.beta.-l-2'-deoxy-nucleosides for the treatment of hepatitis b

Details .beta.-l-2'-deoxy-nucleosides for the treatment of hepatitis b .beta.-l-2'-deoxy-nucleosides for the treatment of hepatitis b

A - Human Necessities

61

K

A61K 31/7072 (2006.01) A61K 31/70 (2006.01) A61K 31/7064 (2006.01) A61K 31/7068 (2006.01) A61K 31/708 (2006.01) A61P 31/12 (2006.01) A61P 31/20 (2006.01) C07H 19/06 (2006.01) C07H 19/10 (2006.01)

Patent

CA 2340156

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-.alpha.-L-erythro- pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2'-deoxy-.beta.-L-erythro-pentofuranonucleoside has formula (I) wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, 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-.beta.-L-erythro- pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2'-deoxy- .beta.-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.

L'invention concerne une méthode de traitement d'un sujet hôte atteint de l'hépatite B consistant à administrer une dose efficace d'un 2'-désoxy- beta -L-érythro-pentofuranonucléoside anti-VHB biologiquement actif ou un sel ou un promédicament pharmaceutiquement acceptable de celui-ci, dans laquelle le 2'-désoxy- beta -L-érythro-pentofuranonucléoside a la formule (I) dans laquelle R est choisi dans le groupe comprenant H, alkyle à chaîne droite, ramifiée ou cyclique, CO-alkyle, CO-aryle, CO-alcoxyalkyle, CO-aryloxyalkyle, CO-aryle substitué, alkylsulfonyle, arylsulfonyle, aralkylsulfonyle, un reste d'acide aminé, monophosphate, diphosphate ou triphosphate ou un dérivé de phosphate; et BASE représente une base purine ou pyrimidine pouvant être facultativement substituée. Le 2'-désoxy- beta -L-érythro-pentofuranonucléoside ou un sel ou un promédicament pharmaceutiquement acceptable de celui-ci peut être administré soit seul soit combiné à un autre 2'-désoxy- beta -L-érythro-pentofuranonucléoside ou en combinaison avec un autre agent anti-hépatite B.

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