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.

Alaric J. Dyckman,Charles M. Langevine,Claude A. 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

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.

2011

Alaric J. Dyckman
Charles M. Langevine
Claude A. 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

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.

Keywords:

Chemical synthesis
Tricyclic
Thiazole
PK/PD models
Rheumatoid arthritis
In vivo
Structure–activity relationship
Stereochemistry
Biochemistry
Pharmacokinetics
Chemistry

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