公开(公告)号：US20230138310A1

公开(公告)日：2023-05-04

申请号：US17759807

申请日：2020-03-26

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  FRONTIER BIOTECHNOLOGIES INC.

Inventor： Hong LIU ,  Jian LI ,  Wenhao DAI ,  Jingjing PENG ,  Xiong XIE ,  Shulei HU ,  Chunpu LI ,  Yechun XU ,  Haitao YANG ,  Leike ZHANG ,  Haixia SU ,  Hualiang JIANG ,  Zhenming JIN ,  Gengfu XIAO ,  Kaixian CHEN

IPC: C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D401/12 ,  C07D411/12 ,  C07D471/04 ,  C07D207/12 ,  A61P31/14

Abstract: Use of an aldehyde-based compound as represented by general formula I, a pharmaceutical composition, a pharmaceutical salt, an enantiomer, a diastereomer and a racemic compound thereof as a novel coronavirus 2019 (2019-nCov) 3CL protease inhibitor in preparation of a medicament for treating and/or preventing and relieving respiratory tract infections, pneumonia and other related diseases caused by the novel coronavirus infection 2019.

公开(公告)号：US20160074373A1

公开(公告)日：2016-03-17

申请号：US14762980

申请日：2014-01-23

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  THE UNIVERSTIY OF CHICAGO

Inventor： Chuan HE ,  Jing WANG ,  Hualiang JIANG ,  Cheng LUO ,  Hong LIU ,  Junyan LU

IPC: A61K31/4365 ,  A61K31/4355 ,  A61K31/4375 ,  A61K31/444

CPC classification number: A61K31/4365 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/444 ,  A61K31/4741 ,  A61K31/4743 ,  A61K45/06 ,  C07D491/048 ,  C07D491/147 ,  C07D495/04 ,  C07D495/14 ,  A61K2300/00

Abstract: Compositions and methods concern organic molecules that bind to human Atox1 and CCS at the copper trafficking interface of these proteins. This binding suppresses copper trafficking, which leads to inhibition of cancer cell proliferation and tumor growth. In addition to serving as an effective treatment of cancer, these organic molecules inhibit cellular copper uptake and can be used as treatment of disorders of copper metabolism such as Wilson's disease, which is characterized by copper overload, as well as wound healing.

Abstract translation: 组合物和方法涉及在这些蛋白质的铜贩运界面处结合人Atox1和CCS的有机分子。 这种结合抑制铜贩运，这导致癌细胞增殖和肿瘤生长的抑制。 除了作为癌症的有效治疗之外，这些有机分子抑制细胞铜摄取，并且可以用作铜代谢紊乱的治疗，例如以铜超载为特征的威尔逊氏病以及伤口愈合。

公开(公告)号：US20240279177A1

公开(公告)日：2024-08-22

申请号：US18392472

申请日：2023-12-21

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

Inventor： Hong LIU ,  Ben NIU ,  Chunpu LI ,  Jianping CHEN ,  Kun HUANG ,  Jiang WANG

IPC: C07D211/60 ,  C07D401/12 ,  C07D409/12

CPC classification number: C07D211/60 ,  C07D401/12 ,  C07D409/12

Abstract: The present invention relates to the fields of medicinal chemistry and pharmaco therapeutics, and specifically to a method for preparing a compound of formula I and a chemically acceptable salt thereof.

公开(公告)号：US20180305390A1

公开(公告)日：2018-10-25

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

CPC classification number: C07H19/01 ,  A61K31/35 ,  A61K31/381 ,  A61K31/427 ,  A61K31/4436 ,  A61P3/08 ,  C07D493/10

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：US20160193195A1

公开(公告)日：2016-07-07

申请号：US14888797

申请日：2014-05-04

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

Inventor： Hong LIU ,  Xin XIE ,  Haifeng SUN ,  Jing LI ,  Fei ZHAO ,  Ying CHEN ,  Zeng LI ,  Yu ZHOU ,  Hualiang JIANG ,  Kaixian CHEN

IPC: A61K31/4375

CPC classification number: A61K31/4375

Abstract: Use of hexahydro-dibenzo[a,g]quinolizine compounds as shown in formula(I) in preparing a medicine for treating and/or preventing benign prostate hyperplasia diseases.

