-
- Christel J Menet, Stephen R Fletcher, Guy Van Lommen, Raphael Geney, Javier Blanc, Koen Smits, Nolwenn Jouannigot, Pierre Deprez, Ellen M van der Aar, Philippe Clement-Lacroix, Liên Lepescheux, René Galien, Béatrice Vayssiere, Luc Nelles, Thierry Christophe, Reginald Brys, Muriel Uhring, Fabrice Ciesielski, and Luc Van Rompaey.
- Galapagos NV , Generaal de Wittelaan L11A3, 2800 Mechelen, Belgium.
- J. Med. Chem. 2014 Nov 26; 57 (22): 9323-42.
AbstractJanus kinases (JAK1, JAK2, JAK3, and TYK2) are involved in the signaling of multiple cytokines important in cellular function. Blockade of the JAK-STAT pathway with a small molecule has been shown to provide therapeutic immunomodulation. Having identified JAK1 as a possible new target for arthritis at Galapagos, the compound library was screened against JAK1, resulting in the identification of a triazolopyridine-based series of inhibitors represented by 3. Optimization within this chemical series led to identification of GLPG0634 (65, filgotinib), a selective JAK1 inhibitor currently in phase 2B development for RA and phase 2A development for Crohn's disease (CD).
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