公开(公告)号：US20220112177A1

公开(公告)日：2022-04-14

申请号：US17267375

申请日：2019-08-09

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences ,  Fudan University

发明人： Hong Liu ,  Shibo Jiang ,  Wenhao Dai ,  Lu Lu ,  Jingjing Peng ,  Shuai Xia ,  Jiang Wang ,  Jian Li ,  Hualiang Jiang ,  Kaixian Chen

IPC分类号： C07D403/12 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D209/20 ,  C07D241/44 ,  C07D413/12 ,  A61P31/12 ,  C07D471/04

摘要： A ketoamide compound and a preparation method, a pharmaceutical composition, and a use thereof. Specifically, the ketoamide compound shown in formula (A), a racemate, an enantiomer, or a diastereoisomer thereof, or any mixture of same, or a pharmaceutically active metabolite thereof, or a pharmaceutically acceptable salt, solvate, or prodrug thereof. The ketoamide compound can effectively inhibit coronavirus or Ebola virus, and thereby implement the prevention or treatment of diseases related to coronavirus or diseases related to Ebola virus.

公开(公告)号：US11873292B2

公开(公告)日：2024-01-16

申请号：US16306751

申请日：2017-06-02

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

发明人： 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分类号： C07D403/12 ,  C07D215/58 ,  C07D209/04 ,  C07D215/00 ,  C07D487/04 ,  C07D209/08 ,  C07D401/12 ,  C07D405/12 ,  A61P35/00

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

摘要： 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：US20140323466A1

公开(公告)日：2014-10-30

申请号：US14361920

申请日：2012-10-23

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  CISEN PHARMACEUTICAL CO., LTD.

发明人： Hong Liu ,  Jia Li ,  Jian Li ,  Jingya Li ,  Jiang Wang ,  Mingbo Su ,  Jie Lian ,  Hualiang Jiang ,  Kaixian Chen

IPC分类号： C07D495/04

CPC分类号： C07D495/04

摘要： 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.

摘要翻译： 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：US20190194185A1

公开(公告)日：2019-06-27

申请号：US16089713

申请日：2017-03-29

申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences

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

IPC分类号： C07D459/00 ,  C07D495/22 ,  A61P3/06

CPC分类号： C07D459/00 ,  A61K31/4745 ,  A61P3/06 ,  C07D471/14 ,  C07D491/22 ,  C07D495/22

摘要： 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：US09637454B2

公开(公告)日：2017-05-02

申请号：US14438457

申请日：2013-10-17

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Hong Liu ,  Haiyan Zhang ,  Yu Zhou ,  Yan Fu ,  Hualiang Jiang ,  Xican Tang ,  Kaixian Chen

IPC分类号： C07D211/32 ,  C07D405/06 ,  C07D451/04 ,  C07D211/38 ,  A61K45/06 ,  C07D211/34 ,  C07D471/08 ,  C07D491/107

CPC分类号： C07D211/32 ,  A61K45/06 ,  C07D211/34 ,  C07D211/38 ,  C07D405/06 ,  C07D451/04 ,  C07D471/08 ,  C07D491/107

摘要： The present invention relates to the field of pharmaceutical chemistry and pharmacotherapeutics, and in particular to compounds of general formula I, racemates, R-isomers, S-isomers, and pharmaceutically acceptable salts thereof and their mixtures, and the preparation methods thereof and a pharmaceutical composition containing the compounds and uses thereof as an acetylcholine esterase inhibitor.

公开(公告)号：US09359372B2

公开(公告)日：2016-06-07

申请号：US14683726

申请日：2015-04-10

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Hong Liu ,  Xin Xie ,  Xuechu Zhen ,  Haifeng Sun ,  Jing Li ,  Liyuan Zhu ,  Zeng Li ,  Ying Chen ,  Hualiang Jiang ,  Kaixian Chen

IPC分类号： A61K31/4741 ,  C07D491/12 ,  C07D491/153 ,  C07D455/03 ,  C07D491/147 ,  C07D491/22 ,  C07C69/736 ,  C07C231/14 ,  C07D217/20 ,  C07D311/20 ,  C07D491/056

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

摘要： 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.

摘要翻译： 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：US09045491B2

公开(公告)日：2015-06-02

申请号：US14361920

申请日：2012-10-23

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  CISEN PHARMACEUTICAL CO., LTD.

发明人： Hong Liu ,  Jia Li ,  Jian Li ,  Jingya Li ,  Jiang Wang ,  Mingbo Su ,  Jie Lian ,  Hualiang Jiang ,  Kaixian Chen

IPC分类号： C07D495/04 ,  A61K31/55

CPC分类号： C07D495/04

摘要： 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.

摘要翻译： 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

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Hong Liu ,  Jia Li ,  Jiang Wang ,  Jingya Li ,  Hui Chen ,  Dan Li ,  Jian Li ,  Yibing Wang ,  Hualiang Jiang ,  Kaixian Chen

IPC分类号： C07H19/01 ,  A61P3/08

摘要： 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

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

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

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

CPC分类号： C07D471/14 ,  C07D455/03 ,  C07D491/147 ,  C07D491/22 ,  C07D495/14 ,  C07D495/22

摘要： 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.

公开(公告)号：US09737517B2

公开(公告)日：2017-08-22

申请号：US14888797

申请日：2014-05-04

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES

发明人： Hong Liu ,  Xin Xie ,  Haifeng Sun ,  Jing Li ,  Fei Zhao ,  Ying Chen ,  Zeng Li ,  Yu Zhou ,  Hualiang Jiang ,  Kaixian Chen

IPC分类号： A61K31/4375

CPC分类号： A61K31/4375

摘要： 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.