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1. 发明授权

EP2570417B1 THIENOPYRIDINE ESTER DERIVATIVE CONTAINING NITRILE, PREPARATION METHOD, USE AND COMPOSITION THEREOF 有权
标题翻译： THIENOPYRIDINESTER衍生腈，工艺制作，它们的用途及其组合物
公开(公告)号：EP2570417B1
公开(公告)日：2015-05-13
申请号：EP11780039.1
申请日：2011-03-23
申请人： Tianjin Institute Of Pharmaceutical Research
发明人： LIU, Dengke , LIU, Ying , YUE, Nan , CHEN, Furong , TAN, Chubing , ZHOU, Yunsong , LIU, Peng , ZHAO, Yigui , ZHI, Deguang , LIU, Mo , LIU, Bingni , HUANG, Changjiang , TANG, Lida
IPC分类号： C07D495/04 , A61K31/4365 , A61P7/02 , A61P9/00 , A61P9/10
CPC分类号： C07D495/04 , A61K9/0019 , A61K9/1652 , A61K9/19 , A61K9/2054 , A61K9/2059 , A61K47/10 , A61K47/26

2. 发明公开

EP2570417A1 THIENOPYRIDINE ESTER DERIVATIVE CONTAINING NITRILE, PREPARATION METHOD, USE AND COMPOSITION THEREOF 有权
标题翻译：三硝基吡啶衍生物麻醉剂NITRIL，HERSTELLUNGSVERFAHRENDAFÜR，VERWENDUNG DAVON UND ZUSAMMENSETZUNG DARAUS
公开(公告)号：EP2570417A1
公开(公告)日：2013-03-20
申请号：EP11780039.1
申请日：2011-03-23
申请人： Tianjin Institute Of Pharmaceutical Research
发明人： LIU, Dengke , LIU, Ying , YUE, Nan , CHEN, Furong , TAN, Chubing , ZHOU, Yunsong , LIU, Peng , ZHAO, Yigui , ZHI, Deguang , LIU, Mo , LIU, Bingni , HUANG, Changjiang , TANG, Lida
IPC分类号： C07D495/04 , A61K31/4365 , A61P7/02 , A61P9/00 , A61P9/10
CPC分类号： C07D495/04 , A61K9/0019 , A61K9/1652 , A61K9/19 , A61K9/2054 , A61K9/2059 , A61K47/10 , A61K47/26
摘要： A compound with the structure of the formula (I) or a pharmaceutically acceptable salt, a preparation method and use thereof are disclosed in the present invention, wherein R is cyano group. The compound provided by the present invention has an antiplatelet aggregation activity and can be used in preparing a medicament for preventing or treating cardiac and cerebral vascular diseases such as coronary artery syndromes, myocardial infarction and myocardial ischemia which are caused by platelet aggregation.
摘要翻译：在本发明中公开了具有式（I）结构的化合物或其药学上可接受的盐，其中R是氰基。本发明提供的化合物具有抗血小板聚集活性，可用于制备预防或治疗由血小板聚集引起的心脑血管疾病如冠状动脉综合征，心肌梗死和心肌缺血的药物。

