公开(公告)号：US20210015824A1

公开(公告)日：2021-01-21

申请号：US16978563

申请日：2019-03-08

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

Inventor： Hong LIU ,  Jia LI ,  Jiang WANG ,  Yi ZANG ,  Jian LI ,  Jingya LI ,  Dandan SUN ,  Hualiang JIANG ,  Kaixian CHEN

IPC: A61K31/5377 ,  A61K31/519 ,  A61P1/16

Abstract: Disclosed is use of a thieno[3,2-d]pyrimidin-4-one compound represented by general formula (I). Definition of each substituent is as stated in the description and claims, and the compound is used for preparing medicines for treating and/or preventing liver fibrosis and related diseases or preparing a DPP-4 inhibitor, or is used as a DPP-4 inhibitor.

公开(公告)号：US20190100507A1

公开(公告)日：2019-04-04

申请号：US16085311

申请日：2017-03-16

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

Inventor： Hong LIU ,  Jia LI ,  Jiang WANG ,  Mingbo SU ,  Shuni WANG ,  Yubo ZHOU ,  Wei ZHU ,  Wei XU ,  Chunpu LI ,  Hualiang JIANG ,  Kaixian CHEN

IPC: C07D401/12 ,  C07D401/06 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D409/06 ,  C07D417/12 ,  C07D471/04 ,  C07D205/04 ,  C07D265/30 ,  C07D211/38 ,  C07D211/96 ,  A61P35/00

Abstract: Provided is a fluorinated cyclopropylamine compound represented by formula I, a racemate thereof, an R-isomer thereof, an S-isomer thereof, a pharmaceutical salt thereof, and a mixture thereof. Also provided are pharmaceutical compositions containing the compound, a preparation method for the compound, and uses thereof as a lysine specific demethylase 1 (LSD1) inhibitor, and in the treatment of cancers.

公开(公告)号：US20150210711A1

公开(公告)日：2015-07-30

申请号：US14683726

申请日：2015-04-10

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: C07D491/153 ,  C07D491/056 ,  C07D217/20 ,  C07D311/20 ,  C07C231/14 ,  C07D455/03 ,  C07C69/736

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：US20240262860A1

公开(公告)日：2024-08-08

申请号：US18014932

申请日：2021-07-05

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

Inventor： Hong LIU ,  Jiang WANG ,  Yichu LIU ,  Changyue YU ,  Yibing WANG ,  Hualiang JIANG ,  Kaixian CHEN

IPC: C07J63/00 ,  A61K31/704 ,  A61P3/10 ,  A61P31/14 ,  A61P31/16

CPC classification number: C07J63/008 ,  A61K31/704 ,  A61P3/10 ,  A61P31/14 ,  A61P31/16

Abstract: The present invention provides a pentacyclic triterpenoid glycoside compound, and a preparation method therefor and a use thereof. Specifically, the present invention provides a compound as shown in formula I. The definition of each group is described in the description. The compound can be used for preparing a medicament for treating metabolic diseases such as diabetes and viral diseases caused by influenza virus, coronavirus and the like.

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：US20240208954A1

公开(公告)日：2024-06-27

申请号：US18013696

申请日：2021-06-29

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

Inventor： Hong LIU ,  Jiang WANG ,  Cen XIE ,  Yameng LIU ,  Shulei HU ,  Cuina LI ,  Feng GAO ,  Kanglong WANG ,  Yong WANG ,  Xianchun ZHONG ,  Yuqiang SHI ,  Hualiang JIANG ,  Kaixian CHEN

IPC: C07D413/10 ,  A61K31/4245 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/498 ,  A61K31/675 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  C07D271/06 ,  C07D413/14 ,  C07F9/6558

CPC classification number: C07D413/10 ,  A61K31/4245 ,  A61K31/454 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/498 ,  A61K31/675 ,  A61P1/16 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  C07D271/06 ,  C07D413/14 ,  C07F9/65583

Abstract: The present invention relates to the fields of pharmaceutical chemistry and pharmacotherapeutics, and in particular to a compound as represented by general formula I, a racemate, an R-isomer, an S-isomer and a pharmaceutically acceptable salt thereof and a mixture of same, a preparation method therefor, a pharmaceutical composition containing the compound and the use thereof as an SIP receptor agonist. The oxadiazole compound involved in the present invention can be used for treating SIP receptor agonist related diseases.

