公开(公告)号：US20220002278A9

公开(公告)日：2022-01-06

申请号：US17075206

申请日：2020-10-20

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

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

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

摘要： 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：US20190031678A1

公开(公告)日：2019-01-31

申请号：US16087318

申请日：2017-03-22

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

发明人： Hong LIU ,  Jiang WANG ,  Jian LI ,  Jia LI ,  Jingya LI ,  Hualiang JIANG ,  Xiaomin LUO ,  Kaixian CHEN

IPC分类号： C07D495/04 ,  A61P3/10

摘要： The invention relates to a salt form of (R)-methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothiophene[3,2-d]pyrimidine-6-carboxylic acid and a preparation method for the salt form. Also disclosed is a pharmaceutical composition of the formula I compound salt form. The salt form of the invention provides powerful in vivo hypoglycemic activity and is expected to be a novel pharmaceutical active ingredient for treating or preventing diabetes mellitus type 2 and/or complications of diabetes mellitus type 2

公开(公告)号：US20240351966A1

公开(公告)日：2024-10-24

申请号：US18290268

申请日：2022-05-11

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

发明人： Fajun NAN ,  Jingya LI ,  Zheng ZHANG ,  Yanan DUAN ,  Yangming ZHANG ,  Dandan CHEN ,  Chengqiu DAI

IPC分类号： C07C39/19 ,  A61K31/05 ,  A61K31/09 ,  A61K31/136 ,  A61K31/145 ,  A61K31/167 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/44 ,  A61K31/505 ,  C07C43/215 ,  C07C43/23 ,  C07C215/76 ,  C07C233/88 ,  C07D213/69 ,  C07D213/74 ,  C07D239/10 ,  C07D307/36 ,  C07D333/06 ,  C07D333/34

CPC分类号： C07C39/19 ,  A61K31/05 ,  A61K31/09 ,  A61K31/136 ,  A61K31/145 ,  A61K31/167 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/44 ,  A61K31/505 ,  C07C43/215 ,  C07C43/23 ,  C07C215/76 ,  C07C233/88 ,  C07D213/69 ,  C07D213/74 ,  C07D239/10 ,  C07D307/36 ,  C07D333/06 ,  C07D333/34

摘要： Provided are a class of alkylphenol compounds and a preparation method therefor. Specifically provided are a new alkyl polyphenol compound as represented by chemical formula I, and a preparation method therefor and the use thereof in the treatment of metabolic syndrome.

公开(公告)号：US20240197900A1

公开(公告)日：2024-06-20

申请号：US18278302

申请日：2022-02-22

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

发明人： Wei HUANG ,  Feng TANG ,  Wei SHI ,  Shang JIAO ,  Siqi WANG

IPC分类号： A61K47/68 ,  A61P35/00 ,  C12N9/04 ,  C12N9/24 ,  C12P19/12

CPC分类号： A61K47/68031 ,  A61K47/68033 ,  A61K47/6883 ,  A61K47/6889 ,  A61P35/00 ,  C12N9/0006 ,  C12N9/2402 ,  C12P19/12 ,  C12Y101/03009 ,  C12Y302/01169

摘要： The present application relates to a disaccharide linker, a disaccharide-small molecule drug conjugate and a sugar chain fixed-point antibody-drug conjugate, a preparation method and the use thereof. The structure of the disaccharide linker is as shown in the following formula I. The present invention provides a new-type fixed-point and quantitative antibody-drug conjugate form, and the stability and cytotoxicity of the antibody-drug conjugate are improved.

公开(公告)号：US20230301947A1

公开(公告)日：2023-09-28

申请号：US18018290

申请日：2021-07-29

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  SHAOXING ZEROIN BIOMEDICINES CO., LTD.

发明人： Huaiyu YANG ,  Yang LI ,  Fei GUO ,  Hualiang JIANG ,  Qiansen ZHANG

IPC分类号： A61K31/18 ,  A61P25/24

CPC分类号： A61K31/18 ,  A61P25/24

摘要： Provided are a compound for preventing and treating psychiatric disorders and the use thereof. In particular, provided is the use of a compound of formula I or a pharmaceutically acceptable salt thereof in (i) the preparation of a pharmaceutical composition or a preparation for preventing and/or treating TREK-1 ion channel-related diseases, (ii) the preparation of a pharmaceutical composition or a preparation for preventing and/or treating psychiatric disorders and/or (iii) the preparation of a TREK-1 ion channel inhibitor.

