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：US20220389025A1

公开(公告)日：2022-12-08

申请号：US17761252

申请日：2020-09-21

Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  China Pharmaceutical University

Inventor： Wenhu DUAN ,  Meiyu GENG ,  Huibin ZHANG ,  Zuoquan XIE ,  Jinpei ZHOU ,  Yifei YANG ,  Xiyuan WANG ,  Xiaojun YANG ,  Yan ZHANG ,  Zhaoxue HU ,  Jian DING

IPC: C07D491/048 ,  C07D519/00 ,  A61P35/00

Abstract: Provided are a heterocyclic amide compound of general formula (I), a pharmaceutically acceptable salt thereof and a preparation method therefor, and the use of the compound in the preparation of a drug for treating diseases related to the activity of STING, in the preparation of an immunologic adjuvant, and in the preparation of a drug for activating STING.

公开(公告)号：US20220204518A1

公开(公告)日：2022-06-30

申请号：US17606121

申请日：2020-04-24

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

Inventor： Ao ZHANG ,  Jian DING ,  Hua XIE ,  Zilan SONG ,  Yu XUE ,  Li XING ,  Linjiang TONG ,  Meiyu GENG

IPC: C07D487/14 ,  A61P35/00

Abstract: The present invention relates to a pyrimido[5,4-b]pyrrolizin compound represented by general formula I, an optical isomer thereof, a preparation method therefor, a pharmaceutical composition containing same, and a use thereof. The compound according to the present invention has good inhibitory activity on the kinase BTK at both the molecular level and the cellular level. Meanwhile, the compound also has good anti-tumor activity and pharmacokinetic properties in vivo.

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：US20170066723A1

公开(公告)日：2017-03-09

申请号：US15120771

申请日：2015-02-15

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

Inventor： Wenhu DUAN ,  Jian DING ,  Yongcong LV ,  Hua XIE

IPC: C07D231/56 ,  C07D261/20 ,  C07D413/12 ,  C07D401/12 ,  C07D491/048 ,  C07D495/04

CPC classification number: C07D231/56 ,  C07D261/20 ,  C07D401/12 ,  C07D413/12 ,  C07D491/048 ,  C07D495/04

Abstract: The present invention relates to a naphthylamide compound of the structure as represented by formula (I), medicinal salts, prodrugs and hydrates or solvates thereof, and also relates to a method of preparing the compounds, pharmaceutical compositions comprising the compounds and the uses thereof as protein tyrosine kinase inhibitors, particularly as VEGFR-2 inhibitors, in preparing drugs for preventing and treating diseases related to abnormal angiogenesis.

Abstract translation: 本发明涉及由式（I）表示的结构的萘酰胺化合物，其药物盐，前药和水合物或溶剂化物，还涉及制备该化合物的方法，包含该化合物的药物组合物及其用途为 蛋白酪氨酸激酶抑制剂，特别是作为VEGFR-2抑制剂，在制备用于预防和治疗与异常血管生成有关的疾病的药物中。

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.