Enantiomerically pure .beta.-D-dioxolane nucleosides with selective anti-hepatitis B virus activity
AssigneeEmory University
InventorRaymond F. Schinazi
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Abstract
A method and composition for the treatment of humans infected with HBV that includes the administration of an HBV treatment amount of a .beta.-dioxolanyl purine nucleoside of the formula: ##STR1## wherein R is OH, Cl, NH.sub.2, or H, or a pharmaceutically acceptable salt or derivative of the compound, optionally in a pharmaceutically acceptable carrier or diluent.
Claims40
A method for the treatment of HBV infection in a human or other host animal, comprising administering an HBV treatment amount of the nucleoside of the formula:
- ##STR3## wherein R is OH or NH.sub.2, and X is selected from the group consisting of hydrogen, acyl, monophosphate, diphosphate, and triphosphate, or its pharmaceutically acceptable salt, and wherein the compound is at least 95% free of the corresponding .beta.-L enantiomer in combination with a compound selected from the group consisting of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane;
- 2-hydroxymethy-5-(cytosin-1-yl)-1,3-oxathiolane;
- carbovir, or interferon.
A method for the treatment of HBV infection in a human or other host animal, comprising administering an HBV treatment amount of the nucleoside of the formula:
- ##STR4## wherein R is NH.sub.2, and X is selected from the group consisting of hydrogen, acyl, monophosphate, diphosphate, and triphosphate, or its pharmaceutically acceptable salt, and wherein the compound is at least 95% free of the corresponding .beta.-L enantiomer in combination with a compound selected from the group consisting of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane;
- 2-hydroxymethyl-5-(cytosin-1-yl)-1,3-oxathiolane;
- carbovir, or interferon.
A method for the treatment of HBV infection in a human or other host animal, comprising administering an HBV treatment amount of the nucleoside of the formula:
- ##STR5## wherein R is NH.sub.2, H or Cl, and X is selected from the group consisting of hydrogen, acyl, monophosphate, diphosphate, and triphosphate, or its pharmaceutically acceptable salt, and Wherein the compound is at least 95% free of the corresponding .beta.-L enantiomer in combination with a compound selected from the group consisting of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane;
- 2-hydroxymethyl-5-(cytosin-l-yl)-1,3-oxathiolane;
- carbovir, or interferon.
A method for the treatment of HBV infection in a human or other host animal, comprising administering an HBV treatment amount of the nucleoside of the formula:
- ##STR6## wherein R is OH or NH.sub.2 and X is selected from the group consisting of hydrogen, acyl, monophosphate, diphosphate, and triphosphate, or its pharmaceutically acceptable salt in combination with a compound selected from the group consisting of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane;
- 2-hydroxymethyl-5-(cytosin-1-yl)-I,3-oxathiolane;
- racemic carbovir, or interferon.
A method for the treatment of HBV infection in a human or other host animal, comprising administering an HBV treatment amount of the nucleoside of the formula:
- ##STR7## wherein R is NH.sub.2, and X is selected from the group consisting of hydrogen, acyl, monophosphate, diphosphate, and triphosphate, or its pharmaceutically acceptable salt in combination with a compound selected from the group consisting of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane;
- 2-hydroxymethyl-5-(cytosin-1-yl)-1,3-oxathiolane;
- carbovir, or interferon.
A method for the treatment of HBV infection in a human or other host animal, comprising administering an HBV treatment amount of the nucleoside of the formula:
- ##STR8## wherein R is NH.sub.2, H or Cl, and X is selected from the group consisting of hydrogen, acyl, monophosphate, diphosphate, and triphosphate, or its pharmaceutically acceptable salt in combination with a compound selected from the group consisting of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane;
- 2-hydroxymethyl-5-(cytosin-1-yl)-1,3-oxathiolane;
- carbovir, or interferon.
Dependencies are inferred from the claim text.