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：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.

公开(公告)号：US20170275291A1

公开(公告)日：2017-09-28

申请号：US15504854

申请日：2015-08-19

Applicant: Shanghai Haihe Pharmaceutical Co., Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Inventor： Meiyu GENG ,  Lei LIU ,  Lei JIANG ,  Min HUANG ,  Chuantao ZHA ,  Jing AI ,  Lei WANG ,  Jianhua CAO ,  Jian DING

IPC: C07D487/04 ,  C07D231/56 ,  C07D519/00 ,  C07D401/12 ,  C07D471/04 ,  C07D403/12 ,  C07D498/04

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.

公开(公告)号：US20160046638A1

公开(公告)日：2016-02-18

申请号：US14926729

申请日：2015-10-29

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

Inventor： Weibo WANG ,  Meiyu GENG ,  Jian DING ,  Xingdong ZHAO ,  Jing AI ,  Qiang TIAN ,  Xia PENG ,  Weipeng ZHANG ,  Hongbin LIU ,  Haohan TAN ,  Ling CHEN

IPC: C07D487/04 ,  C07D405/12 ,  C07D405/14

CPC classification number: C07D487/04 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K45/06 ,  C07D405/12 ,  C07D405/14 ,  A61K2300/00

Abstract: Disclosed herein are protein kinase inhibitors, more particularly novel pyrimidine derivatives and pharmaceutical compositions thereof, and method of use thereof.

Abstract translation: 本文公开了蛋白激酶抑制剂，更具体地是新颖的嘧啶衍生物及其药物组合物及其使用方法。

公开(公告)号：US20230285389A1

公开(公告)日：2023-09-14

申请号：US17802898

申请日：2021-02-26

Applicant: Shanghai Runshi Medical Technology Co., Ltd ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Inventor： Ao ZHANG ,  Meiyu GENG ,  Jing AI ,  Caixia WANG ,  Xia PENG ,  Yang ZHANG ,  Jian DING

IPC: A61K31/496 ,  A61P35/00 ,  C07K16/28

CPC classification number: A61K31/496 ,  A61P35/00 ,  C07K16/2818 ,  C07K16/2827

Abstract: Use of a compound of general formula (A) which is a CFS-1R kinase inhibitor or a pharmaceutically acceptable salt thereof in the preparation of medicaments for treating diseases related to CSF-1R kinase signal transduction pathway or medicaments for regulating immunization. In vivo and in vitro studies show that the compound can significantly inhibit CSF-1R kinase activity; significantly inhibits the proliferation of a CSF-1/CSF-1R-driven mouse myeloid leukemia cell line, inhibits the survival of macrophages induced by CSF-1 and reverses M2 polarization phenotype of macrophages, and has an effect superior to that of the marketed medicament Pexidartinib. In a TAM enriched tumor model (MC38 model), the compound significantly antagonizes the tumor immunosuppressive microenvironment and exhibits significant anti-tumor efficacy. The compound has inhibitory effects on tumors that are not sensitive to immune checkpoint drugs, and can enhance the efficacy of immune checkpoint drugs, and has good clinical application prospects.

公开(公告)号：US20210221807A1

公开(公告)日：2021-07-22

申请号：US17057199

申请日：2019-05-21

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

Inventor： Hong LIU ,  Meiyu GENG ,  Yu ZHOU ,  Jian DING ,  Feifei FANG ,  Jing AI ,  Jian LI ,  Xia PENG ,  Hualiang JIANG ,  Yinchun JI ,  Kaixian CHEN

IPC: C07D471/04 ,  C07D519/00

Abstract: Provided are a class of fused-cyclic pyrazolone formamide compounds and a preparation method therefor, a pharmaceutical composition and the use thereof. Specifically, provided is a compound having the structure as shown in formula (I) (with each group defined in the description). The compound can be used as an AXL inhibitor in the preparation of a pharmaceutical composition for treating tumors.

公开(公告)号：US20200172510A1

公开(公告)日：2020-06-04

申请号：US15998927

申请日：2017-02-17

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

Inventor： Ao ZHANG ,  Meiyu GENG ,  Li XING ,  Jing AI ,  Zilan SONG ,  Xia PENG ,  Wangting GU ,  Jian DING

IPC: C07D401/12 ,  C07D403/12 ,  C07D413/14 ,  C07D417/14 ,  C07D405/12 ,  C07D213/75 ,  A61P35/00

Abstract: Provided in the present invention are a substituted amino six-membered nitric heterocyclic ring compound and a preparation and use thereof. In particular, provided in the present invention is a compound as shown by general formula (I) below, wherein the definition of each group is as described in the description. The compound of the present invention has an excellent tyrosine kinase inhibitory activity, and can thus be used to prepare a series of medicines for treating diseases related to tyrosine kinase inhibitory activity.

公开(公告)号：US20200055838A1

公开(公告)日：2020-02-20

申请号：US16487385

申请日：2018-02-12

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

Inventor： Youhong HU ,  Meiyu GENG ,  Wenming REN ,  Jian DING ,  Xiaocong GUAN ,  Jing AI ,  Lang WANG ,  Xia PENG ,  Yang LIU ,  Yang DAI ,  Limin ZENG

IPC: C07D401/12 ,  C07D405/14 ,  C07D403/12 ,  A61P35/00 ,  B01J31/24 ,  B01J27/122 ,  B01J31/30

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.

公开(公告)号：US20190135818A1

公开(公告)日：2019-05-09

申请号：US16304508

申请日：2017-05-24

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

Inventor： Hualiang JIANG ,  Hong LIU ,  Meiyu GENG ,  Mingyue ZHENG ,  Jing AI ,  Yulan WANG ,  Xiaowei WU ,  Shuangjie LI ,  Xia PENG ,  Chunpu LI ,  Kaixian CHEN ,  Bao WANG

IPC: C07D487/04 ,  A61P35/00

Abstract: The present invention provides a compound comprising a 5-membered heterocycle fused with a pyridazinone, wherein the compound is used as an FGFR kinase inhibitor, and a manufacturing method and application thereof. The invention specifically provides a compound as represented by formula (I). Various radicals are as defined in the specification. The compound provided by the invention effectively inhibits an activity of an FGFR kinase, and can be used to manufacture a pharmaceutical product for treating a disease related to the activity of the FGFR kinase.