3. 发明公开

EP3246324A2 PHENYL C-GLUCOSIDE DERIVATIVE CONTAINING DEOXYGLUCOSE STRUCTURE, PREPARATION METHOD AND USES THEREOF 有权转让
公开(公告)号：EP3246324A2
公开(公告)日：2017-11-22
申请号：EP17176326.1
申请日：2013-12-05
申请人： Tianjin Institute Of Pharmaceutical Research
发明人： ZHAO, Guilong , WANG, Yuli , LIU, Bingni , XIE, Yafei , LIU, Yuqiang , LIU, Peng , WU, Jiang , HOU, Jiajia , WEI, Wei , DU, Wen , XU, Weiren , TANG, Lida , ZOU, Meixiang
IPC分类号： C07D309/10 , C07D409/10 , C07D407/12 , C07D493/10 , C07D493/08 , C07D335/02 , C07H19/01 , C07H9/04 , C07H1/00 , A61K31/351 , A61K31/381 , A61K31/7048 , A61K31/382 , A61P3/10
CPC分类号： C07H19/01 , A61K47/22 , C07D309/06 , C07D309/10 , C07D335/02 , C07D407/12 , C07D409/10 , C07D493/08 , C07D493/10
摘要： The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R 1 -R 7 are as defined in the specification. The present invention also provides a method for synthesizing the phenyl C-glucoside derivative containing a deoxyglucose structure and an intermediate product. The method has advantages of being simple to manage and of low cost, which is suitable for large-scale industrial production. The present invention further provides a cocrystal of (1S)-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1,6-dideoxy-D-glucose and L-proline, and preparation method and uses thereof.

4. 发明公开

EP2933250A1 PHENYL C-GLUCOSIDE DERIVATIVE CONTAINING DEOXYGLUCOSE STRUCTURE, PREPARATION METHOD AND USE THEREOF 失效
标题翻译：苯丙酸胆固醇衍生物
公开(公告)号：EP2933250A1
公开(公告)日：2015-10-21
申请号：EP13864482.8
申请日：2013-12-05
申请人： Tianjin Institute Of Pharmaceutical Research
发明人： ZHAO, Guilong , WANG, Yuli , LIU, Bingni , XIE, Yafei , LIU, Yuqiang , LIU, Peng , WU, Jiang , HOU, Jiajia , WEI, Wei , DU, Wen , XU, Weiren , TANG, Lida , ZOU, Meixiang
IPC分类号： C07D309/10 , C07D409/10 , C07D407/12 , C07D493/10 , C07D493/08 , C07D335/02 , C07H19/01 , C07H9/04 , C07H1/00 , A61K31/351 , A61K31/381 , A61K31/7048 , A61K31/382 , A61P3/10
CPC分类号： C07H19/01 , A61K47/22 , C07D309/06 , C07D309/10 , C07D335/02 , C07D407/12 , C07D409/10 , C07D493/08 , C07D493/10
摘要： The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R 1 -R 7 are as defined in the specification. The present invention also provides a method for synthesizing the phenyl C-glucoside derivative containing a deoxyglucose structure and an intermediate product. The method has advantages of being simple to manage and of low cost, which is suitable for large-scale industrial production. The present invention further provides a cocrystal of (1S)-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1,6-dideoxy-D-glucose and L-proline, and preparation method and uses thereof.
摘要翻译：本发明提供含有式I表示的脱氧葡萄糖结构的苯基C-葡萄糖苷衍生物及其制备方法，含有该脱乙酰葡萄糖结构的药物组合物及其在制备用于治疗糖尿病的药物中的用途，其中取代基R 1〜R 7 如本说明书中所定义。本发明还提供了合成含有脱氧葡萄糖结构和中间产物的苯基C-葡萄糖苷衍生物的方法。该方法管理简单，成本低，适合大规模工业化生产。本发明还提供了（1S）-1- [4-氯-3-（4-乙氧基苄基）苯基] -1,6-二脱氧-D-葡萄糖和L-脯氨酸的共结晶体及其制备方法和用途。

5. 发明授权

EP2404909B1 AMIDE THIAZOLE DERIVATIVE, PREPARATION METHOD AND USES THEREOF 有权
标题翻译： AMIDTHIAZOLDERIVAT，用于生产，并使用
公开(公告)号：EP2404909B1
公开(公告)日：2013-05-29
申请号：EP09832806.5
申请日：2009-11-30
申请人： Tianjin Institute Of Pharmaceutical Research
发明人： ZHAO, Guilong , XU, Weiren , WANG, Yuli , TANG, Lida , LI, Yiliang , ZOU, Meixiang , LIU, Wei , SHAO, Hua , TAN, Chubing , LIU, Peng
IPC分类号： C07D277/46 , C07D417/12 , C07D277/58 , A61K31/426 , A61K31/427 , A61P3/10
CPC分类号： C07D277/46 , C07D277/58 , C07D417/12

