Gilead Sciences, Inc.

Petr Alexander

Ernest J Prisbe

Norbert W Bischofberger

Murty N Arimilli

Michael J Hitchcock

In accordance with this invention novel compounds are provided that are selected from saturated and unsaturated pyrans and furans substituted with at least a phosphonate group and a heterocyclic base. These compounds are useful as antiinfectives, flame retardants, diagnostic oligonucleotides and immunogens.

Compounds and methods for making and using same

The internally cyclized congeners of hydroxy-substituted nucleotide analogues have been found to exhibit substantially lower toxicity in vivo than their uncyclized analogues, while retaining essentially the same antiviral activity. This was unexpected because the prior art suggested that the cyclic analogues offered no significant advantages in respect to toxicity. This finding permits the administration of much greater doses of the cyclic congeners than otherwise would have been possible and allows the clinician to omit toxicity ameliorating interventions. Novel compounds are provided for use in the method of this invention. Novel methods for the preparation of these compounds also are provided.

Method for dosing therapeutic compounds

Methods for making nucleoside analogs

Nucleotide analogues

Method for synthesis

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San Mateo, CA, United States of America

Petr Alexander