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：US11873292B2

公开(公告)日：2024-01-16

申请号：US16306751

申请日：2017-06-02

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

发明人： Hong Liu ,  Jia Li ,  Wei Zhu ,  Yubo Zhou ,  Jiang Wang ,  Mingbo Su ,  Shuni Wang ,  Wei Xu ,  Chunpu Li ,  Weijuan Kan ,  Hualiang Jiang ,  Kaixian Chen

IPC分类号： C07D403/12 ,  C07D215/58 ,  C07D209/04 ,  C07D215/00 ,  C07D487/04 ,  C07D209/08 ,  C07D401/12 ,  C07D405/12 ,  A61P35/00

CPC分类号： C07D403/12 ,  A61P35/00 ,  C07D209/04 ,  C07D209/08 ,  C07D215/00 ,  C07D215/58 ,  C07D401/12 ,  C07D405/12 ,  C07D487/04 ,  Y02P20/55

摘要： The present invention relates to the fields of medicinal chemistry and pharmacotherapy, and specifically relates to the chemical compound of formula (I), and its racemate, R-isomer, S-isomer, pharmaceutically acceptable salt, and mixtures thereof, as well as its method for preparation, a pharmaceutical composition containing said chemical compound, and use as a lysine-specific demethylase 1 (LSD 1) inhibitor. The cyclopropylamine chemical compound to which the present invention relates may be used in the treatment of cancer.

公开(公告)号：US11384073B2

公开(公告)日：2022-07-12

申请号：US17127350

申请日：2020-12-18

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

发明人： Jingshan Shen ,  Yang He ,  Zhen Wang ,  Jianfeng Li ,  Yongjian Liu ,  Jin Suo ,  Guanghui Tian ,  Weiming Chen ,  Feipu Yang ,  Yu Wang ,  Xiangrui Jiang ,  Rongxia Zhang ,  Hualiang Jiang

IPC分类号： C07D409/12

摘要： The present disclosure relates to a maleate salt of a benzothiophene compound, a crystalline form thereof, and a use thereof. Specifically, the present disclosure relates to a compound represented by formula (I-A), a crystalline form A thereof, a preparation method of a pharmaceutical composition including the same, and a use of the pharmaceutical composition in the preparation of drugs for preventing or treating diseases of the central nervous system. The compound represented by formula (I-A) and the crystalline form A thereof in the present disclosure have excellent physical and chemical properties, high oral bioavailability, excellent drugability, and are well-suited for pharmaceutical preparation, application, and preservation.

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：US20210101891A1

公开(公告)日：2021-04-08

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 SCIENC

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：US20140323466A1

公开(公告)日：2014-10-30

申请号：US14361920

申请日：2012-10-23

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

发明人： Hong Liu ,  Jia Li ,  Jian Li ,  Jingya Li ,  Jiang Wang ,  Mingbo Su ,  Jie Lian ,  Hualiang Jiang ,  Kaixian Chen

IPC分类号： C07D495/04

CPC分类号： C07D495/04

摘要： Disclosed are new thienyl[3,2-d]pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.

摘要翻译： 公开了通式（I）所示的新的噻吩并[3,2-d]嘧啶-4-酮化合物，其制备方法，药物组合物及其药理用途。 该化合物是强DPPIV（二肽肽酶IV）抑制剂，可以通过良好地抑制DPPIV来间接增加体内GLP-1的含量并在体内诱导一系列生理作用来治疗II型糖尿病。 因此，这些化合物可被开发为用于治疗糖尿病的新的有希望的药物。

公开(公告)号：US11919923B2

公开(公告)日：2024-03-05

申请号：US17996430

申请日：2021-04-16

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  WUHAN INSTITUTE OF VIROLOGY, CHINESE ACADEMY OF SCIENCE ,  XINJIANG TECHNICAL INSTITUTE OF PHYSICS AND CHEMISTRY, CHINESE ACADEMY OF SCIENCES ,  VIGONVITA LIFE SCIENCES CO., LTD.

