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公开(公告)号：US11040952B2
公开(公告)日：2021-06-22
申请号：US16786710
申请日：2020-02-10
Inventor： Youhong Hu , Jianping Zuo , Dong Lu , Li Yang , Limin Zeng , Feifei Liu , Yunzhe Zhang , Wuhong Chen , Xiankun Tong
IPC: C07D401/04 , A61P31/20 , C07D401/14 , C07D405/14 , C07D413/14
Abstract: 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.
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2.发明授权公开(公告)号：US10988456B2
公开(公告)日：2021-04-27
申请号：US16487385
申请日：2018-02-12
Inventor： Youhong Hu , Meiyu Geng , Wenming Ren , Jian Ding , Xiaocong Guan , Jing Ai , Lang Wang , Xia Peng , Yang Liu , Yang Dai , Limin Zeng
IPC: C07D401/12 , C07D405/14 , C07D403/12 , A61P35/00 , B01J31/24 , B01J27/122 , B01J31/30
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.
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