Nucleotide analogs

Abstract

Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.

1 - 26 . (canceled) 
   
   
       27 . A compound having the structure 
     
       
         
         
             
             
         
       
       wherein R 4  is H, methyl, ethyl, propyl, isopropyl, butyl, t-butyl, phenyl, benzyl, 1-pyridinyl, 3-pyridyl, 1-pyrimidinyl, N-ethylmorpholino, N 2 -propylmorpholino, methoxyethyl, 4-N-methylpiperidinyl, 3-N-methylpiperidinyl, 4-hydroxy-N-methylpiperidinyl, 3-hydroxy-N-methylpiperidinyl, 1-ethylpiperizinyl, phenol substituted with N(R 30 ) 2  wherein R 30  is independently H or C 1 -C 6  alkyl unsubstituted or independently substituted by OH or halogen, or C 6 -C 12  aryl unsubstituted or substituted independently by OH, N(R 7 ) 2  or halogen, wherein R 7  is H or C 1 -C 4  alkyl. 
     
   
   
       28 . The compound of  claim 27  wherein R 4  is H, propyl, isopropyl, t-butyl, phenyl, benzyl, 1-pyridinyl, 1-pyrimidinyl, N-ethylmorpholino, methoxyethyl, 4-hydroxy-N-methylpiperidinyl, 3-hydroxy-N-methylpiperidinyl or 1-ethylpiperazinyl.