➤ Get the DrugPatentWatch Daily Briefing

Get Daily Updates on Generic Entry, Litigation, Biosimilars, and more …

Serving leading biopharmaceutical companies globally:

Colorcon
Medtronic
Merck
Harvard Business School
McKinsey
McKesson

Last Updated: November 27, 2020

DrugPatentWatch Database Preview

Claims for Patent: 6,642,245

➤ Get the DrugPatentWatch Daily Briefing
» See Plans and Pricing

« Back to Dashboard

Summary for Patent: 6,642,245
Title: Antiviral activity and resolution of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane
Abstract:A method and composition for the treatment of HIV and HBV infections in humans is disclosed that includes administering an effective amount of 2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, a pharmaceutically acceptable derivative thereof, including a 5' or N.sup.4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier. A process for the resolution of a racemic mixture of nucleoside enantiomers is also disclosed that includes the step of exposing the racemic mixture to an enzyme that preferentially catalyzes a reaction in one of the enantiomers.
Inventor(s): Liotta; Dennis C. (Stone Mountain, GA), Schinazi; Raymond F. (Decatur, GA), Choi; Woo-Baeg (North Brunswick, NJ)
Assignee: Emory University (Atlanta, GA)
Application Number:08/475,339
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 6,642,245
Patent Claims: 1. A method for treating HIV infection in humans comprising administering an effective amount of (-)-.beta.-L-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, or its physiologically acceptable salt, optionally in a pharmaceutically acceptable carrier.

2. The method of claim 1, wherein the carrier is suitable for oral delivery.

3. The method of claim 1, wherein the carrier comprises a capsule.

4. The method of claim 1, wherein the carrier is in the form of a tablet.

5. The method of claim 1, wherein the administration is parenteral.

6. The method of claim 1, wherein .beta.-L-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is administered in a form that is at least 95% free of its corresponding .beta.-D-enantiomer.

7. The method of claim 1, wherein .beta.-L-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is administered in a form that is at least 95% free of its corresponding .beta.-D-enantiomer.

8. The method of claim 1, wherein .beta.-L-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is administered as an isolated enantiomer.

9. A method for treating HIV infection in humans comprising administering an effective amount of (+)-.beta.-D-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, or its physiologically acceptable salt, optionally in a pharmaceutically acceptable carrier.

10. The method of claim 9, wherein the carrier is suitable for oral delivery.

11. The method of claim 9, wherein the carrier comprises a capsule.

12. The method of claim 9, wherein the carrier is in the form of a tablet.

13. The method of claim 9, wherein the administration is parenteral.

14. The method of claim 9, wherein .beta.-D-2-hydroxymethyl-5-(5-fluorocytosin- 1-yl)-1,3-oxathiolane is administered in a form that is at least 95% free of its corresponding .beta.-L enantiomer.

15. The method of claim 9, wherein .beta.-D-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is administered in a form that is at least 95% free of its corresponding .beta.-L-enantiomer.

16. The method of claim 9, wherein .beta.-D-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is administered as an isolated enantiomer.

17. A method for treating HIV infection in humans comprising administering an effective amount of the monphosphate, diphosphate or triphosphate of .beta.-L-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, or its physiologically acceptable salt, optionally in a pharmaceutically acceptable carrier.

18. The method of claim 17, wherein the phosphate of .beta.-L-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is administered in a form that is at least 95% free of its corresponding .beta.-D-enantiomer.

19. The method of claim 17, wherein the phosphate of .beta.-L-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is administered as an isolated enantiomer.

20. A method for treating HIV infection in humans comprising administering an effective amount of the monophosphate, diphosphate, or triphosphate of .beta.-D-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane, or its physiologically acceptable salt, optionally in a pharmaceutically acceptable carrier.

21. The method of claim 20, wherein the phosphate of .beta.-D-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is administered in a form that is at least 95% free of its corresponding .beta.-L-enantiomer.

22. The method of claim 20, wherein the phosphate of .beta.-D-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is administered as an isolated enantiomer.

Make Better Decisions: Try a trial or see plans & pricing

Serving leading biopharmaceutical companies globally:

AstraZeneca
Merck
Boehringer Ingelheim
Moodys
Harvard Business School
Johnson and Johnson

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.