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
Abstract: C, O-spiro aryl glycoside compounds are provided. Specifically provided are C, O-spiro aryl glycoside compounds represented by the formula (I), wherein the definitions of each variable group are described in the specification. Also provided are methods of preparing and using the C, O-spiro aryl glycoside compounds. The C, O-spiro aryl glycoside compounds can be used as SGLT2 inhibitors and for treating diseases, such as diabetes, atherosclerosis, and adiposity.
Type:
Grant
Filed:
June 23, 2016
Date of Patent:
February 4, 2020
Assignee:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Abstract: The present disclosure relates to the field of pharmaceutical synthesis, and more particularly, relates to a monocyclic ?-lactam-siderophore conjugate as well as a method for synthesizing same and its use in the treatment of bacterial infectious diseases. Provided are a monocyclic ?-lactam-siderophore conjugate represented by formula (I) as described herein, an optical isomer thereof or a pharmaceutically acceptable salt thereof, and a method for synthesizing same, and a use thereof in treating bacterial infectious diseases.
Type:
Application
Filed:
January 18, 2019
Publication date:
December 19, 2019
Applicant:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: The present disclosure relates to the field of pharmaceutical synthesis, and more particularly, relates to a monocyclic ?-lactam-siderophore conjugate as well as a method for synthesizing same and its use in the treatment of bacterial infectious diseases. Provided are a monocyclic ?-lactam-siderophore conjugate represented by formula (I) as described herein, an optical isomer thereof or a pharmaceutically acceptable salt thereof, and a method for synthesizing same, and a use thereof in treating bacterial infectious diseases.
Type:
Grant
Filed:
January 18, 2019
Date of Patent:
December 10, 2019
Assignee:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Abstract: The present invention relates to six-membered ring benzo derivatives as a DPP-4 inhibitor and a use thereof. In particular, the present invention relates to a compound as shown in formula I, a pharmaceutical composition containing the compound as shown in formula I and a use of the compound in the preparation of drugs for treating DPP-4 related diseases or inhibiting DPP-4.
Type:
Grant
Filed:
October 30, 2015
Date of Patent:
November 19, 2019
Assignees:
EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: The present invention relates to a class of fatty acid compounds, a preparation method thereof and use thereof. The fatty acid compounds have the structure of the formula I, which has the ability to activate APMK and inhibit the glucose output in mouse primary hepatocytes. The fatty acid compounds can be used in preparing a medicament for the treatment of obesity or diabetes.
Type:
Grant
Filed:
February 20, 2017
Date of Patent:
September 17, 2019
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: The present invention relates to crystal form A of a compound. The present invention also discloses a preparation method and a pharmaceutical composition of the crystal form A. The crystal form A has strong hypoglycemic activity in vivo and is expected to be a novel pharmaceutically active ingredient for treating or preventing type II diabetes and/or complications of type II diabetes.
Type:
Grant
Filed:
February 3, 2016
Date of Patent:
August 27, 2019
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: The present disclosure relates to the field of pharmaceutical synthesis, and more particularly, relates to a monocyclic ?-lactam-siderophore conjugate as well as a method for synthesizing same and its use in the treatment of bacterial infectious diseases. Provided are a monocyclic ?-lactam-siderophore conjugate represented by formula (I) as described herein, an optical isomer thereof or a pharmaceutically acceptable salt thereof, and a method for synthesizing same, and a use thereof in treating bacterial infectious diseases.
Type:
Application
Filed:
January 18, 2019
Publication date:
August 1, 2019
Applicant:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: A method for preparing a model of an animal suffering from non-human mammal obesity or a related disease, comprising the following steps: (a) providing a cell of a non-human mammal, and inactivating Glce gene in the cell, thereby obtaining a non-human mammal cell with an inactivated Glce gene; and (b) using the cell having an inactivated Glce gene obtained in step (a) to prepare and obtain a model of an animal suffering from Glce gene-inactivated obesity or a related disease. The animal model is an effective model for an animal suffering from obesity or a related disease, which may be used for researching diseases such as obesity, hyperlipidemia, hypertension, and diabetes, and may also be used for screening and testing experiments of specific drugs.
Type:
Application
Filed:
August 22, 2017
Publication date:
July 18, 2019
Applicant:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: 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.
