The inhibition of p38 MAPK utilising oxalic amides attached to an azaindole scaffold

Abstract

This patent application from Scios, Inc. builds upon earlier efforts which identified a distinct scaffold as a p38 mitogen-activated protein kinase (MAPK) inhibitor. A seemingly important characteristic of this company’s scaffold is an indole nucleus, which serves as a core to which groups, such as an oxalic amide and piperidine amide, are attached. This application claims compounds incorporating heteroatoms, such as nitrogen, oxygen and sulfur, into the indole nucleus. Thus, azaindoles, with oxalic amides and piperidine amides attached, are prominently featured throughout this application. The compounds are claimed to be anti-inflammatory agents because of their ability to modulate the release of cytokines from inflammatory cells by interven-ing in the stress-activated signal transduction cascade.

• cytokine
• inflammation
• p38 mitogen-activated protein kinase (MAPK) inhibitor
• signal transduction
• tumour necrosis factor (TNF)