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1. 发明申请

US20150274799A1 GLP-1 ANALOGUE, ITS PREPARATION METHODS AND USE THEREOF 审中-公开
标题翻译： GLP-1类似物，其制备方法及其用途
公开(公告)号：US20150274799A1
公开(公告)日：2015-10-01
申请号：US14405060
申请日：2012-02-08
申请人： Min Gong , Gang Fu , Weiren Xu , Lida Tang , Xiaowen Ren , Peng Liu , Yuli Wang , Jiang Wu , Meixiang Zou
发明人： Min Gong , Gang Fu , Weiren Xu , Lida Tang , Xiaowen Ren , Peng Liu , Yuli Wang , Jiang Wu , Meixiang Zou
IPC分类号： C07K14/605
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: 7HAEX10TFTSX15VSSYLEX22QAAKEFIX30WLX33KGRG37n1X1Cn2X2 (general formula A), wherein X10 is glycine or cysteine, X15 is aspartic acid or cysteine, X22 is glycine or cysteine, X30 is alanine or cysteine, X33 is valine or cysteine, and at least one of X10, X15, X22, X30 and X33 is cysteine, X1 and X2 respectively is glycine, alanine or valine, n1=1-30, n2=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：本发明提供具有通式A所示结构的GLP-1类似物：7HAEX10TFTSX15VSSYLEX22QAAKEFIX30WLX33KGRG37n1X1Cn2X2（通式A），其中X10为甘氨酸或半胱氨酸，X15为天冬氨酸或半胱氨酸，X22为甘氨酸或半胱氨酸，X30为丙氨酸或半胱氨酸 X33是缬氨酸或半胱氨酸，X10，X15，X22，X30和X33中的至少一个是半胱氨酸，X1和X2分别是甘氨酸，丙氨酸或缬氨酸，n1 = 1-30，n2 = 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。

2. 发明授权

US08835134B2 Cycloastragenol monoglucoside, preparation, pharmaceutical composition and application thereof 有权
标题翻译：环糊精单葡糖苷，其制备方法，药物组合物及其应用
公开(公告)号：US08835134B2
公开(公告)日：2014-09-16
申请号：US12678025
申请日：2008-09-08
申请人： Yingmei Han , Guangping Xia , Weiren Xu , Zhuanyou Zhao , Wulin Liu , Naxia Zhao , Peng Liu , Shijun Zhang , Xiaoli Fu , Yuli Wang , Weiting Wang , Lida Tang
发明人： Yingmei Han , Guangping Xia , Weiren Xu , Zhuanyou Zhao , Wulin Liu , Naxia Zhao , Peng Liu , Shijun Zhang , Xiaoli Fu , Yuli Wang , Weiting Wang , Lida Tang
IPC分类号： C12P19/44 , A61K36/481 , A61K31/7048 , C12P19/56 , C07J17/00
CPC分类号： A61K36/481 , A61K31/7048 , C07J17/005 , C12P19/56
摘要： This invention provides a method for preparing cycloastragenol monoglucoside CMG (cycloastragenol-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（环星形胶原蛋白-6-O-＆bgr-D-葡萄糖苷）的方法，包括以下步骤：a。使用常规方法制备的黄芪甲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; b。加入水解酶并允许在恒温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。通过纯化和分离获得产物。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-和bgr-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。

3. 发明授权

US08481577B2 Amide thiazole derivative, preparation method and uses thereof 失效
标题翻译：酰胺噻唑衍生物，其制备方法和用途
公开(公告)号：US08481577B2
公开(公告)日：2013-07-09
申请号：US13162121
申请日：2011-06-16
申请人： Guilong Zhao , Weiren Xu , Yuli Wang , Lida Tang , Yiliang Li , Meixiang Zou , Wei Liu , Hua Shao , Chubing Tan , Peng Liu
发明人： Guilong Zhao , Weiren Xu , Yuli Wang , Lida Tang , Yiliang Li , Meixiang Zou , Wei Liu , Hua Shao , Chubing Tan , Peng Liu
IPC分类号： A61K31/427 , C07D277/46
CPC分类号： C07D277/46 , C07D277/58 , C07D417/12
摘要： The present invention relates to the field of drugs associated with treating 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, R1 is methyl; R2 is phenyl; phenyl, 2-thienyl substituted in a mono-substituted, bi-substituted manner by fluorine and methyl.
摘要翻译：本发明涉及与治疗糖尿病有关的药物领域。特别地，本发明涉及具有式（I）所示结构的二肽基肽酶-IV抑制剂，其含有酰胺噻唑结构并具有治疗糖尿病的作用，以及含有它的制备方法和药物组合物，以及其用于制备用于治疗糖尿病的药物，其中，R 1为甲基; R2是苯基; 苯基，2-取代的噻吩基，被氟和甲基取代，双取代。

