(10S)-10-ethyl-18-fluoro-10-hydroxy-19-methyl-8-oxa-4,15-diazahexacyclo[14.7.1.02,14.04,13.06,11.020,24]tetracosa-1,6(11),14,16,18,20(24)-hexaene-5,9-dione

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: (10S)-10-ethyl-18-fluoro-10-hydroxy-19-methyl-8-oxa-4,15-diazahexacyclo[14.7.1.02,14.04,13.06,11.020,24]tetracosa-1,6(11),14,16,18,20(24)-hexaene-5,9-dione
• 化学式: C₂₄H₂₃FN₂O₄
• 分子量: 422.4
• InChiKey: SJDUMDUVVOTCBR-WIIYFNMSSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  31
• 可旋转键数：
  1
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  79.7
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• Stereoselective synthesis of phosphorus containing actives
  申请人：Gilead Pharmasset LLC

  公开号：EP2752422A1

  公开（公告）日：2014-07-09

  Disclosed herein is a process for preparing an enantiomerically- or a diastereomerically enriched phosphorus-containing active, salt, or pharmaceutically acceptable salt thereof, of formula I-1 , which comprises the steps of: (a) reacting a protected or unprotected Active with a base to form a salt of said active and then reacting said salt with an enantiomerically- or a diastereomerically enriched compound of formula II-1 wherein the Active is a nucleoside, a nucleoside-analog, or a non-nucleoside.

  本文公开了一种制备式 I-1 的对映体或非对映异构体富集的含磷活性物质、盐或其药学上可接受的盐的方法 ，其步骤包括(a) 使受保护或未受保护的活性物质与碱反应，形成所述活性物质的盐，然后使所述盐与富含对映体或非对映异构体的式 II-1 化合物反应； (b) 使受保护或未受保护的活性物质与碱反应，形成所述活性物质的盐，然后使所述盐与富含对映体或非对映异构体的式 II-1 化合物反应。 其中活性物质为核苷、核苷类似物或非核苷。
• ANTIBODY-DRUG CONJUGATE, INTERMEDIATE THEREOF, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
  申请人：Shanghai Fudan-Zhangjiang Bio-Pharmaceutical Co., Ltd.

  公开号：EP3991754A1

  公开（公告）日：2022-05-04

  Disclosed are an antibody-drug conjugate (ADC), an intermediate thereof, a preparation method therefor and an application thereof. The present invention provides an ADC. A structural general formula thereof is Ab-(L 3-L 2-L 1-D)m. The ADC has better biological activity, stability, and uniformity, has reduced toxic and side effects, and has a faster release rate of enzyme cutting in tumor cells. The use of the novel ADC can achieve a wide application of a cytotoxic drug particularly camptothecin in the field of ADCs in treating tumor patients resistant to microtubule ADC.

  本发明公开了一种抗体药物共轭物（ADC）、其中间体、制备方法及其应用。本发明提供了一种 ADC。其结构通式为Ab-(L 3-L 2-L 1-D)m。该ADC具有较好的生物活性、稳定性和均一性，毒副作用较小，在肿瘤细胞中的酶切释放速度较快。使用该新型 ADC 可以实现细胞毒性药物尤其是喜树碱在 ADC 领域的广泛应用，治疗对微管 ADC 耐药的肿瘤患者。
• ANTIBODY-DRUG CONJUGATE
  申请人：Daiichi Sankyo Company, Limited

  公开号：EP2907824B1

  公开（公告）日：2018-04-11