Dual M3 antagonists-PDE4 inhibitors. Part 2: Synthesis and SAR of 3-substituted azetidinyl derivatives

Introduction of 3-substituted azetidinyl substituents onto the 4,6-diaminopyrimidine scaffold allowed the improvement of PDE4 inhibiting activities. Preliminary in vivo activity in pulmonary inflammation models is reported.

The SAR around 3-substituted azetidinylpyrimidine derivatives as potent dual M3 antagonists and PDE4 inhibitors is reported.Figure optionsDownload as PowerPoint slide