Lipid derivatives of phosphonoacids for liposomal...

C - Chemistry – Metallurgy – 07 – F

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C07F 9/38 (2006.01) A61K 9/127 (2006.01) A61K 31/66 (2006.01) A61K 31/70 (2006.01) A61K 47/48 (2006.01) C07F 9/40 (2006.01) C07H 15/04 (2006.01) C07H 19/16 (2006.01)

Patent

CA 2149753

Lipid-containing prodrugs are provided for treating viral infections duo to herpes, influenza, hepatitis B. Epstein-Barr, and varicella-zoster viruses, as well as cytomegalovirus and derivatives of antiviral agents. The compounds comprise phosphonoacids having antiviral activity which are linked, either through the phosphate group or carboxyl group of the phosphonoacid, to one of a selected group of lipids. Phosphonoacetic acid and phosphonoformic acid are thus linked to phospholipids, glycerolipids, sphingolipids, glycolipids, or fatty acids. The compounds persist, after intracellular hydrolysis, as the antiviral phosphonoacids. The lipid prodrugs are effective in improving the efficacy of antiviral phosphonoacids by prolonging their antiviral activity following administration.

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