Evaluation of WO2012080456 and WO2012080457; Boheringer Ingleheim's first CXCR2 antagonists

Abstract

Two applications claim CXCR2 receptor antagonists respectively incorporating arylcarbonyl and arylsulfonyl substituted 2-hydroxyaniline scaffolds. The first application claims both N-aryl,N′-aryl urea and squaramide derivatives, the second focuses on squaramide derivatives. Several examples of the latter scaffold with nanomolar affinity are provided and indicate an alternative modification of the squaramide scaffold that has been explored extensively by other groups.

Keywords::

• chemokine
• COPD
• CXCR2
• IL-8
• inflammation