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Claims for Patent: 5,089,500

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Claims for Patent: 5,089,500

Title: Therapeutic nucleosides
Abstract:The present invention relates to 6-substituted purine carbocyclic nucleosides and their use in medical therapy particularly in the treatment of HIV and HBV infections. Also provided are pharmceutical formulations and processes for the preparation of compounds according to the invention.
Inventor(s): Daluge; Susan M. (Chapel Hill, NC)
Assignee: Burroughs Wellcome Co. (Research Triangle Park, NC)
Application Number:07/697,260
Patent Claims: 1. A method of treatment of a viral infection in a mammal which comprises administering to said mammal an effective antiviral amount of a compound of formula I: ##STR4## wherein R.sup.3 represents hydrogen or C.sub.1-6 alkyl; R.sup.6 represents C.sub.3-8 cycloalkyl, and R.sup.7 represents a hydrogen atom or a branched or straight chain C.sub.l-6 alkyl; or a pharmaceutically acceptable ester or a pharmaceutically acceptable salt thereof.

2. The method according to claim 1 for the treatment of an HIV infections.

3. A method according to claim 1 for the treatment of a hepatitis B infection.

4. A method according to claim 2 wherein the antiviral compound is (-)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-me thanol or racemic or partially resolved mixtures with the (+)-cis enantiomer thereof.

5. A method according to claim 3 wherein the antiviral compound is (-)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-me thanol or racemic or partially resolved mixtures with the (+)-cis enantiomer thereof.

6. A method according to claim 1 comprising administering to said mammal 15 to 60 mg/kg of body weight per day of a compound of formula I or a pharmaceutically acceptable salt or a pharmaceutically acceptable ester thereof.

7. A method according to claim 6 in which the infection is an HIV infection and the mammal is a human.

8. A method according to claim 6 in which the infection is a hepatitis B infection and the mammal is a human.

9. A method of treating an HIV infection in a mammal which comprises administering to said mammal an effective anti-HIV amount of (-)-cis-4-{2-amino-6-(cyclopropylamino)-9H-purin-9-yl}-2-cyclopentene-1-me thanol or racemic or partially resolved mixtures thereof with the (+)-cis-enantiomer or a pharmaceutically acceptable ester or a pharmaceutically acceptable salt thereof.

10. A method of treating an HIV infection in a mammal which comprises administering to said mammal an effective anti-HIV amount of (-)-cis-4-{2-amino-6-(cyclopropylmethylamino)-9H-purin-9-yl{-2-cyclopenten e-1-methanol or racemic or partially resolved mixtures thereof with the (+)-cis-enantiomer or a pharmaceutically acceptable ester or a pharmaceutically acceptable salt thereof.

11. A method according to claim 9 or 10, in which the pharmaceutically acceptable ester is a mono-, di- or triphosphate.

12. A method according to claim 9 or 10, in which the pharmaceutically acceptable salt is hydrochloride.

13. A method according to claim 9 or 10, in which the mammal is a human.

14. A method of treating an HIV infection in a mammal which comprise administering to said mammal an effective anti-HIV amount of (-)-cis-4-{2-amino-6-(cyclopropylamino)-9H-purin-9-yl}-2-cyclopentene-1-me thanol or racemic or partially resolved mixtures thereof with the (+)-cis-enantiomer or a pharmaceutically acceptable ester or a pharmaceutically acceptable salt thereof.

15. A method of treating an HIV infection in a mammal which comprises administering to said mammal an effective anti-HIV amount of (-)-cis-b 4-{2-amino-6-(cyclopropylmethylamino)-9H-purin-9-yl}-2-cyclopentene-1-meth anol or racemic or partially resolved mixtures thereof with the (+)-cis-enantiomer or a pharmaceutically acceptable ester or a pharmaceutically acceptable salt thereof.

16. A method according to claim 14 or 15, in which the pharmaceutically acceptable ester is a mono- , di- or tri-phosphate.

17. A method according to claim 14 or 15, in which the mammal is a human.
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