First Dual M3 Antagonists-PDE4 Inhibitors: Synthesis and SAR of 4,6-Diaminopyrimidine Derivatives.

Abstract SAR around 4,6-diaminopyrimidine derivatives allowed the discovery of the first potent dual M3 antagonists and PDE4 inhibitors. Various chemical modulations around that scaffold led to the discovery of ucb-101333-3 which is characterized by the most interesting profile on both targets.