公开(公告)号：US20240150300A1

公开(公告)日：2024-05-09

申请号：US18278063

申请日：2022-02-18

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

Inventor： Youhong HU ,  Meiyu GENG ,  Daqiang LI ,  Aijun SHEN ,  Zhuo ZHANG ,  Yalei LI ,  Huajie YANG ,  Hongchun LIU ,  Hanyue ZHONG ,  Jian DING

IPC: C07D237/14 ,  A61P35/00 ,  A61P35/02 ,  C07C67/00 ,  C07C67/10 ,  C07D401/04 ,  C07D403/04

CPC classification number: C07D237/14 ,  A61P35/00 ,  A61P35/02 ,  C07C67/00 ,  C07C67/10 ,  C07D401/04 ,  C07D403/04

Abstract: The present invention relates to an S-configuration-containing amino benzamide pyridazinone compound, a preparation method therefor, and a pharmaceutical composition and application thereof. Specifically, the present invention relates to a compound represented by the following general formula I or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition and application thereof. The S-configuration compound of the present application has very strong binding activity on class I histone deacetylase (HDAC1), and shows inhibitory activity on in-vitro proliferation of various tumor cells.

公开(公告)号：US20240351986A1

公开(公告)日：2024-10-24

申请号：US18683623

申请日：2022-07-26

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

Inventor： Youhong HU ,  Yi CHEN ,  Zhicheng XIE ,  Jian DING ,  Xin LI ,  Yanfen FANG ,  Qianqian SHEN

IPC: C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

CPC classification number: C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

Abstract: The present invention relates to a urea compound containing 2-heteroaromatic ring substitution represented by formula (I), its enantiomers, diastereomers, racemates or mixtures thereof, or pharmaceutically acceptable salts thereof, solvate, metabolite or prodrug. The compound of formula (I) of the present invention has inhibitory activity against CDK9, and representative compounds have significant anti-tumor activity against CDK9 high-expressing tumor cells. Representative compounds have plasma stability and low clearance.

公开(公告)号：US20130281426A1

公开(公告)日：2013-10-24

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 ,  C07D413/10 ,  C07D295/155 ,  C07D401/10 ,  C07D403/10

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。

公开(公告)号：US20200055838A1

公开(公告)日：2020-02-20

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.