4-[4-[5-[4-(3-Carboxypropanoylamino)butyl]-3,6-dioxopiperazin-2-yl]butylamino]-4-oxobutanoic acid

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 4-[4-[5-[4-(3-Carboxypropanoylamino)butyl]-3,6-dioxopiperazin-2-yl]butylamino]-4-oxobutanoic acid
• 化学式: C₂₀H₃₂N₄O₈
• 分子量: 456.5
• InChiKey: UJMQHRHRPGIASO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.6
• 重原子数：
  32
• 可旋转键数：
  16
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.7
• 拓扑面积：
  191
• 氢给体数：
  6
• 氢受体数：
  8

文献信息

• Substituted diketopiperazine analogs for use as drug delivery agents
  申请人：Mannkind Corporation

  公开号：EP2862854A1

  公开（公告）日：2015-04-22

  The present invention provides an asymmetrically substituted diketopiperazine having the general structure of: wherein R is H or an alkyl group of 1-10 carbons; n or m = 0 -20; X is an amide, ester, sulfone, sulfoxide, amine, or ketone; and Y is an amide, ester, acid, hydroxyl, phenol, sulfoxide, phosphoric acid, or thiol, for use as a drug delivery system in the delivery of active agents. Further preferred uses include regulating blood glucose levels, reducing or lowering fasting blood glucose levels, and treating diabetes, such as type II diabetes.

  本发明提供了一种不对称取代的二酮哌嗪，其一般结构如下： 其中 R 是 H 或 1-10 个碳原子的烷基；n 或 m = 0 -20；X 是酰胺、酯、砜、亚砜、胺或酮；Y 是酰胺、酯、酸、羟基、酚、亚砜、磷酸或硫醇，可用作给药系统以输送活性剂。进一步的优选用途包括调节血糖水平，降低空腹血糖水平，治疗糖尿病，如 II 型糖尿病。
• GLUCAGON-LIKE PEPTIDE 1(GLP-1) PHARMACEUTICAL FORMULATIONS
  申请人：MannKind Corporation

  公开号：EP2010155A2

  公开（公告）日：2009-01-07
• SUBSTITUTED DIKETOPIPERAZINE ANALOGS FOR USE AS DRUG DELIVERY AGENTS
  申请人：MannKind Corporation

  公开号：EP2379511B1

  公开（公告）日：2014-12-17
• GLUCAGON-LIKE PEPTIDE 1 (GLP-1) PHARMACEUTICAL FORMULATIONS
  申请人：Hokenson Mark J.

  公开号：US20080260838A1

  公开（公告）日：2008-10-23

  A composition is disclosed comprising glucagon-like peptide 1 (GLP-1) particles in combination with diketopiperazine (DKP) that is stable both in vitro and in vivo. The composition has utility as a pharmaceutical formulation for treating diseases such as diabetes, cancers, and obesity but is not limited to such diseases or conditions. In particularly, the composition has utility as a pharmaceutical formulation for pulmonary delivery.
• Cell Transport Compositions and Uses Thereof
  申请人：Gelber Cohava

  公开号：US20090232891A1

  公开（公告）日：2009-09-17

  Compositions and methods have been developed for transporting compounds across membranes with little or no toxicity and, when targeted through the appropriate routes of administration (i.e., lung, gastrointestinal (GI) tract), little or no immune stimulation. The compositions can mediate cellular delivery of compounds that would otherwise not enter cells and enhance the intracellular delivery of compounds that would otherwise enter cells inefficiently. The methods are carried out by contacting a proximal face of a lipid bilayer or membrane (e.g. the surface of an intact cell) with a complex containing a compound (e.g., a therapeutic agent) and a diketopiperazine (DKP). DKP and the compound are non-covalently associated with each other or covalently bound to each other.