Chinese Academy of Sciences

Limin Zeng

Youhong Hu

Yang Liu

Jian Ding

Li Yang

Meiyu Geng

Jianping Zuo

Jing Ai

Xia Peng

Feifei Liu

Xiankun Tong

Yang Dai

Xiaocong Guan

Lang Wang

Wenming Ren

Wuhong Chen

Yunzhe Zhang

Provided are a phthalazinone compound, method for preparation thereof, pharmaceutical composition thereof, and a use thereof; the structure of said phthalazinone compound is as represented by formula I; the compound of said formula I is targeted to a viral nucleocapsid; it can inhibit the replication of a virus by means of interference of the viral nucleocapsid, has a potent activity for inhibiting HBV DNA replication and a good liver targeting, can stably exist and enrich in the liver, and is a new and effective anti-HBV inhibitor. 

Phthalazinone compound, method for preparation thereof, pharmaceutical composition thereof, and use thereof

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. 

O-aminoheteroaryl alkynyl-containing compound, preparation method therefor, and use thereof

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Shanghai, China

Limin Zeng