公开(公告)号：US12240841B2

公开(公告)日：2025-03-04

申请号：US17603823

申请日：2020-04-20

Applicant: Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Van Andel Research Institute

Inventor： Huaqiang Xu ,  Jia Li ,  Jingjing Shi ,  Yi Zang ,  Dandan Sun ,  Mingliang Liu ,  Rongrong Xie ,  Erli You ,  Lixin Gao ,  Qian Tan

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

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：US11873292B2

公开(公告)日：2024-01-16

申请号：US16306751

申请日：2017-06-02

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

Inventor： Hong Liu ,  Jia Li ,  Wei Zhu ,  Yubo Zhou ,  Jiang Wang ,  Mingbo Su ,  Shuni Wang ,  Wei Xu ,  Chunpu Li ,  Weijuan Kan ,  Hualiang Jiang ,  Kaixian Chen

IPC: C07D403/12 ,  C07D215/58 ,  C07D209/04 ,  C07D215/00 ,  C07D487/04 ,  C07D209/08 ,  C07D401/12 ,  C07D405/12 ,  A61P35/00

CPC classification number: C07D403/12 ,  A61P35/00 ,  C07D209/04 ,  C07D209/08 ,  C07D215/00 ,  C07D215/58 ,  C07D401/12 ,  C07D405/12 ,  C07D487/04 ,  Y02P20/55

Abstract: The present invention relates to the fields of medicinal chemistry and pharmacotherapy, and specifically relates to the chemical compound of formula (I), and its racemate, R-isomer, S-isomer, pharmaceutically acceptable salt, and mixtures thereof, as well as its method for preparation, a pharmaceutical composition containing said chemical compound, and use as a lysine-specific demethylase 1 (LSD 1) inhibitor. The cyclopropylamine chemical compound to which the present invention relates may be used in the treatment of cancer.

公开(公告)号：US10793566B2

公开(公告)日：2020-10-06

申请号：US16420140

申请日：2019-05-22

Applicant: Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Inventor： Xibin Liao ,  Jia Li ,  Zhijian Lu ,  Yubo Zhou ,  Anhui Gao

IPC: C07D471/04 ,  C07D403/04 ,  C07D401/04 ,  A61P35/00 ,  A61K31/52

Abstract: Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I):

公开(公告)号：US10414713B2

公开(公告)日：2019-09-17

申请号：US16075528

申请日：2017-02-20

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

Inventor： Fajun Nan ,  Jia Li ,  Jingya Li ,  Mei Zhang ,  Zhifu Xie ,  Jingtao Wang ,  Dongdong Guo

IPC: A61K31/194 ,  C07C55/28 ,  C07C57/13 ,  C07C57/42 ,  C07C57/26 ,  C07C61/16 ,  C07C61/20 ,  C07C61/22 ,  C07C61/35

Abstract: The present invention relates to a class of fatty acid compounds, a preparation method thereof and use thereof. The fatty acid compounds have the structure of the formula I, which has the ability to activate APMK and inhibit the glucose output in mouse primary hepatocytes. The fatty acid compounds can be used in preparing a medicament for the treatment of obesity or diabetes.

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：US10766889B2

公开(公告)日：2020-09-08

申请号：US16329336

申请日：2017-08-24

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

Inventor： Fajun Nan ,  Jia Li ,  Jian Ding ,  Meiyu Geng ,  Yangming Zhang ,  Yi Chen ,  Yubo Zhou ,  Chaojun Gong ,  Mingbo Su ,  Anhui Gao

IPC: C07D277/56 ,  C07D277/60 ,  C07D417/04 ,  A61P35/02 ,  A61K31/427 ,  A61P35/00

Abstract: The invention describes an aryl-2,2′-tandem bisthiazole compound and a preparation method and the use thereof. In particular, disclosed in the present invention are an aryl-2,2′-tandem bisthiazole compound with the structure as shown in general formula I and the preparation method thereof and use thereof as a histone deacetylase inhibitor in the preparation of antitumor drugs.

公开(公告)号：US10358446B2

公开(公告)日：2019-07-23

申请号：US15763095

申请日：2016-10-03

Applicant: Zibo Biopolar Changsheng Pharmaceutical Co. Ltd. ,  Shanghai Institute of Materia Medica, Chinese Academy of Sciences

Inventor： Xibin Liao ,  Jia Li ,  Zhijian Lu ,  Yubo Zhou ,  Anhui Gao

IPC: C07D471/04 ,  A61K31/437 ,  C07D473/34 ,  A61K31/52 ,  A61P35/00 ,  A61P29/00 ,  A61K31/4184 ,  C07D235/22 ,  C07D487/04 ,  A61K31/42 ,  A61K31/4545 ,  A61K31/501 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/56 ,  A61K45/06

Abstract: Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I):

公开(公告)号：US10233180B2

公开(公告)日：2019-03-19

申请号：US15128298

申请日：2015-03-21

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

Inventor： Xiaowu Dong ,  Jia Li ,  Bo Yang ,  Yongzhou Hu ,  Yubo Zhou ,  Qinjie Weng ,  Wenhu Zhan ,  Lei Xu ,  Tao Liu ,  Qiaojun He

IPC: C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: Disclosed are new substituted nitrogen-containing heterocyclic derivatives represented by formula (I) as AKT inhibitors, optical isomers, pharmaceutically acceptable salts or solvates thereof, wherein the definition of R1, R2, R3, R4, R5, R6, ring A, ring C, B, Q, Y, Z and m is shown in the description for details. In addition, medicaments comprising the derivatives as active components are also disclosed, which can be useful for treating proliferative diseases, such as cancer and inflammation, especially diseases relating to AKT kinase.

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：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.