(2S)-2-[[(3S)-3-amino-4-(1H-imidazol-5-yl)-2-oxobutyl]amino]-3-hydroxypropanal

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (2S)-2-[[(3S)-3-amino-4-(1H-imidazol-5-yl)-2-oxobutyl]amino]-3-hydroxypropanal
• 化学式: C₁₀H₁₆N₄O₃
• 分子量: 240.26
• InChiKey: BAKXLTHIAATYBU-BDAKNGLRSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -2.3
• 重原子数：
  17
• 可旋转键数：
  8
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  121
• 氢给体数：
  4
• 氢受体数：
  6

文献信息

• HUMAN INSULIN ANALOGUE AND ACYLATED DERIVATIVE THEREOF
  申请人：Shanghai Hengrui Pharmaceutical Co., Ltd.

  公开号：US20140329745A1

  公开（公告）日：2014-11-06

  The present invention provides a human insulin analogue, an acylated derivative thereof and a physiologically acceptable salt. The present invention further provides a preparation method for the insulin analogue and an application of the insulin analogue as a therapeutic agent, and particularly as a diabetes mellitus therapeutic agent.

  本发明提供了一种人胰岛素类似物、其酰化衍生物和生理上可接受的盐。本发明还提供了一种制备胰岛素类似物的方法以及胰岛素类似物作为治疗剂的应用，特别是作为糖尿病治疗剂的应用。
• CONJUGATES OF A POLYPEPTIDE AND AN OLIGOSACCHARIDE
  申请人：Bos Ebo Sybren

  公开号：US20120039843A1

  公开（公告）日：2012-02-16

  The present invention relates to conjugates of a polypeptide and an oligosaccharide, wherein the polypeptide is conjugated to at least one oligosaccharide-spacer residue, the oligosaccharide being a synthetic sulfated oligosaccharide comprising 4-18 monosaccharide units and per se having affinity to antithrombin III and the spacer being a bond or an essentially pharmacologically inactive flexible linking residue, or a pharmaceutically acceptable salt thereof. The conjugates of the invention have improved pharmacokinetic properties when compared to the original polypeptides (i.e. the corresponding non-conjugated polypeptides per se).

  本发明涉及一种多肽和寡糖的结合物，其中多肽与至少一种寡糖-间隔物残基结合，所述寡糖是一种合成的磺化寡糖，包含4-18个单糖单位，并具有与抗凝血酶III亲和力，所述间隔物是一种化学键或基本上是药理学上不活性的柔性连接残基，或其药学上可接受的盐。与原始多肽（即相应的非结合多肽本身）相比，本发明的结合物具有改善的药代动力学特性。
• ESTER INSULIN
  申请人：Kent Stephen B.H.

  公开号：US20120220522A1

  公开（公告）日：2012-08-30

  Compositions and methods related to ester insulin or derivatives thereof are provided. The compositions include Glu A4 -Thr B30 ester insulin, in which side chains of Glu A4 and Thr B30 of native human insulin or an insulin analogue such as insulin lispro are covalently linked via a single ester bond. The ester insulin is efficiently folded, forming the desired disulfides. The Thr B30 -Glu A4 ester bond can be cleaved in vitro or in vivo to give the desired folded insulin with full biological activity. The ester insulin is readily prepared by total chemical synthesis, and amendable to cost-effective, large scale manufacturing. Also provided are pharmaceutical compositions and kits for use in practicing the subject methods. Also provided are methods of using the subject compositions and kits in the treatment of a variety of different disease conditions, particularly glucose metabolic disorders such as diabetes and obesity.

  本发明提供与酯基胰岛素或其衍生物相关的组合物和方法。其中，所述组合物包括GluA4-ThrB30酯基胰岛素，其中，人源胰岛素或胰岛素类似物如胰岛素利斯普罗的GluA4和ThrB30侧链通过单个酯键共价连接。酯基胰岛素能够高效地折叠，形成所需的二硫键。ThrB30-GluA4酯基键可以在体内或体外被裂解，以得到具有完全生物活性的所需折叠胰岛素。酯基胰岛素可以通过全合成方法轻松制备，并且适用于成本效益高、大规模制造。此外，还提供了用于实施所述方法的制药组合物和工具包。还提供了使用所述组合物和工具包治疗各种不同疾病状态的方法，特别是葡萄糖代谢障碍如糖尿病和肥胖症。
• COMBINATION OF ACYLATED GLUCAGON ANALOGUES WITH INSULIN ANALOGUES
  申请人：Fosgerau Keld

  公开号：US20140011733A1

  公开（公告）日：2014-01-09

  The invention relates to methods for treating metabolic disorders, including diabetes by using a combination of an acylated glucagon analogue and an insulin analogue. The invention also features a kit that includes an acylated glucagon analogue and an insuline analogue.
• INSULIN ANALOGUES OF PROLONGED ACTIVITY
  申请人：INSTYTUT BIOTECHNOLOGII I ANTYBIOTYKOW

  公开号：US20140121353A1

  公开（公告）日：2014-05-01

  New biosynthetic analogues of recombined human insulin of prolonged therapeutical activity, which can find place in prophylactic and treatment of diabetes.