公开(公告)号：US20230010368A1

公开(公告)日：2023-01-12

申请号：US17780449

申请日：2020-11-24

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  JIANGSU KANION PHARMACEUTICAL CO., LTD.

发明人： Hong LIU ,  Yu ZHOU ,  Haiyan ZHANG ,  Yan FU ,  Jian LI ,  Hualiang JIANG ,  Xican TANG ,  Kaixian CHEN

IPC分类号： C07D211/38

摘要： The present invention provides a crystalline form of an acetylcholinesterase inhibitor, a preparation method therefor and application thereof. Specifically, the crystalline form is crystalline form A, crystalline form B and crystalline form C of 2-((1-(2-fluorobenzyl)-4-fluoropiperidin-4-yl) methylene)-5, 6-dimethoxy-2, 3-dihydro-1-indanone. The crystalline form of the present invention does not contain water and solvent, has high stability and low hygroscopicity, is easy to process, and is very suitable for preparing drugs for preventing and/or treating neurodegenerative diseases.

公开(公告)号：US11465984B2

公开(公告)日：2022-10-11

申请号：US16652148

申请日：2018-09-29

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

发明人： Lei Li ,  Meiyu Geng ,  Ying Huang ,  Jian Ding ,  Qiong Zhang ,  Min Huang ,  Shuai Tang ,  Ning Shen ,  Yi Chen

IPC分类号： C07D401/14 ,  C07D403/14 ,  C07D405/14

摘要： The invention relates to a compound of formula (I): wherein variables are as defined in the specification. The compound is an inhibitor of an ERK kinase, e.g. ERK1 and/or ERK2 kinase. The invention also relates to the use of the compound and a method for preparing the compound, and a pharmaceutical composition containing the compound.

公开(公告)号：US11464795B2

公开(公告)日：2022-10-11

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：US11406653B2

公开(公告)日：2022-08-09

申请号：US17256950

申请日：2019-06-28

申请人： GREEN VALLEY (SHANGHAI) PHARMACEUTICALS CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Meiyu Geng ,  Xianliang Xin ,  Zhenqing Zhang ,  Jian Ding

IPC分类号： A61P25/06 ,  A61K31/715 ,  A61K31/7032 ,  A61K31/702 ,  A61P25/04 ,  A61K31/7004 ,  A61K31/7016

摘要： The present invention relates to the use of mannuronic diacid oligosaccharide composition in the treatment of pain.

公开(公告)号：US20220213083A1

公开(公告)日：2022-07-07

申请号：US17603823

申请日：2020-04-20

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

发明人： Huaqiang XU ,  Jia LI ,  Jingjing SHI ,  Yi ZANG ,  Dandan SUN ,  Mingliang LIU ,  Rongrong XIE ,  Erli YOU ,  Lixin GAO ,  Qian TAN

IPC分类号： C07D413/14 ,  C07D487/08 ,  A61P1/16

摘要： An FXR small molecule agonist and a preparation method therefor and a use thereof, having a structure as shown in formula (I). The compound represented by formula (I) has FXR agonistic activity and is capable of preparing drugs for treatment of FXR-related diseases.

公开(公告)号：US20220089561A1

公开(公告)日：2022-03-24

申请号：US17420389

申请日：2019-12-31

申请人： SHANGHAI HAIHE PHARMACEUTICAL CO., LTD. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： Ao ZHANG ,  Meiyu GENG ,  Chunyong DING ,  Zuoquan XIE ,  Jian DING ,  Yan ZHANG ,  Ancheng SHEN ,  Xiyuan WANG

IPC分类号： C07D333/64 ,  C07D409/12

摘要： A fluorine-containing substituted benzothiophene compound and a pharmaceutical composition and an application thereof are described. The compound has the structure as shown in formula (I), in which the definitions of each group and substituent are as described in the description. A preparation method of the compound and an anti-tumor application thereof are also described.

公开(公告)号：US11191761B2

公开(公告)日：2021-12-07

申请号：US15574557

申请日：2016-05-13

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  Shanghai Acebright Pharmaceuticals Co., Ltd.

发明人： Shiyan Guo ,  Yong Gan ,  Ao Zhang ,  Zehong Miao ,  Li Gao ,  Jian Ding

IPC分类号： A61K31/502 ,  A61K47/40 ,  A61K47/38 ,  A61K47/34 ,  A61K47/32 ,  A61K9/48 ,  A61K9/28 ,  A61P35/00 ,  A61K47/10 ,  A61K9/10 ,  A61K9/20 ,  A61K9/08 ,  A61K9/14

摘要： Disclosed is an SOMCL-9112 solid dispersion. The SOMCL-9112 solid dispersion is characterized by being prepared from the following raw materials in percentage by weight: 5 percent to 60 percent of SOMCL-9112, 5 percent to 90 percent of pharmaceutically acceptable matrix polymer, 0 percent to 20 percent of surfactant, 0 percent to 20 percent of flow aid and 0 percent to 20 percent of plasticizer. Also disclosed are a preparation method of the SOMCL-9112 solid dispersion, a solid medicinal preparation containing the solid dispersion and application of the solid dispersion for preparing a medicine for treating cancer.

公开(公告)号：US20210371430A1

公开(公告)日：2021-12-02

申请号：US17289642

申请日：2019-10-08

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

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

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

摘要： 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

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

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

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

摘要： 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

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

发明人： Youhong Hu ,  Jianping Zuo ,  Dong Lu ,  Li Yang ,  Limin Zeng ,  Feifei Liu ,  Yunzhe Zhang ,  Wuhong Chen ,  Xiankun Tong

IPC分类号： C07D401/04 ,  A61P31/20 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14

摘要： 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.