Patents Assigned to Shanghai Institute of Materia Medica Chinese Academy of Sciences
  • Patent number: 10875883
    Abstract: Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-?3-amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.
    Type: Grant
    Filed: September 19, 2017
    Date of Patent: December 29, 2020
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Jiang Wang, Shengbin Zhou, Panfeng Peng, Yong Nian, Shuni Wang, Shuangjie Shu, Hao Shen, Hualiang Jiang, Kaixian Chen
  • Patent number: 10865415
    Abstract: Provided are a dsRNA construct of an orphan G-protein-coupled receptor GPR160 gene related to prostate cancer and the use thereof, wherein the dsRNA construct of the GPR160 gene and a composition thereof can prevent or treat prostate cancer.
    Type: Grant
    Filed: September 29, 2016
    Date of Patent: December 15, 2020
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Caihong Zhou, Xinchuan Dai, Mingwei Wang
  • Patent number: 10836743
    Abstract: Provided is a fluorinated cyclopropylamine compound represented by formula I, a racemate thereof, an R-isomer thereof, an S-isomer thereof, a pharmaceutical salt thereof, and a mixture thereof. Also provided are pharmaceutical compositions containing the compound, a preparation method for the compound, and uses thereof as a lysine specific demethylase 1 (LSD1) inhibitor, and in the treatment of cancers.
    Type: Grant
    Filed: March 16, 2017
    Date of Patent: November 17, 2020
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Hong Liu, Jia Li, Jiang Wang, Mingbo Su, Shuni Wang, Yubo Zhou, Wei Zhu, Wei Xu, Chunpu Li, Hualiang Jiang, Kaixian Chen
  • Patent number: 10822327
    Abstract: A 2-substituted aromatic ring-pyrimidine derivative as shown in a general formula I, and an optical isomer or a pharmaceutically acceptable salt or a solvate thereof are provided. The present invention designs and synthesizes a series of novel small molecular Chk1 inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained through structure-based virtual screening as a lead compound, and carries out Chk1 kinase inhibitory activity test. The experiment confirmed that said compounds possess strong anti-cancer effect, Chk1 kinase inhibitory activity and are promising Chk1 inhibitors. The compounds can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal.
    Type: Grant
    Filed: November 8, 2017
    Date of Patent: November 3, 2020
    Assignees: ZHEJIANG UNIVERSITY, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Tao Liu, Jia Li, Yongzhou Hu, Yubo Zhou, Xiaowu Dong, Anhui Gao, Pinrao Song, Peipei Wang, Lexian Tong, Xiaobei Hu, Mingbo Su
  • Patent number: 10800776
    Abstract: A fluorine-containing triazolopyridine represented by formula (I) and a racemate, R-stereoisomer, S-stereoisomer, pharmaceutically acceptable salt, or mixture thereof are described. The triazolopyridine can be used as a positive allosteric modulator of an mGluR2, and is highly selective in activating the mGluR2, exerting no activation or very limited activation of other homologous metabotropic glutamate receptor. The triazolopyridine can thus be used to prepare a product for treating an mGluR2-related disease, such as a central nervous system disease or neurological disease.
    Type: Grant
    Filed: May 17, 2017
    Date of Patent: October 13, 2020
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Hong Liu, Yu Zhou, Wenjing Xia, Dong Zhang, Hualiang Jiang, Kaixian Chen
  • Patent number: 10793566
    Abstract: Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I):
    Type: Grant
    Filed: May 22, 2019
    Date of Patent: October 6, 2020
    Assignees: ZIBO BIOPOLAR CHANGSHENG PHARMACEUTICAL CO. LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Xibin Liao, Jia Li, Zhijian Lu, Yubo Zhou, Anhui Gao
  • Patent number: 10787422
    Abstract: 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.
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: September 29, 2020
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Jianhua Shen, Yiping Wang, Xinde Chen, Wenwei Xu, Kai Wang
  • Patent number: 10766889
    Abstract: 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.
    Type: Grant
    Filed: August 24, 2017
    Date of Patent: September 8, 2020
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Jia Li, Jian Ding, Meiyu Geng, Yangming Zhang, Yi Chen, Yubo Zhou, Chaojun Gong, Mingbo Su, Anhui Gao
  • Publication number: 20200231623
    Abstract: Disclosed are a pentacyclic triterpene compound as shown in general formula (I) and a preparation method therefor. The compound has an effective antagonistic effect on FXR receptors.
    Type: Application
    Filed: September 17, 2018
    Publication date: July 23, 2020
    Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Fajun NAN, Xin XIE, Chenlu ZHANG, Shimeng GUO, Yangming ZHANG, Siwei WANG
  • Patent number: 10710996
    Abstract: 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.
