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：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：US10927107B2

公开(公告)日：2021-02-23

申请号：US16089713

申请日：2017-03-29

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

Inventor： Hong Liu ,  Yiping Wang ,  Fei Zhao ,  Jing Zhao ,  Jiang Wang ,  Cong Xi ,  Chenglin Wu ,  Hao Shen ,  Xu Han ,  Hualiang Jiang ,  Kaixian Chen

IPC: C07D459/00 ,  C07D495/22 ,  A61K31/4745 ,  C07D491/22 ,  C07D471/14 ,  A61P3/06

Abstract: The present invention relates to phenyl [a]indole[2,3-g]quinolizine compounds represented by formula (I), a preparation method therefor, a pharmaceutical composition, and applications thereof. Specific applications are applications in the preparation of drugs for treating diseases related to a proprotein convertase subtilisin Kexin-9 (PCSK9), comprising the applications in the preparation of drugs for treating hyperlipemia, hypercholesterolemia, hypertriglyceridemia, fatty liver deformation, atherosclerosis, obesity and other metabolic diseases.

公开(公告)号：US10800776B2

公开(公告)日：2020-10-13

申请号：US16302154

申请日：2017-05-17

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

Inventor： Hong Liu ,  Yu Zhou ,  Wenjing Xia ,  Dong Zhang ,  Hualiang Jiang ,  Kaixian Chen

IPC: A61K31/4196 ,  A61K31/437 ,  C07D471/04 ,  A61P25/18 ,  A61P25/28 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/4709 ,  A61K31/496 ,  A61P25/22 ,  A61P25/24

Abstract: A fluorine-containing triazolopyridine represented by formula (I) and a racemate, R-stereoisomer, S-stereoisomer, pharmaceutically acceptable salt, or mixture thereof are described. The triazolopyridine can be used as a positive allosteric modulator of an mGluR2, and is highly selective in activating the mGluR2, exerting no activation or very limited activation of other homologous metabotropic glutamate receptor. The triazolopyridine can thus be used to prepare a product for treating an mGluR2-related disease, such as a central nervous system disease or neurological disease.

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：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：US10966996B2

公开(公告)日：2021-04-06

申请号：US15126676

申请日：2015-03-17

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES ,  NANJING PAILEXING PHARMACEUTICAL TECHNOLOGY LTD.

Inventor： Weiliang Zhu ,  Heyao Wang ,  Yong Zhang ,  Peng Sun ,  Bo Li ,  Zhijian Xu ,  Hualiang Jiang ,  Kaixian Chen

IPC: A61K36/00 ,  A61K31/7048 ,  A61K36/53

Abstract: Disclosed is a Glechoma longituba (Nakai) Kupr. extract, specifically compounds I and II, a preparation method for same, and a use thereof in preparing a medicament for blood glucose decease, blood lipids decrease, weight loss, and kidney disease treatment or a method for treatment of said diseases, and a composition containing the extract.

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.

公开(公告)号：US09751882B2

公开(公告)日：2017-09-05

申请号：US14400203

申请日：2013-05-09

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

Inventor： Hong Liu ,  Xuechu Zhen ,  Haifeng Sun ,  Liyuan Zhu ,  Wangke Qian ,  Leiping Yu ,  Zeng Li ,  Shengbin Zhou ,  Wenxian Cai ,  Hualiang Jiang ,  Kaixian Chen

IPC: C07D471/14 ,  C07D495/14 ,  C07D491/22 ,  C07D491/147 ,  C07D495/22 ,  C07D455/03

CPC classification number: C07D471/14 ,  C07D455/03 ,  C07D491/147 ,  C07D491/22 ,  C07D495/14 ,  C07D495/22

Abstract: The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors.