Beta-L-2'-Deoxy-Nucleosides for the Treatment of Hepatitis B

Abstract

This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′deoxy-β-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-axyl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2′-deoxy-β-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2′-deoxy-β-L-erythro pentofuranonucleoside or in combination with another anti-hepatitis B agent.

1 - 12 . (canceled)  
     
     
         13 . A method for the treatment of a hepatitis B virus infection in a human comprising administering an effective amount of β-L-thymidine of the formula:  
       
         
           
           
               
               
           
         
       
       or a pharmaceutically acceptable salt thereof.  
     
     
         14 . The method of  claim 13 , wherein an effective amount of β-L-thymidine of the formula:  
       
         
           
           
               
               
           
         
       
       is administered.  
     
     
         15 . The method of  claim 13 , wherein an effective amount of a pharmaceutically acceptable salt of β-L-thymidine of the formula:  
       
         
           
           
               
               
           
         
       
       is administered.  
     
     
         16 . The method of  claim 13 , wherein β-L-thymidine or a pharmaceutically acceptable salt thereof is administered orally.  
     
     
         17 . The method of  claim 16 , wherein a unit dosage form comprising β-L-thymidine or a pharmaceutically acceptable salt thereof is administered orally.  
     
     
         18 . The method of  claim 17 , wherein the unit dosage form comprises about 50-1000 mg of β-L-thymidine or a pharmaceutically acceptable salt thereof.  
     
     
         19 . The method of  claim 17 , wherein the unit dosage form is a tablet.  
     
     
         20 . The method of  claim 19 , wherein the unit dosage form further comprises microcrystalline cellulose, magnesium streate, and/or colloidal silicon dioxide.  
     
     
         21 . The method of  claim 13 , wherein β-L-thymidine or a pharmaceutically acceptable salt thereof is administered at the dosage of about 1 to 20 mg/kg of body weight per day.  
     
     
         22 . The method of  claim 13 , wherein β-L-thymidine or a pharmaceutically acceptable salt thereof is at least 95% in its designated enantiomeric form.