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![NOVEL PHARMACEUTICAL USE OF THIOPHENE [3,2-D] PYRIMIDINE-4-KETONE COMPOUND](/abs-image/US/2021/01/21/US20210015824A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210015824A1
公开(公告)日：2021-01-21
申请号：US16978563
申请日：2019-03-08
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.
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公开(公告)号：US20230133600A1
公开(公告)日：2023-05-04
申请号：US17796076
申请日：2021-01-28
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.
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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.
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公开(公告)号：US20190315703A1
公开(公告)日：2019-10-17
申请号：US16461234
申请日：2017-11-17
Applicant: EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY , SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
Inventor： Jian LI , Lefu LAN , Baoli LI , Feifei CHEN , Shuaishuai NI , Yifu LIU , Hanwen WEI , Fei MAO , Jin ZHU
IPC: C07D307/81 , C07D333/58 , C07D409/12 , A61P31/04 , A61P31/10 , C07D307/82
Abstract: Disclosed are benzoheterocyclic alkylamine compounds, or a pharmaceutically acceptable salt thereof, or a stereoisomer thereof, and a preparation method thereof, and use of the same in the manufacture of an antibacterial drug as an inhibitor of staphyloxanthin synthesis in Staphylococcus aureus.
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公开(公告)号：US20190100529A1
公开(公告)日：2019-04-04
申请号：US16087317
申请日：2017-03-20
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.
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Patent Agency Ranking
6.发明申请公开(公告)号：US20180194767A1
公开(公告)日：2018-07-12
申请号：US15566418
申请日：2016-04-15
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.
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公开(公告)号：US20210221807A1
公开(公告)日：2021-07-22
申请号：US17057199
申请日：2019-05-21
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.
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公开(公告)号：US20190031678A1
公开(公告)日：2019-01-31
申请号：US16087318
申请日：2017-03-22
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
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公开(公告)号：US20180030066A1
公开(公告)日：2018-02-01
申请号：US15549918
申请日：2016-02-03
Inventor： Hong LIU , Jian WANG , Jian LI , Jia LI , Jingya LI , Shengbin ZHOU , Mingbo SU , Hualiang JIANG , Xiaomin LUO , Kaixian CHEN
IPC: C07D495/04
CPC classification number: C07D495/04 , A61K31/519 , C07B2200/13
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.
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10.发明申请1-(3-AMINOPROPYL) SUBSTITUTED CYCLIC AMINE COMPOUNDS, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSITIONS AND USES THEREOF 审中-公开1-（3-氨基丙基）取代的环状氨基化合物，其制备方法和药物组合物及其用途公开(公告)号：US20170044187A1
公开(公告)日：2017-02-16
申请号：US15109101
申请日：2014-12-29
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。
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