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：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：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：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：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：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.

公开(公告)号：US20190375727A1

公开(公告)日：2019-12-12

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

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.