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Generated: August 17, 2017

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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 pharmaceutical 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:07/455,201
Patent Claims: 1. 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.1-6 alkyl; or a pharmaceutically acceptable ester or a pharmaceutically acceptable salt thereof.

2. A compound, ester or salt of formula (I) according to claim 1 in which R.sup.3 is hydrogen, R.sup.6 is C.sub.3-6 cycloalkyl and R.sup.7 is methyl or hydrogen.

3. A compound according to claim 2 in which R.sup.6 is cyclopropyl.

4. A compound of formula (I) according to claim 1 selected from:

(-)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-met hanol and

(-)-cis-4-[2-amino-6-(cyclopropylmethylamino)-9H-purin-9-yl]-2-cyclopentene -1-methanol or

racemic or partially resolved mixtures with the (+)-cis enantiomers thereof.

5.

5. (.+-.)-cis-4-[2-amino-6-(cyclopropylamino-9H-purin-9-yl]-2-cyclopentene- 1-methanol.

6. (-)-cis- 4-[2-amino-6-(cyclopropylamino-9H-purin-9-yl]-2-cyclopentene-1-methanol.

7. A pharmaceutically acceptable salt of a compound according to claims 5 or 6.

8. A pharmaceutically acceptable ester of a compound according to claims 5 or 6.

9. A compound of formula (I) according to claim 1 wherein the pharmaceutically acceptable ester is a mono-, di-, or tri-phosphate ester or a pharmaceutically acceptable salt thereof.

10. A compound of formula (I) according to claim 1 wherein the pharmaceutically acceptable ester is the L-valinate or a salt thereof.

11. A compound, ester or salt of claim 3, in which the pharmaceutically acceptable ester is a mono-, di, or tri-phosphate ester or a pharmaceutically acceptable salt thereof.

12. A compound of the formula (I): R1 ? ? ##STR5## wherein R.sup.7 is hydrogen, R.sup.6 is cyclopropyl and R.sup.3 is hydrogen or a pharmaceutically acceptable salt thereof.

13. A compound of the formula (I): ##STR6## wherein R.sup.7 is methyl, R.sup.6 is cyclopropyl and R.sup.3 is hydrogen or a pharmaceutically acceptable salt thereof.

14. A tablet or capsule containing the compound of claim 12.

15. A tablet or capsule containing the compound of claim 13.

16. (.+-.)-cis-4-[2-amino-6-(cyclopropylmethylamino)-9H-puri n-9-yl]-2-cyclopentene-1-methanol.

17. (-)-cis-4-[2-amino-6-(cyclopro pylmethylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol.

18. A pharmaceutical formulation comprising a compound of formula (I) as defined in claim 1 or a pharmaceutically acceptable ester or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier therefor.

19. A formulation according to claim 18 wherein the compound of formula (I) is selected from:

(-)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-met hanol and

(-)-cis-4-[2-amino-6-(cyclopropylmethylamino)-9H-purin-9-yl]-2-cyclopentene -1-methanol or

racemic or partially resolved mixtures with the (+)-cis enantiomers thereof.

20. A tablet or capsule containing 50 to 700 mg of a compound according to claims 5 or 6 or a pharmaceutically acceptable salt or a pharmaceutically acceptable ester thereof.
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