01)

Patent

CA 2477634

A process for preparing an anhydrous benzoate salt in crystallineform having formula (I) and the corresponding benzoate monohydrate in crystalline form. The benzoate salts and pharmaceutical compositions thereof are selective kappa- receptor agonists, and are useful as analgesics, anasthetics, anti- inflammatory or neuroprotective agents, or in the treatment of arthritis, stroke or functional bowel disease.

L'invention concerne un procédé pour préparer un sel de benzoate anhydre sous forme cristallisée, de formule (I), ainsi que le monohydrate de benzoate sous forme cristallisée correspondant. Les sels de benzoate et des compositions pharmaceutiques de ces sels constituent des agonistes sélectifs des récepteurs kappa et sont utiles en tant qu'agents analgésiques, anesthésiques, anti-inflammatoires ou neuroprotecteurs, ou pour traiter l'arthrite, les accidents vasculaires cérébraux ou des maladies intestinales fonctionnelles.

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