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Generated: September 22, 2017

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Title: 1,2,4-Triazole nucleosides
Abstract:As antiviral agents and intermediates therefor, 3-substituted 1-(.beta.-D-glycosyl)-1,2,4-triazoles, O-acylated analogs thereof, and 5'- and 3',5'-cyclic phosphates of the triazole nucleosides, "glycosyl" being .[.a pentofuranosyl moiety, preferably one whose 2'-oxygen is trans to the triazole aglycon, e.g., xylofuranosyl,.]. ribofuranosyl, .[.2-0-methylribofuranosyl, etc.,.]. the triazole aglycon being 3-substituted with cyano, methylcarboxylate, carboxamidoxime, carboxamido-, thiocarboxamido, or carboxamidine. Preparation of these nucleosides is by silylation of the substituted triazole followed by glycosylation with the appropriate blocked glycosyl halide. Alternatively, acid-catalyzed fusion of the requisite 1,2,4-triazole with an O-acylated pentofuranose yields the nucleosides.
Inventor(s): Witkowski; Joseph T. (Laguna Niguel, CA), Robins; Roland K. (Santa Ana, CA)
Assignee: ICN Pharmaceuticals (Irvine, CA)
Application Number:05/782,294
Patent Claims: 1. A compound of structure ##STR8## wherein G is .[.a pentofuranosyl moiety whose 2'-oxygen is trans to the aglycon.]. .Iadd..beta.-D-ribofuranosyl .Iaddend.and R.sub.1 is selected from the group consisting of ##STR9## (d) physiologically acceptable acid addition salts of (c), ##STR10##

2. A compound selected from the group consisting of 5'-phosphates and 3',5'-cyclic phosphates of a compound according to claim 1.

3. A compound selected from the group consisting of (I) compounds of structure: ##STR11## wherein .[.one of R.sub.2 and.]. R.sub.3 .[.are.]. .Iadd.is .Iaddend.hydroxyl.[., the other being.]. .Iadd.and R.sub.2 is .Iaddend.hydrogen, and wherein R.sub.1 is selected from the group consisting of ##STR12## (d) physiologicaly acceptable acid addition salts of (c), ##STR13## (II) a 5'-phosphate of a compound (I); and (III) a 3',5'-cyclic phosphate of a compound (I). .[.

4. A compound according to claim 3 wherein R.sub.2 is hydrogen..].

5. A compound according to claim .[.4.]. .Iadd.3 .Iaddend.wherein otherwise free glycosyl hydroxyls are acyl-blocked.

6. A compound according to claim .[.4.]. .Iadd.3 .Iaddend.wherein R.sub.1 is (a), (b), (c) or (d).

7. A compound according to claim .[.4.]. .Iadd.3 .Iaddend.wherein R.sub.1 is (a), (b) or (d).

8. The ammonium or alkali metal salt of a 5'-phosphate (II) according to claim 7. .[.9. A compound according to claim 3 wherein R.sub.3 is hydrogen..]. .[.10. A compound according to claim 9 wherein otherwise free glycosyl hydroxyls are acyl-blocked..]. .[.11. A compound according to claim 9 and wherein R.sub.1 is (a), (b), (c) or (d)..]. .[.12. A compound according to claim 9 wherein R.sub.1 is (a), (b) or (d)..]. .[.13. The ammonium or alkali metal salt of a 5'-phosphate (II) according to claim

12..]. 14. A compound (I) according to claim .[.4.]. .Iadd.3. .Iaddend.

A compound (II) according to claim .[.4.]. .Iadd.3. .Iaddend. 16. A compound (III) according to claim .[.4.]. .Iadd.3. .Iaddend. .[.17. A compound (I) according to claim 9..]. .[.18. A compound (II) according to

claim 9..]. .[.19. A compound (III) according to claim 9..]. 20. The ammonium salt of the 5'-phosphate of

1-(.beta.-D-ribofuransoyl)-1,2,4-triazole-3-carboxamide.

21. 1(-.beta.-D-ribofuranosyl)-1,2,4-triazole-3-carboxamide.

22. 1-(.beta.-D-ribofuranosyl)-1,2,4-triazole-3-thiocarboxamide.

23. 1-(.beta.-D-ribofuranosyl)-1,2,4-triazole-3-carboxamidine. 24. 1-(2,3,5-tri-O-acetyl-.beta.-D-ribofuranosyl)-1,2,4-triazole-3-carboxa

mide. 25. 1-(.beta.-D-ribofuranosyl)-1,2,4-triazole-3-carboxamide hydrochloride. .[.26.

1-(.beta.-D-xylofuranosyl)-1,2,4-triazole-3-carboxamide..]. 27. 1-(.beta.-D-ribofuranosyl)-1,2,4-triazole-3-carboxamide 3',5'-cyclic

phosphate. 28. The ammonium salt of the compound of claim 27.
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