USE OF 1,3-DIPHENYLPROP-2-EN-1-ONE DERIVATIVES FOR TREATING LIVER DISORDERS

• US 20140309165A1
• Filed: 05/28/2014
• Published: 10/16/2014
• Est. Priority Date: 11/26/2009
• Status: Active Grant

• Current Assignee: Genfit SA
• Original Assignee: Genfit SA
• Inventors: Hanf, Rmy, Hum, Dean, Dufour, Ingrid, DARTEIL, Raphael
• Granted Patent: US 8,895,619 B2
• Time in Patent Office: Days
• US Class Current: 514/6.5
• 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 amino-transferases. 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 liver fibrosis 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 liver fibrosis is liver cirrhosis.

9. The method of claim 5, wherein the liver fibrosis is liver cirrhosis.

10. The method of claim 1, wherein said treatment delays progression of said liver fibrosis.

11. The method of claim 5, wherein said treatment delays progression of said liver fibrosis.