Bebetter Med Inc.

Guangzhou Bebetter Medicine Technology Co., Ltd.

Weicai Xue

Junqi Li

Xiong Cai

Changgeng Qian

Yuanhui Qing

Huajin You

Yanyan Wang

Bin Liu

Yunwo Weng

Shiqing Zhou

Mingsheng Lin

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. 

2,4-bis(nitrogen-containing group)-substituted pyrimidine compound, preparation method and use thereof

The present invention discloses a pyrimidine or pyridopyridone compound as shown in formula (I) and an application thereof relating to the technical field of medicament preparation. The compound can selectively suppress cyclin-dependent kinases (Cdks) CDK4 and CDK6 with almost no suppression of the activity of the kinase CDK2. Thus, the compound can be used for various diseases caused by cell cycle control disorders involving CDK4 and CDK6, and particularly in the treatment of malignant tumors. 

Pyrimidine or pyridopyridone compound and application thereof

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Guangdong, China

Weicai Xue