Patents Assigned to Shanghai Institute of Materia Medica Chinese Academy of Sciences
  • One class of pyrazolone compounds and use thereof
    Patent number: 10196389
    Abstract: Provided are a class of pyrazolone compounds and a use thereof. In particular, a compound represented by formula I is provided, wherein the definition of each variable group is as described in the description. The compounds of formula (I) have a direct AMPK-activating activity and can significantly promote the phosphorylation of AMPK and ACC of L6 myocytes and HepG2 cells in a dose-dependent manner.
    Type: Grant
    Filed: July 14, 2015
    Date of Patent: February 5, 2019
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Fajun Nan, Jia Li, Jingya Li, Mei Zhang, Dakai Chen, Lina Zhang, Runtao Zhang, Zhifu Xie
  • SALT FORM OF DPPIV INHIBITOR AND PREPARATION METHOD THEREOF
    Publication number: 20190031678
    Abstract: 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.
    Type: Application
    Filed: March 22, 2017
    Publication date: January 31, 2019
    Applicants: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong LIU, Jiang WANG, Jian LI, Jia LI, Jingya LI, Hualiang JIANG, Xiaomin LUO, Kaixian CHEN
  • Heterocyclic compounds, process for preparation of the same and use thereof
    Patent number: 10174011
    Abstract: The present invention provides a heterocyclic compound represented by the formula (I), its stereoisomers, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and their use in preparing a medicament for the prevention and/or treatment of central nervous system disease.
    Type: Grant
    Filed: March 9, 2015
    Date of Patent: January 8, 2019
    Assignees: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, SUZHOU VIGONVITA LIFE SCIENCES CO., LTD., TOPHARMAN SHANDONG CO., LTD.
    Inventors: Hualiang Jiang, Zhen Wang, Jianfeng Li, Rongxia Zhang, Yang He, Yongjian Liu, Minghao Bi, Zheng Liu, Guanghui Tian, Weiming Chen, Feipu Yang, Chunhui Wu, Yu Wang, Xiangrui Jiang, Jingjing Yin, Guan Wang, Jingshan Shen
  • 1-(3-aminopropyl) substituted cyclic amine compounds, preparation method therefor, and pharmaceutical compositions and uses thereof
    Patent number: 10167299
    Abstract: Provided are 1-(3-aminopropyl) substituted cyclic amine compounds as represented by frmula (I), pharmaceutically acceptable salts, enantiomers, diastereoisomers, racemates and mixtures thereof, and a method of synthesizing said 1-(3-aminopropyl) substituted cyclic amine compounds by using aromatic heterocyclic formaldehyde as raw material. Said compounds can be used as CCR 5 antagonist for the treatment of HIV infection.
    Type: Grant
    Filed: December 29, 2014
    Date of Patent: January 1, 2019
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Beili Wu, Yongtang Zheng, Xin Xie, Hualiang Jiang, Panfeng Peng, Ronghua Luo, Jing Li, Jian Li, Ya Zhu, Ying Chen, Haonan Zhang, Liumeng Yang, Yu Zhou, Kaixian Chen
  • Methods for preparing brexpiprazole, key intermediates thereof and salts thereof
    Patent number: 10100044
    Abstract: The present invention relates to the methods for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, specifically, the present invention relates to a new method for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, and the key intermediates, and salts thereof provided during the preparation. The preparation method has a mild reaction condition, stable intermediate, easy operation, and uses cheap and easy-to-get reagents, thus it saves the synthesis cost, shortens the production cycle, improves the yield and product quality, and is suitable for mass production.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: October 16, 2018
    Assignees: Suzhou Vigonvita Life Sciences Co., Ltd., Topharman Shanghai Co., Ltd., Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Zheng Liu, Chunhui Wu, Yongjian Liu, Rongxia Zhang, Yang He, Guanghui Tian, Jingshan Shen
  • Amino sulfonyl-based compounds, the preparation method therefor and use thereof
    Patent number: 10093679
    Abstract: Disclosed are aminosulfonyl-based compounds represented by the general formula I or tautomers, enantiomers, racemates or pharmaceutically acceptable salts thereof, a method for preparing the same, pharmaceutical compositions and uses thereof. The compounds can be used to treat epilepsy, convulsions, obesity and the like.
