Posted by kinasepro on November 5, 2006
Hey there Jannsen, I see you and Schering AG have been hitting the Macrocyclic button for kinase inhitors for a little while now. Schering on pyrimidines for Tie2 (EP1674470 / WO2006108695) and you guys on the quinazolines for EGF. They’re a little kookie, but hey I like it. Got to be an entropy thing, eh?
This application looks at a handful of linkers, as you may expect, made via amid coupling, olefin metathesis, and even reductive amination.