Antiviral activity and resolution of 2-hydroxymethyl-5- (5-fluorocytosin-1-yl)-1, 3-oxathiolane

Abstract

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 N 4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for 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.

1 - 25 . (canceled)  
     
     
         26 . A method for treating HIV infection in humans comprising administering an effective amount of (−)-β-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane, or its physiologically acceptable derivative or physiologically acceptable salt, in a gelatin capsule for oral delivery.  
     
     
         27 - 34 . (canceled)  
     
     
         35 . A method for treating HIV infection in humans comprising administering an effective amount of (−)-β-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane, or its physiologically acceptable derivative or physiologically acceptable salt, in a pharmaceutically acceptable carrier for oral delivery wherein the carrier comprises cellulose.  
     
     
         36 . The method of  claim 35  wherein the carrier comprises microcrystalline cellulose.  
     
     
         37 . A method for treating HIV infection in humans comprising administering an effective amount of (−)-β-L-2-hydroxymethyl-5-(5-fluorocytosine-1-yl)-1,3-oxathiolane, or its physiologically acceptable derivative or physiologically acceptable salt, in a pharmaceutically acceptable carrier for oral delivery wherein the carrier comprises magnesium stearate.