4-(2,5-二氢-2,5-二氧代-1H-吡咯-1-基)-苯丁酸 | 100072-54-6

• 物质功能分类: 有机原料 - 羧酸类化合物及衍生物
• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯啉
• 中文名称: 4-(2,5-二氢-2,5-二氧代-1H-吡咯-1-基)-苯丁酸
• 中文别名: 4-马来酰亚胺基苯基丁酸
• 英文名称: 4-N-Maleimidophenyl butanoic acid
• 英文别名: 2-[4-(2,5-dioxopyrrol-1-yl)phenyl]butanoic acid
• CAS: 100072-54-6
• 化学式: C₁₄H₁₃NO₄
• 分子量: 259.26
• InChiKey: JTXKSTIGCAWIEQ-UHFFFAOYSA-N

物化性质

• 沸点：
  472.5±28.0 °C(Predicted)
• 密度：
  1.359±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.21
• 拓扑面积：
  74.7
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Anthracycline immunoconjugates having a novel linker and methods for their production
  申请人：Bristol-Myers Squibb Company

  公开号：EP0328147A2

  公开（公告）日：1989-08-16

  The present invention relates to novel immuno­conjugates, methods for their production, pharmaceutical compositions and method for delivering cytotoxic anthracyclines to a selected population of cells desired to be eliminated. More particularly, the invention relates to immunoconjugates comprised of an antibody reactive with a selected cell population, having a number of anthracycline molecules linked to its structure. Each anthracycline molecule, having a keto group at the C-13 position, is conjugated to the antibody via a linker arm and is bound to that linker arm via an acid-sensitive acylhydrazone bond at the 13-keto position of the anthracycline. The immunoconjugates and methods of the invention are useful in antibody-mediated drug delivery systems for the preferential killing of a selected cell population in the treatment of diseases such as cancers and other tumors, non-cytocidal viral or other pathogenic infections, and autoimmune disorders.

  本发明涉及新型免疫缀合物、其生产方法、药物组合物以及将细胞毒性蒽环类药物输送到所选的待清除细胞群的方法。更具体地说，本发明涉及一种免疫结合剂，它由一种与所选细胞群有反应的抗体组成，该抗体的结构上连接着一些蒽环类分子。每个蒽环类分子的 C-13 位上都有一个酮基，通过连接臂与抗体连接，并通过蒽环类的 13-酮位上的酸敏酰腙键与该连接臂结合。 本发明的免疫共轭物和方法可用于抗体介导的给药系统，在治疗癌症和其他肿瘤、非杀细胞病毒或其他病原体感染以及自身免疫性疾病等疾病时优先杀死选定的细胞群。
• Anthracycline conjugates having a novel linker and methods for their production
  申请人：Bristol-Myers Squibb Company

  公开号：EP0398305A2

  公开（公告）日：1990-11-22

  The present invention relates to novel conjugates, methods for their production, pharmaceutical compositions and methods for delivering cytotoxic anthracyclines to a selected population of cells desired to be eliminated. The anthracycline conjugates comprise at least one anthracycline molecule linked to a ligand that is reactive with a cell population to be eliminated, the anthracycline having a keto group at the C-13 position, and being attached to the ligand via a linker arm and being bound to that linker arm via an acid-sensitive acylhydrazone bond at the 13-keto position of the anthracycline. The conjugates of the invention are therefore useful in antibody- or ligand-mediated drug delivery systems for the preferential killing of a selected cell population in the treatment of diseases such as cancers and other tumors, non-cytocidal viral or other pathogenic infections, and autoimmune disorders.

  本发明涉及新型共轭物、其生产方法、药物组合物以及将细胞毒性蒽环类药物输送到选定的待清除细胞群的方法。蒽环类共轭物包括至少一个蒽环类分子，该分子与配体相连，配体与待清除的细胞群反应，蒽环类在 C-13 位上有一个酮基，通过连接臂与配体相连，并在蒽环类的 13-keto 位上通过酸敏酰腙键与该连接臂结合。 因此，本发明的共轭物可用于抗体或配体介导的给药系统，在治疗癌症和其他肿瘤、非杀细胞病毒或其他病原体感染以及自身免疫性疾病等疾病时优先杀死选定的细胞群。
• Process for treating a biological organism
  申请人：Tuszynski A. Jack

  公开号：US20050249667A1

  公开（公告）日：2005-11-10

  A process for treating cells within a biological organism in which sonic energy is focused on cells within a biological organism while the frequency and/or the power level of such energy is varied. In addition there is provided a process for synergistically combining sonic energy and other forms of energy, or other therapeutic agents, in the treatment of cells in living organisms. Furthermore there is provided a process for assaying the efficacy of other therapeutic agents with sonic energy.

  一种治疗生物机体内细胞的方法，其中声波能量集中在生物机体内的细胞上，同时改变这种能量的频率和/或功率水平。此外，还提供了一种在治疗生物机体内的细胞时将声波能量和其他形式的能量或其他治疗剂协同结合的工艺。此外，还提供了一种用声波能量检测其他治疗剂疗效的方法。
• FURTHER IMPROVEMENTS RELATING TO DRUG DELIVERY SYSTEMS
  申请人：CANCER RESEARCH CAMPAIGN TECHNOLOGY LIMITED

  公开号：EP0414741B1

  公开（公告）日：1995-03-15
• TARGETED LIPOSOMES AND METHODS FOR LIPOSOME-PROTEIN COUPLING
  申请人：THE LIPOSOME COMPANY, INC.

  公开号：EP0478715B1

  公开（公告）日：1996-04-03