Abstract: 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.
Type:
Grant
Filed:
December 18, 2020
Date of Patent:
July 12, 2022
Assignees:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, SUZHOU VIGONVITA LIFE SCIENCES CO., LTD., TOPHARMAN SHANGHAI CO., LTD.
Abstract: The present invention relates to a mannuronic diacid oligosaccharide composition, comprising a mannuronic diacid of Formula (III) or a pharmaceutically acceptable salt thereof, wherein n is an integer from 1 to 9, m is 0, 1 or 2, and m? is 0 or 1, and wherein the total weight of mannuronic diacids wherein n=1-5 is 80-95% of the total weight of the composition, and the ratio of the total weight of mannuronic diacids wherein n=1-3 to the total weight of mannuronic diacids wherein n=4-7 is between 1.0 and 3.5.
Type:
Grant
Filed:
December 27, 2017
Date of Patent:
July 12, 2022
Assignee:
GREEN VALLEY (SHANGHAI) PHARMACEUTICAL CO., LTD. SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES
Abstract: A cubic cyclodextrin framework-RGD composition (RGD-COF) and a preparation method therefor. Specifically, the cyclodextrin framework-RGD composition contains a cyclodextrin framework (COF) having a cubic structure and RGD, and can escape from phagocytosis and clearance of macrophages, enhance migration and adhesiveness to damaged blood vessels, and efficiently target and aggregate activated platelets at damaged blood vessel sites, having application prospects on targeted diagnosis and treatment of diseases associated with uncontrolled hemorrhage, atherosclerosis and cerebral apoplexy. By utilizing the advantage that a cyclodextrin-metal organic framework (CD-MOF) has controllable dimensions, a cubic cyclodextrin framework-RGD composition for nanoscale intravenous injection or microscale topically external use is provided.
Type:
Application
Filed:
January 15, 2020
Publication date:
March 10, 2022
Applicant:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Inventors:
Jiwen ZHANG, Yaping HE, Yong SU, Jian XU, Li WU, Xian SUN
Abstract: The present disclosure relates to 7-substituted pyrrolo[2,1-f][1,2,4]triazine compounds or pharmaceutically acceptable salts thereof, and preparation methods and uses thereof. These compounds show good PI3K inhibitory activity, can effectively inhibit the activity of PI3K kinase, and has significant enhancement and improvement of pharmacokinetic properties, such as bioavailability, due to the introduction of the 7-position group; furthermore, the compounds of the present disclosure exhibit an unpredictable high selectivity and strong inhibitory activity on PI3K?, and thus these compounds can be used for treating diseases related to PI3K pathway, especially for anti-cancer or for the treatment of tumors, leukemias and autoimmune diseases. After further optimizing and screening, the compounds are expected to be developed into a new type of anti-tumor drugs.
Type:
Grant
Filed:
June 22, 2018
Date of Patent:
January 4, 2022
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Inventors:
Chunhao Yang, Linghua Meng, Haoyue Xiang, Jing Li, Xi Zhang, Xiang Wang, Cun Tan, Qian He, Jian Ding, Yi Chen
Abstract: Disclosed is an SOMCL-9112 solid dispersion. The SOMCL-9112 solid dispersion is characterized by being prepared from the following raw materials in percentage by weight: 5 percent to 60 percent of SOMCL-9112, 5 percent to 90 percent of pharmaceutically acceptable matrix polymer, 0 percent to 20 percent of surfactant, 0 percent to 20 percent of flow aid and 0 percent to 20 percent of plasticizer. Also disclosed are a preparation method of the SOMCL-9112 solid dispersion, a solid medicinal preparation containing the solid dispersion and application of the solid dispersion for preparing a medicine for treating cancer.
Type:
Grant
Filed:
May 13, 2016
Date of Patent:
December 7, 2021
Assignees:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, SHANGHAI ACEBRIGHT PHARMACEUTICALS CO., LTD.
Inventors:
Shiyan Guo, Yong Gan, Ao Zhang, Zehong Miao, Li Gao, Jian Ding
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:
Grant
Filed:
September 17, 2018
Date of Patent:
December 7, 2021
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: Disclosed in the present invention are a thiazolidone spiro pyrimidine trione compound, a preparation method therefor and uses thereof, the compound having a structure represented by formula (I). In the formula, the definitions of the substituents are described in the specification and the claims. The thiazolidone spiro pyrimidine trione compound in the present invention has high in vivo and in vitro antibacterial activity, has better metabolic properties, and is obviously superior to existing compounds of the same kind.
Type:
Grant
Filed:
June 21, 2018
Date of Patent:
November 23, 2021
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: Disclosed are a 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, a preparation method therefor and an application thereof. Specifically, disclosed are three crystalline forms, i.e., crystalline forms A, B, and C, of 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride (formula I), preparation methods for the three crystalline forms, and use of the three crystalline forms in preparation of drugs.
Type:
Grant
Filed:
May 31, 2018
Date of Patent:
November 16, 2021
Assignees:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, FUKANG (SHANGHAI) HEALTH TECHNOLOGY CO., LTD.
