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

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.

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。

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。