6. 发明公开

EP2404909A1 AMIDE THIAZOLE DERIVATIVE, PREPARATION METHOD AND USES THEREOF 有权
标题翻译：酰胺噻唑衍生物，其制备方法和用途
公开(公告)号：EP2404909A1
公开(公告)日：2012-01-11
申请号：EP09832806.5
申请日：2009-11-30
申请人： Tianjin Institute Of Pharmaceutical Research
发明人： ZHAO, Guilong , XU, Weiren , WANG, Yuli , TANG, Lida , LI, Yiliang , ZOU, Meixiang , LIU, Wei , SHAO, Hua , TAN, Chubing , LIU, Peng
IPC分类号： C07D277/46 , C07D417/12 , C07D277/58 , A61K31/426 , A61K31/427 , A61P3/10
CPC分类号： C07D277/46 , C07D277/58 , C07D417/12
摘要： The present invention relates to the field of the drugs associated with the diabetes. Particularly, the present invention relates to a dipeptidyl peptidase-IV inhibitor having the structure shown by formula (I), which contains amide thiazole structure and has an effect on treating diabetes, and a preparation method and a pharmaceutical composition containing it, as well as use thereof in manufacture of the drugs for treating the diabetes,

wherein, R 1 is hydrogen, halogen, C 1 -C 5 alkyl, COOR 3 or phenyl, wherein R 3 is C 1 -C 5 alkyl; R 2 is phenyl, substituted phenyl, 2-furanyl, substituted 2-furanyl, 2-thienyl, substituted 2-thienyl, 2-pyrrolyl, or substituted 2-pyrrolyl.
摘要翻译：本发明涉及与糖尿病相关的药物领域。具体地说，本发明涉及具有式（I）所示结构的二肽基肽酶-IV抑制剂及其制备方法和含有它的药物组合物，其中所述二肽基肽酶-IV抑制剂含有酰胺噻唑结构并具有治疗糖尿病的作用，其在制备治疗糖尿病的药物中的用途，其中R1为氢，卤素，C1-C5烷基，COOR3或苯基，其中R3为C1-C5烷基; R2为苯基，取代的苯基，2-呋喃基，取代的2-呋喃基，2-噻吩基，取代的2-噻吩基，2-吡咯基或取代的2-吡咯基。

7. 发明授权

EP2933250B1 PHENYL C-GLUCOSIDE DERIVATIVE CONTAINING DEOXYGLUCOSE STRUCTURE, PREPARATION METHOD AND USE THEREOF 失效
标题翻译：含有脱氧葡萄糖结构的苯基C-葡萄糖苷衍生物，其制备方法及其用途
公开(公告)号：EP2933250B1
公开(公告)日：2017-08-09
申请号：EP13864482.8
申请日：2013-12-05
申请人： Tianjin Institute Of Pharmaceutical Research
发明人： ZHAO, Guilong , WANG, Yuli , LIU, Bingni , XIE, Yafei , LIU, Yuqiang , LIU, Peng , WU, Jiang , HOU, Jiajia , WEI, Wei , DU, Wen , XU, Weiren , TANG, Lida , ZOU, Meixiang
IPC分类号： C07D309/10 , C07D409/10 , C07D407/12 , C07D493/10 , C07D493/08 , C07D335/02 , C07H19/01 , C07H9/04 , C07H1/00 , A61K31/351 , A61K31/381 , A61K31/7048 , A61K31/382 , A61P3/10
CPC分类号： C07H19/01 , A61K47/22 , C07D309/06 , C07D309/10 , C07D335/02 , C07D407/12 , C07D409/10 , C07D493/08 , C07D493/10

