Novel choline cocrystal of epalrestat

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 277/36 (2006.01) A61K 31/19 (2006.01) A61P 3/10 (2006.01) C07D 277/32 (2006.01)

Patent

CA 2738231

The invention relates to a novel choline cocrystal of 5-[(1Z.2E)-2-methyl-3- phenylpropenylidene]-4-oxo-2- thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel choline cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel choline cocrystal and the therapeutic use of the novel choline cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, treating and/or preventing homocystinuria reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients.

L'invention porte sur de nouveaux co-cristaux de choline et d'acide 5-[(1Z.2E)-2-méthyl-3-phénylpropénylidène]-4-oxo-2-thioxo-3-thiazolidineacétique. La préparation et la caractérisation des nouveaux co-cristaux de choline conformément à divers modes de réalisation de l'invention sont décrites. L'invention porte également sur des compositions pharmaceutiques contenant les nouveaux co-cristaux de choline et sur l'utilisation thérapeutique des nouveaux co-cristaux de choline pour traiter et/ou prévenir divers états, comprenant le traitement et/ou la prévention de complications diabétiques, le traitement et/ou la prévention d'une homocystinurie réduisant les taux d'homocystéine dans le sérum sanguin, inhibant l'aldose réductase, et fournissant une cardioprotection dans des patients non diabétiques.

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