Discovery and Preclinical Evaluation of [4-[[1-(3-fluorophenyl)methyl]-1H-indazol-5-ylamino]-5-methylpyrrolo[2,1-f][1,2,4]triazin-6-yl]carbamic Acid, (3S)-3-Morpholinylmethyl Ester (BMS-599626), a Selective and Orally Efficacious Inhibitor of Human Epidermal Growth Factor Receptor 1 and 2 Kinases
Journal of Medicinal Chemistry2009Vol. 52(21), pp. 6527–6530
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Ashvinikumar V. Gavai, Brian E. Fink, David J. Fairfax, Greg S. Martin, Lana M. Rossiter, Christian L. Holst, Soong‐Hoon Kim, Kenneth J. Leavitt, Harold Mastalerz, Wen-Ching Han, Derek Norris, Bindu Goyal, Shankar Swaminathan, Bharat Patel, Arvind Mathur, Dolatrai M. Vyas, John S. Tokarski, Chiang Yu, Simone Oppenheimer, Hongjian Zhang, Punit Marathe, Joseph Fargnoli, Francis Y. Lee, Tai W. Wong, Gregory D. Vite
Abstract
Structure-activity relationships in a series of 4-[1H-indazol-5-ylamino]pyrrolo[2,1-f][1,2,4]triazine-6-carbamates identified dual human epidermal growth factor receptor (HER)1/HER2 kinase inhibitors with excellent biochemical potency and kinase selectivity. On the basis of its favorable pharmacokinetic profile and robust in vivo activity in HER1 and HER2 driven tumor models, 13 (BMS-599626) was selected as a clinical candidate for treatment of solid tumors.
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