马来酰亚胺-三聚乙二醇-五氟苯酚酯 | 1807534-78-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚酯
• 中文名称: 马来酰亚胺-三聚乙二醇-五氟苯酚酯
• 英文名称: perfluorophenyl 3-(2-(2-(2-(2,5-dioxo-2,5-dihydro-1H-pyrrol-1-yl)ethoxy)ethoxy)ethoxy)propanoate
• 英文别名: Mal-PEG3-PFP；(2,3,4,5,6-pentafluorophenyl) 3-[2-[2-[2-(2,5-dioxopyrrol-1-yl)ethoxy]ethoxy]ethoxy]propanoate
• CAS: 1807534-78-6
• 化学式: C₁₉H₁₈F₅NO₇
• 分子量: 467.346
• InChiKey: NTHCDRJWHPEQDJ-UHFFFAOYSA-N

物化性质

• 沸点：
  531.5±50.0 °C(Predicted)
• 密度：
  1.438±0.06 g/cm3(Predicted)
• 溶解度：
  溶于DMSO、DCM、DMF

计算性质

• 辛醇/水分配系数(LogP)：
  0.9
• 重原子数：
  32
• 可旋转键数：
  14
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.42
• 拓扑面积：
  91.4
• 氢给体数：
  0
• 氢受体数：
  12

反应信息

• 作为产物：
  描述：

  氨基-PEG3-羧酸 在 溶剂黄146 、 N,N'-二环己基碳二亚胺 作用下， 以 乙酸乙酯 为溶剂， 生成 马来酰亚胺-三聚乙二醇-五氟苯酚酯
  参考文献：
  名称：

  [EN] COMPOUNDS, COMPOSITIONS, METHODS, AND USES FOR TREATING CANCER AND IMMUNOLOGICAL DISORDERS
  [FR] COMPOSÉS, COMPOSITIONS, MÉTHODES ET UTILISATIONS POUR TRAITER LE CANCER ET DES TROUBLES IMMUNOLOGIQUES

  摘要：

  公开号：

  WO2020014541A3

文献信息

• [EN] CYTOTOXIC AND ANTI-MITOTIC COMPOUNDS, AND METHODS OF USING THE SAME<br/>[FR] COMPOSÉS CYTOTOXIQUES ET ANTIMITOTIQUES ET LEURS PROCÉDÉS D'UTILISATION
  申请人：CDRD VENTURES INC

  公开号：WO2016041082A1

  公开（公告）日：2016-03-24

  Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.

  揭示了具有细胞毒性和/或抗有丝分裂活性的化合物。还揭示了与制备和使用这些化合物相关的方法，以及包含这些化合物的药物组合物。还揭示了具有结构的组合物：(T)-(L)-(D)，其中(T)是靶向基团，(L)是可选的连接剂，(D)是具有细胞毒性和/或抗有丝分裂活性的化合物。
• CYTOTOXIC AND ANTI-MITOTIC COMPOUNDS, AND METHODS OF USING THE SAME
  申请人：CDRD Ventures, Inc.

  公开号：US20160075735A1

  公开（公告）日：2016-03-17

  Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.

  本发明揭示了具有细胞毒性和/或抗有丝分裂活性的化合物。本发明还揭示了与制备和使用此类化合物相关的方法，以及包含此类化合物的制药组合物。还揭示了具有以下结构的组合物：(T)-(L)-(D)，其中(T)是靶向基团，(L)是可选的连接基团，(D)是具有细胞毒性和/或抗有丝分裂活性的化合物。
• Cytotoxic and anti-mitotic compounds, and methods of using the same
  申请人：ZYMEWORKS INC.

  公开号：US10414822B2

  公开（公告）日：2019-09-17

  Compounds having cytotoxic and/or anti-mitotic activity are disclosed. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having cytotoxic and/or anti-mitotic activity.

  本研究公开了具有细胞毒性和/或抗有丝分裂活性的化合物。还公开了与制备和使用此类化合物相关的方法，以及包含此类化合物的药物组合物。还公开了具有以下结构的组合物：(T)-(L)-(D)，其中(T)是靶向分子，(L)是任选连接体，(D)是具有细胞毒性和/或抗有丝分裂活性的化合物。
• COMPOUNDS, COMPOSITIONS, METHODS, AND USES FOR TREATING CANCER AND IMMUNOLOGICAL DISORDERS
  申请人：IL-2RX, Inc.

  公开号：US20210252160A1

  公开（公告）日：2021-08-19

  The present disclosure provides novel polypeptide-therapeutic compound or hormone-therapeutic compound conjugates using cleavable or non-cleavable linkers, whereby the polypeptide or hormone serves to target specific cells using receptor expression on the targeted cell to bind the ligand (polypeptide or hormone) carrying the therapeutic compound unlike antibody drug conjugates. Upon binding, the ligand and the therapeutic compound (multiples of the therapeutic compound in some embodiments) enter the cell by receptor-mediated endocytosis, and release drugs conjugated to the ligand by linkers, to interact with intracellular components to enhance, restore, or block a signal transduction process. The ligands for the polypeptide-therapeutic compound or hormone-therapeutic compound conjugates include, but are not limited to: cytokines, growth factors and hormones among other proteins with corresponding cell surface specific receptors. The disorders targeted by such polypeptide-therapeutic compound or hormone-therapeutic compound conjugates include, but are not limited to: immunological disorders (e.g., allergy and autoimmune disorders) and cancer.
• COMPOUNDS, COMPOSITIONS, METHODS, AND USES FOR TREATING LEPTIN RESISTANCE, OBESITY, DIABETES MELLITUS AND METABOLIC SYNDROME
  申请人：Hurt Clarence

  公开号：US20210324031A1

  公开（公告）日：2021-10-21

  Novel leptin and leptin-fusion protein-small molecule drug conjugates are disclosed, where conjugation takes place through the use of cleavable and non-cleavable linkers. The small molecules chemically linked to the protein carrier are imported into the specific leptin-responsive target tissue or cell through receptor-mediated endocytosis and released from the carrier protein through enzymatic cleavage of the linker-drug moiety or through lysosomal degradation of the carrier protein. Free drug then act to modify leptin receptor-triggered biochemical pathways that are altered in conditions of leptin-resistance. Drug will correct altered pathway allowing resensitization of receptor signaling. This can greatly aid in the resolution of pathologies either initiated at the onset of leptin resistance or exacerbated by it.