公开(公告)号：US20210371430A1

公开(公告)日：2021-12-02

申请号：US17289642

申请日：2019-10-08

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

Inventor： Bing ZHOU ,  Wei TANG ,  Xiangbo YANG ,  Huimin LU ,  Mengying GAO ,  Yaxi YANG ,  Huijin FENG

IPC: C07D513/04 ,  A61P37/06 ,  C07D413/14 ,  C07D413/12 ,  C07D487/04 ,  C07D401/14 ,  C07D401/12 ,  C07D417/14 ,  C07D417/12

Abstract: The present invention relates to a heterocyclic amide inhibiting RIP1 kinase and the use thereof, and specifically, to a compound of formula I, its pharmaceutically acceptable salts, stereoisomers, enantiomers, diastereomers, atropisomers, optical isomers, racemates, polymorphs, solvates or isotopically labeled compounds, a pharmaceutical composition comprising the compound, and the pharmaceutical use thereof. The compound is particularly effective for treatment of diseases or disorders mediated by RIP1 kinase.

公开(公告)号：US11098071B2

公开(公告)日：2021-08-24

申请号：US16490837

申请日：2018-02-28

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

Inventor： Fajun Nan ,  Xin Xie ,  Linhai Chen ,  Qing Zhang ,  Yufeng Xiao ,  Hui Yang

IPC: C07F9/09 ,  C07F9/655 ,  C07F9/6553 ,  C07F9/6561

Abstract: The present invention relates to a GPR84 receptor antagonist and use thereof. The GPR84 receptor antagonist of the present invention has a structure as represented by formula (I), the definitions of R1, R2, R3, R4, L1, L2, L3, L4, L5, L6, Y, Z, and rings A, B, C, and D are as described in the description and claims. The GPR84 receptor antagonist of the present invention can competitively inhibit the activation of the receptor caused by an agonist of GPR84, and can be used in the preparation of a medicament for treating related diseases caused by high expression or high excitability of GPR84 receptor, the diseases including multiple sclerosis, inflammatory bowel disease, arthritis and the like.

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：US20210101891A1

公开(公告)日：2021-04-08

申请号：US17075206

申请日：2020-10-20

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  SUZHOU INSTITUTE OF DRUG INNOVATION, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENC

Inventor： Bing Zhou ,  Cheng Luo ,  Hualiang Jiang ,  Yaxi Yang ,  Lianghe Mei ,  Wenchao Lu ,  Senhao Xiao ,  Shijie Chen ,  Shili Wan ,  Gang Qiao ,  Rukang Zhang

IPC: C07D413/06 ,  C07D417/06 ,  C07D413/14 ,  C07D491/107 ,  C07D513/04 ,  C07D471/04 ,  C07D495/04 ,  C07D495/10

Abstract: Disclosed is a histone acetyltransferase (HAT) inhibitor. Provided are a compound represented by the general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereoisomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method therefor, a pharmaceutical composition comprising same and use thereof in the treatment of various HAT-related diseases or conditions.

公开(公告)号：US20210079019A1

公开(公告)日：2021-03-18

申请号：US16625391

申请日：2018-06-21

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

Inventor： Yushe YANG ,  Yinyong ZHANG ,  Chenghui SHI ,  Qian CHEN

IPC: C07D498/22 ,  A61P31/04

Abstract: Disclosed in the present invention are a thiazolidone spiro pyrimidine trione compound, a preparation method therefor and uses thereof, the compound having a structure represented by formula (I). In the formula, the definitions of the substituents are described in the specification and the claims. The thiazolidone spiro pyrimidine trione compound in the present invention has high in vivo and in vitro antibacterial activity, has better metabolic properties, and is obviously superior to existing compounds of the same kind.

