The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Apr. 27, 2021
Filed:
Feb. 12, 2018
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, CN;
Youhong Hu, Shanghai, CN;
Meiyu Geng, Shanghai, CN;
Wenming Ren, Shanghai, CN;
Jian Ding, Shanghai, CN;
Xiaocong Guan, Shanghai, CN;
Jing Ai, Shanghai, CN;
Lang Wang, Shanghai, CN;
Xia Peng, Shanghai, CN;
Yang Liu, Shanghai, CN;
Yang Dai, Shanghai, CN;
Limin Zeng, Shanghai, CN;
Abstract
An o-aminoheteroaryl alkynyl-containing compound has a structure represented by formula (I), and the compound of formula (I) has advantages of a high FGFR and RET double target inhibitory activity and a relatively low KDR activity, and the compound of formula (I) exhibits a strong inhibitory activity in a human lung cancer cell line NCI-H1581 and a gastric cancer cell line SNU16 as well as an RET-dependent sensitive cell line BaF3-CCDC6-Ret and a mutant thereof. Pharmacokinetic data shows that the o-aminoheteroaryl alkynyl-containing compound has druggability, and exhibits significant relevant inhibition of the growth of related tumors in a long-term animal model of drug efficacy and results in favorable animal condition at effective doses.