1.
ACS Med Chem Lett
; 11(10): 1863-1868, 2020 Oct 08.
Artigo
em Inglês
| MEDLINE
| ID: mdl-33062165
RESUMO
The identification and lead optimization of a series of pyrazolo[3,4-d]pyridazinone derivatives are described as a novel class of potent irreversible BTK inhibitors, resulting in the discovery of compound 8. Compound 8 exhibited high potency against BTK kinase and acceptable PK profile. Furthermore, compound 8 demonstrated significant in vivo efficacy in a mouse-collagen-induced arthritis (CIA) model.