923978-27-2

Usage

Biological Functions

Elafibranor (GFT505) is an agonist of peroxisome proliferator-activated receptor (PPAR) alpha and delta. EC50 values were 45 and 175 nM, respectively. GFT505 is being developed as a dual PPAR-α/PPAR-δ receptor agonist for the treatment of type 2 diabetes and nonalcoholic fatty liver disease. GFT1007 and GFT505 have an active metabolite, both with potent stimulant activity PPAR-α and to a lesser extent PPAR-δ.

Biological Activity

Elafibranor (GFT505) is an agonist of PPAR-alpha and PPAR-delta, improves insulin sensitivity, benefits glucose homeostasis, lipid metabolism and reduces inflammation.

References

1) Cariou?et al.?(2011)?Effects of the New Dual PPARα/δ Agonist GFT505 on Lipid and Glucose Homeostasis in Abdominally Obese Patients With Combined Dyslipidemia or Impaired Glucose Metabolism; Diabetes Care?34?2008 2) Cariou?et al.?(2013)?Dual peroxisome proliferator receptor α/δ agonist GFT505 improves hepatic and peripheral insulin sensitivity in abdominally obese subjects; Diabetes Care?36?2923 3) Hanf?et al.?(2014)?The dual peroxisome proliferator-activated alpha/delta agonist GFT505 exerts anti-diabetic effects in db/db mice without peroxisome proliferator-activated receptor gamma-associated adverse cardiac effects.; Diab. Vasc. Dis. Res.?11?440 4) Staels?et al.?(2013)?Hepatoprotective effects of the dual peroxisome proliferator-activated receptor alpha-delta agonist, GFT505, in rodent models of nonalcoholic fatty liver disease/nonalcoholic steatohepatitis; Hepatology?58?1941 5) Ratziu?et al.?(2016)?Elafibranor, an Agonist of the Peroxisome Proliferator-Activated Receptor-α and -δ, Induces Resolution of Nonalcoholic Steatohepatitis Without Fibrosis Worsening.; Gastroenterology.?39?2951 6) Boeckmans?et al. (2019)?Elafibranor restricts lipogenic and inflammatory responses in a human skin stem cell-derived model of NASH.; Pharmacol. Res.?114?377

Upstream product

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Relevant academic research and scientific papers

POLYMORPHS OF ELAFIBRANOR

The present invention relates to novel crystalline forms of elafibranor.

Preparation method of phenoxyacetic acid derivatives

The invention discloses a preparation method of phenoxyacetic acid derivatives, which adopts a one-step synthesis method and comprises the following steps: reacting (E)-2, 6-dimethyl-4-(3-(4-(methylthio) phenyl)-3-oxopropyl-1-alkene-1-yl) phenol with 2-br

PROCESS FOR PREPARATION OF ELAFIBRANOR

The present invention provides a process for elafibranor, the process comprising reacting compound of formula II or the compound of formula III with a compound of formula IV. The present invention also involve purification of elafibranor by reacting elafi

NOVEL COMPOUNDS AND THEIR USE IN PREPARATION OF ELAFIBRANOR AND PHARMACEUTICAL ACCEPTABLE SALTS THEREOF

The present invention relates to the novel compounds of Formula I, and salts thereof and use of said compounds as intermediates for the preparation of (E)-2-(2,6-dimethyl-4-(3-(4-(methylthio)phenyl)-3-oxoprop-1-en-1-yl)phenoxy)-2-methylpropanoic acid (Elafibranor) of Formula II and its pharmaceutical acceptable salts.

DUAL-ACTION ELAFIBRANOR METFORMIN SALT FOR TREATING OBESITY ASSOCIATED WITH NON-ALCOHOLIC STEATOHEPATITIS (NASH) AND HYPERTRIGLYCERIDAEMIA

Drugs derived from elafibranor. One or more embodiments relate more particularly to a composition comprising at least one active principle, wherein the at least one active principle comprises an elafibranor metformin salt. One or more embodiments also rel

SOLID FORMS OF ELAFIBRANOR AND PROCESSES THEREOF

The present invention relates to solid forms of Elafibranor, processes for preparation thereof, pharmaceutical salts of Elafibranor, their crystalline and amorphous forms and processes for preparation thereof.

PROCESS FOR THE PREPARATION OF ELAFIBRANOR AND NOVEL SYNTHESIS INTERMEDIATES

The present invention relates to a process for the preparation of elafibranor and novel synthesis intermediates.

GFT505 and preparation method for intermediate thereof

The invention discloses GFT505 and a preparation method for an intermediate thereof. The invention provides the preparation method for an intermediate I of GFT505, comprising the following steps: in an organic solvent, carrying out isomerization reaction

Preparation of 1,3-diphenylprop-2-en-1-one derivatives

The invention relates to a method for the preparation of de 1,3-diphenylprop-2-en-1-one substituted on one of the two phenyl groups by a carboxyalkyloxy group or a carboxyalkylthio group.

Substituted 1,3-diphenylprop-2-en-1-one derivatives and preparation and uses thereof

The invention concerns novel substituted 1,3-diphenylprop-2-en-1-one derivatives, pharmaceutical compositions comprising same, their therapeutic uses, in particular for treating cerebral ischemia. The invention also concerns a method for preparing said derivatives.