| US 7,585,851 B2 | ||
| 3′-prodrugs of 2′-deoxy-β-L-nucleosides | ||
| Martin L. Bryant, Carlisle, Mass. (US); Gilles Gosselin, Montpellier (France); and Jean-Louis Imbach, Montpellier (France) | ||
| Assigned to Idenix Pharmaceuticals, Inc., Cambridge, Mass. (US); Centre National de la Recherche Scientifique, Paris (France); and L'Universite Montpellier II, Cagliari (Italy) | ||
| Filed on Oct. 25, 2004, as Appl. No. 10/972,695. | ||
| Application 10/972695 is a division of application No. 09/883033, filed on Jun. 15, 2001, granted, now 6,875,751. | ||
| Claims priority of provisional application 60/212100, filed on Jun. 15, 2000. | ||
| Prior Publication US 2005/0113330 A1, May 26, 2005 | ||
| This patent is subject to a terminal disclaimer. | ||
| Int. Cl. A61K 31/70 (2006.01); C07H 19/073 (2006.01); C07H 19/10 (2006.01) | ||
| U.S. Cl. 514—49 [514/50; 514/51; 536/28.5; 536/28.51; 536/28.52; 536/28.53; 536/28.54; 536/28.55] | 112 Claims |
1. A 3′-substituted-β-L nucleoside of the formula (I)
 or its pharmaceutically acceptable salt thereof, wherein
R1 is hydrogen, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted
aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid acyl residue, mono, di, or triphosphate;
R2 is an amino acid acyl residue;
X is O; and
BASE is selected from the group consisting of 1-thyminyl, 1-cytosinyl, 5-fluoro-1-cytosinyl, 5-methyl-1-cytosinyl, 6-aza-1-pyrimidinyl,
2-mercapto-1-pyrimidinyl, 1-uracilyl, 5-halo-1-uracilyl, C5-alkyl-1-pyrimidinyl, 5-iodo-1-pyrimidinyl, 6-iodo-1-pyrimidinyl, 5-(2-bromovinyl)-1-pyrimidinyl, 6-(2-bromovinyl)-1-pyrimidinyl,
C5-benzyl-1-pyrimidines, C5-halo-1-pyrimidinyl, C5-vinyl-1-pyrimidinyl, C5-acetylenyl pyrimidinyl, C5-acyl 1-pyrimidinyl, C5-cyano-1-pyrimidinyl, C5-nitro-1-pyrimidinyl, C5-amino-1-pyrimidinyl, 5-aza-1-cytidinyl, 5-aza-1-uracilyl.
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