公开(公告)号：US20230133600A1

公开(公告)日：2023-05-04

申请号：US17796076

申请日：2021-01-28

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

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

IPC: A61K31/404 ,  A61K31/4412 ,  A61K31/4025 ,  A61K31/498 ,  A61K31/4709 ,  A61K31/443 ,  A61K31/4545 ,  A61K31/454 ,  A61K31/4535 ,  A61K31/453 ,  A61K31/4525 ,  A61K31/4439 ,  A61K31/437 ,  A61K31/4155

Abstract: A class of ketoamide-based compounds, in particular, a ketoarnide-based compound as represented by general formula A is provided. The ketoamide compound may be used as a 2019 novel coronavirus (2019-nCov) 3 CL protease inhibitor and/or human cathepsin L inhibitor, and/or may be used in the preparation of a medicament for treating and/or preventing and relieving respiratory tract infection, pneumonia and other related diseases caused by 2019 novel coronavirus infection. Pharmaceutical compositions of the class of compounds, pharmaceutical salts, enantiomeric forms, diastereoisomers and racemic compounds thereof in the preparation of a medicament for treating and/or preventing and relieving respiratory tract infections and other related diseases caused by the 2019 novel coronavirus infection are also provided.

公开(公告)号：US20230010368A1

公开(公告)日：2023-01-12

申请号：US17780449

申请日：2020-11-24

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

Inventor： Hong LIU ,  Yu ZHOU ,  Haiyan ZHANG ,  Yan FU ,  Jian LI ,  Hualiang JIANG ,  Xican TANG ,  Kaixian CHEN

IPC: C07D211/38

Abstract: The present invention provides a crystalline form of an acetylcholinesterase inhibitor, a preparation method therefor and application thereof. Specifically, the crystalline form is crystalline form A, crystalline form B and crystalline form C of 2-((1-(2-fluorobenzyl)-4-fluoropiperidin-4-yl) methylene)-5, 6-dimethoxy-2, 3-dihydro-1-indanone. The crystalline form of the present invention does not contain water and solvent, has high stability and low hygroscopicity, is easy to process, and is very suitable for preparing drugs for preventing and/or treating neurodegenerative diseases.

公开(公告)号：US20190233456A1

公开(公告)日：2019-08-01

申请号：US16337338

申请日：2017-09-19

Applicant: SHANGHAI INSTITUTE OF MATERIA MEDICA CHINESE ACADEMY OF SCIENCES

Inventor： Hong LIU ,  Jiang WANG ,  Shengbin ZHOU ,  Panfeng PENG ,  Yong NIAN ,  Shuni WANG ,  Shuangjie SHU ,  Hao SHEN ,  Hualiang JIANG ,  Kaixian CHEN

IPC: C07F15/04 ,  C07D207/16

CPC classification number: C07F15/045 ,  C07C227/34 ,  C07C229/34 ,  C07D207/16 ,  C07D401/04 ,  C07D409/12 ,  C07F15/04 ,  Y02P20/55

Abstract: Disclosed is a method for synthesizing a novel chiral ligand, a metal chelate, a variety of non-natural amino acids, Maraviroc and a key intermediate thereof. In the invention, (R)-2-methyl proline is selected and used as a starting raw material, (S)-β3-amino acid is obtained by asymmetric resolution induced by using a nickel chelate, and Maraviroc is synthesized by using (S)-3-amino-3-phenylpropionic acid as a key intermediate with a high yield and the ee value reaching 98.2% or more. The method of the present invention has widely available materials, mild synthetic process conditions, is easy to control, and produces a product of a high optical purity.

公开(公告)号：US20190100529A1

公开(公告)日：2019-04-04

申请号：US16087317

申请日：2017-03-20

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 describes a polymorph of (R)-methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothiophene[3,2-d]pyrimidine-6-carboxylic acid maleate and a preparation method therefor. The polymorph is a crystal having high stability and low hygroscopicity, and the crystal form is selected from crystal form A, crystal form B and crystal form C. Furthermore, the crystal form has a strong in-vivo hypoglycemic activity and can be used for the preparation of a novel drug for the treatment or prevention of diabetes mellitus type H and/or complications of diabetes mellitus type H.