公开(公告)号：US10800776B2

公开(公告)日：2020-10-13

申请号：US16302154

申请日：2017-05-17

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Hong Liu ,  Yu Zhou ,  Wenjing Xia ,  Dong Zhang ,  Hualiang Jiang ,  Kaixian Chen

IPC: A61K31/4196 ,  A61K31/437 ,  C07D471/04 ,  A61P25/18 ,  A61P25/28 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/4709 ,  A61K31/496 ,  A61P25/22 ,  A61P25/24

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.

公开(公告)号：US20200247781A1

公开(公告)日：2020-08-06

申请号：US16652148

申请日：2018-09-29

Applicant: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Lei LI ,  Meiyu GENG ,  Ying HUANG ,  Jian DING ,  Qiong ZHANG ,  Min HUANG ,  Shuai TANG ,  Ning SHEN ,  Yi CHEN

IPC: C07D401/14 ,  C07D405/14 ,  C07D403/14

Abstract: The invention relates to a compound of formula (I): wherein variables are as defined in the specification. The compound is an inhibitor of an ERK kinase, e.g. ERK1 and/or ERK2 kinase. The invention also relates to the use of the compound and a method for preparing the compound, and a pharmaceutical composition containing the compound.

公开(公告)号：US10683278B2

公开(公告)日：2020-06-16

申请号：US15752896

申请日：2016-08-18

Applicant: JINAN UNIVERSITY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Ke Ding ,  Meiyu Geng ,  Li Tan ,  Jian Ding ,  Zhang Zhang ,  Jing Ai ,  Xiaomei Ren ,  Donglin Gao ,  Zhengchao Tu ,  Xiaoyun Lu ,  Dongmei Zhang

IPC: A61K31/4709 ,  C07D215/233 ,  C07D401/12 ,  C07D471/04 ,  C07D471/06 ,  C07D487/04 ,  C07D491/048 ,  C07D498/06 ,  C07D513/04 ,  C07D519/00

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.

公开(公告)号：US20200157110A1

公开(公告)日：2020-05-21

申请号：US16626254

申请日：2018-06-22

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Chunhao YANG ,  Linghua MENG ,  Haoyue XIANG ,  Jing LI ,  Xi ZHANG ,  Xiang WANG ,  Cun TAN ,  Qian HE ,  Jian DING ,  Yi CHEN

IPC: C07D487/04 ,  C07D519/00

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 PI3Kδ, 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.

公开(公告)号：US20200030284A1

公开(公告)日：2020-01-30

申请号：US16496743

申请日：2018-03-26

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA,CHINESE ACADEMY OF SCIENCES ,  JIANGSU ZUOYOU MEDICINE CO., LTD.

Inventor： Jianping ZUO ,  Wei TANG ,  Yuxi YAN ,  Ping Ll ,  Shijun HE ,  Zemin LIN ,  Xiaoqian YANG ,  Chunlan FENG ,  Fenghua ZHU

IPC: A61K31/357 ,  A61P1/00

Abstract: The present invention provides a use of artemisinin derivatives, or a pharmaceutically acceptable salt thereof, for the manufacture of a medicament for the treatment or adjuvant treatment of inflammatory bowel disease. In an animal model of inflammatory bowel disease induced by dextran sulfate sodium (DSS), the experimental results of the artemisinin derivative, or the pharmaceutically acceptable salt thereof, of the present invention showed that oral gavage administration can effectively alleviate colitis symptoms of IBD mice such as weight loss, diarrhea, and hematochezia, reduce pathological damage in colon tissue, inhibit the infiltration of inflammatory cells in colon tissue of IBD mice, and downregulate levels of disease-related proinflammatory cytokines. The pharmacodynamic and pharmacologic studies demonstrated that this type of compounds has good anti-inflammatory and immunosuppressive effects and a high safety profile, thereby having good application potential in clinical treatment and adjuvant treatment of inflammatory bowel disease.

公开(公告)号：US10392401B2

公开(公告)日：2019-08-27

申请号：US15549918

申请日：2016-02-03

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Hong Liu ,  Jiang Wang ,  Jian Li ,  Jia Li ,  Jingya Li ,  Shengbin Zhou ,  Mingbo Su ,  Hualiang Jiang ,  Xiaomin Luo ,  Kaixian Chen

IPC: C07D495/04 ,  A61K31/519

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.

公开(公告)号：US20190248751A1

公开(公告)日：2019-08-15

申请号：US16299636

申请日：2019-03-12

Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Inventor： Jianhua Shen ,  Yiping Wang ,  Xinde Chen ,  Wenwei Xu ,  Kai Wang

IPC: C07D239/54 ,  C07D239/56 ,  C07D409/04 ,  C07D403/06 ,  C07D403/04 ,  C07D401/12 ,  A61K31/513 ,  C07D413/04 ,  C07D239/545 ,  C07D239/52 ,  C07D239/48 ,  A61K31/541 ,  C07D401/04

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.

公开(公告)号：US20190218540A1

公开(公告)日：2019-07-18

申请号：US16327270

申请日：2017-08-22

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Kan DING ,  Yanling LI

IPC: C12N9/90 ,  C12N15/90 ,  A61K49/00 ,  A01K67/027

CPC classification number: C12N9/90 ,  A01K67/0276 ,  A01K2217/075 ,  A01K2217/077 ,  A01K2217/15 ,  A01K2227/105 ,  A01K2267/0362 ,  A61K49/00 ,  A61K49/0008 ,  C12N15/90 ,  C12N15/907 ,  C12Y501/03017

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.

公开(公告)号：US20190211010A1

公开(公告)日：2019-07-11

申请号：US16331090

申请日：2017-09-06

Applicant: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Xuxing CHEN ,  Meiyu GENG ,  Lei JIANG ,  Yi CHEN ,  Jianhua CAO ,  Qingyun JIANG ,  Qianqian SHEN ,  Jian DING ,  Yucai YAO ,  Zhao ZHAO ,  Yuanfang XIONG

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/5377 ,  A61P35/00 ,  A61P37/06 ,  C07D519/00

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.

公开(公告)号：US20190211005A1

公开(公告)日：2019-07-11

申请号：US16329336

申请日：2017-08-24

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Fajun NAN ,  Jia LI ,  Jian DING ,  Meiyu GENG ,  Yangming ZHANG ,  Yi CHEN ,  Yubo ZHOU ,  Chaojun GONG ,  Mingbo SU ,  Anhui GAO

IPC: C07D417/04 ,  A61P35/02

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.