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COMPOSE PYRIMIDINE A SUBSTITUTION 2,4-DI-(GROUPE AZOTE), SON PROCEDE DE PREPARATION ET SON UTILISATION
专利权人:
GUANGZHOU BEBETTER MEDICINE TECHNOLOGY CO.; LTD.
发明人:
CAI, XIONG,QIAN, CHANGGENG,WENG, YUNWO,LIU, BIN,WANG, YANYAN,LIN, MINGSHENG,LI, JUNQI,QING, YUANHUI,YOU, HUAJIN,ZHOU, SHIQING,XUE, WEICAI
申请号:
CA2997039
公开号:
CA2997039A1
申请日:
2016.07.26
申请国别(地区):
CA
年份:
2017
代理人:
摘要:
Provided are a 2, 4-di-(nitrogen containing group) substituted pyrimidine compound represented by a general formula (I), a pharmaceutically acceptable salt and a stereoisomer thereof, a preparation method thereof, and a use thereof in preparation of anti-tumor drugs. The compound having a structural feature shown in the general formula (I) can selectively suppress activity of mutant epidermal growth factor receptors (EGFR), including single-mutant EGFR (T790M) and double-mutant EGFR (including L858R/T790M and ex19del/T790M), and can suppress activity of single gain-of-function mutant EGFR (including L858R and ex19del) as well. The compound has a weak suppression effect on wild-type EFGR and a very high selectivity, and thus it has a potential to be used in preparation of drugs for treating EGFR mutant tumors, especially non-small cell lung cancer (NSCLC) comprising a T790M EGFR mutation.
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中国工程科技知识中心
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