1227939-82-3Relevant articles and documents
PROCESSES TO MAKE PROTEIN KINASE INHIBITORS
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, (2015/11/03)
Processes to prepare compounds that inhibit protein kinases such as Aurora kinases and the VEGFR and PDGFR families of kinases are discussed.
Thienopyridine ureas as dual inhibitors of the VEGF and Aurora kinase families
Curtin, Michael L.,Frey, Robin R.,Heyman, H. Robin,Soni, Niru B.,Marcotte, Patrick A.,Pease, Lori J.,Glaser, Keith B.,Magoc, Terrance J.,Tapang, Paul,Albert, Daniel H.,Osterling, Donald J.,Olson, Amanda M.,Bouska, Jennifer J.,Guan, Zhiwen,Preusser, Lee C.,Polakowski, James S.,Stewart, Kent D.,Tse, Chris,Davidsen, Steven K.,Michaelides, Michael R.
scheme or table, p. 3208 - 3212 (2012/06/18)
In an effort to identify multi-targeted kinase inhibitors with a novel spectrum of kinase activity, a screen of Abbott proprietary KDR inhibitors against a broad panel of kinases was conducted and revealed a series of thienopyridine ureas with promising activity against the Aurora kinases. Modification of the diphenyl urea and C7 moiety of these compounds provided potent inhibitors with good pharmacokinetic profiles that were efficacious in mouse tumor models after oral dosing. Compound 2 (ABT-348) of this series is currently undergoing Phase I clinical trials in solid and hematological cancer populations.
KINASE INHIBITORS WITH IMPROVED CYP SAFETY PROFILE
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Page/Page column 15, (2010/06/19)
Compounds that inhibit protein kinases such as Aurora-kinases and the VEGFR and PDGFR families of kinases, with an improved safety profile due to low CYP3A4 inhibition, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.