You’re using a public version of DrugPatentWatch with 5 free searches available | Register to unlock more free searches. CREATE FREE ACCOUNT

Last Updated: March 28, 2024

Details for Patent: 6,114,343


✉ Email this page to a colleague

« Back to Dashboard


Title: Antiviral activity and resolution of 2-hydroxymethyl-5-(5-flurocytosin-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)
Filing Date:Jun 07, 1995
Application Number:08/482,875
Claims:1. A pharmaceutical composition comprising an effective amount to treat HIV infection in humans of (+)-.beta.-D-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolan or its physiologically acceptable salt, at least 95% free of the corresponding (-)-.beta.-enantiomer in a pharmaceutically acceptable carrier.

2. A pharmaceutical composition comprising in an amount effective to treat HIV infection in humans, a (+)-.beta.-D-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane at least 95% free of the corresponding (-)-.beta.-enantiomer of the formula: ##STR8## wherein R.sub.1 and R.sub.2 are selected from the group consisting of acetyl, propionyl, butyryl, and pentanoyl or R.sub.1 can be a mono, di or triphosphate ester, and one of R.sub.1 or R.sub.2 can be hydrogen, or its pharmaceutically acceptable salt in a pharmaceutically acceptable carrier.

3. The pharmaceutical composition of claim 2, wherein R.sub.1 is mono, di or triphosphate ester.

4. The pharmaceutical composition of claim 2, wherein R.sub.1 is acetyl and R.sub.2 is hydrogen.

5. A pharmaceutical composition comprising an effective amount to treat HIV infection in humans of (+)-.beta.-D-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane or its physiologically acceptable salt, substantially in the absence of its corresponding .beta.-L-enantiomer in a pharmaceutically acceptable carrier .

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

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.