IP Library › Granted Patent US 9,066,932
Granted Patent B2
US 9,066,932 · App. 14/134,113 · Granted Jun 30, 2015

Hepatitis B antiviral agents

Inventors: George D. Hartman (Doylestown, PA); Osvaldo A. Flores (Doylestown, MA)
Assignee: Novira Therapeutics, Inc.
A61K31/397C07D213/74C07D213/82C07D401/12C07D205/04C07D265/30C07D207/08C07D265/32C07D207/09C07D207/12C07D207/14C07D207/16C07D211/22C07D211/32C07D211/42C07D211/46C07D211/48C07D211/50C07D211/52C07D211/58C07D211/62C07D295/26A61K31/40A61K31/445A61K45/06C07C311/46C07D207/48C07D211/96A61K38/21A61K31/407A61K31/496A61K31/513A61K31/52A61K31/536A61K31/551A61K31/675A61K31/7072A61K31/4015A61K31/4453A61K31/451A61K31/522
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Quick Facts
Patent No.
US 9,066,932
App. No.
14/134,113
Granted
Jun 30, 2015
Kind
B2
Abstract

The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.

Claims (54)

1. A method of treating an HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of a compound of Formula IVc:

or a pharmaceutically acceptable salt thereof;

wherein X is halo;

G 1 is halo;

G 2 is C 1 -C 4 alkyl, or halo; and

G 4 is H, halo, C 1 -C 4 alkyl, or OH.

2. The method of claim 1 , further comprising administering to the individual at least one additional therapeutic agent selected from the group consisting of a HBV polymerase inhibitor, interferon, viral entry inhibitor, viral maturation inhibitor, literature-described capsid assembly modulator, reverse transcriptase inhibitor, a TLR-agonist, and a combination thereof.

3. The method of claim 2 , wherein the reverse transcriptase inhibitor is at least one of Zidovudine, Didano sine, Zalcitabine, 2′,3′-dideoxyadenosine, Stavudine, Lamivudine, Abacavir, Emtricitabine, Entecavir, Apricitabine, Atevirapine, ribavirin, acyclovir, famciclovir, valacyclovir, ganciclovir, valganciclovir, Tenofovir, Adefovir, PMPA, cidofovir, Efavirenz, Nevirapine, Delavirdine, or Etravirine.

4. The method of claim 2 , wherein the TLR-agonist is selected from the group consisting of SM360320 (9-benzyl-8-hydroxy-2-(2-methoxy-ethoxy)adenine) and AZD 8848 (methyl[3-({[3-(6-amino-2-butoxy-8-oxo-7,8-dihydro-9H-purin-9-yl)propyl][3-(4-morpholinyl)propyl]amino}methyl)phenyl]acetate).

5. The method of claim 2 , wherein the compound and the at least one additional therapeutic agent are co-formulated.

6. The method of claim 2 , wherein the compound and the at least one additional therapeutic agent are co-administered.

7. The method of claim 2 , wherein before administering the therapeutically effective amount of the compound of formula IVc, the individual is known to be refractory to a compound selected from the group consisting of a HBV polymerase inhibitor, interferon, viral entry inhibitor, viral maturation inhibitor, distinct capsid assembly modulator, and combination thereof.

8. The method of claim 2 , wherein the administering of the compound reduces viral load in the individual to a greater extent compared to the administering of a compound selected from the group consisting of a HBV polymerase inhibitor, interferon, viral entry inhibitor, viral maturation inhibitor, distinct capsid assembly modulator, and combination thereof.

9. The method of claim 2 , wherein the administering of the compound causes a lower incidence of viral mutation and/or viral resistance than the administering of a compound selected from the group consisting of a HBV polymerase inhibitor, interferon, viral entry inhibitor, viral maturation inhibitor, distinct capsid assembly modulator, and combination thereof.

10. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

11. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

12. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

13. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

14. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

15. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

16. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

17. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

18. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

19. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

20. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

21. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

22. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

23. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

24. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

25. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

26. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

27. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

28. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

29. The method of claim 1 , wherein the compound of Formula IVc is:

or a pharmaceutically acceptable salt thereof.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Apr 24, 2014
From: HARTMAN, GEORGE D.; FLORES, OSVALDO A.
To: NOVIRA THERAPEUTICS, INC.
Reel/Frame 032749/0299 →
Continuity (4)
Division 13723869 · Dec 21, 2012
Provisional Application 61578716 · Dec 21, 2011
Provisional Application 61709331 · Oct 3, 2012
Related Publication 20140178337A1 · Jun 26, 2014