First dual M 3 antagonists-PDE4 inhibitors: synthesis and SAR of 4, 6-diaminopyrimidine derivatives

L Provins, B Christophe, P Danhaive, J Dulieu…

Index: Provins, Laurent; Christophe, Bernard; Danhaive, Pierre; Dulieu, Jacques; Durieu, Veronique; Gillard, Michel; Lebon, Florence; Lengele, Sebastien; Quere, Luc; Van Keulen, Berendjan Bioorganic and Medicinal Chemistry Letters, 2006 , vol. 16, # 7 p. 1834 - 1839

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Citation Number: 27

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.