1-(2,5-Dioxopyrrol-1-yl)-4-oxo-4-(2,3,4,5,6-pentafluorophenoxy)butane-2-sulfonic acid

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚酯
• 英文名称: 1-(2,5-Dioxopyrrol-1-yl)-4-oxo-4-(2,3,4,5,6-pentafluorophenoxy)butane-2-sulfonic acid
• 英文别名: 1-(2,5-dioxopyrrol-1-yl)-4-oxo-4-(2,3,4,5,6-pentafluorophenoxy)butane-2-sulfonic acid
• 化学式: C₁₄H₈F₅NO₇S
• 分子量: 429.27
• InChiKey: OPFDSYWPZVIHCQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  28
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  126
• 氢给体数：
  1
• 氢受体数：
  12

文献信息

• [EN] CELL PROLIFERATION INHIBITORS AND CONJUGATES THEREOF<br/>[FR] INHIBITEURS DE LA PROLIFÉRATION CELLULAIRE ET LEURS CONJUGUÉS
  申请人：NOVARTIS AG

  公开号：WO2014151030A1

  公开（公告）日：2014-09-25

  Disclosed herein are immunoconjugates comprising an inhibitor of Eg5 linked to an antigen binding moiety such as an antibody, useful for treating cell proliferative disorders. Also disclosed are novel inhibitors of Eg5 that can be used either alone or as part of an immunoconjugate to treat cell proliferation disorders. The Eg5 inhibitors include compounds of this formula as described herein: [insert last structure from page 68 here] The invention further provides pharmaceutical compositions comprising these compounds and immunoconjugates, optionally including a therapeutic co-agent, and methods to use these compounds, conjugates and compositions for treating cell proliferation disorders.

  本发明公开了包含Eg5抑制剂的免疫偶联物，该抑制剂与抗原结合部分如抗体相连，用于治疗细胞增殖紊乱。还公开了新颖的Eg5抑制剂，可以单独使用或作为免疫偶联物的一部分来治疗细胞增殖紊乱。Eg5抑制剂包括如本文所述的这种化合物的化合物：[在此插入第68页的最后一个结构]本发明进一步提供了包含这些化合物和免疫偶联物的药物组合物，可选地包括治疗共剂，以及使用这些化合物、偶联物和组合物来治疗细胞增殖紊乱的方法。
• CKIT antibody drug conjugates
  申请人：Novartis AG

  公开号：US10786578B2

  公开（公告）日：2020-09-29

  The present invention relates to anti-cKIT antibodies, antibody fragments, antibody drug conjugates, and their uses for the treatment of cancer.

  本发明涉及抗 KIT 抗体、抗体片段、抗体药物共轭物及其治疗癌症的用途。
• CELL PROLIFERATION INHIBITORS AND CONJUGATES THEREOF
  申请人：Novartis AG

  公开号：EP2968591A1

  公开（公告）日：2016-01-20
• CKIT ANTIBODY DRUG CONJUGATES
  申请人：Novartis AG

  公开号：US20180193475A1

  公开（公告）日：2018-07-12

  The present invention relates to anti-cKIT antibodies, antibody fragments, antibody drug conjugates, and their uses for the treatment of cancer.
• [EN] CKIT ANTIBODY DRUG CONJUGATES<br/>[FR] CONJUGUÉS ANTICORPS CKIT-MÉDICAMENT
  申请人：NOVARTIS AG

  公开号：WO2016020791A1

  公开（公告）日：2016-02-11

  The present invention relates to anti-cKIT antibodies, antibody fragments, antibody drug conjugates, and their uses for the treatment of cancer.