Abstract: Provided are a 1,3-di-substituted ketene compound having a structure as represented by formula (I) and an application thereof. Such a type of compound primarily activates peroxisome proliferator-activated receptor (PPAR) ?, and also activates PPPA? and PPPA?. The compound may be used to treat various diseases associated with PPAR regulation and control abnormality, such as non-alcoholic fatty liver disease, and especially in treating non-alcoholic hepatitis, and may potentially be used in the treatment of diseases comprising diabetes, obesity, fibrotic diseases, cardiovascular diseases (comprising heart failure, atherosclerosis, and so on), kidney diseases (comprising chronic kidney disease, renal failure, and so on), and brain degenerative diseases (comprising Alzheimer's disease and so on), having great application value.
Type:
Grant
Filed:
June 29, 2018
Date of Patent:
April 19, 2022
Assignee:
BEBETTER MED INC.
Inventors:
Xiong Cai, Changgeng Qian, Chunqiang Ye, Qijie He
Abstract: 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.