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：US20240351986A1

公开(公告)日：2024-10-24

申请号：US18683623

申请日：2022-07-26

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

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

IPC: 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 classification number: 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

Abstract: 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

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：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：US20200172502A1

公开(公告)日：2020-06-04

申请号：US16623297

申请日：2018-05-31

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  FUKANG (SHANGHAI) HEALTH TECHNOLOGY CO., LTD.

Inventor： Chunhao YANG ,  Zehong MIAO ,  Cun TAN ,  Xiajuan HUAN ,  Jian DING ,  Yi CHEN

IPC: C07D307/84

Abstract: Disclosed are a 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride polymorph, a preparation method therefor and an application thereof. Specifically, disclosed are three crystalline forms, i.e., crystalline forms A, B, and C, of 2-[4-(methylaminomethyl)phenyl]-5-fluoro-benzofuran-7-carboxamide hydrochloride (formula I), preparation methods for the three crystalline forms, and use of the three crystalline forms in preparation of drugs.

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：US20180133215A1

公开(公告)日：2018-05-17

申请号：US15574557

申请日：2016-05-13

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  Shanghai Acebright Pharmaceuticals Co., Ltd.

Inventor： Shiyan GUO ,  Yong GAN ,  Ao ZHANG ,  Zehong MIAO ,  Li GAO ,  Jian DING

IPC: A61K31/502 ,  A61K47/40 ,  A61K47/38 ,  A61K47/34 ,  A61K47/32 ,  A61K9/48 ,  A61K9/28 ,  A61P35/00

CPC classification number: A61K31/502 ,  A61K9/08 ,  A61K9/10 ,  A61K9/146 ,  A61K9/2018 ,  A61K9/2054 ,  A61K9/28 ,  A61K9/4858 ,  A61K9/4866 ,  A61K47/10 ,  A61K47/32 ,  A61K47/34 ,  A61K47/38 ,  A61K47/40 ,  A61P35/00

Abstract: Disclosed is an SOMCL-9112 solid dispersion. The SOMCL-9112 solid dispersion is characterized by being prepared from the following raw materials in percentage by weight: 5 percent to 60 percent of SOMCL-9112, 5 percent to 90 percent of pharmaceutically acceptable matrix polymer, 0 percent to 20 percent of surfactant, 0 percent to 20 percent of flow aid and 0 percent to 20 percent of plasticizer. Also disclosed are a preparation method of the SOMCL-9112 solid dispersion, a solid medicinal preparation containing the solid dispersion and application of the solid dispersion for preparing a medicine for treating cancer.

公开(公告)号：US20180036293A1

公开(公告)日：2018-02-08

申请号：US15523315

申请日：2015-11-01

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

Inventor： Xingdong ZHAO ,  Jian DING ,  Linghua MENG ,  Meiyu GENG ,  Tongshuang LI ,  Zuwen ZHOU ,  Ling CHEN ,  Qihong LIU ,  Xianlong WANG ,  Lijun YANG ,  Yue RONG ,  Rui TAN ,  Chuiliang YU ,  Lihua JIANG ,  Yanxin LIU ,  Li LINGHU ,  Jing SUN ,  Weibo WANG

IPC: A61K31/437 ,  C07D519/00 ,  A61K45/06 ,  A61K31/4375 ,  A61K31/52

CPC classification number: A61K31/437 ,  A61K31/4375 ,  A61K31/505 ,  A61K31/52 ,  A61K45/06 ,  C07D519/00 ,  A61K2300/00

Abstract: Provided are certain PI3K inhibitors, pharmaceutical compositions thereof, and methods of use therefor.