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公开(公告)号：EP2786998B1
公开(公告)日：2018-07-25
申请号：EP12853993.9
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： LIU, Hong , LI, Jia , LI, Jian , LI, Jingya , WANG, Jiang , SU, Mingbo , LIAN, Jie , JIANG, Hualiang , CHEN, Kaixian
IPC分类号： C07D495/04 , A61K31/519 , A61K31/55 , A61P3/10
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.
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公开(公告)号：EP3521274A1
公开(公告)日：2019-08-07
申请号：EP17854729.5
申请日：2017-09-19
发明人： LIU, Hong , WANG, Jiang , ZHOU, Shengbin , PENG, Panfeng , NIAN, Yong , WANG, Shuni , SHU, Shuangjie , SHEN, Hao , JIANG, Hualiang , CHEN, Kaixian
IPC分类号： C07D207/16 , C07D409/12 , C07F15/04 , C07C227/34 , C07C229/34 , C07D401/04
摘要： 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)-β 3 -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.
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公开(公告)号：EP3434677A1
公开(公告)日：2019-01-30
申请号：EP17769393.4
申请日：2017-03-20
发明人： LIU, Hong , WANG, Jiang , LI, Jian , LI, Jia , LI, Jingya , JIANG, Hualiang , LUO, Xiaomin , CHEN, Kaixian
IPC分类号： C07D495/04 , A61K31/519 , A61P3/10
摘要： A polymorph of (R) methyl-2-(3-aminopiperidin-1-yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothioph ene[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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4.发明公开
公开(公告)号：EP3315502A1
公开(公告)日：2018-05-02
申请号：EP16813720.6
申请日：2016-06-23
发明人： LIU, Hong , LI, Jia , WANG, Jiang , LI, Jingya , CHEN, Hui , LI, Dan , LI, Jian , WANG, Yibing , JIANG, Hualiang , CHEN, Kaixian
IPC分类号： C07D493/10 , A61K31/35 , A61K31/381 , A61K31/427 , A61K31/4436 , A61P3/10 , A61P3/04 , A61P9/10
CPC分类号： C07H19/01 , A61K31/35 , A61K31/381 , A61K31/427 , A61K31/4436 , A61P3/08 , C07D493/10
摘要： The present invention provides C, O-spiro aryl glycoside compounds, preparation therefor and use thereof. Specifically provided are the compounds represented by the formula (I), wherein the definitions of each group are described in the specification. The compound can be used as SGLT2 inhibitors in preparing the pharmaceutical compositions for treating diseases such as diabetes, atherosclerosis, adiposity and etc.
摘要翻译： 本发明提供C，O-螺芳基糖苷化合物，其制备方法及其用途。 具体提供了由式（I）表示的化合物，其中每个基团的定义在说明书中描述。 该化合物可以作为SGLT2抑制剂用于制备治疗糖尿病，动脉粥样硬化，肥胖症等疾病的药物组合物。
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公开(公告)号：EP3434678A1
公开(公告)日：2019-01-30
申请号：EP17769445.2
申请日：2017-03-22
发明人： LIU, Hong , WANG, Jiang , LI, Jian , LI, Jia , LI, Jingya , JIANG, Hualiang , LUO, Xiaomin , CHEN, Kaixian
IPC分类号： C07D495/04 , A61K31/519 , A61P3/10 , A61P9/12 , A61P9/10 , A61P13/12 , A61P25/00 , A61P9/00 , A61P27/02
摘要： The present invention relates to a salt form of (R)-methyl-2-(3-aminopiperidin-1 -yl)-3-(2-cyanobenzyl)-4-carbonyl-3,4-dihydrothioph ene[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 present 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：EP3438108A1
公开(公告)日：2019-02-06
申请号：EP17773232.8
申请日：2017-03-29
发明人： LIU, Hong , WANG, Yiping , ZHAO, Fei , ZHAO, Jing , WANG, Jiang , XI, Cong , WU, Chenglin , SHEN, Hao , HAN, Xu , JIANG, Hualiang , CHEN, Kaixian
IPC分类号： C07D471/14 , C07D491/22 , C07D495/22 , A61K31/4745 , A61P3/06 , A61P3/00 , A61P1/16 , A61P9/10 , A61P3/04
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.
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7.发明公开
公开(公告)号：EP3835296A1
公开(公告)日：2021-06-16
申请号：EP19847084.1
申请日：2019-08-09
发明人： LIU, Hong , JIANG, Shibo , DAI, Wenhao , LU, Lu , PENG, Jingjing , XIA, Shuai , WANG, Jiang , LI, Jian , JIANG, Hualiang , CHEN, Kaixian
IPC分类号： C07D403/12 , C07D401/12 , C07D405/12 , C07D409/12 , C07D241/44 , C07D209/42 , A61K31/498 , A61K31/404 , A61K31/454 , A61K31/4025 , A61K31/4525 , A61K31/4709 , A61P31/14
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.
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8.发明公开
公开(公告)号：EP4458820A1
公开(公告)日：2024-11-06
申请号：EP22914967.9
申请日：2022-12-28
发明人： LIU, Hong , LI, Jia , WANG, Jiang , ZANG, Yi , CHEN, Feiyang , GAO, Lixin , ZHAO, Jing , SUN, Dandan , WANG, Ke'an , JIANG, Hualiang , XIE, Rongrong
IPC分类号： C07D403/12 , C07D403/14 , C07D401/12 , C07D401/14 , C07D407/14 , C07C409/14 , C07D471/00 , C07D405/14 , C07K14/705 , C07K14/72 , A61K31/53 , A61P1/16 , A61P9/10 , A61P9/12 , A61P3/04 , A61P3/06 , A61P3/10 , A61P3/00 , A61P9/00
摘要： Provided in the present invention are a class of quinoline compounds and a preparation method therefor, a pharmaceutical composition and the use thereof. Specifically, provided in the present invention are a compound as shown in formula(I), and a stereoisomer, a deuterated compound, a solvate, a metabolite, a pharmaceutically acceptable salt, a eutectic or a prodrug thereof, and a pharmaceutical composition thereof. Further provided in the present invention are a preparation method for the compound and the use thereof in the preparation of a drug for treating diseases mediated by thyroid hormone receptors. Related diseases include, but are not limited to, diseases such as non-alcoholic fatty liver diseases, atherosclerosis, coronary heart disease, hypertension, hypercholesterolemia, hyperlipidemia, hypertriglyceridemia, dyslipidemia, obesity, diabetes, metabolic disorders, lipid metabolism disorders, 1A type glycogen storage diseases, hypothyroidism and thyroid cancer.
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9.发明公开
公开(公告)号：EP4180445A1
公开(公告)日：2023-05-17
申请号：EP21838780.1
申请日：2021-07-05
发明人： LIU, Hong , WANG, Jiang , LIU, Yichu , YU, Changyue , WANG, Yibing , JIANG, Hualiang , CHEN, Kaixian
摘要： 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.
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10.发明公开
公开(公告)号：EP4177255A1
公开(公告)日：2023-05-10
申请号：EP21834664.1
申请日：2021-06-29
发明人： LIU, Hong , WANG, Jiang , XIE, Cen , LIU, Yameng , HU, Shulei , LI, Cuina , GAO, Feng , WANG, Kanglong , WANG, Yong , ZHONG, Xianchun , SHI, Yuqiang , JIANG, Hualiang , CHEN, Kaixian
IPC分类号： C07D413/14 , C07D413/12 , C07D271/06 , A61K31/4245 , A61P3/00
摘要： 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.
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