2-(2-(2-azidoethoxy)ethoxy)acetaldehyde | 184006-13-1

• 分子结构分类: 有机化合物 - 有机1,3-偶极化合物 - 烯丙基型1,3-偶极有机化合物
• 英文名称: 2-(2-(2-azidoethoxy)ethoxy)acetaldehyde
• 英文别名: [2-(2-Azido-ethoxy)-ethoxy]-acetaldehyde；Ald-CH2-PEG2-Azide；2-[2-(2-azidoethoxy)ethoxy]acetaldehyde
• CAS: 184006-13-1
• 化学式: C₆H₁₁N₃O₃
• 分子量: 173.172
• InChiKey: OJEKEINAGFAPKG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.4
• 重原子数：
  12
• 可旋转键数：
  8
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  49.9
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  2-(2-(2-azidoethoxy)ethoxy)acetaldehyde 在 palladium on activated charcoal 盐酸 、 氢气 、 sodium cyanoborohydride 作用下， 以 四氢呋喃 、 甲醇 为溶剂， 生成 (S)-2-{2-[2-(2-Amino-ethoxy)-ethoxy]-ethylamino}-pentanedioic acid dihexadecyl ester
  参考文献：
  名称：

  Liposome-like fucopeptides as sialyl lewis X mimetics

  摘要：

  Several fucodipeptides and their liposome-like derivatives were prepared and tested as inhibitors of sialyl Lewis X binding to E-selectin. It has been found that trans-hydroxyproline (D or L) can be used to mimic the galactose residue of sialyl Lewis X, and the mimetic containing 3,4-dihydroxy-D-proline is the most active with IC50 value (50 mu M) 10-fold greater than sialyl Lewis X. Derivatization of a hydroxythreonine-containing fucodipeptides into a covalent liposome-like derivative, however, provides a mimetic with only IC50 similar to 30 mu M. Copyright (C) 1996 Elsevier Science Ltd

  DOI：

  10.1016/s0960-894x(96)00509-4
• 作为产物：
  描述：

  2-[2-(2-叠氮基乙氧基)乙氧基]乙醇 在 草酰氯 、 三乙胺 作用下， 以 二氯甲烷 、 二甲基亚砜 为溶剂， 反应 1.5h， 以48%的产率得到2-(2-(2-azidoethoxy)ethoxy)acetaldehyde
  参考文献：
  名称：

  [EN] CONJUGATES COMPRISING PEPTIDE GROUPS AND METHODS RELATED THERETO
  [FR] CONJUGUÉS COMPRENANT DES GROUPES PEPTIDIQUES ET PROCÉDÉS ASSOCIÉS À CEUX-CI

  摘要：

  在某些方面，本发明涉及一种抗体药物偶联物，包括：抗体；连接体；以及至少两个活性剂。在优选的实施例中，连接体包括由多个氨基酸组成的肽序列，其中至少两个活性剂通过共价键与氨基酸的侧链连接。抗体药物偶联物可以包括自焚基团，优选地是两个自焚基团。连接体可以包括O-取代的肟，例如，其中肟的氧原子被取代以与活性剂形成共价键连接；肟的碳原子被取代以与抗体形成共价键连接。

  公开号：

  WO2017089894A1

文献信息

• [EN] CONJUGATES COMPRISING PEPTIDE GROUPS AND METHODS RELATED THERETO<br/>[FR] CONJUGUÉS COMPRENANT DES GROUPES PEPTIDIQUES ET PROCÉDÉS ASSOCIÉS À CEUX-CI
  申请人：LEGOCHEM BIOSCIENCES INC

  公开号：WO2017089894A1

  公开（公告）日：2017-06-01

  In some aspects, the invention relates to an antibody-drug conjugate, comprising an antibody; a linker; and at least two active agents. In preferred embodiments, the linker comprises a peptide sequence of a plurality of amino acids, and at least two of the active agents are covalently coupled to side chains of the amino acids. The antibody-drug conjugate may comprise a self-immolative group, preferably two-self-immolative groups. The linker may comprise an O-substituted oxime, e.g., wherein the oxygen atom of the oxime is substituted with a group that covalently links the oxime to the active agent; and the carbon atom of the oxime is substituted with a group that covalently links the oxime to the antibody.

  在某些方面，本发明涉及一种抗体药物偶联物，包括：抗体；连接体；以及至少两个活性剂。在优选的实施例中，连接体包括由多个氨基酸组成的肽序列，其中至少两个活性剂通过共价键与氨基酸的侧链连接。抗体药物偶联物可以包括自焚基团，优选地是两个自焚基团。连接体可以包括O-取代的肟，例如，其中肟的氧原子被取代以与活性剂形成共价键连接；肟的碳原子被取代以与抗体形成共价键连接。
• Highly functionalized diaminocyclopentanes: A new route to potent and selective inhibitors of human O-GlcNAcase
  作者：Patrick Weber、Zuzana Mészáros、Pavla Bojarová、Manuel Ebner、Roland Fischer、Vladimír Křen、Natalia Kulik、Philipp Müller、Miluše Vlachová、Kristýna Slámová、Arnold E. Stütz、Martin Thonhofer、Ana Torvisco、Tanja M. Wrodnigg、Andreas Wolfsgruber

  DOI：10.1016/j.bioorg.2023.106819

  日期：2023.11

  A new class of compounds inhibiting de-O-glycosylation of proteins has been identified. Highly substituted diaminocyclopentanes are impressively selective reversible non-transition state O-β-N-acetyl-d-glucosaminidase (O-GlcNAcase) inhibitors. The ease of preparative access and remarkable biological activities provide highly viable leads for the development of anti-tau-phosphorylation agents with a

  已经鉴定出一类新的抑制蛋白质去-O-糖基化的化合物。高度取代的二氨基环戊烷是令人印象深刻的选择性可逆非过渡态O -β- N -乙酰基-d-氨基葡萄糖苷酶 ( O -GlcNAcase) 抑制剂。易于制备和显着的生物活性为抗 tau 磷酸化药物的开发提供了高度可行的线索，以期最终改善阿尔茨海默病。
• [EN] CONJUGATES COMPRISING SELF-IMMOLATIVE GROUPS AND METHODS RELATED THERETO<br/>[FR] CONJUGUÉS COMPRENANT DES GROUPES AUTO-IMMOLABLES ET PROCÉDÉS ASSOCIÉS
  申请人：LEGOCHEM BIOSCIENCES INC

  公开号：WO2017089890A8

  公开（公告）日：2018-07-19
• COMPOSITIONS FOR AFFECTING WEIGHT LOSS
  申请人：Weber Eckard

  公开号：US20070270450A1

  公开（公告）日：2007-11-22

  Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is an opioid antagonist and the second compound causes increased agonism of a melanocortin 3 receptor (MC3-R) or a melanocortin 4 receptor (MC4-R) compared to normal physiological conditions. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual to antagonize opioid receptor activity and to enhance α-MSH activity.
• US7375111B2
  申请人：——

  公开号：US7375111B2

  公开（公告）日：2008-05-20