927962-42-3Relevant articles and documents
Design, Synthesis, and Evaluation of a Novel Series of Indole Sulfonamide Peroxisome Proliferator Activated Receptor (PPAR) α/γ/δ Triple Activators: Discovery of Lanifibranor, a New Antifibrotic Clinical Candidate
Boubia, Bena?ssa,Poupardin, Olivia,Barth, Martine,Binet, Jean,Peralba, Philippe,Mounier, Laurent,Jacquier, Elise,Gauthier, Emilie,Lepais, Valérie,Chatar, Maryline,Ferry, Stéphanie,Thourigny, Anne,Guillier, Fabrice,Llacer, Jonathan,Amaudrut, JéRome,Dodey, Pierre,Lacombe, Olivier,Masson, Philippe,Montalbetti, Christian,Wettstein, Guillaume,Luccarini, Jean-Michel,Legendre, Christiane,Junien, Jean-Louis,Broqua, Pierre
, p. 2246 - 2265 (2018/03/26)
Here, we describe the identification and synthesis of novel indole sulfonamide derivatives that activate the three peroxisome proliferator activated receptor (PPAR) isoforms. Starting with a PPARα activator, compound 4, identified during a high throughput screening (HTS) of our proprietary screening library, a systematic optimization led to the discovery of lanifibranor (IVA337) 5, a moderately potent and well balanced pan PPAR agonist with an excellent safety profile. In vitro and in vivo, compound 5 demonstrated strong activity in models that are relevant to nonalcoholic steatohepatitis (NASH) pathophysiology suggesting therapeutic potential for NASH patients.
HSP-90 BINDING COMPOUNDS, COMPOSITIONS THEREOF, AND THEIR USE FN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISEASES
-
Page/Page column 50; 51, (2011/04/24)
The invention relates to therapeutic compounds that bind to HSP90. The compounds disclosed herein bind HSP90 and alter the chaperoning capability of HSP90 proteins. The invention also relates to pharmaceutical compositions comprising these compounds, and methods of treating diseases and disorders such as cancer, autoimmune disease and other diseases.