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：US20180194767A1

公开(公告)日：2018-07-12

申请号：US15566418

申请日：2016-04-15

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

Inventor： Hong LIU ,  Yu ZHOU ,  Dong ZHANG ,  Jian LI ,  Hualiang JIANG ,  Kaixian CHEN

IPC: C07D487/04 ,  C07D213/56 ,  C07D491/10 ,  C07D277/30 ,  C07D231/56 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D401/06 ,  C07D417/06 ,  C07D401/14 ,  C07D401/12 ,  C07D239/26 ,  C07D413/12 ,  C07D263/32 ,  C07D413/10 ,  C07D261/08

CPC classification number: C07D487/04 ,  C07D213/56 ,  C07D213/75 ,  C07D213/82 ,  C07D231/56 ,  C07D239/26 ,  C07D261/08 ,  C07D263/32 ,  C07D277/30 ,  C07D277/32 ,  C07D401/06 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D413/10 ,  C07D413/12 ,  C07D417/06 ,  C07D417/10 ,  C07D417/12 ,  C07D417/14 ,  C07D491/10

Abstract: Compounds of formula I are provided. Also provided are methods of preparing the compounds of formula (I), and methods of using the compounds of formula (I) as a negative allosteric modulator of a metabotropic glutamate receptor (mGluR) subtype 5.

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：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：US20170044187A1

公开(公告)日：2017-02-16

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 ,  C07D451/04 ,  C07D401/14 ,  C07D409/14

CPC classification number: C07D519/00 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/46 ,  A61K45/06 ,  C07D401/14 ,  C07D409/14 ,  C07D451/04 ,  A61K2300/00

Abstract: Provided are 1-(3-aminopropyl) substituted cyclic amine compounds as represented by formula (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.

Abstract translation: 提供由式（I）表示的1-（3-氨基丙基）取代的环胺化合物，其药学上可接受的盐，对映体，非对映异构体，外消旋体及其混合物，以及合成所述1-（3-氨基丙基）取代的环胺 化合物采用芳香族杂环甲醛为原料。 所述化合物可用作治疗HIV感染的CCR5拮抗剂。