Discovery of 3-Cyano- N-(3-(1-isobutyrylpiperidin-4-yl)-1-methyl-4-(trifluoromethyl)-1 H-pyrrolo[2,3- b]pyridin-5-yl)benzamide: A Potent, Selective, and Orally Bioavailable Retinoic Acid Receptor-Related Orphan Receptor C2 Inverse Agonist

Autor: Martin Hegen, David C. Wood, Patrik Rhönnstad, Felix Vajdos, Atli Thorarensen, Mark E. Schnute, Timothy Braden, Kimberly Crouse, Maria Sjöberg, John I. Trujillo, Ravi G. Kurumbail, Bolette Husman, Konrad F. Koehler, Mattias Wennerstål, Tomas Bonn, Joakim Löfstedt, Eva Backström-Rydin, Bo Carlsson, Aron Sundell, Ming Z. Chen, Steven E. Heasley, John David Trzupek, Annika Goos-Nilsson, Carol A. Menard, Peter Harris, James R. Kiefer, Martin Bengtsson, Leon P. Collis, Michael J. Prinsen, Philippe Nuhant, Jennifer Alley, Scott A. Long, Alexander E. Hromockyj, Andrew C. Flick, Johnny Sandberg, Christoph W. Zapf, Edouard Zamaratski, Xiao Hu, Lee Napierata, Björn Kauppi, Nicole Caspers, Kimberly F. Fennell, Robert E. Kyne, Gabriel Berstein, Neelu Kaila, Lars Kruger, Wei Li, Li Xing, Ray Unwalla, Elisabet Kallin, Matthew J. Pelc, Susan Fish, James Robert Blinn, Hjalmar Gullberg, Marvin J. Meyers, Scot Richard Mente, Chulho Choi, Falgun Shah, Mathias Färnegårdh, Dean Messing, Peter G. Jones, Yajuan Zhao, Alexandria P. Taylor, Maria Sandström, Charles W. Bolten, Daniel Nöteberg, Robin A. Weinberg, Tomasz Janosik, John D. Knafels, Anna Wilhelmsson

Publikováno v: Journal of medicinal chemistry. 61(23)

The nuclear hormone receptor retinoic acid receptor-related orphan C2 (RORC2, also known as RORγt) is a promising target for the treatment of autoimmune diseases. A small molecule, inverse agonist of the receptor is anticipated to reduce production

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::9b335f732a3ffd4d00a80bd0f813c732
https://pubmed.ncbi.nlm.nih.gov/30130103