| Title: | Diphenylpropane Derivatives as Agonist of PPAR Nuclear Receptors | ||
| Patent/Patent Application Number: | WO 2013098374 A1 | Publication date: | July 04, 2013 |
| Priority Application: | EP 2011-306790 | Priority date: | December 28, 2011 |
| Inventors: | Dubernet, M.; Delhomel, J.-F.; Bertrand, K. | ||
| Assignee Company: | Genfit, France | ||
| Disease Area: | Metabolic, inflammatory, neurodegenerative diseases | Biological Target: | PPAR nuclear receptors |
| Summary: | This application claims derivatives of diphenylpropane as agonists of PPAR receptors for the treatment of a wide variety of diseases including metabolic, inflammatory, and neurodegenerative diseases such as Alzheimer’s and Parkinson’s diseases. | ||
| Important Compound Classes: |  |
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| Key Structures: |  |
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| Biological Assay: | The agonist activity of the compounds against the PPAR receptors was evaluated in a recombinant assay using monkey kidney COS-7 cells. The in vivo efficacy of one (1) compound was tested in an Alzheimer’s disease model using APPPS1 mice. | ||
| Pharmacological Data: | Thirty-seven compounds were tested against PPAR receptors. The agonist activity of selected compounds is shown below.
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| Compound 14-2-1 had an estimated bioavailability of 92.9% and a brain/plasma ratio of 0.37. | |||
| Compound 14-2-1 was tested in vivo using APPPS1 mice. Compound 14-2-1 showed efficacy in the Morris–Water maze assay and also decreased beta-amyloid accumulation in the brain at 1 and 10 mg/kg. The route of administration was not described. | |||
The authors declare no competing financial interest.