公开(公告)号：US20210078972A1

公开(公告)日：2021-03-18

申请号：US17044322

申请日：2019-03-29

Applicant: HAIHE BIOPHARMA CO., LTD. ,  JINAN UNIVERSITY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Ke DING ,  Meiyu GENG ,  Shingpan CHAN ,  Jian DING ,  Li TAN ,  Jing AI ,  Zhang ZHANG ,  Xia PENG ,  Xiaomei REN ,  Yinchun JI ,  Zhengchao TU ,  Yang DAI ,  Xiaoyun LU

IPC: C07D401/12 ,  A61P35/00

Abstract: The present invention relates to quinoline or quinazoline compound represented by the formula (I), a pharmaceutically acceptable salt thereof, a stereoisomer thereof, a prodrug molecule thereof, or a deuterated compound thereof. The compound of the present invention is effective in inhibiting the action of AXL protein kinase and can inhibit proliferation, migration, and invasion of various tumor cells. Further, the quinoline or quinazoline compound of the present invention has excellent metabolic stability, high in vivo antitumor activity, low toxic side effects, and can be used for preparing a drug for preventing hyperproliferative diseases such as tumors in humans and other mammals.

公开(公告)号：US10829464B2

公开(公告)日：2020-11-10

申请号：US16461234

申请日：2017-11-17

Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Jian Li ,  Lefu Lan ,  Baoli Li ,  Feifei Chen ,  Shuaishuai Ni ,  Yifu Liu ,  Hanwen Wei ,  Fei Mao ,  Jin Zhu

IPC: C07D307/81 ,  A61P31/04 ,  A61P31/10 ,  C07D307/82 ,  C07D333/58 ,  C07D409/12

Abstract: Disclosed are benzoheterocyclic alkylamine compounds, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, and a preparation method thereof, and use of the same in the manufacture of an antibacterial drug as an inhibitor of staphyloxanthin synthesis in Staphylococcus aureus.

公开(公告)号：US10787422B2

公开(公告)日：2020-09-29

申请号：US16299636

申请日：2019-03-12

Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Inventor： Jianhua Shen ,  Yiping Wang ,  Xinde Chen ,  Wenwei Xu ,  Kai Wang

IPC: A61K31/513 ,  C07D239/54 ,  A61K31/541 ,  C07D401/04 ,  C07D403/04 ,  C07D239/48 ,  C07D409/04 ,  C07D239/52 ,  C07D239/545 ,  C07D239/56 ,  C07D401/12 ,  C07D403/06 ,  C07D413/04

Abstract: The present invention relates to pyrimidone compounds used as Lp-PLA2 inhibitors and pharmaceutical compositions thereof. The structure of the pyrimidone compounds is represented by general formula (I), wherein R1, R2, R3, X, Ar, Y and n are defined as in the specification and claims. The compounds of general formula (I) in the present invention, stereoisomers and pharmaceutically acceptable salts thereof can be used as Lp-PLA2 inhibitors for preventing, treating and/or ameliorating diseases associated with the activity of Lp-PLA2 enzyme.

公开(公告)号：US10766889B2

公开(公告)日：2020-09-08

申请号：US16329336

申请日：2017-08-24

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

Inventor： Fajun Nan ,  Jia Li ,  Jian Ding ,  Meiyu Geng ,  Yangming Zhang ,  Yi Chen ,  Yubo Zhou ,  Chaojun Gong ,  Mingbo Su ,  Anhui Gao

IPC: C07D277/56 ,  C07D277/60 ,  C07D417/04 ,  A61P35/02 ,  A61K31/427 ,  A61P35/00

Abstract: The invention describes an aryl-2,2′-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2′-tandem bisthiazole compound with the structure as shown in general formula I and the preparation method thereof and use thereof as a histone deacetylase inhibitor in the preparation of antitumor drugs.

公开(公告)号：US20200261459A1

公开(公告)日：2020-08-20

申请号：US16651510

申请日：2018-08-29

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  SUZHOU SUPLEAD LIFE SCIENCES CO., LTD.

Inventor： Bing ZHOU ,  Cheng LUO ,  Yaxi YANG ,  Yuanyuan ZHANG ,  Daohai DU ,  Hualiang JIANG ,  Gang QIAO ,  Xinjun WANG

IPC: A61K31/519 ,  C07D487/04

Abstract: The present invention provides a compound represented by formula I, pharmaceutically acceptable salts, enantiomers, diastereomers or racemates thereof, the preparation method thereof, the pharmaceutical composition comprising the same, and the use thereof in the preparation of a medicament for treating a disease or condition mediated by EED and/or PRC2. The compound of the present invention can be used treating PRC2-mediated diseases or conditions.