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Last Updated: April 24, 2024

Claims for Patent: 6,641,843


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Summary for Patent: 6,641,843
Title: Pharmaceutical compositions
Abstract:The present invention relates to pharmaceutical compostions of (1S,4R)-cis-4-[2-amino-6-cyclopropylamino}-9H-purin-9-yl]-2-cyclopentene-1 -methanol (1592U89).
Inventor(s): Brooks; Nikki Thoennes (Glen Allen, VA)
Assignee: SmithKline Beecham Corporation (Philadelphia, PA)
Application Number:09/601,671
Patent Claims: 1. A pharmaceutical composition for oral administration comprising (1S,4R)-cis-4-[(2-amino-6-cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene- 1-methanol, or a pharmaceutically acceptable derivative thereof, together with citrate and at least one sweetener selected from sorbitol and saccharin, at a pH range of 2.0 to 4.5.

2. A pharmaceutical composition for oral administration comprising (1S,4R)-cis-4-[(2-amino-6-cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene- 1-methanol, or a pharmaceutically acceptable derivative thereof, together with citrate and at least one sweetener selected from sorbitol and saccharin, at a pH range of 6.6 to 7.5.

3. A pharmaceutical composition as claimed in claim 1 wherein the sweetener is saccharin and the composition further comprises fructose and acesulfame.

4. A pharmaceutical composition as claimed in claim 2 wherein the sweetener is saccharin and the composition further comprises fructose and acesulfame.

5. A pharmaceutical composition as claimed in claim 1 wherein the pharmaceutically acceptable derivative of (1S,4R)-cis-4-[(2-amino-6-cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene- 1-methanol is the hemisulfate salt.

6. A process for formulating (1S,4R)-cis-4-[(2-amino-6-cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene- 1-methanol for oral administration comprising the step of bringing (1S,4R)-cis-4-[(2-amino-6-cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene- 1-methanol, or a pharmaceutically acceptable derivative thereof, into association with citrate and a sweetening agent which does not contain a carboxyl group.

7. A process as claimed in claim 6 wherein the (1S,4R)-cis-4-[(2-amino-6-cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene- 1-methanol is in the form of its hemisulfate salt.

8. A pharmaceutical composition for oral administration comprising (1S,4R)-cis-4-[2-amino-6-cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1 -methanol, or a pharmaceutically acceptable derivative thereof, citrate, and a sweetening agent compatible with said (1S,4R)-cis-4-[2-amino-6-cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1 -methanol, or pharmaceutically acceptable derivative thereof.

9. A pharmaceutical composition as claimed in claim 8 at a pH range of 2.0 to 4.5.

10. A pharmaceutical composition according to claim 9 wherein the pH range is 3.8.

11. A pharmaceutical composition according to claim 10 wherein the pH is 4.1.

12. A pharmaceutical composition as claimed in claim 8 wherein the sweetening agent is selected from the group consisting of sorbitol, saccharin, acesulfame, fructose, sucralose, and aspartame.

13. A pharmaceutical composition according to claim 8 wherein the citrate ion concentration is in the range of 0.01 M to 0.1 M.

14. A pharmaceutical composition according to claim 1 in the form of a solution.

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