N-(4-methylsalicyloyl)-8-aminocaprylic 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: N-(4-methylsalicyloyl)-8-aminocaprylic acid
• 英文别名: 8-(2-Hydroxy-4-methylbenzamido)octanoic acid；8-[(2-hydroxy-4-methylbenzoyl)amino]octanoic acid
• 化学式: C₁₆H₂₃NO₄
• 分子量: 293.363
• InChiKey: RPGCTYSHAIQANM-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 N-(4-methylsalicyloyl)-8-aminocaprylic 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

• Compositions and methods for enhanced mucosal delivery of Y2 receptor-binding peptides and methods for treating and preventing obesity
  申请人：Nastech Pharmaceutical Company Inc.

  公开号：US20040157777A1

  公开（公告）日：2004-08-12

  Pharmaceutical compositions and methods are described comprising at least one Y2 receptor-binding peptide, such as peptide YY(PYY), Neuropeptide Y (NPY) or Pancreatic Peptide (PP) and one or more mucosal delivery-enhancing agents for enhanced nasal mucosal delivery of the peptide YY, for treating a variety of diseases and conditions in mammalian subjects, including obesity.

  描述了包含至少一种Y2受体结合肽（如肽YY（PYY）、神经肽Y（NPY）或胰岛素肽（PP））和一种或多种黏膜传递增强剂的药物组合物和方法，以增强肽YY在鼻黏膜中的传递，用于治疗哺乳动物主体中的多种疾病和病况，包括肥胖。
• Intranasal administration of glucose-regulating peptides
  申请人：Quay C. Steven

  公开号：US20050143303A1

  公开（公告）日：2005-06-30

  Pharmaceutical compositions and methods are described comprising at least one glucose-regulating peptide, such as amylin, glucagon-like peptide-1 (GLP), pramlintide or exendin-4 and one or more mucosal delivery-enhancing agents for enhanced nasal mucosal delivery of the amylin, for treating a variety of diseases and conditions in mammalian subjects, including obesity and diabetes mellitus.

  本文介绍了一种药物组合和方法，其中包括至少一种调节葡萄糖的肽类，如降淀粉样肽、胰高血糖素样肽-1（GLP）、普拉林肽或外肽-4，以及一种或多种黏膜传递增强剂，以增强降淀粉样肽在鼻黏膜上的传递，用于治疗哺乳动物主体中的多种疾病和病况，包括肥胖和糖尿病。
• Pulmonary delivery of active agents
  申请人：Emisphere Technologies, Inc.

  公开号：US20030072740A1

  公开（公告）日：2003-04-17

  The present invention provides methods for administering an active agent to an animal in need of the agent by the pulmonary route. This method comprises administering via the pulmonary route, a composition comprising (a) an active agent and (b)(i) an acylated amino acid, (ii) a sulfonated amino acid, or (iii) a combination of (i) and (ii). Administration of the compositions of the present invention provide improved pulmonary delivery and greater bioavailability of the active agent than administration of the active agent alone. As a result, lesser amounts of the active agent may be administered to obtain a desired result when contained in the composition of the present invention than when administered alone.

  本发明提供了一种通过肺部途径给需要该药物的动物给药的方法。该方法包括通过肺部途径给予一种组合物，该组合物包括（a）一种活性药物和（b）（i）一种酰化氨基酸，（ii）一种磺化氨基酸或（iii）（i）和（ii）的组合物。本发明的组合物给药提供了比单独给药更好的肺部输送和更高的活性药物生物利用度。因此，当包含在本发明的组合物中时，可以给予更少的活性药物以获得所需的结果，而不是单独给药。
• 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。
• COMPOSITIONS AND METHODS FOR ENHANCED MUCOSAL DELIVERY OF PYY PEPTIDE
  申请人：Quay C. Steven

  公开号：US20070129299A1

  公开（公告）日：2007-06-07

  Pharmaceutical compositions are described comprising PYY(3-36) (SEQ ID NO: 2), a solubilizing agent, a lipid, a polyol.

  本文描述了一种药物组合物，其中包含PYY(3-36) (序列ID号：2)，一种溶解剂，一种脂质和一种多元醇。