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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
发明人： Hong LIU , Jia LI , Jiang WANG , Yi ZANG , Jian LI , Jingya LI , Dandan SUN , Hualiang JIANG , Kaixian CHEN
IPC分类号： A61K31/5377 , A61K31/519 , A61P1/16
摘要： 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：US20190039989A1
公开(公告)日：2019-02-07
申请号：US16075528
申请日：2017-02-20
发明人： Fajun NAN , Jia LI , Jingya LI , Mei ZHANG , Zhifu XIE , Jingtao WANG , Dongdong GUO
CPC分类号： C07C61/35 , A61K31/194 , C07C55/28 , C07C57/13 , C07C57/26 , C07C57/42 , C07C61/16 , C07C61/20 , C07C61/22 , C07C2601/08 , C07C2601/16 , Y02P20/55
摘要： The present invention relates to a class of fatty acid compounds, a preparation method thereof and use thereof. The fatty acid compounds have the structure of the formula I, which has the ability to activate APMK and inhibit the glucose output in mouse primary hepatocytes. The fatty acid compounds can be used in preparing a medicament for the treatment of obesity or diabetes.
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公开(公告)号：US20240351966A1
公开(公告)日：2024-10-24
申请号：US18290268
申请日：2022-05-11
发明人： Fajun NAN , Jingya LI , Zheng ZHANG , Yanan DUAN , Yangming ZHANG , Dandan CHEN , Chengqiu DAI
IPC分类号： C07C39/19 , A61K31/05 , A61K31/09 , A61K31/136 , A61K31/145 , A61K31/167 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/505 , C07C43/215 , C07C43/23 , C07C215/76 , C07C233/88 , C07D213/69 , C07D213/74 , C07D239/10 , C07D307/36 , C07D333/06 , C07D333/34
CPC分类号： C07C39/19 , A61K31/05 , A61K31/09 , A61K31/136 , A61K31/145 , A61K31/167 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/44 , A61K31/505 , C07C43/215 , C07C43/23 , C07C215/76 , C07C233/88 , C07D213/69 , C07D213/74 , C07D239/10 , C07D307/36 , C07D333/06 , C07D333/34
摘要： Provided are a class of alkylphenol compounds and a preparation method therefor. Specifically provided are a new alkyl polyphenol compound as represented by chemical formula I, and a preparation method therefor and the use thereof in the treatment of metabolic syndrome.
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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
发明人： Hong LIU , Jiang WANG , Jian LI , Jia LI , Jingya LI , Hualiang JIANG , Xiaomin LUO , Kaixian CHEN
IPC分类号： C07D495/04 , A61P3/10
摘要： 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
发明人： Hong LIU , Jian WANG , Jian LI , Jia LI , Jingya LI , Shengbin ZHOU , Mingbo SU , Hualiang JIANG , Xiaomin LUO , Kaixian CHEN
IPC分类号： C07D495/04
CPC分类号： C07D495/04 , A61K31/519 , C07B2200/13
摘要： 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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公开(公告)号：US20190100529A1
公开(公告)日：2019-04-04
申请号：US16087317
申请日：2017-03-20
发明人： Hong LIU , Jiang WANG , Jian LI , Jia LI , Jingya LI , Hualiang JIANG , Xiaomin LUO , Kaixian CHEN
IPC分类号： C07D495/04 , A61P3/10
摘要： 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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公开(公告)号：US20170313715A1
公开(公告)日：2017-11-02
申请号：US15523058
申请日：2015-10-30
申请人： EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGY , SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES
发明人： Honglin LI , Hualiang JIANG , Yufang XU , Jia LI , Zhenjiang ZHAO , Jingya LI , Hongling XU , Shiliang LI
IPC分类号： C07D493/04 , C07D311/92 , C07D311/60
摘要： The present invention relates to six-membered ring benzo derivatives as a DPP-4 inhibitor and a use thereof. In particular, the present invention relates to a compound as shown in formula I, a pharmaceutical composition containing the compound as shown in formula I and a use of the compound in the preparation of drugs for treating DPP-4 related diseases or inhibiting DPP-4.
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公开(公告)号：US20170247371A1
公开(公告)日：2017-08-31
申请号：US15326310
申请日：2015-07-14
发明人： Fajun NAN , Jia LI , Jingya LI , Mei ZHANG , Dakai CHEN , Lina ZHANG , Runtao ZHANG , Zhifu XIE
IPC分类号： C07D471/04 , C12N9/12 , C07D211/78
CPC分类号： C07D471/04 , A61K31/437 , C07D211/78 , C12N9/12 , C12Y207/11031
摘要： Provided are a class of pyrazolone compounds and a use thereof. In particular, a compound represented by formula I is provided, wherein the definition of each variable group is as described in the description. The compounds of formula (I) have a direct AMPK-activating activity and can significantly promote the phosphorylation of AMPK and ACC of L6 myocytes and HepG2 cells in a dose-dependent manner.
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公开(公告)号：US20180305390A1
公开(公告)日：2018-10-25
申请号：US15738675
申请日：2016-06-23
发明人： Hong LIU , Jia LI , Jiang WANG , Jingya LI , Hui CHEN , Dan LI , Jian LI , Yibing WANG , Hualiang JIANG , Kaixian CHEN
CPC分类号： C07H19/01 , A61K31/35 , A61K31/381 , A61K31/427 , A61K31/4436 , A61P3/08 , C07D493/10
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.
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