805316-74-9Relevant academic research and scientific papers
Novel tricyclic inhibitors of 1κB kinase
Kempson, James,Spergel, Steven H.,Guo, Junqing,Quesnelle, Claude,Gill, Patrice,Belanger, Dominique,Dyckman, Alaric J.,Li, Tianle,Watterson, Scott H.,Langevine, Charles M.,Das, Jagabandhu,Moquin, Robert V.,Furch, Joseph A.,Marinier, Anne,Dodier, Marco,Martel, Alain,Nirschl, David,Van Kirk, Katy,Burke, James R.,Pattoli, Mark A.,Gillooly, Kathleen,McIntyre, Kim W.,Laishun, Chen,Zheng, Yang,Marathe, Punit H.,Wang-Iverson, David,Dodd, John H.,McKinnon, Murray,Barrish, Joel C.,Pitts, William J.
experimental part, p. 1994 - 2005 (2009/12/31)
The design and synthesis of a novel series of oxazole-, thiazole-, and imidazole-based inhibitors of IκB kinase (IKK) are reported. Biological activity was improved compared to the pyrazolopurine lead, and the expedient synthesis of the new tricyclic systems allowed for efficient exploration of structure-activity relationships. This, combined with an iterative rat cassette dosing strategy, was used to identify compounds with improved pharmacokinetic (PK) profiles to advance for in vivo evaluation.
IMIDAZO-FUSED OXAZOLO[4,5-B]PYRIDINE AND IMIDAZO-FUSED THIAZOLO[4,5-B]PYRIDINE BASED TRICYCLIC COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME
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Page 59, (2010/02/09)
The present invention provides for pyrazolopurine-based tricyclic compounds having the formula (I),[chemical structure] wherein R1, R2, R3, R4, R5 and R6 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.
