公开(公告)号：US20240150300A1

公开(公告)日：2024-05-09

申请号：US18278063

申请日：2022-02-18

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

Inventor： Youhong HU ,  Meiyu GENG ,  Daqiang LI ,  Aijun SHEN ,  Zhuo ZHANG ,  Yalei LI ,  Huajie YANG ,  Hongchun LIU ,  Hanyue ZHONG ,  Jian DING

IPC: C07D237/14 ,  A61P35/00 ,  A61P35/02 ,  C07C67/00 ,  C07C67/10 ,  C07D401/04 ,  C07D403/04

CPC classification number: C07D237/14 ,  A61P35/00 ,  A61P35/02 ,  C07C67/00 ,  C07C67/10 ,  C07D401/04 ,  C07D403/04

Abstract: The present invention relates to an S-configuration-containing amino benzamide pyridazinone compound, a preparation method therefor, and a pharmaceutical composition and application thereof. Specifically, the present invention relates to a compound represented by the following general formula I or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition and application thereof. The S-configuration compound of the present application has very strong binding activity on class I histone deacetylase (HDAC1), and shows inhibitory activity on in-vitro proliferation of various tumor cells.

公开(公告)号：US20230032101A1

公开(公告)日：2023-02-02

申请号：US17772334

申请日：2020-10-23

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

Inventor： Wenhu DUAN ,  Meiyu GENG ,  Zhengsheng ZHAN ,  Zuoquan XIE ,  Kaiyan ZHAO ,  Yuting GUO ,  Xiyuan WANG ,  Yan ZHANG ,  Xiaoqian ZHOU ,  Jian DING

IPC: C07D409/04 ,  C07D405/04 ,  C07D333/22 ,  C07D407/04 ,  C07D495/04 ,  C07D417/04 ,  C07D471/04 ,  C07D409/14 ,  A61P35/00

Abstract: A five-membered heterocyclic oxocarboxylic acid compound and the medical use thereof are described. Specifically, provided are a compound as represented by formula (I) and a pharmaceutically acceptable salt, prodrug, hydrate, solvate or crystal form thereof, and also a method for preparing the compound, a pharmaceutical composition containing the compound, and the medical use thereof as a secretion regulator of type I interferon, especially as a STING agonist, and the preparation of a drug for preventing and/or treating diseases related to type I interferon.

公开(公告)号：US20220089561A1

公开(公告)日：2022-03-24

申请号：US17420389

申请日：2019-12-31

Applicant: SHANGHAI HAIHE PHARMACEUTICAL CO., LTD. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Inventor： Ao ZHANG ,  Meiyu GENG ,  Chunyong DING ,  Zuoquan XIE ,  Jian DING ,  Yan ZHANG ,  Ancheng SHEN ,  Xiyuan WANG

IPC: C07D333/64 ,  C07D409/12

Abstract: A fluorine-containing substituted benzothiophene compound and a pharmaceutical composition and an application thereof are described. The compound has the structure as shown in formula (I), in which the definitions of each group and substituent are as described in the description. A preparation method of the compound and an anti-tumor application thereof are also described.

公开(公告)号：US20210078972A1

公开(公告)日：2021-03-18

申请号：US17044322

申请日：2019-03-29

Applicant: HAIHE BIOPHARMA CO., LTD. ,  JINAN UNIVERSITY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Ke DING ,  Meiyu GENG ,  Shingpan CHAN ,  Jian DING ,  Li TAN ,  Jing AI ,  Zhang ZHANG ,  Xia PENG ,  Xiaomei REN ,  Yinchun JI ,  Zhengchao TU ,  Yang DAI ,  Xiaoyun LU

IPC: C07D401/12 ,  A61P35/00

Abstract: The present invention relates to quinoline or quinazoline compound represented by the formula (I), a pharmaceutically acceptable salt thereof, a stereoisomer thereof, a prodrug molecule thereof, or a deuterated compound thereof. The compound of the present invention is effective in inhibiting the action of AXL protein kinase and can inhibit proliferation, migration, and invasion of various tumor cells. Further, the quinoline or quinazoline compound of the present invention has excellent metabolic stability, high in vivo antitumor activity, low toxic side effects, and can be used for preparing a drug for preventing hyperproliferative diseases such as tumors in humans and other mammals.

公开(公告)号：US20230382871A1

公开(公告)日：2023-11-30

申请号：US18027759

申请日：2021-09-22

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

Inventor： Jian DING ,  Wenhu DUAN ,  Hua XIE ,  Meiyu GENG ,  Caixia WANG ,  Zhengsheng ZHAN ,  Na GAO ,  Yang ZHANG

IPC: C07D231/56 ,  A61P35/00 ,  C07K16/28

CPC classification number: C07D231/56 ,  A61P35/00 ,  C07K16/2818 ,  C07K16/2827 ,  A61K2039/505

Abstract: Provided is the use of a CSF1R kinase inhibitor compound or a pharmaceutically acceptable salt thereof in the preparation of drugs for treating diseases related to the CSF1R kinase signal transduction pathway or drugs for regulating immunization.

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：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.

公开(公告)号：US20220324869A1

公开(公告)日：2022-10-13

申请号：US17640424

申请日：2020-09-03

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

Inventor： Wenhu DUAN ,  Meiyu GENG ,  Hefeng ZHANG ,  Jian DING ,  Jing AI ,  Xia PENG ,  Yinchun JI

IPC: C07D487/04 ,  A61P35/00 ,  C07D401/14 ,  C07D405/14 ,  C07F7/08

Abstract: A compound having Axl and c-Met kinase inhibitory activity, a preparation method therefor and an application thereof are provided. Specifically, provided herein are a compound having the structure represented by formula (I), a preparation method therefor and an application thereof in the preparation of a medication for the treatment and/or prevention of tumor-associated diseases and/or kinase-related diseases.

公开(公告)号：US20180265496A1

公开(公告)日：2018-09-20

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: C07D401/12 ,  C07D487/04 ,  C07D471/04 ,  C07D519/00 ,  C07D513/04 ,  C07D471/06 ,  C07D498/06 ,  C07D491/048

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.