公开(公告)号：US20230285389A1

公开(公告)日：2023-09-14

申请号：US17802898

申请日：2021-02-26

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

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

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

CPC分类号： A61K31/496 ,  A61P35/00 ,  C07K16/2818 ,  C07K16/2827

摘要： 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：US20240150300A1

公开(公告)日：2024-05-09

申请号：US18278063

申请日：2022-02-18

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

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

CPC分类号： C07D237/14 ,  A61P35/00 ,  A61P35/02 ,  C07C67/00 ,  C07C67/10 ,  C07D401/04 ,  C07D403/04

摘要： 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：US20240351986A1

公开(公告)日：2024-10-24

申请号：US18683623

申请日：2022-07-26

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Youhong HU ,  Yi CHEN ,  Zhicheng XIE ,  Jian DING ,  Xin LI ,  Yanfen FANG ,  Qianqian SHEN

IPC分类号： C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

CPC分类号： C07D213/75 ,  A61K31/4418 ,  A61K31/443 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/4985 ,  A61K31/505 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/55 ,  A61P35/00 ,  C07D239/42 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D487/04 ,  C07D498/04

摘要： The present invention relates to a urea compound containing 2-heteroaromatic ring substitution represented by formula (I), its enantiomers, diastereomers, racemates or mixtures thereof, or pharmaceutically acceptable salts thereof, solvate, metabolite or prodrug. The compound of formula (I) of the present invention has inhibitory activity against CDK9, and representative compounds have significant anti-tumor activity against CDK9 high-expressing tumor cells. Representative compounds have plasma stability and low clearance.

公开(公告)号：US20230032101A1

公开(公告)日：2023-02-02

申请号：US17772334

申请日：2020-10-23

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

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

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

摘要： 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

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

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

IPC分类号： C07D333/64 ,  C07D409/12

摘要： 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

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

发明人： 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分类号： C07D401/12 ,  A61P35/00

摘要： 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：US20220389025A1

公开(公告)日：2022-12-08

申请号：US17761252

申请日：2020-09-21

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

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

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

摘要： 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

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

IPC分类号： C07D487/14 ,  A61P35/00

摘要： 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

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

IPC分类号： C07D471/04 ,  C07D519/00

摘要： 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

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

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

摘要： 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.