2-(4-methoxycarbonylbenzyl)phenyl 2,3,4,6-tetra-O-acetyl-β-D-glucopyranoside | 433331-35-2

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 2-(4-methoxycarbonylbenzyl)phenyl 2,3,4,6-tetra-O-acetyl-β-D-glucopyranoside
• 英文别名: 2-(4-methoxycarbonyl-benzyl)phenyl 2,3,4,6-tetra-O-acetyl-beta-D-glucopyranoside；methyl 4-[[2-[(2S,3R,4S,5R,6R)-3,4,5-triacetyloxy-6-(acetyloxymethyl)oxan-2-yl]oxyphenyl]methyl]benzoate
• CAS: 433331-35-2
• 化学式: C₂₉H₃₂O₁₂
• 分子量: 572.566
• InChiKey: GPTBYQSLAAMKIR-LJNCTHMASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.3
• 重原子数：
  41
• 可旋转键数：
  15
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  150
• 氢给体数：
  0
• 氢受体数：
  12

反应信息

• 作为反应物：
  描述：

  2-(4-methoxycarbonylbenzyl)phenyl 2,3,4,6-tetra-O-acetyl-β-D-glucopyranoside 在 sodium hydroxide 作用下， 以 甲醇 为溶剂， 生成 2-(4-Carboxybenzyl)phenyl β-D-glucopyranoside
  参考文献：
  名称：

  EP1344780

  摘要：

  公开号：
• 作为产物：
  描述：

  2-苄氧基溴苯 在 10% palladium on activated carbon 盐酸 、 三氟化硼乙醚 、 氢气 、 magnesium 作用下， 以 四氢呋喃 、 乙醇 、 二氯甲烷 、 甲苯 为溶剂， 反应 19.0h， 生成 2-(4-methoxycarbonylbenzyl)phenyl 2,3,4,6-tetra-O-acetyl-β-D-glucopyranoside
  参考文献：
  名称：

  GLUCOPYRANOSYLOXYBENZYLBENZENE DERIVATIVES AND MEDICINAL USE THEREOF

  摘要：

  公开号：

  EP1367060B1

文献信息

• Glucopyranosyloxybenzylbenzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
  申请人：Fujikura Hideki

  公开号：US20050113315A1

  公开（公告）日：2005-05-26

  The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein R 1 represents a hydrogen atom, a hydroxy group, a substituted or unsubstituted amino group, a carbamoyl group, a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group etc.; R 2 represents a hydrogen atom or a lower alkyl group; and R 3 represents a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group, a substituted or unsubstituted(lower alkylthio) group etc., or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complication or obesity, pharmaceutical compositions comprising the same and intermediates thereof.

  本发明涉及一种由通式表示的葡萄糖吡喃氧基苯基苯乙烯衍生物： 其中，R1表示氢原子，羟基，取代或未取代的氨基，氨基甲酰基，取代或未取代的（较低烷基）基团，取代或未取代的（较低烷氧基）基团等；R2表示氢原子或较低烷基基团；R3表示取代或未取代的（较低烷基）基团，取代或未取代的（较低烷氧基）基团，取代或未取代的（较低烷硫基）基团等，或其药学上可接受的盐，其具有对人类SGLT2的抑制活性，可用作预防或治疗与高血糖相关的疾病，如糖尿病、糖尿病并发症或肥胖症的药物，以及包含它们的制药组合物和中间体。
• Glucopyranosyloxybenzylbenzene derivatives and medicinal use thereof
  申请人：——

  公开号：US20040138148A1

  公开（公告）日：2004-07-15

  The present invention provides glucopyranosyloxybenzylbenzene derivatives represented by the general formula: 1 wherein P represents a hydrogen atom or a group forming a prodrug; R 1 represents a hydrogen atom, an optionally substituted amino group, a carbamoyl group, an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, etc.; R 2 represents a hydrogen atom or a lower alkyl group; and R 3 represents an optionally substituted lower alkyl group, an optionally substituted lower alkoxy group, an optionally substituted lower alkylthio group, etc., which have an improved oral absorption, and exert an inhibitory activity in human SGLT2, and therefore are useful as drugs for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complications or obesity, or pharmaceutically acceptable salts thereof, and pharmaceutical uses thereof.

