Sri International

Elmer J Reist

Priscilla A Sturm

Pricilla A Sturm

Wallace W Bradford

Nurulain T Zaveri

Beatrice Ruhland-Fritsch

Cyclic and acyclic 2-aminopurine phosphonate nucleotide analogs useful to treat herpes viral infections are provided in enantiomerically pure form. Pharmaceutical compositions and methods for treating herpes viral infections are provided as well, as is a chiral synthesis for preparing the novel compounds in enantiomerically pure form.

Enantiomerically pure 2-aminopurine phosphonate nucleotide analogs as

Benzothiophene analogs useful to treat herpes viral infections, particularly cytomegalovirus, are provided. These antiviral agents have the structural formula (I) ##STR1## wherein R and R.sup.1 are as defined herein, and may be in free base or acid addition salt form. Pharmaceutical compositions are provided containing the antiviral agents, as are methods of treating herpes-infected individuals.

Benzothiophene analogs as antiviral agents

Method for treating herpes viral infections using benzothiophene analogs.

Acyclic purine phosphonate nucleotide analogs useful to treat herpes viral infections are provided in enantiomerically pure form. These antiviral agents have the structural formula (Ia) or (Ib) ##STR1## and may be in acid, salt or ester form. Such compounds may also be dehydrated to provide antiviral agents in cyclic form. Pharmaceutical compositions are provided containing the antiviral agents, as is a chiral synthesis which may be used to prepare the agents in enantiomerically pure form or as a racemic mixture.

Acyclic purine phosphonate nucleotide analogs as antiviral agents, and

Benzothiophen analogs as antiviral agents

Certain open chain purine nucleoside phosphonate derivatives have antiviral activity against the Herpes group of viruses, and also show effective antiviral activity against retroviruses, including human immunodeficiency virus (HIV). These compounds have the formula ##STR1## wherein B represents a substituted or unsubstituted purine base, especially adenine or guanine and their halogenated derivatives. R1 is selected from H, methyl, hydroxymethyl, halomethyl, azidomethyl, and cyano; R2 is selected from H, methyl, hydroxymethyl, halomethyl, azidomethyl, cyano, and OH; also when R2 is OH the carbon to which it is attached may be oxidized so that the H there shown and R2 together may be =0; and n is an integer of 0-5. The compounds of the invention further include the pharmaceutically acceptable mono and dibasic salts and the mono- and diesters of the phosphonate moiety and the acid addition salts of the murine-substituted purines. In addition, when R1 or R2 is --CH.sub.2 OH, or when R2 is OH, the acyl (1-6C) esters of these alcohols are included in the invention. Further, when n is 0, 1, or 2 and R1 is CH.sub.2 OH, the compounds of Formula 1 include the cyclic forms wherein formal dehydration between R1 and one of the --OH groups on the phosphonate results in compounds of the formula: ##STR2## and their corresponding salts and esters.

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Menlo Park, CA, United States of America

Elmer J Reist