Citraconyl-β-alanin | 90222-78-9

• 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: Citraconyl-β-alanin
• 英文别名: 3-(3-Methyl-2,5-dioxopyrrol-1-yl)propanoic acid
• CAS: 90222-78-9
• 化学式: C₈H₉NO₄
• 分子量: 183.164
• InChiKey: AVUBGZFAQGHELQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  74.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  Citraconyl-β-alanin 在 N-羟基丁二酰亚胺 、 三氟乙酸 、 N,N'-二异丙基碳二亚胺 作用下， 以 四氢呋喃 、 二氯甲烷 、 二甲基亚砜 为溶剂， 生成
  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：

  柠康酸酐 、 β-丙氨酸 在 溶剂黄146 作用下， 生成 Citraconyl-β-alanin
  参考文献：
  名称：

  [EN] IMIDAZO[4,5-c]QUINOLINE-4-AMINE COMPOUNDS AND CONJUGATES THEREOF, THEIR PREPARATION, AND THEIR THERAPEUTIC APPLICATIONS
  [FR] COMPOSÉS IMIDAZO[4,5-C]QUINOLÉINE-4-AMINE ET LEURS CONJUGUÉS, LEUR PRÉPARATION ET LEURS APPLICATIONS THÉRAPEUTIQUES

  摘要：

  SANOFI "IMIDAZO[4,5-c]QUINOLINE-4-AMINE COMPOUNDS AND CONJUGATES THEREOF, THEIR PREPARATION, AND THEIR THERAPEUTIC APPLICATIONS" The present disclosure relates to compounds of formula (I) (I) wherein n is an integer from 1 to 50; R1 represents a hydrogen atom, a -(C1-C6)alkylene-O-(C1-C6)alkyl group, a -(C1-C6)alkylene-NH-(C1-C6)alkyl group, or a -(C1-C6)alkyl group; R2 represents a -(C1-C6)alkylene- group; R3 represents -O-, -NH- or a -N((C1-C6)alkyl)- group; R4 represents a hydrogen atom, a -(C1-C6)alkyl group or a -(C1-C6)alkoxy group; R5 represents a -(C1-C6)alkylene- group; and R6 represents a -L1-RCG1 group or a -RCG1 group. The present disclosure also relates to conjugates of formula (II), to processes for their preparation, to compositions comprising them and to their therapeutic uses, especially in the prevention and/or in the treatment of a disease or a disorder that may benefit of an activation of the immune system, such as cancers.

  公开号：

  WO2023057564A1

文献信息

• Disulfur bridge linkers for conjugation of a cell-binding molecule
  申请人：Suzhou M-Conj Biotech Co., Ltd.

  公开号：US10307391B2

  公开（公告）日：2019-06-04

  The present invention relates to novel disulfur bridge linkers containing hydrazine used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking a pair of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

  本发明涉及新型含肼二硫桥连接体，用于通过桥接细胞结合分子上的一对硫醇，将化合物/细胞毒剂与细胞结合分子特异性连接。本发明还涉及制造这种连接体的方法、使用这种连接体制造均相共轭物的方法，以及应用这种共轭物治疗癌症、感染和自身免疫性疾病的方法。
• 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