1407520-42-6Relevant articles and documents
EGFR INHIBITORS, COMPOSITIONS AND METHODS THERE OF
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Page/Page column 18-19; 28-29, (2020/10/20)
The present invention relates to compounds of Formula I, methods of using the compounds as EGFR inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders s
Discovery of a potent dual ALK and EGFR T790M inhibitor
Jang, Jaebong,Son, Jung Beom,To, Ciric,Bahcall, Magda,Kim, So Young,Kang, Seock Yong,Mushajiang, Mierzhati,Lee, Younho,J?nne, Pasi A.,Choi, Hwan Geun,Gray, Nathanael S.
, p. 497 - 510 (2017/05/22)
The mutational activations of anaplastic lymphoma kinase (ALK) and epidermal growth factor receptor (EGFR) are validated oncogenic events and the targets of approved drugs to treat non-small cell lung cancer (NSCLC). Here we report highly potent dual small molecule inhibitors of both ALK and EGFR, particularly the T790M mutant which confers resistance to first generation EGFR inhibitors. Dual ALK/EGFR inhibitors may provide an efficient approach to prevent resistance that arises as a consequence of clinically reported reciprocal activation mechanisms. Our lead compound 7c displayed remarkable inhibitory activities against both ALK and EGFR in enzymatic and cellular assays. We demonstrate that 7c is capable of recapitulating the signaling effects and antiproliferative activity of combined treatment with the approved ALK inhibitor ceritinib and T790M EGFR inhibitor osimertinib against patient-derived non-small cell lung cancer cell line, DFCI032 which harbors both EML4-ALK and activated EGFR.
COMPOUNDS FOR INHIBITING CELL PROLIFERATION IN EGFR-DRIVEN CANCERS
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, (2013/12/03)
The invention features compounds, pharmaceutical compositions and methods for treating patients who have an EGFR-driven cancer of Formula (I), wherein the variables are as defined herein.