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

  • Bioorg Med Chem Lett. 2011 Jan 1;21(1):383-6. doi: 10.1016/j.bmcl.2010.10.133.
Alaric J Dyckman  1 ,  Charles M Langevine ,  Claude Quesnelle ,  James Kempson ,  Junqing Guo ,  Patrice Gill ,  Steven H Spergel ,  Scott H Watterson ,  Tianle Li ,  David S Nirschl ,  Kathleen M Gillooly ,  Mark A Pattoli ,  Kim W McIntyre ,  Laishun Chen ,  Murray McKinnon ,  John H Dodd ,  Joel C Barrish ,  James R Burke ,  William J Pitts
Affiliations
  • 1. Bristol-Myers Squibb, Research and Development, Princeton, NJ 08543-4000, USA. [email protected]
PMID: 21087862 DOI: 10.1016/j.bmcl.2010.10.133
Abstract

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.