Abstract translation: 式（I）所示的六氢 - 二苯并[a，g]喹嗪化合物在制备治疗和/或预防良性前列腺增生疾病的药物中的用途。

公开(公告)号：US20140088130A1

公开(公告)日：2014-03-27

申请号：US14091979

申请日：2013-11-27

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

Inventor： Hong LIU ,  Xin XIE ,  Xuechu ZHEN ,  Haifeng SUN ,  Jing LI ,  Liyuan ZHU ,  Zeng LI ,  Ying CHEN ,  Hualiang JIANG ,  Kaixian CHEN

IPC: C07D491/147 ,  C07D491/22 ,  C07D455/03

CPC classification number: C07D491/153 ,  C07C69/736 ,  C07C231/14 ,  C07D217/20 ,  C07D311/20 ,  C07D455/03 ,  C07D491/056 ,  C07D491/147 ,  C07D491/22

Abstract: The present invention relates to a novel hexahydrodibenzo[a,g]quinoline compound represented by general formula (I) and its derivatives, enantiomer, diastereoisomer, raceme and mixtures thereof, as well as pharmaceutically acceptable salts thereof. The present invention further relates to a method for preparing the compound, and the compound has good prevention and treatment effect on neurological diseases, especially diseases associated with dopamine receptor and 5-hydroxytryptamine receptor. The bioactivity experiment demonstrates that, the compound is expected to be developed into a novel and potent chemical entity for treating diseases associated with dopamine receptor and 5-hydroxytryptamine receptor, especially schizophrenia, Parkinson's disease, drug addiction, migraine and so on.

Abstract translation: 本发明涉及由通式（I）表示的新型六氢二苯并[a，g]喹啉化合物及其衍生物，对映体，非对映异构体，外消旋及其混合物，以及其药学上可接受的盐。 本发明还涉及一种制备该化合物的方法，该化合物对神经系统疾病，特别是与多巴胺受体和5-羟色胺受体相关的疾病具有良好的预防和治疗作用。 生物活性实验表明，该化合物预计将发展成为一种新颖有力的化学实体，用于治疗与多巴胺受体和5-羟色胺受体，特别是精神分裂症，帕金森病，药物成瘾，偏头痛等有关的疾病。

公开(公告)号：US20210221807A1

公开(公告)日：2021-07-22

申请号：US17057199

申请日：2019-05-21

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

Inventor： Hong LIU ,  Meiyu GENG ,  Yu ZHOU ,  Jian DING ,  Feifei FANG ,  Jing AI ,  Jian LI ,  Xia PENG ,  Hualiang JIANG ,  Yinchun JI ,  Kaixian CHEN

IPC: C07D471/04 ,  C07D519/00

Abstract: Provided are a class of fused-cyclic pyrazolone formamide compounds and a preparation method therefor, a pharmaceutical composition and the use thereof. Specifically, provided is a compound having the structure as shown in formula (I) (with each group defined in the description). The compound can be used as an AXL inhibitor in the preparation of a pharmaceutical composition for treating tumors.

公开(公告)号：US20190202827A1

公开(公告)日：2019-07-04

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: C07D471/04 ,  A61P25/24 ,  A61P25/22

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：US20190135818A1

公开(公告)日：2019-05-09

申请号：US16304508

申请日：2017-05-24

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

Inventor： Hualiang JIANG ,  Hong LIU ,  Meiyu GENG ,  Mingyue ZHENG ,  Jing AI ,  Yulan WANG ,  Xiaowei WU ,  Shuangjie LI ,  Xia PENG ,  Chunpu LI ,  Kaixian CHEN ,  Bao WANG

IPC: C07D487/04 ,  A61P35/00

Abstract: The present invention provides a compound comprising a 5-membered heterocycle fused with a pyridazinone, wherein the compound is used as an FGFR kinase inhibitor, and a manufacturing method and application thereof. The invention specifically provides a compound as represented by formula (I). Various radicals are as defined in the specification. The compound provided by the invention effectively inhibits an activity of an FGFR kinase, and can be used to manufacture a pharmaceutical product for treating a disease related to the activity of the FGFR kinase.

公开(公告)号：US20190031678A1

公开(公告)日：2019-01-31

申请号：US16087318

申请日：2017-03-22

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

Inventor： Hong LIU ,  Jiang WANG ,  Jian LI ,  Jia LI ,  Jingya LI ,  Hualiang JIANG ,  Xiaomin LUO ,  Kaixian CHEN

IPC: C07D495/04 ,  A61P3/10

Abstract: The invention relates to a salt form of (R)-methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothiophene[3,2-d]pyrimidine-6-carboxylic acid and a preparation method for the salt form. Also disclosed is a pharmaceutical composition of the formula I compound salt form. The salt form of the invention provides powerful in vivo hypoglycemic activity and is expected to be a novel pharmaceutical active ingredient for treating or preventing diabetes mellitus type 2 and/or complications of diabetes mellitus type 2