Imidazo[4,5-d]thiazolo[5,4-b]pyridine based inhibitors of IKK2: Synthesis, SAR, PK/PD and activity in a preclinical model of rheumatoid arthritis
The synthesis, structure-activity relationships (SAR) and biological evaluation of thiazole based tricyclic inhibitors of IKK2 are described. Compound 9 was determined to be orally efficacious in a murine model of rheumatoid arthritis.
Dyckman, Alaric J.,Langevine, Charles M.,Quesnelle, Claude,Kempson, James,Guo, Junqing,Gill, Patrice,Spergel, Steven H.,Watterson, Scott H.,Li, Tianle,Nirschl, David S.,Gillooly, Kathleen M.,Pattoli, Mark A.,McIntyre, Kim W.,Chen, Laishun,McKinnon, Murray,Dodd, John H.,Barrish, Joel C.,Burke, James R.,Pitts, William J.
scheme or table
p. 383 - 386
(2011/02/27)
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