L-nucleosides for the treatment of hepatitis b-virus and...

C - Chemistry – Metallurgy – 07 – H

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C07H 19/06 (2006.01) A61K 31/7064 (2006.01) A61K 31/7076 (2006.01) C07H 19/16 (2006.01) C07H 21/00 (2006.01)

Patent

CA 2182273

A method for the treatment of a host, and in particular, a human, infected with HBV or EBV is provided that includes administering an HBV- or EBV- treatment amount of an L-nucleoside of formula(I) wherein R is a purine or pyrimidine base. In one preferred embodiment, the active compound is 2'-fluoro- 5-methyl-.beta.-L-arabinofuranosyluridine (also referred to as L-FMAU). This compound is a potent antiviral agent against HBV and EBV and exhibits low cytotoxicity. Other specific examples of active compounds include N1-(2'-deoxy- 2'-fluoro-.beta.-L-arabinofuranosyl)-5-ethyluracil, N1-(2'-deoxy-2'-fluoro- .beta.-L-arabinofuranosyl)-5-iodocytosine), and N1-(2'-deoxy-2'-fluoro-.beta.- L-arabinofuranosyl)-5-iodouracil.

Méthode de traitement d'un hôte (humain en particulier) infecté par le VHB ou le VEB et consistant à lui administrer une dose adéquate d'un nucléoside-L de formule (I) dans laquelle R est une base purique ou pyrimidique. Dans un mode préféré de réalisation, le principe actif est une 2'-fluoro-méthyl-.beta.-L-arabinofuranosyluridine (L-FMAU), composé antiviral puissant contre le VHB et le VEB, présentant une faible cytotoxicité. D'autres exemples spécifiques de composés actifs comprennent le N¿1?-(2'-désoxy-2'-fluoro-.beta.-L-arabinofuranosyl)-5-éthyluracyl; le N¿1?-(2'-désoxy-2'-fluoro-.beta.-L-arabinofuranosyl)-5-iodocytosine; et le N¿1?-(2'-déoxy-2'-fluoro-.beta.-L-arabinofuranosyl)-5-iodouracil.

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