公开(公告)号：US10988456B2

公开(公告)日：2021-04-27

申请号：US16487385

申请日：2018-02-12

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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.

公开(公告)号：US11040952B2

公开(公告)日：2021-06-22

申请号：US16786710

申请日：2020-02-10

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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.

公开(公告)号：US09212146B2

公开(公告)日：2015-12-15

申请号：US13921009

申请日：2013-06-18

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Youhong Hu ,  Liguang Lou ,  Shijun Lin ,  Hongbing Zhao ,  Zhende Liu ,  Yongping Xu ,  Bo Chao

IPC: C07D237/14 ,  C07D401/10 ,  C07D403/10 ,  C07D295/155 ,  C07D413/10 ,  A61K31/501 ,  A61K31/50 ,  A61K31/5377

CPC classification number: C07D237/14 ,  A61K31/50 ,  A61K31/501 ,  A61K31/5377 ,  C07D295/155 ,  C07D401/10 ,  C07D403/10 ,  C07D413/10

Abstract: The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.

Abstract translation: 本发明涉及一类式I的哒嗪酮，其包含作为母核的6- [3-（三氟甲基）苯基]哒嗪-3（2H） - 酮，其制备方法及其在制备药物中的用途 肿瘤，特别是肝癌。