公开(公告)号：US11591325B2

公开(公告)日：2023-02-28

申请号：US16348499

申请日：2017-11-08

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

Inventor： Tao Liu ,  Jia Li ,  Yongzhou Hu ,  Yubo Zhou ,  Xiaowu Dong ,  Anhui Gao ,  Pinrao Song ,  Peipei Wang ,  Lexian Tong ,  Xiaobei Hu ,  Mingbo Su

IPC: C07D413/14 ,  A61P35/02 ,  A61P35/00 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14

Abstract: The present invention provides a 2-polysubstituted aromatic ring-pyrimidine derivative and an optical isomer thereof, or a pharmaceutically acceptable salt or solvate thereof, the compound, and an optical isomer thereof or a pharmaceutically thereof acceptable salts or solvates can be used in the preparation of anti-tumor drugs. The invention designs and synthesizes a series of novel small molecule Chk1 inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained by structure-based virtual screening as a lead compound, and carries out Chk1 kinase inhibitory activity test. The experiment confirmed that said compounds possess potent anticancer activity, Chk1 kinase inhibitory activity, and are promising Chk1 inhibitors, and can be used as new cancer therapeutic drugs, which can be applied to treat solid tumors or hematologic tumors related to proliferative disease of human or animal. The 2-polysubstituted aromatic ring-pyrimidine derivatives provided by the present invention has the structure of the formula I:

公开(公告)号：US20230054250A1

公开(公告)日：2023-02-23

申请号：US17792499

申请日：2021-01-14

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

Inventor： Yong GAN ,  Shiyan GUO ,  Yinyin SUN

IPC: A61K9/127 ,  A61K31/167 ,  A61K31/277 ,  A61K31/5415 ,  A61K31/4748 ,  A61K31/445 ,  A61K31/138 ,  A61K31/475 ,  A61K31/4365 ,  A61K31/245 ,  A61K31/366 ,  A61K31/4422 ,  A61K47/10 ,  A61K47/24 ,  A61K47/14 ,  A61K47/44 ,  A61K47/28 ,  A61K9/00

Abstract: A non-aqueous sustained release drug delivery system, which contains, based on the total weight of the sustained release drug delivery system, about 0.1-20% of an active agent, about 0.5-50% of a drug solvent, about 1-98% of a drug sustained release agent, about 0.1-85% of a drug solubilizer, about 0.1-10% of an efficacy enhancer, about 0-1% of an antioxidant, and about 0-8% of an acid-base regulator. The non-aqueous sustained release drug delivery system can yield an improved sustained release effect, improve bioavailability, and enhance the therapeutic effect.

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：US20230010368A1

公开(公告)日：2023-01-12

申请号：US17780449

申请日：2020-11-24

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

Inventor： Hong LIU ,  Yu ZHOU ,  Haiyan ZHANG ,  Yan FU ,  Jian LI ,  Hualiang JIANG ,  Xican TANG ,  Kaixian CHEN

IPC: C07D211/38

Abstract: The present invention provides a crystalline form of an acetylcholinesterase inhibitor, a preparation method therefor and application thereof. Specifically, the crystalline form is crystalline form A, crystalline form B and crystalline form C of 2-((1-(2-fluorobenzyl)-4-fluoropiperidin-4-yl) methylene)-5, 6-dimethoxy-2, 3-dihydro-1-indanone. The crystalline form of the present invention does not contain water and solvent, has high stability and low hygroscopicity, is easy to process, and is very suitable for preparing drugs for preventing and/or treating neurodegenerative diseases.

公开(公告)号：US11465984B2

公开(公告)日：2022-10-11

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 ,  C07D403/14 ,  C07D405/14

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：US11464795B2

公开(公告)日：2022-10-11

申请号：US16630309

申请日：2018-07-12

Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY ,  YUNNAN UNIVERSITY ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Honglin Li ,  Weilie Xiao ,  Lili Zhu ,  Lina Quan ,  Qiao Li ,  Yanyan Diao ,  Zhenjiang Zhao ,  Hualiang Jiang

IPC: A61K31/704 ,  A61P35/00 ,  A61K31/56

Abstract: Provided are use of a saponin compound of formula (I) or (II), or a pharmaceutically acceptable salt, prodrug or solvate thereof, in the manufacture of a medicament targeting PD-1. The medicament targeting PD-1 is one which treats a disease by inhibiting PD-1 from binding to a ligand thereof. The disease may be a tumor, an infection caused by a bacterium, a virus or a fungus, or an inflammatory disease.

公开(公告)号：US11406653B2

公开(公告)日：2022-08-09

申请号：US17256950

申请日：2019-06-28

Applicant: GREEN VALLEY (SHANGHAI) PHARMACEUTICALS CO., LTD. ,  SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

Inventor： Meiyu Geng ,  Xianliang Xin ,  Zhenqing Zhang ,  Jian Ding

IPC: A61P25/06 ,  A61K31/715 ,  A61K31/7032 ,  A61K31/702 ,  A61P25/04 ,  A61K31/7004 ,  A61K31/7016

Abstract: The present invention relates to the use of mannuronic diacid oligosaccharide composition in the treatment of pain.

公开(公告)号：US20220213083A1

公开(公告)日：2022-07-07

申请号：US17603823

申请日：2020-04-20

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

Inventor： Huaqiang XU ,  Jia LI ,  Jingjing SHI ,  Yi ZANG ,  Dandan SUN ,  Mingliang LIU ,  Rongrong XIE ,  Erli YOU ,  Lixin GAO ,  Qian TAN

IPC: C07D413/14 ,  C07D487/08 ,  A61P1/16

Abstract: An FXR small molecule agonist and a preparation method therefor and a use thereof, having a structure as shown in formula (I). The compound represented by formula (I) has FXR agonistic activity and is capable of preparing drugs for treatment of FXR-related diseases.

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：US11191761B2

公开(公告)日：2021-12-07

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 ,  A61K47/10 ,  A61K9/10 ,  A61K9/20 ,  A61K9/08 ,  A61K9/14

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.