5-(2-hydroxy-4-chlorobenzoyl)aminovaleric acid | 403789-58-2

• 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: 5-(2-hydroxy-4-chlorobenzoyl)aminovaleric acid
• 英文别名: 5-[(4-Chloro-2-hydroxybenzoyl)amino]pentanoic acid
• CAS: 403789-58-2
• 化学式: C₁₂H₁₄ClNO₄
• mdl: MFCD19411193
• 分子量: 271.7
• InChiKey: STUTZVFDKINXJF-UHFFFAOYSA-N

物化性质

• 沸点：
  501.0±50.0 °C(Predicted)
• 密度：
  1.352±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  18
• 可旋转键数：
  6
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.333
• 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：

  4-氯-2-羟基苯甲酰胺 、 7-chlorocarsalam 、 5-溴戊酸乙酯 、 氯甲酸乙酯 、 碳酸氢钠 生成 5-(2-hydroxy-4-chlorobenzoyl)aminovaleric acid
  参考文献：
  名称：

  摘要：

  DOI：

文献信息

• (5-(2-Hydroxy-4-chlorobenzoyl) aminovaleric acid and salts thereof and compositions containing the same for delivering active agents
  申请人：——

  公开号：US20040023847A1

  公开（公告）日：2004-02-05

  (5-(2-hydroxy-4-chlorobenzoyl) aminovaleric acid, salts thereof, and compositions containing the same for the delivery of active agents are provided. Methods of administration, treatment of disease and preparation are provided as well.

  提供了5-(2-羟基-4-氯苯甲酰)氨基戊酸及其盐和含有它们的药物组成物，用于传递活性药物。同时还提供了治疗疾病的给药方法、制备方法。
• 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）。
• GLP-1 fusion peptides conjugated to polymer(s), their production and use
  申请人：Biocompatibles UK Limited

  公开号：EP1972349A1

  公开（公告）日：2008-09-24

  The present invention provides fusion peptides having GLP-1 activity and enhanced stability in vivo, in particular resistancy to dipeptidyl peptidase IV conjugated to polymers, thereby forming conjugate molecules. The fusion peptide of the conjugate molecule comprises as component (I) N-terminally a GLP-1(7-35, 7-36 or 7-37) sequence and as component (II) Gterminally a peptide sequence of at least 9 amino acids or a functional fragment, variant or derivative thereof. A synthetic polymer and/or a protein, e.g transferrin or albumin, is covalently or non-covalently bound to the fusion peptide to form the conjugate molecule. Component (II) is preferably a full or partial version of IP2 (intervening peptide 2). A preferred embodiment comprises the sequence GLP-1(7-35, 36 or 37)/IP2/GLP-1(7-35, 36 or 37) or GLP-2 and a polymeric component, e.g. a natural or non-natural polymer. The fusion peptide may be produced in engineered cells or synthetically and is e.g. conjugated to the polymeric component by chemical synthesis. The conjugate molecule may be used for the preparation of a medicament for treating various diseases or disorders, e.g. diabetes type 1 or 2, apoptosis related diseases or neurodegenerative disorders.

  本发明提供的融合肽具有 GLP-1 活性和更强的体内稳定性，特别是对二肽基肽酶 IV 的抗性，与聚合物共轭，从而形成共轭分子。共轭分子的融合肽包括作为组分（I）的 N 端 GLP-1（7-35、7-36 或 7-37）序列和作为组分（II）的 G 端至少 9 个氨基酸的肽序列或其功能片段、变体或衍生物。合成聚合物和/或蛋白质（如转铁蛋白或白蛋白）与融合肽共价或非共价结合，形成共轭分子。成分（II）最好是完整版或部分版的 IP2（中间肽 2）。优选的实施方案包括序列 GLP-1（7-35、36 或 37）/IP2/GLP-1（7-35、36 或 37）或 GLP-2 和聚合物成分，例如天然或非天然聚合物。融合肽可以在工程细胞中产生，也可以人工合成，例如通过化学合成与聚合物成分共轭。该共轭分子可用于制备治疗各种疾病或失调的药物，如 1 型或 2 型糖尿病、细胞凋亡相关疾病或神经退行性疾病。
• (5-(2-HYDROXY-4-CHLOROBENZOYL) AMINOVALERIC ACID AND SALTS THEREOF AND COMPOSITIONS CONTAINING THE SAME FOR DELIVERING ACTIVE AGENTS
  申请人：Emisphere Technologies, Inc.

  公开号：EP1322595B1

  公开（公告）日：2008-05-28
• GLP-1 Fusion Peptides Conjugated to Polymer(s), Their Production and Use
  申请人：Wallrapp Christine

  公开号：US20100160556A1

  公开（公告）日：2010-06-24

  The present invention provides fusion peptides having GLP-1 activity and enhanced stability in vivo, in particular resistancy to dipeptidyl peptidase IV conjugated to polymers, thereby forming conjugate molecules. The fusion peptide of the conjugate molecule comprises as component (I) N-terminally a GLP-1(7-35, 7-36 or 7-37) sequence and as component (II) C-terminally a peptide sequence of at least 9 amino acids or a functional fragment, variant or derivative thereof. A synthetic polymer and/or a protein, e.g transferrin or albumin, is covalently or non-covalently bound to the fusion peptide to form the conjugate molecule. Component (II) is preferably a full or partial version of IP2 (intervening peptide 2). A preferred embodiment comprises the sequence GLP-1(7-35, 36 or 37)/IP2/GLP-1(7-35, 36 or 37) or GLP-2 and a polymeric component, e.g. a natural or non-natural polymer. The fusion peptide may be produced in engineered cells or synthetically and is e.g. conjugated to the polymeric component by chemical synthesis. The conjugate molecule may be used for the preparation of a medicament for treating various diseases or disorders, e.g. diabetes type 1 or 2, apoptosis related diseases or neurodegenerative disorders.