4. 发明授权

US07790759B2 Glycyrrhetinic acid-30-amide derivatives and their use 有权
标题翻译：甘草次酸 - 酰胺衍生物及其用途
公开(公告)号：US07790759B2
公开(公告)日：2010-09-07
申请号：US12090169
申请日：2006-10-16
申请人： Jianwu Wang , Weiren Xu , Jianping Wong , Lida Tang , Shijun Zhang , Lijun Liu , Yuli Wang , Xiaowen Ren
发明人： Jianwu Wang , Weiren Xu , Jianping Wong , Lida Tang , Shijun Zhang , Lijun Liu , Yuli Wang , Xiaowen Ren
IPC分类号： A61K31/42 , C07D261/06
CPC分类号： C07D261/08 , A61K31/415 , C07D413/04
摘要： The present invention relates to the field of a medicine for treating diseases associated with inflammation, immunity or infection, and in particular, to glycyrrhetinic acid-30-amide derivatives of general formula I and their preparation, and a pharmaceutical composition containing the same. Said derivatives and composition exhibit anti-inflammatory, analgesic, anti-allergic, cough-preventing, liver-protecting and anti-viral properties, wherein each group is as defined in the description.
摘要翻译：本发明涉及用于治疗与炎症，免疫或感染有关的疾病的药物领域，特别涉及通式I的甘草次酸 - 酰胺衍生物及其制备方法及含有该药物的药物组合物。所述衍生物和组合物表现出抗炎，镇痛，抗过敏，咳嗽预防，肝保护和抗病毒性质，其中每组如说明书中所定义。

5. 发明申请

US20150232527A1 GLUCAGON-LIKE PEPTIDE-1 ANALOGUE MONOMER AND DIMER, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF 审中-公开
标题翻译： GLUCAGON-like肽类1型模拟单体和二聚体，其制备方法及其应用
公开(公告)号：US20150232527A1
公开(公告)日：2015-08-20
申请号：US14405066
申请日：2012-03-28
申请人： Min Gong , Weiren Xu , Lida Tang , Gang Fu , Meixiang Zou , Jiang Wu
发明人： Min Gong , Weiren Xu , Lida Tang , Gang Fu , Meixiang Zou , Jiang Wu
IPC分类号： C07K14/605
CPC分类号： C07K14/605 , A61K38/00 , A61K38/26
摘要： Provided are a glucagon-like peptide-1 (GLP-1) analogue monomer and dimmer, a preparation method thereof, and an application thereof. The GLP-1 analogue monomer comprises one cysteine; and the dimer is formed by two monomer molecules connected via an intermolecular disulfide bond formed by the cysteine. The GLP-1 monomer comprising cysteine has the following general formula: 7HAEX10TFTSX15VSSYLEX22X23AAKEFIX30WLX33KGRG37, wherein X10 is glycine or cysteine, X15 is aspartate or cysteine, X22 is glycine or cysteine, X23 is glutamine or cysteine, X30 is alanine or cysteine, and X33 is valine or cysteine; and only one of X10, X15, X22, X23, X30, and X33 is cysteine. The glucagon-like peptide-1 analogue dimer of the present invention has an in vivo half-life of more than 8 to 96 hours, thus facilitating clinical promotion and application.
摘要翻译：提供胰高血糖素样肽-1（GLP-1）类似物单体和二聚体，其制备方法及其应用。 GLP-1类似物单体包含一个半胱氨酸; 并且二聚体由通过由半胱氨酸形成的分子间二硫键连接的两个单体分子形成。包含半胱氨酸的GLP-1单体具有以下通式：7HAEX10TFTSX15VSSYLEX22X23AAKEFIX30WLX33KGRG37，其中X10是甘氨酸或半胱氨酸，X15是天冬氨酸或半胱氨酸，X22是甘氨酸或半胱氨酸，X23是谷氨酰胺或半胱氨酸，X30是丙氨酸或半胱氨酸，X33是缬氨酸或半胱氨酸; 并且X10，X15，X22，X23，X30和X33中只有一个是半胱氨酸。本发明的胰高血糖素样肽-1类似物二聚体的体内半衰期大于8〜96小时，因此有助于临床推广和应用。

