Bristol-Myers Squibb Symposium-NOTE EVENT, TIME & LOCATION CHANGES

The human epidermal growth factor receptor (HER) and the vascular endothelial growth factor receptor (VEGFR) signaling pathways have been implicated in the processes governing tumor growth and proliferation. Thus, development of potent and selective inhibitors of HER and VEGFR may provide clinical benefit in the treatment of a range of solid malignancies. As part of an ongoing program in our laboratories, the functionalized pyrrolotriazine BMS-690514 was identified as an orally active, selective and potent dual inhibitor of HER and VEGFR.

The results of our development activities that led to the successful preparation of BMS-690514 on multi-100-kilogram scale will be presented. In addition, laboratory development of an alternate end game that addressed all of the manufacturing issues of the current route will be described.