Patent · US Active

Diaryl macrocyclic compound and pharmaceutical composition, and use thereof

US12129258B2 · kind B2 · utility

0Cited by
1References
7Claims
0Family size

Assignee

Inventors

Key dates

Filing dateApr 22, 2019
Grant dateOct 29, 2024
Priority date
Expiry dateFeb 8, 2042

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D515/16
  • WIPO fieldOrganic fine chemistry
  • WIPO sectorChemistry

Abstract

The present invention provides a compound as represented by formula (1) or a pharmaceutically acceptable salt, a solvate, an active metabolite, a polymorph, an isotope label, an isomer or a prodrug thereof. The present invention also provides a pharmaceutical composition containing the same and the use of the compound and the pharmaceutical composition in preparation of drugs for treating tyrosine kinase-mediated diseases. The compound and the pharmaceutical composition comprising same provided by the present disclosure have significant tyrosine kinase inhibitory activity, can overcome tumor drug resistance, and break through blood-brain barrier, also have excellent pharmacokinetic properties and excellent oral bioavailability, and can be administered in a small dosage, thereby reducing treatment costs and possible side effects to a patient. Thus, the application potential is very great.

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