Patent · US Active

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

US11267802B2 · kind B2 · utility

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Key dates

Filing dateJul 26, 2016
Grant dateMar 8, 2022
Priority date
Expiry dateApr 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.