N-(3-cyano-4,5-dimethyl-2-pyrrylcarbamoylmethyl)iminodiacetic acid | 75297-21-1

• 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: N-(3-cyano-4,5-dimethyl-2-pyrrylcarbamoylmethyl)iminodiacetic acid
• 英文别名: Glycine, N-(carboxymethyl)-N-(2-((3-cyano-4,5-dimethyl-1H-pyrrol-2-yl)amino)-2-oxoethyl)-；2-[carboxymethyl-[2-[(3-cyano-4,5-dimethyl-1H-pyrrol-2-yl)amino]-2-oxoethyl]amino]acetic acid
• CAS: 75297-21-1
• 化学式: C₁₃H₁₆N₄O₅
• 分子量: 308.294
• InChiKey: BVXRFBZNNRXJGR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.8
• 重原子数：
  22
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  147
• 氢给体数：
  4
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  2-chloroacetamido-3-cyano-4,5-dimethylpyrrole 、 iminodiacetic acid disodium salt 在 sodium hydroxide 作用下， 以 甲醇 、 水 为溶剂， 反应 24.0h， 生成 N-(3-cyano-4,5-dimethyl-2-pyrrylcarbamoylmethyl)iminodiacetic acid
  参考文献：
  名称：

  评价99mTc标记的取代2-氨基吡咯的亚氨基二乙酸衍生物作为肝胆显像剂。一世。

  摘要：

  合成了N-（3-氰基-4,5-二甲基-2-吡啶基氨基甲酰基甲基）亚氨基二乙酸（IIa）和N-（3-氰基-4-甲基-5-苄基-2-吡啶基氨基甲酰基甲基）亚氨基二乙酸（IIb），用99m tech标记，然后与99mTc标记的对异丙基乙酰基苯胺亚氨基二乙酸（I）进行比较，以观察大鼠的肝胆活动。所有这三种化合物均显示出从血液中清除放射性的相似作用。注射后1小时比较各个器官的放射性量，结果表明I和IIb之间无显着差异。化合物IIa在胃肠道中的放射性明显降低，而在肾脏和膀胱中的放射性较高。

  DOI：

  10.1002/jps.2600690634

文献信息

• Lipid construct for delivery of insulin to a mammal
  申请人：SDG, INC.

  公开号：US10004686B2

  公开（公告）日：2018-06-26

  The instant invention is drawn to a hepatocyte targeted composition comprising insulin associated with a lipid construct comprising an amphipathic lipid and an extended amphipathic lipid that targets the construct to a receptor displayed by an hepatocyte. The composition can comprise a mixture of free insulin and insulin associated with the complex. The composition can be modified to protect insulin and the complex from degradation. The invention also includes methods for the manufacture of the composition and loading insulin into the composition and recycling various components of the composition. Methods of treating individuals inflicted with diabetes.

  本发明涉及一种肝细胞靶向组合物，该组合物包含与脂质构建物相关联的胰岛素，脂质构建物包括两性脂质和扩展两性脂质，该构建物可靶向肝细胞显示的受体。 该组合物可包括游离胰岛素和与复合物相关的胰岛素的混合物。 可以对组合物进行修饰，以保护胰岛素和复合物不被降解。 本发明还包括制造组合物、将胰岛素装入组合物以及回收组合物中各种成分的方法。 治疗糖尿病患者的方法。
• Orally bioavailable lipid-based constructs
  申请人：SDG, INC.

  公开号：US10568835B2

  公开（公告）日：2020-02-25

  The present invention is embodied by a composition capable of chaperoning a typically non-orally available therapeutic or diagnostic agent through the environment of the digestive tract such that the therapeutic or diagnostic agent is bioavailable. The composition may or may not be targeted to specific cellular receptors, such as hepatocytes. Therapeutic agents include, but are not limited to, insulin, calcitonin, serotonin, and other proteins. Targeting is accomplished with biotin or metal based targeting agents.

  本发明体现为一种组合物，它能够通过消化道环境对通常非口服的治疗剂或诊断剂进行陪衬，从而使治疗剂或诊断剂具有生物可利用性。该组合物可以针对或不针对特定的细胞受体，如肝细胞。治疗剂包括但不限于胰岛素、降钙素、血清素和其他蛋白质。生物素或金属靶向剂可实现靶向。
• Hepatocyte delivery vehicle for delivery of a combination of recombinant human regular insulin and recombinant human insulin isophane to a mammal
  申请人：Lau R. John

  公开号：US20060222697A1

  公开（公告）日：2006-10-05

  The instant invention is drawn to a hepatocyte targeted composition comprising a mixture of free recombinant human insulin isophane and free Recombinant human regular insulin insulin and a mixture of recombinant human insulin isophane and Recombinant human regular insulin insulin associated with a water insoluble target molecule complex, wherein the complex comprises multiple linked individual units and a supra-molecular lipid construct matrix. Recombinant human insulin isophane and Recombinant human regular insulin insulin are present within the complex in at least one form wherein the recombinant human insulin isophane and Recombinant human regular insulin insulin have regions of positive charge which interacts with a negative charge on the complex. The invention also includes methods for the manufacture of the composition and methods of managing blood glucose levels in individuals with Type I and Type II diabetes.

  本发明涉及一种肝细胞靶向组合物，该组合物包括游离重组人胰岛素异构体和游离重组人普通胰岛素胰岛素的混合物，以及与水不溶性靶分子复合物相关联的重组人胰岛素异构体和重组人普通胰岛素胰岛素的混合物，其中该复合物包括多个相连的单个单元和超分子脂质构建基质。重组人胰岛素异构体和重组人普通胰岛素以至少一种形式存在于复合物中，其中重组人胰岛素异构体和重组人普通胰岛素具有正电荷区域，与复合物上的负电荷相互作用。本发明还包括组合物的制造方法和管理 I 型和 II 型糖尿病患者血糖水平的方法。
• Hepatocyte delivery vehicle for delivery of glargine insulin to a mammal
  申请人：Lau R. John

  公开号：US20060222698A1

  公开（公告）日：2006-10-05

  The instant invention is drawn to a hepatocyte targeted composition comprising a mixture of free glargine insulin and glargine insulin associated with a water insoluble target molecule complex, wherein the complex comprises multiple linked individual units and a supra-molecular lipid construct matrix. Glargine insulin is present within the complex in at least one form wherein the glargine insulin has a positive charge which interacts with a negative charge on the complex. The invention also includes methods for the manufacture of the composition and methods of managing blood glucose levels in individuals with Type I and Type II diabetes.

  本发明涉及一种肝细胞靶向组合物，该组合物包括游离格列宁胰岛素和与水不溶性靶分子复合物相关的格列宁胰岛素的混合物，其中复合物包括多个相连的单个单元和超分子脂质结构基质。格列宁胰岛素至少以一种形式存在于复合物中，其中格列宁胰岛素带有正电荷，与复合物上的负电荷相互作用。本发明还包括制造该组合物的方法和管理 I 型和 II 型糖尿病患者血糖水平的方法。
• HEPATOCYTE DIRECTED VESICLE DELIVERY SYSTEM
  申请人：GEHO, W., Blair

  公开号：EP0274467A1

  公开（公告）日：1988-07-20