# US 8,772,342 B2 · Use of 1,3-diphenylprop-2-en-1-one derivatives for treating liver disorders

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- Number: US 8,772,342 B2
- Document ID: US8772342B2
- Status: Granted
- Kind: B2
- Application number: 13/511,170
- Filed: 2010-11-26
- Published: 2012-10-04
- Granted: 2014-07-08
- Earliest claimed: 2009-11-26
- Assignees: Genfit
- Applicants: Raphael Darteil; Rémy Hanf; Dean Hum; Ingrid Dufour
- Inventors: Raphael Darteil; Rémy Hanf; Dean Hum; Ingrid Dufour
- Web page: https://patentgrep.com/patent/US8772342B2

## CPC

- A61K 31/192: having aromatic groups, e.g. sulindac, 2-aryl-propionic acids, ethacrynic acid {(cannabinoids A61K31/658)}
- A61K 31/155: Amidines ([IMAGE cpc-sch-A61K-1029.gif]), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
- A61K 31/216: of acids having aromatic rings, e.g. benactizyne, clofibrate
- A61K 38/28: Insulins
- A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 1/16: for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
- A61P 3/04: Anorexiants; Antiobesity agents
- A61P 3/06: Antihyperlipidemics
- A61P 3/10: for hyperglycaemia, e.g. antidiabetics
- A61P 29/00: Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## 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

### Claim 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.

### Claim 2 (depends on 1)

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

### Claim 3 (depends on 1)

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.

### Claim 4 (depends on 1)

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

### Claim 5 (depends on 1)

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.

### Claim 6 (depends on 5)

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.

### Claim 7 (depends on 5)

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

### Claim 8 (depends on 1)

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

### Claim 9 (depends on 5)

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

### Claim 10 (depends on 1)

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

### Claim 11 (depends on 5)

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