Polymorphic and other crystalline forms of cis-ftc

Details Polymorphic and other crystalline forms of cis-ftc Polymorphic and other crystalline forms of cis-ftc

C - Chemistry, Metallurgy

07

D

C07D 411/04 (2006.01) A61K 31/513 (2006.01) A61P 31/18 (2006.01)

Patent

CA 2439831

Solid phases of (-)-cis-FTC, which are designated herein as amorphous (-)-FTC and Forms II and III (-)-cis-FTC) are provided that can be distinguished from Form I (-)-cis-FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. A hydrated crystalline form of (.plusmn.)-cis-FTC (i.e. racemic cis-FTC), and a dehydrated form of the hydrate, are also provided, and can similarly be distinguished from other forms of FTC by X-ray powder diffraction patterns, thermal properties, and methods of manufacture. These FTC forms can be used in the manufacture of other forms of FTC, or in pharmaceutical compositions. Particularly preferred uses of these forms are in the treatment of HIV or hepatitis B.

L'invention concerne des phases solides de FTC-(-)-cis, désignées comme FTC-(-) amorphes, et des formes II et III de FTC-(-)-cis) qui se distinguent de la forme I FTC-(-)-cis par leurs diagrammes de diffraction des rayons X sur poudre, propriétés thermiques et procédés de production. L'invention concerne également une forme cristalline hydratée de FTC-(.plusmn.)-cis (notamment racémique FTC-cis) et une forme déshydratée de l'hydrate qui, par analogie, se distinguent des autres formes de FTC par leurs diagrammes de diffraction des rayons X sur poudre, propriétés thermiques et procédés de production. Ces formes FTC peuvent être utilisées dans la production d'autres formes de FTC ou de compositions pharmaceutiques. Les domaines d'application de ces formes sont, de préférence, le traitement du virus HIV ou de l'hépatite B.

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