8-(2-hydroxy-5-methylbenzoylamino)octanoic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 8-(2-hydroxy-5-methylbenzoylamino)octanoic acid
• 英文别名: 8-[(2-Hydroxy-5-methylbenzoyl)amino]octanoic acid
• 化学式: C₁₆H₂₃NO₄
• 分子量: 293.363
• InChiKey: BVEZKUMIIDQCTG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  21
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  86.6
• 氢给体数：
  3
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  8-氨基辛酸 在 sodium hydroxide 作用下， 以 二氯甲烷 为溶剂， 反应 4.5h， 生成 8-(2-hydroxy-5-methylbenzoylamino)octanoic acid
  参考文献：
  名称：

  Synthesis and Evaluation of Compounds That Facilitate the Gastrointestinal Absorption of Heparin

  摘要：

  A family of novel compounds (delivery agents) that promote the gastrointestinal absorption of USP heparin in rats and primates has been discovered. The delivery agents in combination with heparin were administered either orally or intracolonically in an aqueous propylene glycol solution and caused dramatic increases in both plasma heparin concentrations (anti-Factor Xa) and clotting times (APTT). Using one of the most effective delivery agents in this series, an estimated relative bioavailability of 8% can be achieved following oral administration to cynomolgus monkeys. To establish a correlation between the in vivo data and an in vitro parameter, immobilized artificial membrane (IAM) chromatography was performed. Log relative k' values were correlated to the efficiency of oral heparin delivery.

  DOI：

  10.1021/jm970811m

文献信息

• VALACYCLOVIR FORMULATIONS
  申请人：Oyewumi Moses

  公开号：US20090124639A1

  公开（公告）日：2009-05-14

  The present invention relates to valacyclovir formulations having improved bioavailability resulting in better efficacy and/or requiring less frequent administration.

  本发明涉及瓦拉西韦制剂，其具有改善的生物利用度，从而具有更好的疗效和/或需要更少的频繁给药。
• COMPOUNDS AND COMPOSITIONS FOR DELIVERING ACTIVE AGENTS
  申请人：Sarubbi Donald J.

  公开号：US20090324540A1

  公开（公告）日：2009-12-31

  Carrier compounds and compositions therewith which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

  本发明提供了用于传递活性剂的载体化合物和组合物。同时还提供了其治疗方法和制备方法。
• POLYMERIC DELIVERY AGENTS AND DELIVERY AGENT COMPOUNDS
  申请人：Milstein J. Sam

  公开号：US20070141022A1

  公开（公告）日：2007-06-21

  Polymeric delivery agents, delivery agent compounds and compositions comprising them which are useful in the delivery of active agents are provided. Methods of administration and preparation are provided as well.

  本发明提供了用于传递活性物质的高分子传递剂、传递剂化合物和包含它们的组合物。同时还提供了用于制备和管理的方法。
• Compositions for delivering peptide YY and PYY agonists
  申请人：Dinh Steve

  公开号：US20050009748A1

  公开（公告）日：2005-01-13

  The present invention provides a composition (e.g., a pharmaceutical composition) comprising at least one delivery agent compound and at least one of peptide YY (PYY) and a PYY agonist. Preferably, the composition includes a therapeutically effective amount of peptide YY or the PYY agonist and the delivery agent compound. The composition of the present invention facilitates the delivery of PYY, a PYY agonist, or a mixture thereof and increases its bioavailability compared to administration without the delivery agent compound. PPY and PYY agonists possess activity as agents to reduce nutrient availability, including reduction of food intake

  本发明提供了一种组合物（例如药物组合物），该组合物包含至少一种递送剂化合物以及肽YY（PYY）和PYY激动剂中的至少一种。优选地，该组合物包括治疗有效量的肽 YY 或PYY 激动剂和递质化合物。本发明的组合物有利于PYY、PYY激动剂或其混合物的递送，与不使用递送剂化合物的给药相比，可提高其生物利用度。PY和PYY激动剂具有降低营养供应的活性，包括减少食物摄入量。
• EP1015008A4
  申请人：——

  公开号：EP1015008A4

  公开（公告）日：2006-08-09