This poster describes the identification and optimization of a novel class of pyrazole carboxamides as highly Jak1 selective inhibitors, which originated from historical Merck Jak2 preferring molecules. Guided by extensive in-vitro studies, Liabilities related to both oxidative metabolism and plasma stability were successfully addressed. Evidence suggested that active transport might be the main mechanism of clearance resulting in the observed poor in-vitro-in-vivo clearance correlation.

Discovery and optimization of pyrazole carboxamides as Jak1 selective inhibitors for rheumatoid arthritis

248th National Meeting (2014)

The official archive and repository for all ACS Meetings & Expositions abstracts and select posters or presentations.