2-[3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4-dihydroxy-3,4-dihydro-2H-pyran-6-carboxylic acid

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-[3-acetamido-2,5-dihydroxy-6-(hydroxymethyl)oxan-4-yl]oxy-3,4-dihydroxy-3,4-dihydro-2H-pyran-6-carboxylic acid
• 化学式: C₁₄H₂₁NO₁₁
• 分子量: 379.32
• InChiKey: DLGJWSVWTWEWBJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -3.3
• 重原子数：
  26
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.71
• 拓扑面积：
  195
• 氢给体数：
  7
• 氢受体数：
  11

文献信息

• PROCESS FOR PRODUCING WATER-SOLUBLE HYALURONIC ACID MODIFICATION
  申请人：YASUGI Kenji

  公开号：US20120183567A1

  公开（公告）日：2012-07-19

  The present invention provides a water-soluble modified HA practically used as a drug carrier and a production method thereof. The present invention provides: a water-soluble modified hyaluronic acid, the residence time in blood of which is elongated to a practical level, which is produced by introducing a substituent into the carboxy group of the glucuronic acid of hyaluronic acid or a derivative thereof, via an amide bond, at a lower limit of an introduction ratio of 5 mole % or more, using a BOP condensing agent in an aprotic polar solvent; and a production method thereof. Moreover, by cross-linking the modified hyaluronic acid, the present invention provides a hyaluronic acid gel capable of extremely long drug sustained-release even at the same cross-linking functional group introduction ratio as that of the conventionally known gel.

  本发明提供了一种水溶性改性透明质酸，可实际用作药物载体及其生产方法。本发明提供一种水溶性改性透明质酸，其在血液中的停留时间延长到实际水平，通过在无极性极性溶剂中使用BOP缩合剂，将取代基通过酰胺键引入透明质酸或其衍生物的葡萄糖醛酸羧基中，引入比例的下限为5摩尔％或更高；以及其生产方法。此外，通过交联改性透明质酸，本发明提供一种透明质酸凝胶，即使与传统已知凝胶相同的交联功能基引入比例，也能实现极长时间的药物缓释。
• Process for producing water-soluble hyaluronic acid modification
  申请人：Yasugi Kenji

  公开号：US20090148534A1

  公开（公告）日：2009-06-11

  The present invention provides a water-soluble modified HA practically used as a drug carrier and a production method thereof. The present invention provides: a water-soluble modified hyaluronic acid, the residence time in blood of which is elongated to a practical level, which is produced by introducing a substituent into the carboxy group of the glucuronic acid of hyaluronic acid or a derivative thereof, via an amide bond, at a lower limit of an introduction rate of 5 mole % or more, using a BOP condensing agent in an aprotic polar solvent; and a production method thereof. Moreover, by cross-linking the modified hyaluronic acid, the present invention provides a hyaluronic acid gel capable of extremely long drug sustained-release even at the same cross-linking functional group introduction rate as that of the conventionally known gel.

  本发明提供一种水溶性的改性透明质酸，可实际用作药物载体及其生产方法。本发明提供一种水溶性的改性透明质酸，其在血液中的停留时间延长到实际水平，通过在无极性极性溶剂中使用BOP缩合剂，将取代基通过酰胺键引入到透明质酸或其衍生物的葡萄糖醛酸羧基中，引入速率的下限为5摩尔％或更高，并提供其生产方法。此外，通过交联改性透明质酸，本发明提供一种透明质酸凝胶，即使交联功能团引入速率与传统已知凝胶相同，也能实现极长时间的药物持续释放。
• CONJUGATE OF WATER-SOLUBLE HYALURONIC ACID MODIFICATION PRODUCT WITH GLP-A ANALOGUE
  申请人：Nakamura Teruo

  公开号：US20090082266A1

  公开（公告）日：2009-03-26

  To provide a GLP-1 analogue long-acting prophylactic or therapeutic agent for diabetes, diabetic complications and/or obesity due to diabetes which provides an extended half-life of a GLP-1 analogue in the blood to prevent frequent administration, and is biodegradable and safe. The present invention provides a conjugate obtained by binding, to a GLP-1 analogue into which a mercapto group is incorporated, water soluble hyaluronic acid modification product obtained by incorporating a substituent via an amide bond to the carboxyl group of glucuronic acid portion of hyaluronic acid as a derivative thereof, using a specific condensing agent in an aprotic polar solvent; and a prophylactic or therapeutic agent having a durable blood glucose lowering effect for diabetes, diabetic complications or obesity.
• US8143391B2
  申请人：——

  公开号：US8143391B2

  公开（公告）日：2012-03-27
• US9394379B2
  申请人：——

  公开号：US9394379B2

  公开（公告）日：2016-07-19