Upadacitinib, also known as ABT-494, is a potent and selective JAK inhibitors in development for rheumatoid arthritis. ABT-494 is approximately 74 fold selective for Jak1 over Jak2 in cellular assays dependent on specific, relevant cytokines. ABT-494 demonstrates efficacy in rat arthritis models. Preliminary evidence suggests that compared to tofacitinib, ABT-494 may spare Jak2 and Jak3 dependent signaling.
Pangan, Aileen L.; Teixeira, Henrique D.; Allian, Ayman D.; Borchardt, Thomas B.; Jayanth, Jayanthy; Marroum, Patrick J.; Nordstrom, Fredrik Lars; Sheikh, Ahmad Y.; Mohamed, Mohamed-Eslam F.; Othman, Ahmed A.; Mayer, Peter T. Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof for disease treatment. Assignee AbbVie Inc., USA. US 20180298016. (2018).
Wishart, Neil; Argiriadi, Maria A.; Calderwood, David J.; Ericsson, Anna M.; Fiamengo, Bryan R.; Frank, Kristine E.; Friedman, Michael; George, Dawn M.; Goedken, Eric R.; Josephsohn, Nathan S.; Li, Biqin C.; Morytko, Michael J.; Stewart, Kent D.; Voss, Jeffrey W.; Wallace, Grier A.; Wang, Lu; Woller, Kevin R. Preparation of novel nitrogen-containing tricyclic compounds as kinase inhibitors. Assignee Abbott Laboratories, USA. US 20110311474. (2011).
