Polymorphs of elafibranor

Patent metadata

Field	Value
Publication number	US-12522564-B2
Application number	US-202117798484-A
Country	US
Kind code	B2
Filing date	Feb 4, 2021
Priority date	Feb 10, 2020
Publication date	Jan 13, 2026
Grant date	Jan 13, 2026

Abstract

The present invention relates to novel crystalline forms of elafibranor.

First claim

The invention claimed is:

1 . A crystal form of elafibranor having a X-ray diffraction pattern comprising the following diffraction peaks (2θ in angular degrees ±0.2°): 17.7°, 23.3°, 27.3°, 34.3°, and 34.6°.

2 . The crystal form of elafibranor according to claim 1 , wherein the X-ray diffraction pattern further comprises a diffraction peak (2θ in angular degrees ±0.2°) at 28.9°.

3 . The crystal form of elafibranor according to claim 1 , wherein the X-ray diffraction pattern comprises at least one more peak (2θ in angular degrees ±0.2°) selected from the group consisting of: 8.9°, 10.1°, 10.7°, 11.3°, 32.0° and 35.5°.

4 . The crystal form of elafibranor according to: claim 1 , wherein the X-ray diffraction pattern comprises the following diffraction peaks (2θ in angular degrees ±0.2°): 8.9°, 10.1°, 10.7°, 11.3°, 17.7°, 23.3°, 27.3°, 28.9°, 32.0°, 34.3°, 34.6° and 35.5°.

5 . A crystal form of elafibranor having a X-ray diffraction pattern comprising the following diffraction peaks (2θ in angular degrees ±0.2°): 10.9°, 15.6°, 16.1°, 18.6°, 19.9° and 20.7°.

6 . The crystal form of elafibranor according to claim 5 , wherein the X-ray diffraction pattern further comprises at least one further diffraction peak (2θ in angular degrees ±0.2°) selected in the group consisting of 7.8°, 17.7°, 18.1°, 21.9°, 22.3° and 24.6°.

7 . The crystal form of elafibranor according to claim 6 , wherein the X-ray diffraction pattern further comprises at least one further diffraction peak (2θ in angular degrees ±0.2°) selected from the group consisting of 9.3°, 12.9°, 13.4°, 14.7°, 24.1°, 25.1°, 25.5°, 25.8°, 26.1°, 27.3°, 28.0°, 28.4°, 29.2°, 29.9°, 32.3°, 32.9° and 33.6°.

8 . The crystal form of elafibranor according to claim 5 , wherein the X-ray diffraction pattern comprises the following diffraction peaks (2θ in angular degrees ±0.2°): 7.8°, 9.3°, 10.9°, 12.9°, 13.4°, 14.7°, 15.6°, 16.1°, 17.7°, 18.1°, 18.6°, 19.9°, 20.7°, 21.9°, 22.3°, 24.1°, 24.6°, 25.1°, 25.5°, 25.8°, 26.1°, 27.3°, 28.0°, 28.4°, 29.2°, 29.9°, 32.3°, 32.9° and 33.6°.

9 . A crystal form of elafibranor having a X-ray diffraction pattern comprising the following diffraction peaks (2θ in angular degrees ±0.2°): 13.3°, 15.1°, 17.1° and 29.5°.

10 . The crystal form of elafibranor according to claim 9 , wherein the X-ray diffraction pattern further comprises at least one further diffraction peak (2θ in angular degrees ±0.2°) selected from the group consisting of 18.1°, 25.2°, 25.9° and 26.2°.

11 . The crystal form of elafibranor according to claim 10 , wherein the X-ray diffraction pattern further comprises at least one further diffraction peak (2θ in angular degrees ±0.2°) selected from the group consisting of 7.6°, 8.6°, 11.2°, 16.1°, 16.9°, 17.8° and 22.8°.

12 . The crystal form of elafibranor according to claim 9 , wherein the X-ray diffraction pattern comprises the following diffraction peaks (2θ in angular degrees ±0.2°): 7.6°, 8.6°, 11.2°, 13.3°, 15.1°, 17.1°, 16.1°, 16.9°, 17.8°, 18.1°, 22.8°, 25.2°, 25.9°, 26.2° and 29.5°.

13 . A pharmaceutical composition comprising the crystal form of elafibranor according to claim 1 , and at least one pharmaceutically acceptable excipient.

14 . The pharmaceutical composition according to claim 13 , wherein said composition is formulated in the form of a tablet, injectable suspension, gel, oil, pill, suppository, powder, gel cap, capsule, aerosol or a prolonged release galenic form or a slow release galenic form.

15 . A method of treating a liver disorder, comprising administering to a subject in need thereof an effective amount of the crystal form of elafibranor according to claim 1 , wherein the liver disorder is selected from the group consisting of non-alcoholic fatty liver disease (NAFLD), and non-alcoholic steatohepatitis (NASH), liver cirrhosis.

16 . A method of treating a cholestatic disease, comprising administering to a subject in need thereof an effective amount of the crystal form of elafibranor according to claim 1 , wherein the cholestatic disease is primary biliary cholangitis (PBC) or primary sclerosing cholangitis (PSC).

17 . A method of treating a liver disorder, comprising administering to a subject in need thereof an effective amount of the pharmaceutical composition according to claim 13 , wherein the liver disorder is selected from the group consisting of non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and liver cirrhosis.

18 . A method of treating a cholestatic disease, comprising administering to a subject in need thereof an effective amount of the pharmaceutical composition according to claim 13 , wherein the cholestatic disease is primary biliary cholangitis (PBC) or primary sclerosing cholangitis (PSC).

19 . A method of treating a liver disorder or a cholestatic disease, comprising administering to a subject in need thereof an effective amount of the crystal form of elafibranor according to claim 5 , wherein the liver disorder is selected from the group consisting of non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and liver cirrhosis, and wherein the cholestatic disease is primary biliary cholangitis (PBC) or primary sclerosing cholangitis (PSC).

20 . A method of treating a liver disorder or a cholestatic disease, comprising administering to a subject in need thereof an effective amount of the crystal form of elafibranor according to claim 9 , wherein the liver disorder is selected from the group consisting of non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and liver cirrhosis, and wherein the cholestatic disease is primary biliary cholangitis (PBC) or primary sclerosing cholangitis (PSC).

21 . A pharmaceutical composition comprising a crystal form of elafibranor according to claim 5 , and at least one pharmaceutically acceptable excipient.

22 . A pharmaceutical composition comprising the crystal form of elafibranor according to claim 9 , and at least one pharmaceutically acceptable excipient.

Assignees

• Genfit

Inventors

• Bertrand Karine
• Delhomel Jean-François
• Roudot Alice

Classifications

• A61P1/16

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

• C07B2200/13

  Crystalline forms, e.g. polymorphs · CPC title

• A61K31/192

  having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid  {(cannabinoids A61K31/658)} · CPC title

• C07C323/62 Primary

  having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton · CPC title