Merck + Co., Inc.

Arthur K Field

Richard L Tolman

Wallace T Ashton

Alfred A Tytell

Maurice R Hilleman

Richard J Harwood

Edgar M Scattergood

George P Lampson

John D Karkas

Laura F Canning

(S)-9-(2,3-dihydroxy-1-propoxymethyl)guanine has potent antiherpetic activity which is superior to the corresponding racemic mixture or the (R)-enantiomer and also is much more potent than 9-(2-hydroxyethoxymethyl)guanine. Acyl derivatives (prodrugs) of the (S)-enantiomer, which are more effective than the corresponding (R)-enantiomer analogs or related racemic mixtures provide formulation advantages and even higher plasma half lives in animals or man than the (S)-isomer.

Guanine derivatives

9-(1,3-Dihydroxy-2-propoxymethyl)guanine and 9-(2,3-dihydroxy-1-propoxymethyl)guanine have been found to have potent anti-viral activity against herpes viruses. These compounds, their acyl derivatives, their phosphate derivatives and their pharmaceutically acceptable salts, pharmaceutical formulations containing these compounds, the treatment of DNA viral or herpes viral infections with these compounds, method of preparing these compounds, and novel intermediates useful in their preparation are all disclosed. The compounds may be prepared by reaction of the appropriate acetoxymethyl ether with diacetylguanine, followed by deprotection. The acetoxymethyl ethers may be obtained by reaction of glycerol formal with acetic anhydride in the presence of a catalyst.

Anti-viral guanine compounds

Virus infections of eye, skin and mucous membrane tissue are effectively treated by controlled release topical application of interferon inducers.

Topical application of interferon inducers

The invention provides an improved process for the growth of lymphoblastoid cells in a medium supplemented with human albumin. The invention further provides for the production of interferon by viral infection of these lymphoblastoid cells in a medium also supplemented with human albumin. This invention eliminates the necessity for adding animal proteins.

Replacement of animal serum proteins by human albumin for growth and

Polynucleotides which are multistranded are active as inducers of interferon production in living animal cells. They may be:

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North Wales, PA, United States of America

Arthur K Field