IP Library Granted Patent US 8,765,710
Granted Patent B2
US 8,765,710 · App. 13/324,068 · Granted Jul 1, 2014

2′,4′-substituted nucleosides as antiviral agents

Inventors: Michael Joseph Sofia (Doylestown, PA); Jinfa Du (New Hope, PA)
Assignee: Gilead Pharmasset LLC
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Quick Facts
Patent No.
US 8,765,710
App. No.
13/324,068
Granted
Jul 1, 2014
Kind
B2
Abstract

Embodiments of the invention are to compounds, methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention are 2′,4′-substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.

Claims (13)

1. A method of treating a Hepatitis B Virus (HBV) infection comprising administering to a subject in need thereof an effective amount of a compound of the following formula:

or a pharmaceutically acceptable salt thereof, wherein:

(a) R 2 is CH 3 , CH 2 F, CHF 2 , CF 3 , CN, C 2-4 alkenyl, C 2-4 alkynyl, or C 1-4 alkyl optionally substituted with amino, hydroxyl, or 1 to 3 fluorine or chlorine atoms;

(f) Base is a naturally occurring or modified purine base represented by the following structure:

wherein for:

R 5 and R 6 are independently H, OH or NH 2 .

2. The method of claim 1 , wherein the compound is selected from the group consisting of:

3. The method of claim 1 , further comprising administering one or more antiviral agents, antibacterial agents, antiproliferative agents, or a combination thereof.

4. The method of claim 1 , wherein he compound is administered orally.

5. The method of claim 4 , wherein between about 0.1 g and about 10 g of the compound is administered daily in a monotherapy or a combination therapy.

6. The method of claim 5 , wherein between about 0.5 g and about 7.5 g of the compound is administered daily.

7. The method of claim 6 , wherein between about 1.5 g and about 6.0 g of the compound is administered daily.

8. The method of claim 4 , wherein the compound is administered in an initial loading dose fallowed by a decreased dose.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 28, 2022
From: GILEAD PHARMASSET LLC
To: GILEAD SCIENCES, INC.
Reel/Frame 060217/0738 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 3, 2014
From: SOFIA, MICHAEL J.; DU, JINFA
To: PHARMASSET, INC.
Reel/Frame 032124/0650 →
CHANGE OF NAME Recorded Apr 18, 2012
From: PHARMASSET, INC.
To: GILEAD PHARMASSET LLC
Reel/Frame 028069/0936 →
Continuity (3)
Continuation 12271388 · Nov 14, 2008
Provisional Application 60989296 · Nov 20, 2007
Related Publication 20120232029A1 · Sep 13, 2012