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：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：US20230295144A1

公开(公告)日：2023-09-21

申请号：US18100782

申请日：2023-01-24

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

CPC classification number: C07D413/14 ,  A61P35/00 ,  A61P35/02 ,  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：US20210284625A1

公开(公告)日：2021-09-16

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

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：US20190210998A1

公开(公告)日：2019-07-11

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 ,  A61P35/00 ,  C07D209/08 ,  C07D405/12 ,  C07D401/12 ,  C07D215/58

CPC classification number: C07D403/12 ,  A61P35/00 ,  C07D209/04 ,  C07D209/08 ,  C07D215/00 ,  C07D215/58 ,  C07D401/12 ,  C07D405/12 ,  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：US10822327B2

公开(公告)日：2020-11-03

申请号：US16348502

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: C07D401/14 ,  A61P35/00 ,  C07D401/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

Abstract: A 2-substituted aromatic ring-pyrimidine derivative as shown in a general formula I, and an optical isomer or a pharmaceutically acceptable salt or a solvate thereof are provided. The present invention designs and synthesizes a series of novel small molecular Chk1 inhibitors by using N-substituted pyridin-2-aminopyrimidine obtained through structure-based virtual screening as a lead compound, and carries out Chk1 kinase inhibitory activity test. The experiment confirmed that said compounds possess strong anti-cancer effect, Chk1 kinase inhibitory activity and are promising Chk1 inhibitors. The compounds 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.