Novel 2,3,4,5-tetrahydro-benzo[d]azepine derivatives of 2,4-diaminopyrimidine, selective and orally bioavailable ALK inhibitors with antitumor efficacy in ALCL mouse models |
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| Authors: | Mesaros Eugen F Burke Jason P Parrish Jonathan D Dugan Benjamin J Anzalone Andrew V Angeles Thelma S Albom Mark S Aimone Lisa D Quail Matthew R Wan Weihua Lu Lihui Huang Zeqi Ator Mark A Ruggeri Bruce A Cheng Mangeng Ott Gregory R Dorsey Bruce D |
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| Institution: | Worldwide Discovery Research, Cephalon, Inc., 145 Brandywine Parkway, West Chester, PA 19380, USA |
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| Abstract: | The synthesis and biological evaluation of potent and selective anaplastic lymphoma kinase (ALK) inhibitors from a novel class of 2,4-diaminopyrimidines, incorporating 2,3,4,5-tetrahydro-benzod]azepine fragments, is described. An orally bioavailable analogue (18) that displayed antitumor efficacy in ALCL xenograft models in mice was identified and extensively profiled. |
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| Keywords: | Kinase ALK ALCL Diaminopyrimidine Inhibitors |
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