Fused bi-heteroaryl substituted hydantoin compounds as TACE inhibitors

摘要

We have identified a series of hydantoin-derived TNF-a converting enzyme (TACE) inhibitors containing a pendant fused bi-heteroaryl group, which demonstrate sub-nanomolar potency (Ki), excellent activity in human whole blood assay, and improved DMPK profiles over prior series. (C) 2017 Published by Elsevier Ltd.