Dual M sub(3) 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.

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2007-06, Vol.17 (11), p.3077-3080
Hauptverfasser: Provins, Laurent, Christophe, Bernard, Danhaive, Pierre, Dulieu, Jacques, Gillard, Michel, Quere, Luc, Stebbins, Karin
Format: Artikel
Sprache:eng
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Zusammenfassung: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2007.03.047