8. 发明公开

EP2894163A1 A GLP-1 ANALOGUE, ITS PREPARATION METHODS AND USE THEREOF 审中-公开
标题翻译： GLP-1-ANALOG，HERSTELLUNGSVERFAHRENDAFÜRUND VERWENDUNG DAVON
公开(公告)号：EP2894163A1
公开(公告)日：2015-07-15
申请号：EP12749806.1
申请日：2012-02-08
申请人： Tianjin Institute Of Pharmaceutical Research
发明人： GONG, Min , FU, Gang , XU, Weiren , TANG, Lida , REN, Xiaowen , LIU, Peng , WANG, Yuli , WU, Jiang , ZOU, Meixiang
IPC分类号： C07K14/605 , C07K19/00 , C07K1/06 , C07K1/04 , A61K38/26 , A61P3/10
CPC分类号： C07K14/605 , A61K38/00
摘要： Provided is a GLP-1 analogue having the structure as shown in the general formula A:

7 HAEX 10 TFTSX 15 VSSYLEX 22 QAAKEFIX 30 WLX 33 KGRG 37 n 1 X 1 Cn 2 X 2 (general 1 formula A),

wherein X 10 is glycine or cysteine, X 15 is aspartic acid or cysteine, X 22 is glycine or cysteine, X 30 is alanine or cysteine, X 33 is valine or cysteine, and at least one of X 10 , X 15 , X 22 , X 30 and X 33 is cysteine, X 1 and X 2 respectively is glycine, alanine or valine, n 1 =1-30, n 2 =1-30. The general formula A contains two cysteines to form disulfide bonds. Also provided are the preparation methods and the use of said GLP-1 analogue. Said GLP-1 analogue has a prolonged blood half-life compared with GLP-1, and can be used for the treatment of diabetes and obesity.
摘要翻译：本发明提供了具有通式A所示结构的GLP-1类似物：ƒ€ƒ€ƒ€ƒ€ƒ€ƒ7 HAEX 10 TFTSX 15 VSSYLEX 22 QAAKEFIX 30 WLX 33 KGRG 37 n 1 X 1 Cn 2 X 2€ƒ€ƒ€ƒ€ƒ（通用1式A），其中X 10是甘氨酸或半胱氨酸，X 15是天冬氨酸或半胱氨酸，X 22是甘氨酸或半胱氨酸，X 30是丙氨酸或半胱氨酸，X 33是缬氨酸或半胱氨酸，X 10，X 15，X 22，X 30和X 33中的至少一个是半胱氨酸，X 1和X 2分别是甘氨酸，丙氨酸或缬氨酸，n 1 = 1-30 ，n 2 = 1-30。通式A包含形成二硫键的两个半胱氨酸。还提供了所述GLP-1类似物的制备方法和用途。所述GLP-1类似物与GLP-1相比具有延长的血液半衰期，并且可用于治疗糖尿病和肥胖症。

