Use of 1,3-diphenylprop-2-en-1-one derivatives for treating liver disorders

• US 8,772,342 B2
• Filed: 11/26/2010
• Issued: 07/08/2014
• Est. Priority Date: 11/26/2009
• Status: Active Grant

• Current Assignee: Genfit SA
• Original Assignee: Genfit SA
• Inventors: Darteil, Raphael, Hum, Dean, Hanf, Rmy, Dufour, Ingrid
• Primary Examiner(s): Zucker, Paul A
• Application Number:
  US13/511,170
• Publication Number:
  US 20120252725A1
• Time in Patent Office: 1,320 Days
• US Class Current: 514/571
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/155 Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
• CPC Class Codes: A61K 31/192 having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid cannabinoids A61K31/658
• CPC Class Codes: A61K 31/216 of acids having aromatic rings, e.g. benactizyne, clofibrate
• CPC Class Codes: A61K 38/28 Insulins
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 1/00 Drugs for disorders of the alimentary tract or the digestive system
• CPC Class Codes: A61P 1/16 for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• CPC Class Codes: A61P 3/04 Anorexiants; Antiobesity agents
• CPC Class Codes: A61P 3/06 Antihyperlipidemics
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The invention provides 1,3-diphenylprop-2-en-1-one derivatives and pharmaceutical compositions comprising the same for treating liver disorders, in particular those requiring the reduction of plasma level of biochemical markers such as aminotransferases. The 1,3-diphenylprop-2-en-1-one derivatives of General Formula (I) have hepatoprotective properties and can be used in methods for treating liver disorders involving the pathological disruption, inflammation, degeneration, and/or proliferation of liver cells, such as liver fibrosis or fatty liver disease.

Claims

1. A method for the treatment of a non-alcoholic fatty liver disease in a subject in need thereof, comprising administering to the subject a compound selected from 1-[4-methylthiophenyl]-3-[3,5-dimethyl-4-carboxydimethylmethyloxyphenyl]prop-2-en-1-one or a pharmaceutically acceptable salt or a stereoisomer thereof.

2. The method according to claim 1, wherein the compound is orally administered.

3. The method of claim 1, wherein the compound is administered as an injectable suspension, a gel, a oil, a pill, a suppository, a powder, a gel cap, a capsule, an aerosol, a galenic form, a prolonged release formulation or a slow release form.

4. The method of claim 1, wherein the compound is administered in combination with metformin, insulin, a thiazolidinedione, a glitazone, or a statin.

5. The method of claim 1, comprising administering a pharmaceutical composition comprising 1-[4-methylthiophenyl]-3-[3,5-dimethyl-4-carboxydimethylmethyloxyphenyl]prop-2-en-1-one or a pharmaceutically acceptable salt or a stereoisomer thereof.

6. The method of claim 5, wherein said composition is formulated in the form of an injectable suspension, a gel, an oil, a pill, a suppository, a powder, a gel cap, a capsule, an aerosol, a galenic form, a prolonged release formulation or a slow release form.

7. The method of claim 5, wherein said composition is in an oral form.

8. The method of claim 1, wherein the non-alcoholic fatty liver disease is non-alcoholic steatohepatitis.

9. The method of claim 5, wherein the non-alcoholic fatty liver disease is non-alcoholic steatohepatitis.

10. The method of claim 1, wherein said treatment delays progression of said non-alcoholic fatty liver disease.

11. The method of claim 5, wherein said treatment delays progression of said non-alcoholic fatty liver disease.