发明人： Yuanchao Xie ,  Gengfu Xiao ,  Yang He ,  Leike Zhang ,  Haji Akber Aisa ,  Hualiang Jiang ,  Jingshan Shen

IPC分类号： C07H7/06 ,  A61P31/14 ,  A61P31/16

CPC分类号： C07H7/06 ,  A61P31/14 ,  A61P31/16 ,  C07B2200/05

摘要： The present invention relates to an antiviral application of nucleoside analogs. Specifically, the present invention relates to uses of nucleoside analogs and a pharmaceutical composition thereof as: (a) inhibitors for inhibiting the replication of coronaviruses, influenza viruses, respiratory syncytial viruses, flaviviridae viruses, filoviridae viruses and/or porcine epidemic diarrhea virus (PEDV); and/or (b) medicines for treating and/or preventing and mitigating diseases caused by coronavirus, influenza virus, respiratory syncytial virus, flaviviridae virus, filoviridae virus and/or porcine epidemic diarrhea virus (PEDV) infections. The nucleoside analogs according to the invention may treat and/or prevent and mitigate respiratory infection, pneumonia (COVID-19) and other related diseases caused by 2019 novel coronavirus infection.

公开(公告)号：US11731965B2

公开(公告)日：2023-08-22

申请号：US16639394

申请日：2018-08-14

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

发明人： Yang He ,  Xiangrui Jiang ,  Jianfeng Li ,  Yu Wang ,  Zhen Wang ,  Weiming Chen ,  Fuqiang Zhu ,  Chunhui Wu ,  Rongxia Zhang ,  Jingshan Shen ,  Hualiang Jiang

IPC分类号： C07D455/03 ,  C07D498/14 ,  A61P25/20

CPC分类号： C07D455/03 ,  A61P25/20 ,  C07D498/14

摘要： The present invention provides a tetrahydroprotoberberine compound represented by the formula (I), enantiomers, diastereomers, racemates and mixtures thereof, and pharmaceutically acceptable salts, crystalline hydrates and solvates thereof. The invention also provides a method for preparing the compound and the use thereof in the preparation of a medicament for preventing and/or treating central nervous system diseases.

公开(公告)号：US20220112177A1

公开(公告)日：2022-04-14

申请号：US17267375

申请日：2019-08-09

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

发明人： Hong Liu ,  Shibo Jiang ,  Wenhao Dai ,  Lu Lu ,  Jingjing Peng ,  Shuai Xia ,  Jiang Wang ,  Jian Li ,  Hualiang Jiang ,  Kaixian Chen

IPC分类号： C07D403/12 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D209/20 ,  C07D241/44 ,  C07D413/12 ,  A61P31/12 ,  C07D471/04

摘要： A ketoamide compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically, the ketoamide compound shown in formula (A), a racemate, an enantiomer, or a diastereoisomer thereof, or any mixture of same, or a pharmaceutically active metabolite thereof, or a pharmaceutically acceptable salt, solvate, or prodrug thereof. The ketoamide compound can effectively inhibit coronavirus or Ebola virus, and thereby implement the prevention or treatment of diseases related to coronavirus or diseases related to Ebola virus.

公开(公告)号：US20190194185A1

公开(公告)日：2019-06-27

申请号：US16089713

申请日：2017-03-29

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

发明人： Hong Liu ,  Yiping Wang ,  Fei Zhao ,  Jing Zhao ,  Jiang Wang ,  Cong Xi ,  Chenglin Wu ,  Hao Shen ,  Xu Han ,  Hualiang Jiang ,  Kaixian Chen

IPC分类号： C07D459/00 ,  C07D495/22 ,  A61P3/06

CPC分类号： C07D459/00 ,  A61K31/4745 ,  A61P3/06 ,  C07D471/14 ,  C07D491/22 ,  C07D495/22

摘要： The present invention relates to phenyl [a]indole[2,3-g]quinolizine compounds represented by formula (I), a preparation method therefor, a pharmaceutical composition, and applications thereof. Specific applications are applications in the preparation of drugs for treating diseases related to a proprotein convertase subtilisin Kexin-9 (PCSK9), comprising the applications in the preparation of drugs for treating hyperlipemia, hypercholesterolemia, hypertriglyceridemia, fatty liver deformation, atherosclerosis, obesity and other metabolic diseases.