公开(公告)号：US20210078972A1

公开(公告)日：2021-03-18

申请号：US17044322

申请日：2019-03-29

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

发明人： 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分类号： C07D401/12 ,  A61P35/00

摘要： 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

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

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

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

摘要： 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

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： Jianhua Shen ,  Yiping Wang ,  Xinde Chen ,  Wenwei Xu ,  Kai Wang

IPC分类号： 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

摘要： 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

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

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

摘要： 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

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

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

IPC分类号： A61K31/519 ,  C07D487/04

摘要： 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.

公开(公告)号：US10710996B2

公开(公告)日：2020-07-14

申请号：US15575903

申请日：2016-05-23

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Yaqiu Long ,  Meiyu Geng ,  Zhongliang Xu ,  Jing Ai

IPC分类号： C07D471/04 ,  A61K31/501 ,  A61K31/4985 ,  A61K31/4375 ,  A61K31/496 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/5377 ,  A61P35/00

摘要： The present invention discloses a pyrido-azacyclic compound represented by formula I, an isomer thereof, a pharmaceutically acceptable salt or a pharmaceutically acceptable solvate thereof, a preparation process thereof and a composition comprising the compound, and a use thereof as a multi-target protein kinase inhibitor in the preparation of a medicament for the treatment of diseases that are associated with protein kinase, especially c-Met, such as cancer and the like. The compound represented by formula I has potent inhibitory activity on tumor cells with overexpression of c-Met kinase, can effectively target c-Met-mediated signaling pathway, and can be used in the treatment of diseases such as cancer and the like that is caused by the overexpression of c-Met kinase.

公开(公告)号：US20200163983A1

公开(公告)日：2020-05-28

申请号：US16630309

申请日：2018-07-12

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

发明人： Honglin LI ,  Weilie XIAO ,  Lili ZHU ,  Lina QUAN ,  Qiao LI ,  Yanyan DIAO ,  Zhenjiang ZHAO ,  Hualiang JIANG

IPC分类号： A61K31/704 ,  A61P35/00 ,  A61K31/56

摘要： Provided are use of a saponin compound of formula (I) or (II), or a pharmaceutically acceptable salt, prodrug or solvate thereof, in the manufacture of a medicament targeting PD-1. The medicament targeting PD-1 is one which treats a disease by inhibiting PD-1 from binding to a ligand thereof. The disease may be a tumor, an infection caused by a bacterium, a virus or a fungus, or an inflammatory disease.

公开(公告)号：US20200079727A1

公开(公告)日：2020-03-12

申请号：US16490186

申请日：2018-03-01

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Caiguang YANG ,  Yue HUANG ,  Ze DONG ,  Tao ZHANG ,  Hongjiao XU

IPC分类号： C07C229/58 ,  A61P35/00 ,  C07D261/08 ,  A61K31/42 ,  A61K31/196 ,  C07C227/16 ,  C07D231/12 ,  A61K31/415 ,  C07D213/38 ,  A61K31/4418 ,  C07D333/20 ,  A61K31/381 ,  C07D239/26 ,  A61K31/505 ,  C07D333/40 ,  C07D239/42 ,  C07D211/70 ,  C07D209/14 ,  A61K31/404 ,  C07D233/64 ,  A61K31/4164 ,  C07D257/04 ,  A61K31/41 ,  C07D407/12 ,  A61K31/422 ,  A61K31/4245 ,  C07D401/12 ,  A61K31/4439 ,  A61K31/5355

摘要： The invention provides 2-(substituted phenylhetero) aromatic formate FTO inhibitors, a preparation method thereof, and applications thereof. Specifically, disclosed in the present invention are a 2-(substituted phenylhetero) aromatic formate compound represented by the following formula (I), and a pharmaceutically acceptable salt, a hydrate or a solvate thereof, which can be used as an FTO targeting inhibitor for treating diseases associated with FTO targets, including obesity, metabolic syndrome (MS), type 2 diabetes (T2D), Alzheimer's diseases, and cancers such as breast cancers, small-cell lung cancers, human bone marrow rhabdomyosarcoma, pancreatic cancer, malignant glioblastoma and the like.

公开(公告)号：US20190315703A1

公开(公告)日：2019-10-17

申请号：US16461234

申请日：2017-11-17

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

发明人： Jian LI ,  Lefu LAN ,  Baoli LI ,  Feifei CHEN ,  Shuaishuai NI ,  Yifu LIU ,  Hanwen WEI ,  Fei MAO ,  Jin ZHU

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

摘要： 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：US20190292183A1

公开(公告)日：2019-09-26

申请号：US16463868

申请日：2017-11-24

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Ao Zhang ,  Jian Ding ,  Hua Xie ,  Zilan Song ,  Yu Xue ,  Linjiang Tong ,  Meiyu Geng

IPC分类号： C07D471/14 ,  C07D487/14 ,  A61P35/00

摘要： The present disclosure relates to a Pyrimido[5,4-b]indolizine or pyrimido[5,4-b]pyrrolizine compound, preparation method thereof and use thereof. The compounds of the present invention have good inhibitory activities against BTK at the molecular and cellular levels. Importantly, the compounds of the present invention have low activity against Ramos cells of normal human B lymphoma cells, and have high activity against BTK-sensitive human diffuse large B lymphoma TMD8 cells, indicating that these type of compounds with novel structural are highly selective, off-target phenomenon and corresponding side effects are low. Thus it is a selective inhibitor of BTK with development potential.