Xanthine phosphodiesterase v inhibitor polymorphs

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 473/04 (2006.01) A61K 31/522 (2006.01) A61P 9/00 (2006.01) A61P 15/00 (2006.01)

Patent

CA 2486174

Crystalline polymorphs of 1-ethyl-3,7-dihydro-8-~(1R, 2R)- (hydroxycyclopentyl)amino~-3-(2-hydroxyethyl)-7-~(3-bromo-4- methoxyphenyl)methyl~-1H-Purine-2,6-dione in Form 1 and Form 2, which exhibit x-ray powder diffraction profiles substantially the same as those shown in FIGS. 5 and 6, respectively, and which exhibit differential scanning calorimtery profiles substantially the same as those shown in FIGS. 2 and 4, respectively, and are represented by the formula (I). Pharmaceutical compositions comprising the polymorph Form 1 or 2 of Compound 13 and at least one excipient or carrier, and methods of using the polymorph Form 1 or 2 of Compound 13 to treat a variety of physiological disorders, such as erectile dysfunction.

L'invention concerne des polymorphes cristallins de 1-éthyl-3,7-dihydro-8-Ý(1R, 2R)-(hydroxycyclopentyl)amino¨-3-(2-hydroxyéthyl)-7-Ý(3-bromo-4-méthoxyphényl)méthyl¨-1<I>H</I>-purine-2,6-dione, sous la forme 1 et sous la forme 2, présentant des profils de diffraction à poudre de diffraction des rayons X, sensiblement identiques, respectivement, à ceux des figures 5 et 6, et présentant des profils de calorimétrie de scannage différentiel sensiblement identiques, respectivement, à ceux des figures 2 et 4, lesquels polymorphes étant représentés par la formule (I) (composé 13). L'invention concerne des compositions pharmaceutiques comprenant la forme polymorphique 1 ou 2 du composé 13, et au moins un excipient ou un support solide, l'invention concerne également des méthodes d'utilisation de la forme polymorphique 1 ou 2 du composé 13, pour traiter une variété de troubles physiologiques, notamment une dysérection.

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