6-Methyl-2,3-bis-iodmethyl-chinoxalin | 3298-88-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 6-Methyl-2,3-bis-iodmethyl-chinoxalin
• 英文别名: 2,3-bis-iodomethyl-6-methyl-quinoxaline；2,3-Bis(iodomethyl)-6-methylquinoxaline
• CAS: 3298-88-2
• 化学式: C₁₁H₁₀I₂N₂
• 分子量: 424.023
• InChiKey: LVZWTYUSZVBVJW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.7
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  25.8
• 氢给体数：
  0
• 氢受体数：
  2

文献信息

• [EN] NOVEL CYTOTOXIC AGENTS AND CONJUGATES THEREOF<br/>[FR] NOUVEAUX AGENTS CYTOTOXIQUES ET LEURS CONJUGUÉS
  申请人：POLYTHERICS LTD

  公开号：WO2018051109A1

  公开（公告）日：2018-03-22

  Provided herein are novel maytansinoid compounds of general formula I. Also provided herein are conjugates comprising the compounds linked to a binding protein via a linker, and conjugating reagents comprising the compounds attached via a linker to at least one functional group capable of reacting with a binding protein. Also provided herein are pharmaceutical compositions comprising the compounds and conjugates, therapeutic methods and uses involving the compounds and conjugates, for example in cancer therapy, and novel synthetic processes.

  本文提供了一般式I的新型马丹西酮类化合物。本文还提供了将这些化合物通过连接剂连接到结合蛋白上的共轭物，以及将这些化合物通过连接剂连接到至少一个能与结合蛋白发生反应的功能基团的共轭试剂。本文还提供了包含这些化合物和共轭物的药物组合物，涉及这些化合物和共轭物的治疗方法和用途，例如在癌症治疗中，并提供了新的合成过程。
• [EN] CONJUGATES AND CONJUGATING REAGENTS COMPRISING A LINKER THAT INCLUDES AT LEAST TWO (-CH2-CH2-0-) UNITS IN A RING<br/>[FR] CONJUGUÉS ET RÉACTIFS DE CONJUGAISON COMPRENANT UN LIEUR QUI COMPREND AU MOINS DEUX MOTIFS (-CH2-CH2-O-) DANS UN CYCLE
  申请人：POLYTHERICS LTD

  公开号：WO2017178828A1

  公开（公告）日：2017-10-19

  A conjugate comprising a protein or peptide conjugated to a therapeutic, diagnostic or labelling agent via a linker, characterised in that the linker includes at least two ~(CH2-CH2- 0-)~ units within a ring, said ring being attached via a single tethering atom within the ring to the rest of the linker, or said ring being attached via two or more tethering atoms within the ring to the rest of the linker at a single point.

  一种由蛋白质或肽共轭到治疗、诊断或标记试剂的共轭物，其特征在于该连接剂包含至少两个 ~(CH2- - 0-)~ 单元构成的环，所述环通过环内的单个锚定原子连接到连接剂的其余部分，或者所述环通过环内的两个或更多锚定原子连接到连接剂的其余部分的单一点。
• Cytotoxic agents and conjugates thereof
  申请人：POLYTHERICS LIMITED

  公开号：US10654873B2

  公开（公告）日：2020-05-19

  Provided herein are novel maytansinoid compounds of general formula I. Also provided herein are conjugates comprising the compounds linked to a binding protein via a linker, and conjugating reagents comprising the compounds attached via a linker to at least one functional group capable of reacting with a binding protein. Also provided herein are pharmaceutical compositions comprising the compounds and conjugates, therapeutic methods and uses involving the compounds and conjugates, for example in cancer therapy, and novel synthetic processes.

  本文提供了通式 I 的新型 maytansinoid 化合物。本文还提供了包含通过连接体与结合蛋白连接的化合物的共轭物，以及包含通过连接体与至少一个能与结合蛋白反应的官能团连接的化合物的共轭试剂。本文还提供了包含化合物和共轭物的药物组合物、涉及化合物和共轭物的治疗方法和用途（例如在癌症治疗中）以及新型合成工艺。
• NOVEL CYTOTOXIC AGENTS AND CONJUGATES THEREOF
  申请人：Polytherics Limited

  公开号：EP3512856B1

  公开（公告）日：2021-03-24
• Novel Cytotoxic Agents And Conjugates Thereof
  申请人：POLYTHERICS LIMITED

  公开号：US20190202839A1

  公开（公告）日：2019-07-04

  Provided herein are novel maytansinoid compounds of general formula I. Also provided herein are conjugates comprising the compounds linked to a binding protein via a linker, and conjugating reagents comprising the compounds attached via a linker to at least one functional group capable of reacting with a binding protein. Also provided herein are pharmaceutical compositions comprising the compounds and conjugates, therapeutic methods and uses involving the compounds and conjugates, for example in cancer therapy, and novel synthetic processes.