公开(公告)号：US20230285389A1

公开(公告)日：2023-09-14

申请号：US17802898

申请日：2021-02-26

申请人： Shanghai Runshi Medical Technology Co., Ltd ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： Ao ZHANG ,  Meiyu GENG ,  Jing AI ,  Caixia WANG ,  Xia PENG ,  Yang ZHANG ,  Jian DING

IPC分类号： A61K31/496 ,  A61P35/00 ,  C07K16/28

CPC分类号： A61K31/496 ,  A61P35/00 ,  C07K16/2818 ,  C07K16/2827

摘要： Use of a compound of general formula (A) which is a CFS-1R kinase inhibitor or a pharmaceutically acceptable salt thereof in the preparation of medicaments for treating diseases related to CSF-1R kinase signal transduction pathway or medicaments for regulating immunization. In vivo and in vitro studies show that the compound can significantly inhibit CSF-1R kinase activity; significantly inhibits the proliferation of a CSF-1/CSF-1R-driven mouse myeloid leukemia cell line, inhibits the survival of macrophages induced by CSF-1 and reverses M2 polarization phenotype of macrophages, and has an effect superior to that of the marketed medicament Pexidartinib. In a TAM enriched tumor model (MC38 model), the compound significantly antagonizes the tumor immunosuppressive microenvironment and exhibits significant anti-tumor efficacy. The compound has inhibitory effects on tumors that are not sensitive to immune checkpoint drugs, and can enhance the efficacy of immune checkpoint drugs, and has good clinical application prospects.

公开(公告)号：US11730742B2

公开(公告)日：2023-08-22

申请号：US16978563

申请日：2019-03-08

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

发明人： Hong Liu ,  Jia Li ,  Jiang Wang ,  Yi Zang ,  Jian Li ,  Jingya Li ,  Dandan Sun ,  Hualiang Jiang ,  Kaixian Chen

IPC分类号： A61K31/5377 ,  A61K31/519 ,  A61P1/16

CPC分类号： A61K31/5377 ,  A61K31/519 ,  A61P1/16

摘要： Disclosed is use of a thieno[3,2-d]pyrimidin-4-one compound represented by general formula (I). Definition of each substituent is as stated in the description and claims, and the compound is used for preparing medicines for treating and/or preventing liver fibrosis and related diseases or preparing a DPP-4 inhibitor, or is used as a DPP-4 inhibitor.

公开(公告)号：US20230167129A1

公开(公告)日：2023-06-01

申请号：US18045149

申请日：2022-10-08

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 ,  C07D401/12 ,  C07D401/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D487/04

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

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：US20230138930A1

公开(公告)日：2023-05-04

申请号：US18050240

申请日：2022-10-27

申请人： FUDAN UNIVERSITY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  SHANGHAI MIRACOGEN INC.

发明人： Ke YU ,  Jingkang SHEN ,  Tao MENG ,  Lanping MA ,  Xuesai ZHANG ,  Qingrou LI ,  Qing LIN

IPC分类号： A61K47/68 ,  C07K16/36 ,  A61P35/00 ,  A61K31/537 ,  A61K47/54 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/5365

摘要： A tissue factor (TF)-targeted antibody-drug conjugate (ADC) and a method for preparing the ADC. The ADC is capable of binding to TF antigen with high specificity, and has high affinity, low immunogenicity, high cytotoxicity, and significant anti-tumor activity.

公开(公告)号：US11534495B2

公开(公告)日：2022-12-27

申请号：US16326886

申请日：2017-06-09

申请人： FUDAN UNIVERSITY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  SHANGHAI MIRACOGEN INC.

发明人： Ke Yu ,  Jingkang Shen ,  Tao Meng ,  Lanping Ma ,  Xuesai Zhang ,  Qingrou Li ,  Qing Lin

IPC分类号： C07K16/36 ,  A61K47/68 ,  A61P35/00 ,  A61K31/537 ,  A61K47/54 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/5365

摘要： A tissue factor (TF)-targeted antibody-drug conjugate (ADC) and a method for preparing the ADC. The ADC is capable of binding to TF antigen with high specificity, and has high affinity, low immunogenicity, high cytotoxicity, and significant anti-tumor activity.