    Type: Grant
    Filed: September 11, 2015
    Date of Patent: October 9, 2018
    Assignees: SUZHOU VIGONVITA LIFE SCIENCES CO., LTD, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, TOPHARMAN SHANGHAI CO., LTD
    Inventors: Jingshan Shen, Zheng Liu, Zhen Wang, Guanghui Tian, Jianfeng Li, Xiaojun Yang
  • Substituted triazolopiperazine PARP inhibitor, preparation method therefor and use thereof
    Publication number: 20180265516
    Abstract: The present invention relates to a class of substituted triazolopiperazine compounds, tautomers, enantiomers, diastereomers, racemates, metabolites, metabolic precursors, and pharmaceutically acceptable salts, esters, prodrugs or hydrate thereof, a preparation methods therefor, intermediates and a use thereof in the preparation of drugs for prevention and treatment of diseases associated with PARP including various ischemic diseases, neurodegenerative diseases and cancers.
    Type: Application
    Filed: May 23, 2018
    Publication date: September 20, 2018
    Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Ao Zhang, Zehong Miao, Pingyuan Wang, Shanshan Song, Zilan Song, Xiajuan Huan, Zhoulong Fan, Jian Ding
  • SUBSTITUTED QUINOLONE DERIVATIVES, OR PHARMACEUTICALLY ACCEPTABLE SALTS OR STEREOISOMERS THEREOF, AND PHARMACEUTICAL COMPOSITIONS AND USE THEREOF
    Publication number: 20180265496
    Abstract: Provided are a substituted quinolone derivative as shown by formula (I), or a pharmaceutically acceptable salt and a prodrug molecule thereof, and a pharmaceutical composition thereof, as well as the use of same in preparing drugs for the prevention and treatment of a tumor. The quinolone derivative, salt, prodrug molecule, and pharmaceutical composition thereof can be used as a protein kinase inhibitor, which is effective in inhibiting the activity of AXL protein kinase, and is capable of inhibiting the proliferation, migration and invasion of various tumor cells; and can be used in the preparation of anti-tumor drugs, especially drugs for treating hyperproliferative diseases such as a tumor in human beings and other mammals.
    Type: Application
    Filed: August 18, 2016
    Publication date: September 20, 2018
    Applicants: JINAN UNIVERSITY, SHANGHAI INSTITUTE OF MATERIA MEDICA,CHINESE ACADEMY OF SCIENCES
    Inventors: Ke DING, Meiyu GENG, Li TAN, Jian DING, Zhang ZHANG, Jing AI, Xiaomei REN, Donglin GAO, Zhengchao TU, Xiaoyun LU, Dongmei ZHANG
  • KCNQ potassium channel agonists, method of preparation and method of use thereof
    Patent number: 10077245
    Abstract: The present invention provides a compound represented by general formula I or a pharmaceutical acceptable salt thereof, the preparation method therefor and the use thereof in preparing a medicine for treating a neurological disease, such as epilepsy, convulsion, neuropathic pain, acute ischemic stroke, and a neurodegenerative disease. The compound according to present invention has a better absorption in brain tissue when compared with RTG. In addition, the compound provided by present invention has not only a greatly enhanced efficacy, but also a neurotoxicity greatly lower than that of RTG, and thus possesses a wider safety window.
    Type: Grant
    Filed: April 22, 2015
    Date of Patent: September 18, 2018
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Fajun Nan, Min Li, Zhaobing Gao, Yangming Zhang, Haining Hu, Haiyan Xu, Huanan Liu, Xiaoping Pi
  • 2-aminopyrimidine compound and pharmaceutical composition and use thereof
    Patent number: 10059694
    Abstract: Disclosed are a 2-aminopyrimidine compound and pharmaceutical composition and use thereof. The structure of the 2-aminopyrimidine compound is as represented by formula I, in the formula, R1, R2, R3, R4, R5, X, Y, Z, W, (i) being as defined in the specification and the claims. Such compounds effectively inhibit the growth of a variety of tumor cells and have inhibitory effects on EGFR and IGF1R protease, and can be used for preparing antineoplastic drugs and overcome the tolerance induced by the existing drugs such as gefitinib, erlotinib and the like. The compound has selectivity for tumors, in particular the wild-type non-small cell lung cancer and have good pharmacokinetic characteristics.
