公开(公告)号：US10829464B2

公开(公告)日：2020-11-10

申请号：US16461234

申请日：2017-11-17

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

Inventor： Jian Li ,  Lefu Lan ,  Baoli Li ,  Feifei Chen ,  Shuaishuai Ni ,  Yifu Liu ,  Hanwen Wei ,  Fei Mao ,  Jin Zhu

IPC: C07D307/81 ,  A61P31/04 ,  A61P31/10 ,  C07D307/82 ,  C07D333/58 ,  C07D409/12

Abstract: Disclosed are benzoheterocyclic alkylamine compounds, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, and a preparation method thereof, and use of the same in the manufacture of an antibacterial drug as an inhibitor of staphyloxanthin synthesis in Staphylococcus aureus.

公开(公告)号：US20140323466A1

公开(公告)日：2014-10-30

申请号：US14361920

申请日：2012-10-23

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

Inventor： Hong Liu ,  Jia Li ,  Jian Li ,  Jingya Li ,  Jiang Wang ,  Mingbo Su ,  Jie Lian ,  Hualiang Jiang ,  Kaixian Chen

IPC: C07D495/04

CPC classification number: C07D495/04

Abstract: Disclosed are new thienyl[3,2-d]pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.

Abstract translation: 公开了通式（I）所示的新的噻吩并[3,2-d]嘧啶-4-酮化合物，其制备方法，药物组合物及其药理用途。 该化合物是强DPPIV（二肽肽酶IV）抑制剂，可以通过良好地抑制DPPIV来间接增加体内GLP-1的含量并在体内诱导一系列生理作用来治疗II型糖尿病。 因此，这些化合物可被开发为用于治疗糖尿病的新的有希望的药物。

公开(公告)号：US10392401B2

公开(公告)日：2019-08-27

申请号：US15549918

申请日：2016-02-03

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

Inventor： Hong Liu ,  Jiang Wang ,  Jian Li ,  Jia Li ,  Jingya Li ,  Shengbin Zhou ,  Mingbo Su ,  Hualiang Jiang ,  Xiaomin Luo ,  Kaixian Chen

IPC: C07D495/04 ,  A61K31/519

Abstract: The present invention relates to crystal form A of a compound. The present invention also discloses a preparation method and a pharmaceutical composition of the crystal form A. The crystal form A has strong hypoglycemic activity in vivo and is expected to be a novel pharmaceutically active ingredient for treating or preventing type II diabetes and/or complications of type II diabetes.

公开(公告)号：US10167299B2

公开(公告)日：2019-01-01

申请号：US15109101

申请日：2014-12-29

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

Inventor： Hong Liu ,  Beili Wu ,  Yongtang Zheng ,  Xin Xie ,  Hualiang Jiang ,  Panfeng Peng ,  Ronghua Luo ,  Jing Li ,  Jian Li ,  Ya Zhu ,  Ying Chen ,  Haonan Zhang ,  Liumeng Yang ,  Yu Zhou ,  Kaixian Chen

IPC: C07D519/00 ,  C07D409/14 ,  C07D451/04 ,  C07D401/14 ,  A61K45/06 ,  A61K31/46 ,  A61K31/4545 ,  A61K31/454

Abstract: Provided are 1-(3-aminopropyl) substituted cyclic amine compounds as represented by frmula (I), pharmaceutically acceptable salts, enantiomers, diastereoisomers, racemates and mixtures thereof, and a method of synthesizing said 1-(3-aminopropyl) substituted cyclic amine compounds by using aromatic heterocyclic formaldehyde as raw material. Said compounds can be used as CCR 5 antagonist for the treatment of HIV infection.

