3-(13-hydroxy-10-oxotetradecyl)-5,7-dimethoxy-3H-2-benzofuran-1-one

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: 3-(13-hydroxy-10-oxotetradecyl)-5,7-dimethoxy-3H-2-benzofuran-1-one
• 化学式: C₂₄H₃₆O₆
• 分子量: 420.5
• InChiKey: LPYQDDHAJRABQA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  30
• 可旋转键数：
  15
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  82.1
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• HUMAN GLUCAGON-LIKE-PEPTIDE-1 MODULATORS AND THEIR USE IN THE TREATMENT OF DIABETES AND RELATED CONDITIONS
  申请人：Ewing William R.

  公开号：US20080242593A1

  公开（公告）日：2008-10-02

  The present invention provides novel human glucagon-like peptide-1 (GLP-1)-receptor modulators that have biological activity similar or superior to native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 receptor modulators exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration. The peptides of this invention show desirable pharmacokinetic properties and desirable potency in efficacy models of diabetes.

  本发明提供了新型的人类胰高血糖素样肽-1（GLP-1）受体调节剂，其生物活性类似或优于天然GLP-1肽，因此可用于治疗或预防与GLP活性相关的疾病或障碍。此外，本发明提供了新型的化学修饰肽，不仅能刺激2型糖尿病患者的胰岛素分泌，还能产生其他有益的胰岛素促进反应。这些合成肽GLP-1受体调节剂具有较高的蛋白酶水解稳定性，使其成为口服或静脉注射的理想治疗候选药物。本发明的肽具有理想的药代动力学特性和糖尿病疗效模型的理想效力。
• HUMAN GLUCAGON-LIKE PEPTIDE-1 MIMICS AND THEIR USE IN THE TREATMENT OF DIABETES AND RELATED CONDITIONS
  申请人：Natarajan Iyer Sesha

  公开号：US20070287670A1

  公开（公告）日：2007-12-13

  The present invention provides novel human glucagon-like peptide-1 (GLP-1) peptide mimics that mimic the biological activity of the native GLP-1 peptide and thus are useful for the treatment or prevention of diseases or disorders associated with GLP activity. Further, the present invention provides novel, chemically modified peptides that not only stimulate insulin secretion in type II diabetics, but also produce other beneficial insulinotropic responses. These synthetic peptide GLP-1 mimics exhibit increased stability to proteolytic cleavage making them ideal therapeutic candidates for oral or parenteral administration.

  本发明提供了新型的人类胰高血糖素样肽-1 (GLP-1) 肽类模拟物，这些模拟物模仿了天然的 GLP-1 肽的生物活性，因此可用于治疗或预防与 GLP 活性相关的疾病或疾病。此外，本发明提供了新型的化学修饰肽，这些肽不仅可以刺激 II 型糖尿病患者的胰岛素分泌，还可以产生其他有益的胰岛素促进反应。这些合成的 GLP-1 模拟物肽类表现出对蛋白酶水解的稳定性增加，使它们成为口服或静脉注射治疗的理想候选药物。
• US7238671B2
  申请人：——

  公开号：US7238671B2

  公开（公告）日：2007-07-03
• US7417028B2
  申请人：——

  公开号：US7417028B2

  公开（公告）日：2008-08-26
• US7960349B2
  申请人：——

  公开号：US7960349B2

  公开（公告）日：2011-06-14