Patent · US Active

Nitrogenous heterocyclic compound, preparation method, intermediate, composition and use

US10828305B2 · kind B2 · utility

1Cited by
4References
17Claims
0Family size

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Key dates

Filing dateMar 1, 2017
Grant dateNov 10, 2020
Priority date
Expiry dateMar 1, 2037

Classification

  • Technology area (CPC Y)Emerging Cross-Sectional Technologies
  • CPC primaryY02P20/55
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

Disclosed are a nitrogenous heterocyclic compound, intermediates, a preparation method, a composition and use thereof. The nitrogenous heterocyclic compound in the present invention is as shown in formula I. The compound has a high inhibitory activity towards ErbB2 tyrosine kinase and a relatively good inhibitory activity towards human breast cancer BT-474 and human gastric cancer cell NCI-N87 which express ErbB2 at a high level, and at the same time has a relatively weak inhibitory activity towards EGFR kinase. Namely, the compound is a highly selective small-molecule inhibitor targeted at ErbB2, and hence it has a high degree of safety, and can effectively enlarge the safety window in the process of taking the drug.

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.