Type:
Application
Filed:
June 2, 2017
Publication date:
July 11, 2019
Applicant:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Inventors:
Hong Liu, Jia Li, Wei Zhu, Yubo Zhou, Jiang Wang, Mingbo Su, Shuni Wang, Wei Xu, Chunpu Li, Weijuan Kan, Hualiang Jiang, Kaixian Chen
Abstract: 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.
Type:
Application
Filed:
March 29, 2017
Publication date:
June 27, 2019
Applicant:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Abstract: Provided are certain PI3K inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
Type:
Grant
Filed:
November 1, 2015
Date of Patent:
June 25, 2019
Assignees:
SHANGHAI FOCHON PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES, CHONGQING FOCHON PHARMACEUTICAL CO., LTD.
Abstract: Provided is a process of synthesizing a substituted pyridine and pyrimidine compound. Particularly, provided is a method for preparing a compound of formula III via a compound of formula II?, wherein the definition of each of groups is as described as the description. Compound with other methods, the method in the present invention has features of high yield and a result product being easier to separate.
Type:
Grant
Filed:
March 24, 2016
Date of Patent:
June 11, 2019
Assignees:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shandong Luoxin Pharmaceutical Group Stock Co., Ltd.
Inventors:
Jingkang Shen, Tao Meng, Ting Yu, Lanping Ma, Xin Wang, Lin Chen
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:
January 12, 2018
Date of Patent:
June 11, 2019
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
Abstract: Application of a phosphodiesterase PDE3A and genes thereof in judgment of a tumor treatment effect of Anagrelide. Specifically provided is usage of a PDE3A gene sequence, protein, or anti-PDE3A protein specific antibody in preparation of a diagnostic reagent or a diagnostic kit. The diagnostic reagent or kit is used for (a) judging a tumor treatment effect of Anagrelide, and/or (b) judging whether Anagrelide is appropriate for treating a tumor patient. Also provided is a corresponding detection kit.
Type:
Application
Filed:
April 25, 2017
Publication date:
May 16, 2019
Applicant:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
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:
December 28, 2015
Date of Patent:
May 7, 2019
Assignee:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Inventors:
Jianhua Shen, Yiping Wang, Xinde Chen, Wenwei Xu, Kai Wang
Abstract: The present invention relates to a series of analogs of natural product Pyripyropene A represented by general formula I and a preparation method and use thereof. More particularly, the present invention relates to analogs of the natural product Pyripyropene A, a preparation method and use thereof as the acyl-CoA:cholesterol acyltransferase 2 (ACAT2) inhibitors for the treatment of cardiovascular diseases such as atherosclerosis and the like.
Type:
Grant
Filed:
March 3, 2016
Date of Patent:
May 7, 2019
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: The present invention relates to a method for preparing magnesium lithospermate B. The method is characterized in that: magnesium lithospermate B is extracted or purified from a Salvia miltiorrhiza plant material or a Salvia miltiorrhiza extract in the presence of an added magnesium salt. The present invention also relates to a high-purity magnesium lithospermate B product prepared by the method of the present invention, wherein the content of magnesium lithospermate B is more than 95% by weight.
Type:
Grant
Filed:
February 9, 2015
Date of Patent:
April 16, 2019
Assignees:
SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES, SHANGHAI GREEN VALLEY PHARMACEUTICAL CO., LTD.
Abstract: Disclosed are new substituted nitrogen-containing heterocyclic derivatives represented by formula (I) as AKT inhibitors, optical isomers, pharmaceutically acceptable salts or solvates thereof, wherein the definition of R1, R2, R3, R4, R5, R6, ring A, ring C, B, Q, Y, Z and m is shown in the description for details. In addition, medicaments comprising the derivatives as active components are also disclosed, which can be useful for treating proliferative diseases, such as cancer and inflammation, especially diseases relating to AKT kinase.
Type:
Grant
Filed:
March 21, 2015
Date of Patent:
March 19, 2019
Assignees:
ZHEJIANG UNIVERSITY, SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Inventors:
Xiaowu Dong, Jia Li, Bo Yang, Yongzhou Hu, Yubo Zhou, Qinjie Weng, Wenhu Zhan, Lei Xu, Tao Liu, Qiaojun He