    Type: Grant
    Filed: November 18, 2015
    Date of Patent: August 28, 2018
    Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, GUANGZHOU INSTITUTES OF BIOMEDICINE AND HEALTH, CHINESE ACADEMY OF SCIENCES
    Inventors: Ke Ding, Jian Ding, Shingpan Chan, Meiyu Geng, Xiaomei Ren, Hua Xie, Zhengchao Tu, Yi Chen
  • Sulfated polygulonic acid polysaccharide or pharmaceutical salt thereof, preparation method therefor and use thereof
    Patent number: 10058566
    Abstract: A polygulonic acid sulfate or pharmaceutically acceptable salt thereof, preparation method therefor and use thereof in the preparation of tumor growth and/or metastasis inhibitors are disclosed. The polygulonic acid sulfate or pharmaceutically acceptable salt thereof of the present invention can be used in the preparation of any one or more of tumor growth inhibitors, tumor metastasis inhibitors, angiogenesis inhibitors, heparanase inhibitors, C-Met enzyme inhibitors, microtubule polymerization inhibitors, actin-depolymerizing factor activity inhibitors and actin-aggregation inhibitors.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: August 28, 2018
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES
    Inventors: Jian Ding, Jing Ai, Yi Chen, Xun Huang
  • Five-member-heterocycle fused pyridine compounds, method of producing the same, and use thereof
    Patent number: 9988381
    Abstract: This invention provides a class of five-member-heterocycle fused pyridine compounds as shown below in Formula (X), pharmaceutically acceptable salts or pharmaceutically acceptable solvates thereof, a method of producing the same, pharmaceutical compositions containing the compound, and use of the compounds in preparing medicament for preventing and/or treating diseases and tumors associated with abnormal protein tyrosine kinase.
    Type: Grant
    Filed: June 18, 2014
    Date of Patent: June 5, 2018
    Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Haihe Pharmaceutical Co., Ltd.
    Inventors: Jingkang Shen, Meiyu Geng, Jian Ding, Bing Xiong, Jing Al, Yuchi Ma, Xin Wang, Xia Peng, Yuelei Chen, Danqi Chen, Tao Meng, Lanping Ma, Yinchun Ji
  • Highly potent glucocorticoids
    Patent number: 9975918
    Abstract: The present invention relates to novel glucocorticoid compounds. The invention also relates to methods of using these compounds, the synthesis of these compounds, and to compositions and formulations comprising the glucocorticoid compounds, and uses thereof.
    Type: Grant
    Filed: September 25, 2014
    Date of Patent: May 22, 2018
    Assignees: VAN ANDEL RESEARCH INSTITUTE, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Huaqiang Eric Xu, Yuanzheng He, Karsten Melcher, Wei Yi, Jingjing Shi
  • Naphthylamide compound, preparation method and use thereof
    Patent number: 9914707
    Abstract: The present invention relates to a naphthylamide compound of the structure as represented by formula (I), medicinal salts, prodrugs and hydrates or solvates thereof, and also relates to a method of preparing the compounds, pharmaceutical compositions comprising the compounds and the uses thereof as protein tyrosine kinase inhibitors, particularly as VEGFR-2 inhibitors, in preparing drugs for preventing and treating diseases related to abnormal angiogenesis.
    Type: Grant
    Filed: February 15, 2015
    Date of Patent: March 13, 2018
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Wenhu Duan, Jian Ding, Yongcong Lv, Hua Xie
  • CERTAIN PROTEIN KINASE INHIBITORS
    Publication number: 20180036293
    Abstract: Provided are certain PI3K inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
    Type: Application
    Filed: November 1, 2015
    Publication date: February 8, 2018
    Applicants: Shanghai Fochon Pharmaceutical Co., Ltd., Shanghai Institute of Materia Medica Chinese Academy of Sciences, ChongQing Fochon Pharmaceutical Co., Ltd.
    Inventors: Xingdong ZHAO, Jian DING, Linghua MENG, Meiyu GENG, Tongshuang LI, Zuwen ZHOU, Ling CHEN, Qihong LIU, Xianlong WANG, Lijun YANG, Yue RONG, Rui TAN, Chuiliang YU, Lihua JIANG, Yanxin LIU, Li LINGHU, Jing SUN, Weibo WANG
  • Tripeptide epoxyketone compound constructed by heterocycle and preparation method and use thereof
    Patent number: 9856288
    Abstract: Disclosed are a tripeptide epoxyketone compound, a preparation method thereof, and a use thereof in the preparation of anti-tumor drugs.
