2,4-bis(nitrogen-containing group)-substituted pyrimidine compound, preparation method and use thereof
US11267802B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Jul 26, 2016 |
| Grant date | Mar 8, 2022 |
| Priority date | — |
| Expiry date | Apr 11, 2038 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D471/04
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
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.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.