Spiroquinazolinones as novel, potent, and selective PDE7 inhibitors. Part 2: Optimization of 5,8-disubstituted derivatives

  • Bioorg Med Chem Lett. 2004 Sep 20;14(18):4627-31. doi: 10.1016/j.bmcl.2004.07.010.
Patrick Bernardelli  1 ,  Edwige Lorthiois ,  Fabrice Vergne ,  Chrystelle Oliveira ,  Abdel-Kader Mafroud ,  Emmanuelle Proust ,  Nga Pham ,  Pierre Ducrot ,  François Moreau ,  Moulay Idrissi ,  Anita Tertre ,  Bernadette Bertin ,  Magali Coupe ,  Eric Chevalier ,  Arnaud Descours ,  Françoise Berlioz-Seux ,  Patrick Berna ,  Mei Li
Affiliations
  • 1. Pfizer Global Research and Development, 3-9 rue de la Loge 94265 Fresnes, France. [email protected]
PMID: 15324877 DOI: 10.1016/j.bmcl.2004.07.010
Abstract

The optimization of 5,8-disubstituted spirocyclohexane-quinazolinones into potent, selective, soluble PDE7 inhibitors with acceptable in vivo pharmacokinetic parameters is presented.