8-[(2-fluorobenzoyl)amino]octanoic Acid | 183990-47-8

• 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-fluorobenzoyl)amino]octanoic Acid
• CAS: 183990-47-8
• 化学式: C₁₅H₂₀FNO₃
• 分子量: 281.327
• InChiKey: YMUPHHVDDUBVOP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  20
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  66.4
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  8-氨基辛酸 生成 8-[(2-fluorobenzoyl)amino]octanoic Acid
  参考文献：
  名称：

  Compounds and compositions for delivering active agents

  摘要：

  本发明提供了具有以下化学式或其盐的化合物，有助于传递活性剂。还提供了包括本发明化合物和至少一种活性剂（如肽、粘多糖、碳水化合物或脂质）的组合物和剂量单位形式。同时还提供了本发明化合物和组合物的给药方法和制备方法。

  公开号：

  US06346242B1

文献信息

• 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。
• Modified amino acids and compositions comprising them for delivering active agents
  申请人：Emisphere Technologies, Inc.

  公开号：EP1792624A1

  公开（公告）日：2007-06-06

  Modified amino acid compounds useful in the delivery of active agents are provided. The active agents can be peptides, such as rhGH. Methods of administration, such as oral, subcutaneous, sublingual, and intranasal administration, are provided, and methods of preparation of the modified amino acid compound are provided.

  本研究提供了可用于输送活性剂的改性氨基酸化合物。活性剂可以是肽，如 rhGH。提供了给药方法，如口服、皮下注射、舌下含服和鼻内给药，还提供了改性氨基酸化合物的制备方法。
• Fast-acting plant-based medicinal compounds and nutritional supplements
  申请人：RECEPTOR HOLDINGS, INC.

  公开号：US11246852B2

  公开（公告）日：2022-02-15

  Plant-based medicinal compounds or nutritional supplements in various carrier combinations are described. The carriers can include N-acylated fatty amino acids, penetration enhancers, and/or various other beneficial carriers. The plant-based composition/carrier combinations can create administration benefits.

  本文介绍了各种载体组合中的植物药用化合物或营养补充剂。载体可包括 N-酰化脂肪氨基酸、渗透促进剂和/或其他各种有益载体。植物性组合物/载体组合可带来用药益处。
• Studies Directed at the Use of a Parallel Synthesis Matrix to Increase Throughput in an in Vivo Assay
  作者：Andrea Leone-Bay、John Freeman、Doris O'Toole、Connie Rosado-Gray、Sirpa Salo-Kostmayer、Monica Tai、Frank Mercogliano、Robert A. Baughman

  DOI：10.1021/jm990416r

  日期：2000.9.1

  Heparin is the anticoagulant of choice for hospitalized patients, but it is dosed only by injection because it is not absorbed following oral administration. We have discovered and prepared compounds (delivery agents) that facilitate the gastrointestinal absorption of heparin in rats, monkeys, and humans when given orally. We are currently developing a parallel synthesis approach to increase our delivery agent screening throughput in vivo. This approach has been used to produce micromolar quantities of compounds for testing in rats in a 5 x 5 parallel synthesis array. Using an amine benzoylation reaction sequence, 10 mixtures were prepared. These mixtures contained equal weight quantities of five N-substituted, non-alpha, amino acid delivery agents. Each of these mixtures was orally administered to rats in combination with heparin, and plasma clotting times (APTT) were measured to determine activity. Deconvolution of the data accurately identified the most active individual components. Independent synthesis of these compounds verified their activity. This parallel synthesis approach is an effective tool for the screening of oral heparin delivery agents and has increased screening throughput significantly.
• Synthesis and Evaluation of Compounds That Facilitate the Gastrointestinal Absorption of Heparin
  作者：Andrea Leone-Bay、Duncan R. Paton、John Freeman、Christine Lercara、Doris O'Toole、David Gschneidner、Eric Wang、Elizabeth Harris、Connie Rosado、Theresa Rivera、Aldonna DeVincent、Monica Tai、Frank Mercogliano、Rajesh Agarwal、Harry Leipold、Robert A. Baughman

  DOI：10.1021/jm970811m

  日期：1998.3.1

  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.