112077-95-9Relevant articles and documents
Discovery of selective irreversible inhibitors for EGFR-T790M
Zhou, Wenjun,Ercan, Dalia,Jaenne, Pasi A.,Gray, Nathanael S.
, p. 638 - 643 (2011/03/18)
Targeting the epidermal growth factor receptor kinase (EGFR) with ATP-competitive kinase inhibitors results in dramatic but short-lived responses in patients with EGFR mutant non small cell lung cancer. A series of novel covalent EGFR kinase inhibitors with selectivity for the clinically relevant T790M 'gatekeeper' resistance mutation relative to wild-type EGFR were discovered by library screening. A representative compound 3i was obtained through a systematic SAR study guided by mutant EGFR-dependent cellular proliferation assays.
Purine derivatives inhibitors of tyrosine protein kinase SYK
-
, (2008/06/13)
Disclosed are compounds of the formula in free or salt form, wherein X, R1, R2, R3, and R4are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment o