公开(公告)号：US12152017B2

公开(公告)日：2024-11-26

申请号：US17267375

申请日：2019-08-09

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

Inventor： Hong Liu ,  Shibo Jiang ,  Wenhao Dai ,  Lu Lu ,  Jingjing Peng ,  Shuai Xia ,  Jiang Wang ,  Jian Li ,  Hualiang Jiang ,  Kaixian Chen

IPC: C07D403/12 ,  A61P31/12 ,  C07D209/20 ,  C07D241/44 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D471/04

Abstract: A ketoamide compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically, the ketoamide compound shown in formula (A), a racemate, an enantiomer, or a diastereoisomer thereof, or any mixture of same, or a pharmaceutically active metabolite thereof, or a pharmaceutically acceptable salt, solvate, or prodrug thereof. The ketoamide compound can effectively inhibit coronavirus or Ebola virus, and thereby implement the prevention or treatment of diseases related to coronavirus or diseases related to Ebola virus.

公开(公告)号：US20220112177A1

公开(公告)日：2022-04-14

申请号：US17267375

申请日：2019-08-09

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

Inventor： Hong Liu ,  Shibo Jiang ,  Wenhao Dai ,  Lu Lu ,  Jingjing Peng ,  Shuai Xia ,  Jiang Wang ,  Jian Li ,  Hualiang Jiang ,  Kaixian Chen

IPC: C07D403/12 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D209/20 ,  C07D241/44 ,  C07D413/12 ,  A61P31/12 ,  C07D471/04

Abstract: A ketoamide compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically, the ketoamide compound shown in formula (A), a racemate, an enantiomer, or a diastereoisomer thereof, or any mixture of same, or a pharmaceutically active metabolite thereof, or a pharmaceutically acceptable salt, solvate, or prodrug thereof. The ketoamide compound can effectively inhibit coronavirus or Ebola virus, and thereby implement the prevention or treatment of diseases related to coronavirus or diseases related to Ebola virus.

公开(公告)号：US09045491B2

公开(公告)日：2015-06-02

申请号：US14361920

申请日：2012-10-23

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

Inventor： Hong Liu ,  Jia Li ,  Jian Li ,  Jingya Li ,  Jiang Wang ,  Mingbo Su ,  Jie Lian ,  Hualiang Jiang ,  Kaixian Chen

IPC: C07D495/04 ,  A61K31/55

CPC classification number: C07D495/04

Abstract: Disclosed are new thienyl [3,2-d] pyrimidin-4-one compounds shown as the general formula (I), preparation method, pharmaceutical compositions and pharmacological use thereof. The compounds are strong DPPIV (dipeptide peptidase IV) inhibitors and can treat type II diabetes through well inhibiting DPPIV indirectly increasing the content of GLP-1 in vivo and inducing a series of physiological actions in vivo. Therefore, the compounds could be developed as new promising drugs for treating diabetes.

Abstract translation: 公开了通式（I）所示的新的噻吩并[3,2-d]嘧啶-4-酮化合物，其制备方法，药物组合物及其药理用途。 该化合物是强DPPIV（二肽肽酶IV）抑制剂，可以通过良好地抑制DPPIV来间接增加体内GLP-1的含量并在体内诱导一系列生理作用来治疗II型糖尿病。 因此，这些化合物可被开发为用于治疗糖尿病的新的有希望的药物。

公开(公告)号：US10550143B2

公开(公告)日：2020-02-04

申请号：US15738675

申请日：2016-06-23

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

Inventor： Hong Liu ,  Jia Li ,  Jiang Wang ,  Jingya Li ,  Hui Chen ,  Dan Li ,  Jian Li ,  Yibing Wang ,  Hualiang Jiang ,  Kaixian Chen

IPC: C07H19/01 ,  A61P3/08

Abstract: C, O-spiro aryl glycoside compounds are provided. Specifically provided are C, O-spiro aryl glycoside compounds represented by the formula (I), wherein the definitions of each variable group are described in the specification. Also provided are methods of preparing and using the C, O-spiro aryl glycoside compounds. The C, O-spiro aryl glycoside compounds can be used as SGLT2 inhibitors and for treating diseases, such as diabetes, atherosclerosis, and adiposity.