Methods and pharmaceutical compositions for the treatment of hepatitis b virus infection

Patent metadata

Field	Value
Publication number	US-10071108-B2
Application number	US-201815898944-A
Country	US
Kind code	B2
Filing date	Feb 19, 2018
Priority date	Sep 11, 2013
Publication date	Sep 11, 2018
Grant date	Sep 11, 2018

Abstract

The present invention relates to methods and pharmaceutical compositions for the treatment of hepatitis B virus infection. In particular, the present invention relates to farnesoid X receptor (FXR) agonists for use in a method for the treatment of hepatitis B virus infection in a subject in need thereof.

First claim

The invention claimed is:

1. A method for treating a chronic hepatitis B virus infection in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a farnesoid X receptor (FXR) agonist.

2. The method of claim 1 , wherein the subject is infected with a hepatitis B virus genotype selected from genotype A, B, C, and D.

3. The method of claim 1 , wherein the farnesoid X receptor (FXR) agonist is a selective FXR agonist.

4. The method of claim 1 , wherein the farnesoid X receptor (FXR) agonist is selected from the group consisting of the compounds identified by the CAS REGISTRY NUMBERS 1192171-69-9, 6ECDCA, GW4064, PXL0914, and PXL0743.

5. The method of claim 1 , wherein the farnesoid X receptor (FXR) agonist is selected from the group consisting of the compounds identified by the CAS REGISTRY NUMBERS 1192171-69-9 and 6ECDCA.

6. The method of claim 1 , wherein the subject has failed to respond to a previous treatment for HBV infection.

7. The method of claim 6 , wherein the previous treatment is selected from the group consisting of lamivudine (Epivir), adefovir (Hepsera), tenofovir (Viread), telbivudine (Tyzeka), entecavir (Baraclude), interferon alpha-2a, PEGylated interferon alpha-2a (Pegasys) and interferon alpha-2b (ViraferonPeg or Introna).

8. The method of claim 1 , wherein the FXR agonist is administered in combination with a treatment selected from the group consisting of lamivudine (Epivir), adefovir (Hepsera), tenofovir (Viread), telbivudine (Tyzeka), entecavir (Baraclude), interferon alpha-2a, PEGylated interferon alpha-2a (Pegasys) and interferon alpha-2b (ViraferonPeg or Introna).

9. A method for reducing synthesis and/or secretion of HBsAg and/or HBeAG or for reducing serum HBV DNA in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a farnesoid X receptor (FXR) agonist.

10. The method of claim 9 , wherein the subject is infected with a hepatitis B virus genotype selected from genotype A, B, C, and D.

11. The method of claim 9 , wherein the farnesoid X receptor (FXR) agonist is a selective FXR agonist.

12. The method of claim 9 , wherein the farnesoid X receptor (FXR) agonist is selected from the group consisting of the compounds identified by the CAS REGISTRY NUMBERS 1192171-69-9, 6ECDCA, GW4064, PXL0914, and PXL0743.

13. The method of claim 9 , wherein the farnesoid X receptor (FXR) agonist is selected from the group consisting of the compounds identified by the CAS REGISTRY NUMBERS 1192171-69-9 and 6ECDCA.

14. The method of claim 9 , wherein the subject has failed to respond to a previous treatment for HBV infection.

15. The method of claim 14 , wherein the previous treatment is selected from the group consisting of lamivudine (Epivir), adefovir (Hepsera), tenofovir (Viread), telbivudine (Tyzeka), entecavir (Baraclude), interferon alpha-2a, PEGylated interferon alpha-2a (Pegasys) and interferon alpha-2b (ViraferonPeg or Introna).

16. The method of claim 9 , wherein the FXR agonist is administered in combination with a treatment selected from the group consisting of lamivudine (Epivir), adefovir (Hepsera), tenofovir (Viread), telbivudine (Tyzeka), entecavir (Baraclude), interferon alpha-2a, PEGylated interferon alpha-2a (Pegasys) and interferon alpha-2b (ViraferonPeg or lntrona).

Assignees

• Inst Nat Sante Rech Med
• Univ Claude Bernard—Lyon 1
• Ens—Ecole Normale Superieure De Lyon
• Centre Nat Rech Scient
• Edelris
• Poxel
• Inst Nat Sante Rech Med
• Univ Claude Bernard—Lyon 1
• Ens—Ecole Normale Superieure De Lyon

Inventors

• Andre Patrice
• Lotteau Vincent
• Radreau Pauline
• Gilardone Marine
• Patin Amaury
• Roche Didier
• Cravo Daniel
• Hallakou-Bozec Sophie

Classifications

• A61P31/20

  for DNA viruses · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P1/16

  for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics · CPC title

• A61P1/00

  Drugs for disorders of the alimentary tract or the digestive system · CPC title

• A61K31/42

  Oxazoles · CPC title