Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
AssigneeEmory University
InventorsDennis C. Liotta, Raymond F. Schinazi, Woo-Baeg Choi
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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 N4 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.
Claims22
A method for treating HIV infection in humans comprising administering an effective amount of (−)-β-L-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, or its physiologically acceptable salt, optionally in a pharmaceutically acceptable carrier.
A method for treating HIV infection in humans comprising administering an effective amount of (+)-β-D-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, or its physiologically acceptable salt, optionally in a pharmaceutically acceptable carrier.
A method for treating HIV infection in humans comprising administering an effective amount of the monphosphate, diphosphate or triphosphate of β-L-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, or its physiologically acceptable salt, optionally in a pharmaceutically acceptable carrier.
A method for treating HIV infection in humans comprising administering an effective amount of the monophosphate, diphosphate, or triphosphate of β-D-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, or its physiologically acceptable salt, optionally in a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.