3-[2-[2-[3-(3-Methyl-2,5-dioxopyrrol-1-yl)propanoylamino]ethoxy]ethoxy]propanoic acid | 1374666-24-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: 3-[2-[2-[3-(3-Methyl-2,5-dioxopyrrol-1-yl)propanoylamino]ethoxy]ethoxy]propanoic acid
• CAS: 1374666-24-6
• 化学式: C₁₅H₂₂N₂O₇
• 分子量: 342.349
• InChiKey: FBEAXQFRHUPAAU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  24
• 可旋转键数：
  12
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.6
• 拓扑面积：
  122
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  {4-[3-keto-3-(2-ketoazaetidin-1-yl)propyl]phenyl}amine 、 3-[2-[2-[3-(3-Methyl-2,5-dioxopyrrol-1-yl)propanoylamino]ethoxy]ethoxy]propanoic acid 在 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、 N,N-二异丙基乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 生成 3-(3-methyl-2,5-dioxopyrrol-1-yl)-N-[2-[2-[3-oxo-3-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]propoxy]ethoxy]ethyl]propanamide
  参考文献：
  名称：

  Development of novel linkers to conjugate pharmacophores to a carrier antibody

  摘要：

  We have developed modified maleimide novel linkers with improved chemical stability that could potentially be used in conjugating various pharmacophores such as oligo nucleotides, peptides, and proteins to antibodies to afford novel biologics with well-defined therapeutic benefits and improved pharmacokinetic properties. These linkers expand the array of tools available for bioconjugation of pharmacophores to antibodies. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.05.040
• 作为产物：
  描述：

  Tert-butyl 3-[2-[2-[3-(3-methyl-2,5-dioxopyrrol-1-yl)propanoylamino]ethoxy]ethoxy]propanoate 在 三氟乙酸 作用下， 以 二氯甲烷 为溶剂， 生成 3-[2-[2-[3-(3-Methyl-2,5-dioxopyrrol-1-yl)propanoylamino]ethoxy]ethoxy]propanoic acid
  参考文献：
  名称：

  Development of novel linkers to conjugate pharmacophores to a carrier antibody

  摘要：

  We have developed modified maleimide novel linkers with improved chemical stability that could potentially be used in conjugating various pharmacophores such as oligo nucleotides, peptides, and proteins to antibodies to afford novel biologics with well-defined therapeutic benefits and improved pharmacokinetic properties. These linkers expand the array of tools available for bioconjugation of pharmacophores to antibodies. (C) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.05.040

文献信息

• ANTI-TROP2 ANTIBODY-DRUG CONJUGATE
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP3424955A1

  公开（公告）日：2019-01-09

  Provided is a method for producing an antibody-drug conjugate comprising reacting a compound represented by the following formula:          (maleimid-N-yl)-(CH2)n3-C(=O)-L2-LP-NH-(CH2)n1-La-(CH2)n2- C(=O)-(NH-DX) with an anti-TROP2 antibody or a reactive derivative thereof and conjugating a drug-linker moiety to the antibody by a method for forming a thioether bond at a disulfide bond site present in a hinge part of the antibody.

  本发明提供了一种生产抗体-药物共轭物的方法，该方法包括使下式所代表的化合物发生反应： (maleimid-N-yl)-(CH2)n3-C(=O)-L2-LP-NH-( )n1-La-( )n2- C(=O)-(NH-DX) 与抗-TROP2 抗体或其活性衍生物结合，并通过在抗体铰链部分的二硫键位点形成硫醚键的方法将药物连接分子与抗体结合。
• ANTI-DIABETIC COMPOUNDS
  申请人：CovX Technologies Ireland Limited

  公开号：EP2635309A2

  公开（公告）日：2013-09-11
• PROCESS FOR PURIFYING A SAMPLE OF H38C2 ANTIBODY
  申请人：Pfizer Inc.

  公开号：EP2793928B1

  公开（公告）日：2017-03-15
• Anti-Diabetic Compounds
  申请人：Das Tapan Kanti

  公开号：US20120282279A1

  公开（公告）日：2012-11-08

  The present invention provides a FGF21 molecule covalently attached to the combining site of an antibody via a linker, wherein the linker is covalently attached to the side chain of a linking residue within FGF21. Various uses of the compounds are provided, including methods to prevent or treat diabetes or diabetes-related conditions.
• US8722622B2
  申请人：——

  公开号：US8722622B2

  公开（公告）日：2014-05-13