9. 发明公开

EP3246324A3 PHENYL C-GLUCOSIDE DERIVATIVE CONTAINING DEOXYGLUCOSE STRUCTURE, PREPARATION METHOD AND USES THEREOF 有权转让
标题翻译：含有脱氧葡萄糖结构的苯基C-葡萄糖苷衍生物，其制备方法及其用途
公开(公告)号：EP3246324A3
公开(公告)日：2018-01-10
申请号：EP17176326.1
申请日：2013-12-05
申请人： Tianjin Institute Of Pharmaceutical Research
发明人： ZHAO, Guilong , WANG, Yuli , LIU, Bingni , XIE, Yafei , LIU, Yuqiang , LIU, Peng , WU, Jiang , HOU, Jiajia , WEI, Wei , DU, Wen , XU, Weiren , TANG, Lida , ZOU, Meixiang
IPC分类号： C07D309/10 , C07D409/10 , C07D407/12 , C07D493/10 , C07D493/08 , C07D335/02 , C07H19/01 , C07H9/04 , C07H1/00 , A61K31/351 , A61K31/381 , A61K31/7048 , A61K31/382 , A61P3/10
CPC分类号： C07H19/01 , A61K47/22 , C07D309/06 , C07D309/10 , C07D335/02 , C07D407/12 , C07D409/10 , C07D493/08 , C07D493/10
摘要： The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R 1 -R 7 are as defined in the specification. The present invention also provides a method for synthesizing the phenyl C-glucoside derivative containing a deoxyglucose structure and an intermediate product. The method has advantages of being simple to manage and of low cost, which is suitable for large-scale industrial production. The present invention further provides a cocrystal of (1S)-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1,6-dideoxy-D-glucose and L-proline, and preparation method and uses thereof.
摘要翻译：本发明提供了式I所示的含有脱氧葡萄糖结构的苯基C-葡萄糖苷衍生物，其制备方法，含有该衍生物的药物组合物及其在制备治疗糖尿病药物中的用途，其中取代基R1-R7为在规范中定义。本发明还提供了合成含有脱氧葡萄糖结构和中间产物的苯基C-葡萄糖苷衍生物的方法。该方法管理简单，成本低廉，适合大规模工业化生产。本发明还提供了（1S）-1- [4-氯-3-（4-乙氧基苄基）苯基] -1,6-二脱氧-D-葡萄糖和L-脯氨酸的共结晶及其制备方法和用途。

10. 发明公开

EP2199402A1 CYCLOASTRAGENOL MONOGLUCOSIDE, PREPARATION, PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF 审中-公开
标题翻译： CYCLOASTRAGENOL-MONOGLUCOSID，HERSTELLUNG，PHARMAZEUTISCHE ZUSAMMENSETZUNG UND ANWENDUNG DAVON
公开(公告)号：EP2199402A1
公开(公告)日：2010-06-23
申请号：EP08783682.1
申请日：2008-09-08
申请人： TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCH
发明人： HAN, Yingmei , XIA, Guangping , XU, Weiren , ZHAO, Zhuanyou , LIU, Wulin , ZHAO, Naxia , LIU, Peng , ZHANG, Shijun , WANG, Yuli , WANG, Weiting , TANG, Lida , FU, Xiaoli
IPC分类号： C12P19/56 , C07H17/04 , A61K31/7048 , A61K9/00 , A61K9/08 , A61K9/12 , A61K9/19 , A61P9/00 , A61K36/481
CPC分类号： A61K36/481 , A61K31/7048 , C07J17/005 , C12P19/56
摘要： This invention provides a method for preparing cycloastragenol monoglucoside CMG (cydoastragenol-6-O-β-D-glucoside), comprising the steps of: a. using astragaloside IV or Astragali extracts prepared by a conventional method as raw materials and adding an appropriate solvent thereinto to form a raw material solution; b. adding hydrolase and allowing for hydrolysis at a constant temperature to obtain a hydrolysate; c. separating the hydrolysate with macroporous adsorption resin; and d. obtaining the product by purification and separation. The present invention further provides cycloastragenol-6-O-β-D-glucoside prepared according to the method of this invention as well as its use in the preparation of a medicament for treating cardiovascular diseases and pharmaceutical compositions comprising the same.
摘要翻译：本发明提供了一种制备环草酮醇一葡萄糖苷CMG（cydolistragenol-6-O-2-D-glucoside）的方法，包括以下步骤：a。使用常规方法制备的黄芪苷或黄芪提取物作为原料，并加入适当的溶剂以形成原料溶液; 湾加入水解酶并允许在恒定温度下水解得到水解产物; C。用大孔吸附树脂分离水解产物; 和d。通过净化和分离获得产品。本发明还提供了根据本发明的方法制备的环状天门菊胶-6-O-2-D-葡萄糖苷及其在制备用于治疗心血管疾病的药物中的用途以及包含其的药物组合物。

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