8-[N-(2,5-dihydroxybenzoyl)amino]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-[N-(2,5-dihydroxybenzoyl)amino]octanoic acid
• 英文别名: 8-[(2,5-dihydroxybenzoyl)amino]octanoic Acid
• 化学式: C₁₅H₂₁NO₅
• 分子量: 295.335
• InChiKey: BVHPIFVSUMSTPM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  21
• 可旋转键数：
  9
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  107
• 氢给体数：
  4
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  8-氨基辛酸 在 sodium hydroxide 作用下， 反应 12.0h， 生成 8-[N-(2,5-dihydroxybenzoyl)amino]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

• N-benzoyl amino acid derivatives pharmaceutical compositions containing
  申请人：Gyogyszerkutato Intezet KFT

  公开号：US05705529A1

  公开（公告）日：1998-01-06

  The invention relates to novel N-benzoylamino acid derivatives of the general formula (I), ##STR1## wherein R.sup.1 and R.sup.2, which are the same or different, stand for a hydroxyl group optionally bearing an acetyl group; or a C.sub.1-6 alkoxy group optionally substituted by a phenyl group; n means an integer from 2 to 15 as well as their tautomers, racemates and optically active individual (pure) isomers or mixtures thereof and the salts of these compounds and pharmaceutical compositions containing these compounds. The invention relates also to a process for the preparation of compounds of the general formula (I). The compounds of general formula (I) inhibit the peroxidation of lipids and therefore, they are expected to be useful for the treatment of diseases being in an indirect or direct connection with pathological oxidation processes, chiefly for the treatment and/or prevention of ischaemic and reperfusion tissue injuries, inflammatory reactions, atherosclerosis, various degenerative neurological disorders as well as for delaying the natural process of the ageing of cells.

  本发明涉及一种新的N-苯甲酰氨基酸衍生物，其一般式为(I)：##STR1##其中R^1和R^2相同或不同，代表可选地带有乙酰基的羟基；或可选地被苯基取代的C1-6烷氧基；n表示2到15的整数，以及它们的互变异构体、外消旋体和光学活性单体（纯异构体）或其混合物以及这些化合物的盐和含有这些化合物的药物组合物。本发明还涉及一种制备一般式（I）化合物的方法。一般式（I）化合物抑制脂质过氧化，因此，它们预计可用于治疗与病理氧化过程间接或直接相关的疾病，主要用于治疗和/或预防缺血和再灌注组织损伤、炎症反应、动脉粥样硬化、各种退行性神经疾病以及延缓细胞自然老化进程。
• 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。
• Neuroprotective Compositions and Methods
  申请人：Lipton Stuart A.

  公开号：US20120296112A1

  公开（公告）日：2012-11-22

  Neurite outgrowth-promoting prostaglandins (NEPPs) and other electrophilic compounds bind to Keap1, a negative regulator of the transcription factor Nrf2, and prevent Keap1-mediated inactivation of Nrf2 and, thus, enhance Nrf2 translocation into the nucleus of neuronal cells. Therefore, neuroprotective compositions and related methods are provided that employ such neuroprotective compounds, and prodrugs of such compounds, to cause dissociation of Nrf2 from a Keap1/Nrf2 complex.

  神经突起促进前列腺素（NEPPs）和其他电子亲和力化合物结合到Keap1上，Keap1是转录因子Nrf2的负调节因子，防止Keap1介导的Nrf2失活，并增强Nrf2进入神经元细胞核的转位。因此，提供了使用这些神经保护化合物及其前药的神经保护组合物和相关方法，以使Nrf2与Keap1 / Nrf2复合物解离的方法。
• N-benzoylamino acid derivatives, pharmaceutical compositions containing them and process for preparing same
  申请人：NISSHIN FLOUR MILLING CO., LTD.

  公开号：EP0576941B1

  公开（公告）日：1997-09-03
• COMPOSITIONS OF PENTOSAN POLYSULFATE SALTS FOR ORAL ADMINISTRATION AND METHODS OF USE
  申请人：Urigen Pharmaceuticals, Inc.

  公开号：EP3110427A1

  公开（公告）日：2017-01-04