First dual M sub(3) antagonists-PDE4 inhibitors: Synthesis and SAR of 4,6- diaminopyrimidine derivatives

First dual M sub(3) antagonists-PDE4 inhibitors: Synthesis and SAR of 4,6- diaminopyrimidine derivatives

SAR around 4,6-diaminopyrimidine derivatives allowed the discovery of the first potent dual M sub(3) 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.

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-04, Vol.16 (7), p.1834-1839
Hauptverfasser: Provins, Laurent, Christophe, Bernard, Danhaive, Pierre, Dulieu, Jacques, Durieu, Veronique, Gillard, Michel, Lebon, Florence, Lengele, Sebastien, Quere, Luc, Van Keulen, BerendJan
Format: Artikel
Sprache:eng
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
Beschreibung
Zusammenfassung:SAR around 4,6-diaminopyrimidine derivatives allowed the discovery of the first potent dual M sub(3) 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.01.006