Fmocfluorenylmethyloxycarbonyl chloride

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: Fmocfluorenylmethyloxycarbonyl chloride
• 英文别名: 9H-fluoren-9-ylmethyl 2-carbonochloridoyloxy-2-(9H-fluoren-1-yl)acetate
• 化学式: C₃₀H₂₁ClO₄
• 分子量: 480.9
• InChiKey: KXNOSLDXWRGCBP-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.5
• 重原子数：
  35
• 可旋转键数：
  7
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.13
• 拓扑面积：
  52.6
• 氢给体数：
  0
• 氢受体数：
  4

文献信息

• Antibody-SN-38 immunoconjugates with a CL2A linker
  申请人：Immunomedics, Inc.

  公开号：US10034950B2

  公开（公告）日：2018-07-31

  The present invention concerns improved methods and compositions for preparing SN-38 conjugates of proteins or peptides, preferably immunoconjugates of antibodies or antigen-binding antibody fragments. More preferably, the SN-38 is attached to the antibody or antibody fragment using a CL2A linker, with 1-12, more preferably 6 or less, most preferably 1-5 SN-38 moieties per antibody or antibody fragment. Most preferably, the immunoconjugate is prepared in large scale batches, with various modifications to the reaction scheme to optimize yield and recovery in large scale. Other embodiments concern optimized dosages and/or schedules of administration of immunoconjugate to maximize efficacy for disease treatment and minimize side effects of administration.

  本发明涉及制备蛋白质或多肽 SN-38 共轭物的改进方法和组合物，最好是抗体或抗原 结合抗体片段的免疫共轭物。更优选的是，使用 CL2A 连接剂将 SN-38 连接到抗体或抗体片段上，每个抗体或抗体片段有 1-12 个 SN-38 分子，更优选 6 个或更少，最优选 1-5 个 SN-38 分子。最优选的是大规模批量制备免疫共轭物，并对反应方案进行各种修改，以优化大规模制备的产量和回收率。其他实施方案涉及优化免疫共轭物的剂量和/或给药时间，以最大限度地提高疾病治疗效果，减少给药副作用。
• ANTIBODY-SN-38 IMMUNOCONJUGATES WITH A CL2A LINKER
  申请人：Immunomedics, Inc.

  公开号：US20140227180A1

  公开（公告）日：2014-08-14

  The present invention concerns improved methods and compositions for preparing SN-38 conjugates of proteins or peptides, preferably immunoconjugates of antibodies or antigen-binding antibody fragments. More preferably, the SN-38 is attached to the antibody or antibody fragment using a CL2A linker, with 1-12, more preferably 6 or less, most preferably 1-5 SN-38 moieties per antibody or antibody fragment. Most preferably, the immunoconjugate is prepared in large scale batches, with various modifications to the reaction scheme to optimize yield and recovery in large scale. Other embodiments concern optimized dosages and/or schedules of administration of immunoconjugate to maximize efficacy for disease treatment and minimize side effects of administration.
• US9107960B2
  申请人：——

  公开号：US9107960B2

  公开（公告）日：2015-08-18
• US9375489B2
  申请人：——

  公开号：US9375489B2

  公开（公告）日：2016-06-28
• US9629926B2
  申请人：——

  公开号：US9629926B2

  公开（公告）日：2017-04-25