Inventors:
Chunhao Yang, Zehong Miao, Cun Tan, Xiajuan Huan, Jian Ding, Yi Chen
Abstract: An antidepressant steroid compound and a preparation method and an application thereof; the structure of said compound is shown in formula (I), and the definition of each substituent is as described in the description and claims. Compound of the present invention may be used in the prevention, treatment, therapy or alleviation of a plurality of diseases and conditions such as depression.
Type:
Grant
Filed:
December 29, 2017
Date of Patent:
October 12, 2021
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: The present invention relates to a GPR84 receptor antagonist and use thereof. The GPR84 receptor antagonist of the present invention has a structure as represented by formula (I), the definitions of R1, R2, R3, R4, L1, L2, L3, L4, L5, L6, Y, Z, and rings A, B, C, and D are as described in the description and claims. The GPR84 receptor antagonist of the present invention can competitively inhibit the activation of the receptor caused by an agonist of GPR84, and can be used in the preparation of a medicament for treating related diseases caused by high expression or high excitability of GPR84 receptor, the diseases including multiple sclerosis, inflammatory bowel disease, arthritis and the like.
Type:
Grant
Filed:
February 28, 2018
Date of Patent:
August 24, 2021
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: The present invention relates to dihydroquinoxaline bromodomain recognition protein inhibitor, preparation method and use thereof. The inhibitor of the present invention is compound represented by general formula (I), or stereoisomer, pharmaceutically acceptable salt, prodrug, solvate, hydrate and crystal form thereof. The definition of each substituent is as described in the description and claims. The compound represented by general formula (I) of the present invention may inhibit bromodomain recognition protein and may be used for preparing medicament which regulates the apparent state of cells and treats series of diseases and symptoms which are mediated by the bromodomain recognition protein.
Type:
Grant
Filed:
March 5, 2018
Date of Patent:
August 3, 2021
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
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:
Grant
Filed:
February 10, 2020
Date of Patent:
June 22, 2021
Assignee:
Shanghai Institute of Materia Medica, Chinese Academy of Sciences
Abstract: The present invention provides a compound represented by formula I, pharmaceutically acceptable salts, enantiomers, diastereomers or racemates thereof, the preparation method thereof, the pharmaceutical composition comprising the same, and the use thereof in the preparation of a medicament for treating a disease or condition mediated by EED and/or PRC2. The compound of the present invention can be used treating PRC2-mediated diseases or conditions.
Type:
Grant
Filed:
August 29, 2018
Date of Patent:
May 25, 2021
Assignees:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, SUZHOU SUPLEAD LIFE SCIENCES CO., LTD.
Inventors:
Bing Zhou, Cheng Luo, Yaxi Yang, Yuanyuan Zhang, Daohai Du, Hualiang Jiang, Gang Qiao, Xinjun Wang
Abstract: An o-aminoheteroaryl alkynyl-containing compound has a structure represented by formula (I), and the compound of formula (I) has advantages of a high FGFR and RET double target inhibitory activity and a relatively low KDR activity, and the compound of formula (I) exhibits a strong inhibitory activity in a human lung cancer cell line NCI-H1581 and a gastric cancer cell line SNU16 as well as an RET-dependent sensitive cell line BaF3-CCDC6-Ret and a mutant thereof. Pharmacokinetic data shows that the o-aminoheteroaryl alkynyl-containing compound has druggability, and exhibits significant relevant inhibition of the growth of related tumors in a long-term animal model of drug efficacy and results in favorable animal condition at effective doses.
Type:
Grant
Filed:
February 12, 2018
Date of Patent:
April 27, 2021
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Inventors:
Youhong Hu, Meiyu Geng, Wenming Ren, Jian Ding, Xiaocong Guan, Jing Ai, Lang Wang, Xia Peng, Yang Liu, Yang Dai, Limin Zeng
Abstract: The present invention provides a pyrido five-element aromatic ring compound, and a preparation method therefor and a use thereof. The compound provided in the present invention has an inhibitory effect on wild-type and/or mutant EZH2, and is well positioned to become a novel anti-tumor drug or a drug for the treatment of autoimmune diseases.
Type:
Grant
Filed:
September 6, 2017
Date of Patent:
April 6, 2021
Assignees:
SHANGHAI HAIHE PHARMACEUTICAL CO., LTD., SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Abstract: Disclosed is a Glechoma longituba (Nakai) Kupr. extract, specifically compounds I and II, a preparation method for same, and a use thereof in preparing a medicament for blood glucose decease, blood lipids decrease, weight loss, and kidney disease treatment or a method for treatment of said diseases, and a composition containing the extract.
Type:
Grant
Filed:
March 17, 2015
Date of Patent:
April 6, 2021
Assignees:
SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES, NANJING PAILEXING PHARMACEUTICAL TECHNOLOGY LTD.
Abstract: Provided are a class of vancomycin derivatives with a structure as shown in the general formula below and pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition containing the compound thereof, and the use of these compounds in preparing drugs for treating and/or preventing bacterial infection diseases, in particular drugs for treating infection diseases caused by Gram-positive bacteria.
Type:
Grant
Filed:
April 26, 2017
Date of Patent:
March 30, 2021
Assignee:
SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES