Nitrogen-containing polycyclic fused ring compound, pharmaceutical composition thereof, preparation method therefor and use thereof

US12338253B2 · kind B2 · utility

Assignee

• Applied Pharmaceutical Science, Inc. · CN

Inventors

• Jun Zhong · Beijing, CN
• Yongbo Liu · Shanghai, CN
• Libin Liu · Beijing, CN
• Xiaohu Chen · Mountain View, US
• Hao Wang · Beijing, CN
• Ying Lu · Beijing, CN

Key dates

• Filing date: Aug 5, 2020
• Grant date: Jun 24, 2025
• Expiry date: Oct 27, 2042

Classification

• Technology area (CPC Y): Emerging Cross-Sectional Technologies
• CPC primary: Y02P20/55
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

A nitrogen-containing polycyclic fused ring compound of formula I, a pharmaceutical composition thereof, a preparation method therefor and use thereof are related to the field of medicinal chemistry. The compound can be used as a selective and effective RET inhibitor. It has strong inhibitory effect on the RET gatekeeper residue mutant RET V804M, RET solvent-front residue mutant RET G810R and other clinically relevant RET mutants, as well as RET wt. The compound can also inhibit the growth of TT cell line derived from thyroid cancer and Ba/F3 cells transformed with various RET mutants, and induce the death of TT cells.