    Type: Grant
    Filed: May 23, 2016
    Date of Patent: July 14, 2020
    Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Yaqiu Long, Meiyu Geng, Zhongliang Xu, Jing Ai
  • Patent number: 10682352
    Abstract: Provided in the present invention are a compound having the effects of preventing and treating diseases related to IDH mutation, and a preparation method and use thereof.
    Type: Grant
    Filed: March 21, 2017
    Date of Patent: June 16, 2020
    Assignees: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Lei Jiang, Meiyu Geng, Qiangang Zheng, Min Huang, Huixin Wan, Shuai Tang, Xianlei Fu, Xiaojing Lan, Jianhua Cao, Feifei Liu, Jian Ding
  • Publication number: 20200181121
    Abstract: The present disclosure relates to a cocrystal of telmisartan and hydrochlorothiazide, a preparation method and use thereof. In the cocrystal, the molar ratio of telmisartan and hydrochlorothiazide is 1:1. The cocrystal of telmisartan and hydrochlorothiazide was characterized by X-ray powder diffraction (XRPD), proton nuclear magnetic resonance spectra (1H-NMR), thermal gravimetric analysis (TG), scanning differential calorimetry (DSC) and infrared (IR) spectra, and it was found that the maximum plasma concentration of the cocrystal in SD rats was higher than that of any one of hydrochlorothiazide and telmisartan itself. The cocrystal of telmisartan and hydrochlorothiazide has a simple preparation method and good physical and chemical properties.
    Type: Application
    Filed: February 14, 2020
    Publication date: June 11, 2020
    Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Xuefeng Mei, Jianrong Wang, Qihui Yu
  • Publication number: 20200181109
    Abstract: 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.
    Type: Application
    Filed: February 10, 2020
    Publication date: June 11, 2020
    Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
    Inventors: Youhong Hu, Jianping Zuo, Dong Lu, Li Yang, Limin Zeng, Feifei Liu, Yunzhe Zhang, Wuhong Chen, Xiankun Tong
  • Patent number: 10662187
    Abstract: Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I):
    Type: Grant
    Filed: January 17, 2017
    Date of Patent: May 26, 2020
    Assignees: Zibo Biopolar Changsheng Pharmaceutical Co. Ltd., Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Xibin Liao, Jia Li, Zhijian Lu, Yubo Zhou, Anhui Gao
  • Publication number: 20200140415
    Abstract: The present disclosure relates to a salt of phenyl pyrimidinone compound, a polymorph thereof and a pharmaceutical composition comprising the same and a use thereof, particularly relates to the hydrochlorate of phenyl pyrimidinone compound of following formula (I-A) and a pharmaceutically acceptable polymorph, solvate, hydrate, co-crystal, anhydrous substance, or amorphous form thereof, a pharmaceutical composition and a pharmaceutical unit dosage comprising the same, the preparing method and use thereof.
    Type: Application
    Filed: January 7, 2020
    Publication date: May 7, 2020
    Applicants: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, SUZHOU VIGONVITA LIFE SCIENCES CO., LTD., TOPHARMAN SHANGHAI CO., LTD.
    Inventors: Jingshan Shen, Yang He, Weiming Chen, Jianfeng Li, Guanghui Tian, Xudong Gong, Zhen Wang, Rongxia Zhang, Yongjian Liu, Hualiang Jiang
  • Patent number: 10640514
    Abstract: The invention describes a polymorph of (R)-methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothiophene[3,2-d]pyrimidine-6-carboxylic acid maleate and a preparation method therefor. The polymorph is a crystal having high stability and low hygroscopicity, and the crystal form is selected from crystal form A, crystal form B and crystal form C. Furthermore, the crystal form has a strong in-vivo hypoglycemic activity and can be used for the preparation of a novel drug for the treatment or prevention of diabetes mellitus type H and/or complications of diabetes mellitus type H.
    Type: Grant
    Filed: March 20, 2017
    Date of Patent: May 5, 2020
    Assignee: 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
  • Patent number: 10618900
    Abstract: Compounds of formula I are provided. Also provided are methods of preparing the compounds of formula (I), and methods of using the compounds of formula (I) as a negative allosteric modulator of a metabotropic glutamate receptor (mGluR) subtype 5.
    Type: Grant
    Filed: April 15, 2016
    Date of Patent: April 14, 2020
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Hong Liu, Yu Zhou, Dong Zhang, Jian Li, Hualiang Jiang, Kaixian Chen
  • Patent number: 10611774
    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: Grant
    Filed: March 22, 2017
    Date of Patent: April 7, 2020
    Assignee: 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
  • Patent number: 10597399
    Abstract: A class of substituted triazolopiperazine compounds represented by formula (I), 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: Grant
    Filed: May 23, 2018
    Date of Patent: March 24, 2020
    Assignee: 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
  • Patent number: 10562900
    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: Grant
    Filed: August 19, 2015
    Date of Patent: February 18, 2020
    Assignees: 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