1345250-86-3Relevant academic research and scientific papers
Imidazo[1,5-a]quinoxalines as irreversible BTK inhibitors for the treatment of rheumatoid arthritis
Kim, Kyung-Hee,Maderna, Andreas,Schnute, Mark E.,Hegen, Martin,Mohan, Shashi,Miyashiro, Joy,Lin, Laura,Li, Evelyn,Keegan, Sean,Lussier, Jennifer,Wrocklage, Christopher,Nickerson-Nutter, Cheryl L.,Wittwer, Arthur J.,Soutter, Holly,Caspers, Nicole,Han, Seungil,Kurumbail, Ravi,Dunussi-Joannopoulos, Kyri,Douhan III, John,Wissner, Allan
, p. 6258 - 6263 (2011/11/29)
Imidazo[1,5-a]quinoxalines were synthesized that function as irreversible Bruton's tyrosine kinase (BTK) inhibitors. The syntheses and SAR of this series of compounds are presented as well as the X-ray crystal structure of the lead compound 36 in complex with a gate-keeper variant of ITK enzyme. The lead compound showed good in vivo efficacy in preclinical RA models.
