Organic compounds -- part of the class 532-570 series – Organic compounds – Four or more ring nitrogens in the bicyclo ring system
Patent
1990-01-22
1991-09-10
Rivers, Diana
Organic compounds -- part of the class 532-570 series
Organic compounds
Four or more ring nitrogens in the bicyclo ring system
558183, 544276, A61K 31675, C07F 96561
Patent
active
050475339
ABSTRACT:
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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Reist Elmer J.
Sturm Priscilla A.
Rivers Diana
SRI - International
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