    Type: Grant
    Filed: March 11, 2015
    Date of Patent: January 2, 2018
    Assignees: ZHEJIANG UNIVERSITY, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Yongzhou Hu, Jia Li, Tao Liu, Jiankang Zhang, Yubo Zhou, Bo Yang, Qiaojun He, Lei Xu, Xiaobei Hu
  • 2-AMINOPYRIMIDINE COMPOUND AND PHARMACEUTICAL COMPOSITION AND USE THEREOF
    Publication number: 20170283398
    Abstract: Disclosed are a 2-aminopyrimidine compound and pharmaceutical composition and use thereof. The structure of the 2-aminopyrimidine compound is as represented by formula I, in the formula, R1, R2, R3, R4, R5, X, Y, Z, W, (i) being as defined in the specification and the claims. Such compounds effectively inhibit the growth of a variety of tumor cells and have inhibitory effects on EGFR and IGF1R protease, and can be used for preparing antineoplastic drugs and overcome the tolerance induced by the existing drugs such as gefitinib, erlotinib and the like. The compound has selectivity for tumors, in particular the wild-type non-small cell lung cancer and have good pharmacokinetic characteristics.
    Type: Application
    Filed: November 18, 2015
    Publication date: October 5, 2017
    Applicants: Shanghai Institute Of Materia Medica, Chinese Academy Of Sciences, GUANGZHOU INSTITUTES OF BIOMEDICINE AND HEALTH, CHINESE ACADEMY OF SCIENCES
    Inventors: Ke Ding, Jian Ding, Shingpan Chan, Meiyu Geng, Xiaomei Ren, Hua Xie, Zhengchao Tu, Yi Chen
  • INDAZOLE COMPOUNDS AS FGFR KINASE INHIBITOR, PREPARATION AND USE THEREOF
    Publication number: 20170275291
    Abstract: The present invention provides an indazole compound as a FGFR kinase inhibitor, preparation and use thereof. Specifically, the present invention provides a compound represented by formula (I), wherein the definitions of each group are described in the specification. The compound of the present invention has good FGFR kinase-inhibiting activity, and can be used in preparing a series of medicines for treating FGFR kinase activity related diseases.
    Type: Application
    Filed: August 19, 2015
    Publication date: September 28, 2017
    Applicants: Shanghai Haihe Pharmaceutical Co., Ltd., Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Meiyu GENG, Lei LIU, Lei JIANG, Min HUANG, Chuantao ZHA, Jing AI, Lei WANG, Jianhua CAO, Jian DING
  • Pharmaceutical use of hexahydro-dibenzo[a,g]quinolizine compounds
    Patent number: 9737517
    Abstract: Use of hexahydro-dibenzo[a,g]quinolizine compounds as shown in formula(I) in preparing a medicine for treating and/or preventing benign prostate hyperplasia diseases.
    Type: Grant
    Filed: May 4, 2014
    Date of Patent: August 22, 2017
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Xin Xie, Haifeng Sun, Jing Li, Fei Zhao, Ying Chen, Zeng Li, Yu Zhou, Hualiang Jiang, Kaixian Chen
  • Pyrrolo[2,1-F[1,2,4]triazine compounds, preparation methods and applications thereof
    Patent number: 9724352
    Abstract: The present invention relates to a pyrrolo[2,1-f][1,2,4]triazine compound, an isomer thereof or a pharmaceutically acceptable salt, ester or hydrate thereof, and a preparation method and application thereof. The pyrrolo[2,1-f][1,2,4]triazine compound has a structure expressed in general formula (I). The pyrrolo[2,1-f][1,2,4]triazine compound expressed in general formula (I) can inhibit a phosphatidylinositol-3 kinase (PI3K) signal pathway, thereby being used to prepare medicine for treating phosphatidylinositol-3 kinase related diseases such as cancer.
    Type: Grant
    Filed: September 19, 2016
    Date of Patent: August 8, 2017
    Assignees: Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai Haihe Pharmaceutical Co., Ltd.
    Inventors: Chunhao Yang, Linghua Meng, Yanhong Chen, Xiang Wang, Cun Tan, Jiapeng Li, Jian Ding, Yi Chen