Nucleosides with anti-hepatitis b virus activity

C - Chemistry – Metallurgy – 07 – H

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C07H 19/06 (2006.01) A61K 31/70 (2006.01) A61P 31/12 (2006.01) C07H 19/10 (2006.01)

Patent

CA 2348470

Compounds and pharmaceutical compositions active against hepatitis B virus are provided, as is a method for the treatment of hepatitis B virus infection in humans and other host animals is provided comprising administering an effective amount of a .beta.-L-(2' or 3'- azido)-2',3'-dideoxy-5-fluorocytosine of formula (1) wherein R is H, acyl, monophosphate, diphosphate, or triphosphate, or a stabilized phosphate derivative (to form a stabilized nucleotide prodrug), and R' is H, acyl, or alkyl.

L'invention concerne des composés et des compositions pharmaceutiques dirigés contre le virus de l'hépatite B ainsi qu'un procédé de traitement de l'infection par le virus de l'hépatite B de l'humain et d'autres animaux hôtes, le procédé consistant à administrer une quantité efficace de beta -L-(2' ou 3'-azido)-2',3'-didéoxy-5-fluorocytosine correspondant à la formule (I): dans laquelle R est H, acyle, monophosphate, diphosphate ou triphosphate, ou un dérivé stabilisé de phosphate (pour former un promédicament stabilisé à base de nucléotides), et dans laquelle R' est H, acyle ou alkyle.

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