RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: Synthesis and biological evaluation

(±)-1-(anti-3-Hydroxy-cyclopentyl)-3-(4-methoxy-phenyl)-7-phenylamino-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one (RO4383596) is a potent and selective inhibitor of the pro-angiogenic receptor tyrosine kinases KDR, FGFR, and PDGFR. This agent has an excellent pharmacokinetic profile and is highly efficacious in rodent models of angiogenesis upon oral administration.

The synthesis and anti-angiogenic efficacy of RO4383596, a pyrimidopyrimidone inhibitor of the KDR, FGFR, and PDGFR receptor tyrosine kinases, are described.Figure optionsDownload as PowerPoint slide