4-Salicylamido-phenylessigsaeure | 61126-74-7

• 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: 4-Salicylamido-phenylessigsaeure
• 英文别名: 4-[(2-Hydroxybenzoyl)amino]benzeneacetic acid；2-[4-[(2-hydroxybenzoyl)amino]phenyl]acetic acid
• CAS: 61126-74-7
• 化学式: C₁₅H₁₃NO₄
• 分子量: 271.273
• InChiKey: ILYRIYLUHFDIJM-UHFFFAOYSA-N

物化性质

• 沸点：
  414.8±35.0 °C(Predicted)
• 密度：
  1.397±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  20
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 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：

  邻乙酰水杨酰氯 在 sodium hydroxide 、 三乙胺 作用下， 以 乙酸乙酯 为溶剂， 反应 6.0h， 生成 4-Salicylamido-phenylessigsaeure
  参考文献：
  名称：

  4-[4-[(2-Hydroxybenzoyl)amino]phenyl]butyric Acid as a Novel Oral Delivery Agent for Recombinant Human Growth Hormone

  摘要：

  A series of N-acetylated, non-alpha, aromatic amino acids was prepared and shown to promote the absorption of recombinant human growth hormone (rhGH) from the gastrointestinal tract. Seventy compounds in this family were tested in vivo in rats. Of the compounds tested, 4-[4-[(2-hydroxybenzoyl)amino]phenyl]butyric acid was identified as a preclinical candidate and was used to demonstrate the oral delivery of rhGH in primates. A significant positive correlation was found between the relative log k' of the delivery agents, as determined by HPLC on an immobilized artificial membrane (IAM) column, and serum rhGH concentrations following oral or colonic dosing in rats. Structure-activity relationships have also been developed on the basis of electronic effects and hydrogen-bonding characteristics of the aromatic amide substituents.

  DOI：

  10.1021/jm960038f

文献信息

• 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。
• Oral GLP-1 Formulations
  申请人：Sarubbi Donald J.

  公开号：US20100016229A1

  公开（公告）日：2010-01-21

  The present invention provides pharmaceutical compositions comprising of at least one delivery agent and GLP-1. These pharmaceutical compositions facilitate the oral delivery of GLP-1, providing improved (e.g. increased) bioavailability of GLP-1 compared to administration of GLP-1 without a delivery agent.

  本发明提供了包含至少一种传递剂和GLP-1的药物组合物。这些药物组合物促进了GLP-1的口服给药，相比于没有传递剂的GLP-1给药，提高了GLP-1的生物利用度（例如，增加了生物利用度）。
• Method for administering GLP-1 molecules
  申请人：Emisphere Technologies, Inc.

  公开号：EP2409569A2

  公开（公告）日：2012-01-25

  The invention encompasses formulations that demonstrate the feasibility of oral absorption comprising GLP-1 compounds and specified delivery agents.

  本发明包括能证明口服吸收 GLP-1 化合物和特定给药剂可行性的制剂。
• METHOD FOR ADMINISTERING GLP-1 MOLECULES
  申请人：Emisphere Technologies, Inc.

  公开号：EP1478233B1

  公开（公告）日：2016-11-09
• EP2409569B1
  申请人：——

  公开号：EP2409569B1

  公开（公告）日：2017-08-16