6. 发明授权

US09062087B2 Phenyl C-glucoside derivatives, preparation methods and uses thereof 有权
标题翻译：苯基C-葡萄糖苷衍生物，其制备方法和用途
公开(公告)号：US09062087B2
公开(公告)日：2015-06-23
申请号：US13575258
申请日：2011-01-14
申请人： Guilong Zhao , Hua Shao , Weiren Xu , Wei Liu , Yuli Wang , Lida Tang , Chubing Tan , Bingni Liu , Shijun Zhang
发明人： Guilong Zhao , Hua Shao , Weiren Xu , Wei Liu , Yuli Wang , Lida Tang , Chubing Tan , Bingni Liu , Shijun Zhang
IPC分类号： C07H7/04 , C07H7/06 , A61K31/70 , A61K31/351 , C07D309/10 , C07D409/10
CPC分类号： C07H7/04 , A61K31/351 , A61K31/70 , C07D309/10 , C07D409/10 , C07H7/06
摘要： The present invention relates to a sodium glucose cotransporter 2 (SGLT2) inhibitor with a phenyl C-glucoside structure, its preparation method, a pharmaceutical composition containing the same, and its use in treating diabetes and preparing an anti-diabetes medicament. The invention provides a compound with the structure of general formula I and a pharmaceutically acceptable salt and prodrug ester thereof,wherein, the definitions of R5 and R6 are selected from the following:(1) R5=R6=Me; (2) R5=Me, R6=OMe; (3) R5=Me, R6=H; (4) R5=Me, R6=F; (5) R5=F, R6=H; and (6) R5=OMe, R6=H.
摘要翻译：本发明涉及具有苯基C-葡萄糖苷结构的钠葡萄糖协同转运蛋白2（SGLT2）抑制剂及其制备方法，含有该葡糖苷结构的药物组合物及其在治疗糖尿病中的用途以及制备抗糖尿病药物。本发明提供具有通式I结构的化合物及其药学上可接受的盐和前药酯，其中R5和R6的定义选自如下：（1）R5 = R6 = Me; （2）R5 = Me，R6 = OMe; （3）R5 = Me，R6 = H; （4）R5 = Me，R6 = F; （5）R5 = F，R6 = H; 和（6）R5 = OMe，R6 = H。

7. 发明申请

US20110281922A1 AMIDE THIAZOLE DERIVATIVE, PREPARATION METHOD AND USES THEREOF 失效
标题翻译：酰胺衍生物，制备方法及其用途
公开(公告)号：US20110281922A1
公开(公告)日：2011-11-17
申请号：US13162121
申请日：2011-06-16
申请人： Guilong ZHAO , Weiren Xu , Yuli Wang , Lida Tang , Yiliang Li , Meixiang Zou , Wei Liu , Hua Shao , Chubing Tan , Peng Liu
发明人： Guilong ZHAO , Weiren Xu , Yuli Wang , Lida Tang , Yiliang Li , Meixiang Zou , Wei Liu , Hua Shao , Chubing Tan , Peng Liu
IPC分类号： A61K31/426 , A61P3/10 , C07D277/38
CPC分类号： C07D277/46 , C07D277/58 , C07D417/12
摘要： The present invention relates to the field of drugs associated with treating 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, R1 is methyl; R2 is phenyl; phenyl, 2-thienyl substituted in a mono-substituted, bi-substituted manner by fluorine and methyl.
摘要翻译：本发明涉及与治疗糖尿病有关的药物领域。特别地，本发明涉及具有式（I）所示结构的二肽基肽酶-IV抑制剂，其含有酰胺噻唑结构并具有治疗糖尿病的作用，以及含有它的制备方法和药物组合物，以及其用于制备用于治疗糖尿病的药物，其中，R 1为甲基; R2是苯基; 苯基，2-取代的噻吩基，被氟和甲基取代，双取代。

