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

Laurent Provins,Bernard Christophe,Pierre Danhaive,Jacques Dulieu,Michel Gillard,Luc Quéré,Karin Stebbins

Bioorganic & medicinal chemistry letters（2007）

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摘要

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.

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