  本发明提供了由下式表示的葡萄糖吡喃基氧基苄基苯衍生物：1其中P代表氢原子或形成前药的基团；R1代表氢原子、可选取代氨基、氨基甲酰基、可选取代的低碳基、可选取代的低碳氧基等；R2代表氢原子或低碳基；R3代表可选取代的低碳基、可选取代的低碳氧基、可选取代的低碳硫基等。这些衍生物具有良好的口服吸收性，并在人类SGLT2中表现出抑制活性，因此可用于预防或治疗与高血糖相关的疾病，如糖尿病、糖尿病并发症或肥胖症，或其药学上可接受的盐和药用用途。
• Glucopyranosyloxybenzyl benzene derivatives, medicinal compositions containing the same and intermediates in the production thereof
  申请人：——

  公开号：US20040063170A1

  公开（公告）日：2004-04-01

  The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: 1 wherein R 1 represents a hydrogen atom, a hydroxy group, a substituted or unsubstituted amino group, a carbamoyl group, a substituted or unsubstituted (lower alkyl) group, a substituted or unsubstituted (lower alkoxy) group etc.; R 2 represents a hydrogen atom or a lower alkyl group; and R 3 represents a substituted or unsubstituted (lower alkyl) group, a substituted or unsubstituted (lower alkoxy) group, a substituted or unsubstituted (lower alkylthio) group etc., or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complication or obesity, pharmaceutical compositions comprising the same and intermediates thereof.

  本发明涉及由下式表示的葡萄糖吡喃基氧基苯基苯基衍生物： 其中，R1代表氢原子、羟基、取代或未取代的氨基、氨基甲酰基、取代或未取代的(较低烷基)基团、取代或未取代的(较低烷氧基)基团等；R2代表氢原子或较低烷基基团；R3代表取代或未取代的(较低烷基)基团、取代或未取代的(较低烷氧基)基团、取代或未取代的(较低烷硫基)基团等，或其药学上可接受的盐，其在人类SGLT2中具有抑制活性，并且可用作预防或治疗与高血糖有关的疾病，如糖尿病、糖尿病并发症或肥胖症的药剂。本发明还涉及包含上述衍生物的制药组合物及其中间体。
• GLUCOPYRANOSYLOXYBENZYL BENZENE DERIVATIVES, MEDICINAL COMPOSITIONS CONTAINING THE SAME AND INTERMEDIATES IN THE PRODUCTION THEREOF
  申请人：Kissei Pharmaceutical Co., Ltd.

  公开号：EP1344780A1

  公开（公告）日：2003-09-17

  The present invention relates to glucopyranosyloxybenzylbenzene derivatives represented by the general formula: wherein R1 represents a hydrogen atom, a hydroxy group, a substituted or unsubstituted amino group, a carbamoyl group, a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group etc.; R2 represents a hydrogen atom or a lower alkyl group; and R3 represents a substituted or unsubstituted(lower alkyl) group, a substituted or unsubstituted(lower alkoxy) group, a substituted or unsubstituted (lower alkylthio) group etc., or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of a disease associated with hyperglycemia such as diabetes, diabetic complication or obesity, pharmaceutical compositions comprising the same and intermediates thereof.

  本发明涉及通式代表的葡糖基吡喃氧基苄基苯衍生物： 其中R1代表氢原子、羟基、取代或未取代的氨基、氨基甲酰基、取代或未取代的(低级烷基)基团、取代或未取代的(低级烷氧基)基团等；R2代表氢原子或低级烷基；R3代表取代或未取代的(低级烷基)基团、取代或未取代的(低级烷氧基)基团、取代或未取代的(低级烷硫基)基团等、或其药学上可接受的盐，它们对人类 SGLT2 具有抑制活性，可用作预防或治疗与高血糖有关的疾病（如糖尿病、糖尿病并发症或肥胖症）的制剂、包含这些制剂的药物组合物及其中间体。
• US7053060B2
  申请人：——

  公开号：US7053060B2

  公开（公告）日：2006-05-30