8. 发明申请

US20130023486A1 PHENYL C-GLUCOSIDE DERIVATIVES, PREPARATION METHODS AND USES THEREOF 有权
标题翻译：苯乙酰胆碱衍生物，制备方法及其用途
公开(公告)号：US20130023486A1
公开(公告)日：2013-01-24
申请号：US13575258
申请日：2011-01-14
申请人： Guilong Zhao , Hua Shao , Weiren Xu , Wei Liu , Yuli Wang , Lida Tang , Chubing Tan , Bingni Liu , Shijun Zhang
发明人： Guilong Zhao , Hua Shao , Weiren Xu , Wei Liu , Yuli Wang , Lida Tang , Chubing Tan , Bingni Liu , Shijun Zhang
IPC分类号： C07H15/207 , A61P3/10 , A61K31/7034 , A61K31/7042 , C07H15/26 , C07H1/00
CPC分类号： C07H7/04 , A61K31/351 , A61K31/70 , C07D309/10 , C07D409/10 , C07H7/06
摘要： The present invention relates to a sodium glucose cotransporter 2 (SGLT2) inhibitor with a phenyl C-glucoside structure, its preparation method, a pharmaceutical composition containing the same, and its use in treating diabetes and preparing an anti-diabetes medicament. The invention provides a compound with the structure of general formula I and a pharmaceutically acceptable salt and prodrug ester thereof,wherein, the definitions of R5 and R6 are selected from the following: (1) R5=R6=Me; (2) R5=Me, R6=OMe; (3) R5=Me, R6=H; (4) R5=Me, R6=F; (5) R5=F, R6=H; and (6) R5=OMe, R6=H.
摘要翻译：本发明涉及具有苯基C-葡萄糖苷结构的钠葡萄糖共转运蛋白2（SGLT2）抑制剂及其制备方法，含有该葡糖苷结构的药物组合物及其在治疗糖尿病中的用途以及制备抗糖尿病药物。本发明提供具有通式I结构的化合物及其药学上可接受的盐和前药酯，其中R5和R6的定义选自如下：（1）R5 = R6 = Me; （2）R5 = Me，R6 = OMe; （3）R5 = Me，R6 = H; （4）R5 = Me，R6 = F; （5）R5 = F，R6 = H; 和（6）R5 = OMe，R6 = H。

9. 发明申请

US20110218161A1 CYCLOASTRAGENOL MONOGLUCOSIDE, PREPARATION, PHARMACEUTICAL COMPOSITION AND APPLICATION THEREOF 有权
标题翻译： CYCLOASTRAGENOL MONOGLUCOSIDE，制剂，药物组合物及其应用
公开(公告)号：US20110218161A1
公开(公告)日：2011-09-08
申请号：US12678025
申请日：2008-09-08
申请人： Yingmei Han , Guangping Xia , Weiren Xu , Zhuanyou Zhao , Wulin Liu , Naxia Zhao , Peng Liu , Shijun Zhang , Xiaoli Fu , Yuli Wang , Weiting Wang , Lida Tang
发明人： Yingmei Han , Guangping Xia , Weiren Xu , Zhuanyou Zhao , Wulin Liu , Naxia Zhao , Peng Liu , Shijun Zhang , Xiaoli Fu , Yuli Wang , Weiting Wang , Lida Tang
IPC分类号： A61K31/7048 , C07H15/24 , A61P9/00 , C12P19/56 , B65B31/00
CPC分类号： A61K36/481 , A61K31/7048 , C07J17/005 , C12P19/56
摘要： This invention provides a method for preparing cycloastragenol monoglucoside CMG (cycloastragenol-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（环星形胶原蛋白-6-O-＆bgr-D-葡萄糖苷）的方法，包括以下步骤：a。使用常规方法制备的黄芪甲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; b。加入水解酶并允许在恒温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。通过纯化和分离获得产物。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-和bgr-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。

10. 发明申请

US20080214636A1 Glycyrrhetinic Acid-30-Amide Derivatives and Their Use 有权
标题翻译：甘草次酸30-酰胺衍生物及其用途
公开(公告)号：US20080214636A1
公开(公告)日：2008-09-04
申请号：US12090169
申请日：2006-10-16
申请人： Jianwu Wang , Weiren Xu , Jianping Yong , Lida Tang , Shijun Zhang , Lijun Liu , Yuli Wang , Xiaowen Ren
发明人： Jianwu Wang , Weiren Xu , Jianping Yong , Lida Tang , Shijun Zhang , Lijun Liu , Yuli Wang , Xiaowen Ren
IPC分类号： A61K31/42 , C07D261/08
CPC分类号： C07D261/08 , A61K31/415 , C07D413/04
摘要： The present invention relates to the field of a medicine for treating diseases associated with inflammation, immunity or infection, and in particular, to glycyrrhetinic acid-30-amide derivatives of general formula I and their preparation, and a pharmaceutical composition containing the same. Said derivatives and composition exhibit anti-inflammatory, analgesic, anti-allergic, cough-preventing, liver-protecting and anti-viral properties, wherein each group is as defined in the description.
摘要翻译：本发明涉及用于治疗与炎症，免疫或感染有关的疾病的药物领域，特别涉及通式I的甘草次酸 - 酰胺衍生物及其制备方法及含有该药物的药物组合物。所述衍生物和组合物表现出抗炎，镇痛，抗过敏，咳嗽预防，肝保护和抗病毒性质，其中每组如说明书中所定义。

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