Antiviral activity and resolution of...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 411/04 (2006.01) A61K 31/506 (2006.01) C07H 19/06 (2006.01) C12P 41/00 (2006.01)

Patent

CA 2513440

A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3- oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5' or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process fot the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.

Sont divulguées dans l'invention une méthode et une préparation destinées au traitement des infections par le VIH et par le VHB chez l'humain, laquelle comprend l'administration d'une quantité efficace de 2-hydroxyméthyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, un dérivé pharmaceutiquement acceptable de celui-ci, y compris un dérivé alkylé ou acylé 5' ou N4, ou un sel pharmaceutiquement acceptable de celui-ci, dans un vecteur pharmaceutiquement acceptable. Un procédé permettant la résolution d'un mélange racémique d'énantiomères de nucléoside est également divulgué, lequel comprend une étape où le mélange racémique subit une catalyse par une enzyme qui réagit préférablement avec l'un des énantiomères.

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