3-[2-[2-(3-methyl-2,5-dioxopyrrol-1-yl)ethoxy]ethoxy]-N-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]phenyl]propanamide | 1374666-27-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: 3-[2-[2-(3-methyl-2,5-dioxopyrrol-1-yl)ethoxy]ethoxy]-N-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]phenyl]propanamide
• CAS: 1374666-27-9
• 化学式: C₂₄H₂₉N₃O₇
• 分子量: 471.51
• InChiKey: BCYMRRRNBDGAAY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  34
• 可旋转键数：
  13
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  122
• 氢给体数：
  1
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  柠康酸酐 在 盐酸 、 1-羟基苯并三唑 、 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、 N,N-二异丙基乙胺 、 N,N'-二异丙基碳二亚胺 作用下， 以 N,N-二甲基甲酰胺 、 乙腈 为溶剂， 生成 3-[2-[2-(3-methyl-2,5-dioxopyrrol-1-yl)ethoxy]ethoxy]-N-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]phenyl]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

文献信息

• 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.
• ANTI-DIABETIC COMPOUNDS
  申请人：PFIZER INC.

  公开号：US20130164310A1

  公开（公告）日：2013-06-27

  The present invention provides a composition of the formula: [FGF21-1 st Linker]-[Ab]-[2 nd -Linker-Ex4]; wherein FGF21 is an FGF21 homologue; and Ex4 is an Exendin4 homologue; and Ab is an aldolase catalytic antibody or antigen binding portion thereof; and the 1 st linker is covalently attached to the side chain of a protein-linking residue in FGF21 and to a combining site of the antibody, and the 2 nd linker is covalently attached to the side chain of a peptide-linking residue in Ex4 and to a combining site of the antibody, and wherein the first and second linker are the same or different. 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
• US9163227B2
  申请人：——

  公开号：US9163227B2

  公开（公告）日：2015-10-20