1232397-36-2Relevant academic research and scientific papers
2,7-Disubstituted-pyrrolo[2,1- f ][1,2,4]triazines: New variant of an old template and application to the discovery of anaplastic lymphoma kinase (ALK) inhibitors with in vivo antitumor activity
Ott, Gregory R.,Wells, Gregory J.,Thieu, Tho V.,Quail, Matthew R.,Lisko, Joseph G.,Mesaros, Eugen F.,Gingrich, Diane E.,Ghose, Arup K.,Wan, Weihua,Lu, Lihui,Cheng, Mangeng,Albom, Mark S.,Angeles, Thelma S.,Huang, Zeqi,Aimone, Lisa D.,Ator, Mark A.,Ruggeri, Bruce A.,Dorsey, Bruce D.
, p. 6328 - 6341 (2011/11/12)
A novel 2,7-disubstituted-pyrrolo[2,1-f][1,2,4]triazine scaffold has been designed as a new kinase inhibitor platform mimicking the bioactive conformation of the well-known diaminopyrimidine motif. The design, synthesis, and validation of this new pyrrolo[2,1-f][1,2,4]triazine scaffold will be described for inhibitors of anaplastic lymphoma kinase (ALK). Importantly, incorporation of appropriate potency and selectivity determinants has led to the discovery of several advanced leads that were orally efficacious in animal models of anaplastic large cell lymphoma (ALCL). A lead inhibitor (30) displaying superior efficacy was identified and in depth in vitro/in vivo characterization will be presented.
PYRROLOTRIAZINES AS ALK AND JAK2 INHIBITORS
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Page/Page column 351, (2010/08/05)
The present invention provides a compound of formula (I) or a salt form thereof, wherein Q1, Q2, Q3, and Q4 are as defined herein. The compound of formula (I) has ALK and/or JAK2 inhibitory activity, and may be used to treat proliferative disorders.
