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Claims for Patent: 4,808,614

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Claims for Patent: 4,808,614

Title: Difluoro antivirals and intermediate therefor
Abstract:A 2,2-difluoro-2-desoxycarbohydrate is used to prepare antiviral nucleosides.
Inventor(s): Hertel; Larry W. (Indianapolis, IN)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Application Number:07/058,219
Patent Claims: 1. A nucleoside of the formula ##STR11## wherein R is a base selected from the group consisting of ##STR12## wherein R.sup.1 is hydrogen, methyl, bromo, fluoro, chloro oriodo;

R.sup.2 is hydroxy;

R.sup.3 is hydrogen, bromo, chloro or iodo.

2. A nucleoside of claim 1 wherein the carbohydrate moiety is in the ribose form.

3. A nucleoside of claim 2 wherein the base is of the formula ##STR13##

4. A nucleoside of claim 1 wherein the base is of the formula ##STR14##

5. A nucleoside of claim 4 wherein R.sup.1 is methyl.

6. A nucleoside of claim 3 wherein R.sup.1 is methyl.

7. A nucleoside of claim 1 wherein the base is of the formula ##STR15##

8. A nucleoside of claim 2 wherein the base is of the formula ##STR16##

9. A nucleoside of claim 7 wherein R.sup.1 is iodo.

10. A nucleoside of claim 8 wherein R.sup.1 is iodo.

11. A nucleoside of claim 7 wherein R.sup.1 is hydrogen.

12. A nucleoside of claim 8 wherein R.sup.1 is hydrogen.

13. A method of treating Herpes viral infections in mammals comprising administering to a mammal in need of such treatment an anti-Herpes viral effective amount of a compound of claim 1.

14. A pharmaceutical composition useful for treating Herpes viral infections comprising an anti-Herpes viral effective amount of a compound of claim 1 and a pharmaceutically-acceptable carrier, diluent or excipient therefor.
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