Crystalline form of abacavir that is essentially free of...

Details Crystalline form of abacavir that is essentially free of... Crystalline form of abacavir that is essentially free of...

C - Chemistry, Metallurgy

07

D

C07D 473/16 (2006.01) A61K 31/52 (2006.01) A61P 31/00 (2006.01)

Patent

CA 2711059

Crystalline form of abacavir that is essentially free of solvent of formula (I), in particular crystalline Form I, and its preparation process which comprises the follow-ing steps: a) crystallizing abacavir from a solution of said compound in a(C1-C4)- alcohol, dichloromethane, acetonitrile/water, or mixtures thereof; b) isolating the crystalline form of abacavir that appears in the prior step; and c) removing the solvent from the crystalline form of abacavir thus obtained. Crystalline Form I can also be obtained by dispersion of abacavir in acetonitrile. The crystalline form of abacavir that is essentially free of solvent is useful for the preparation of pharmaceutical compositions for use in the treatment and/or prophylaxis of HIV infections.

L'invention porte sur une forme cristalline d'abacavir qui est essentiellement exempte de solvant, représentée par la formule (I), en particulier la forme cristalline I, et sur son procédé de préparation qui consiste à : a) cristalliser l'abacavir à partir d'une solution dudit composé dans un alcool en C1-C4, du dichlorométhane, un mélange acétonitrile/eau ou des mélanges de ceux-ci ; b) isoler la forme cristalline d'abacavir qui apparaît dans l'étape antérieure ; et c) éliminer le solvant de la forme cristalline d'abacavir ainsi obtenue. La forme cristalline I peut également être obtenue par dispersion d'abacavir dans de l'acétonitrile. La forme cristalline d'abacavir qui est essentiellement exempte de solvant est utile pour la préparation de compositions pharmaceutiques destinées à être utilisées dans le traitement et/ou la prophylaxie d'infections par le VIH.

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