2-甲基磺酰基硫基乙基N-(2-二甲基氨基乙基)氨基甲酸酯 | 187592-54-7

• 分子结构分类: 有机化合物 - 有机硫化合物 - 磺酰类
• 中文名称: 2-甲基磺酰基硫基乙基N-(2-二甲基氨基乙基)氨基甲酸酯
• 英文名称: Mtsac cpd
• 英文别名: 2-methylsulfonylsulfanylethyl N-[2-(dimethylamino)ethyl]carbamate
• CAS: 187592-54-7
• 化学式: C₈H₁₈N₂O₄S₂
• 分子量: 270.4
• InChiKey: HVXOQQDJVAPFIA-UHFFFAOYSA-N

物化性质

• 溶解度：
  溶于DMSO、甲醇

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  16
• 可旋转键数：
  8
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.88
• 拓扑面积：
  109
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• [EN] PYRROLOBENZODIAZEPINE PRODRUGS AND ANTIBODY CONJUGATES THEREOF<br/>[FR] PROMÉDICAMENTS DE PYRROLOBENZODIAZÉPINE ET CONJUGUÉS D'ANTICORPS DE CEUX-CI
  申请人：GENENTECH INC

  公开号：WO2018031662A1

  公开（公告）日：2018-02-15

  The invention relates generally to pyrrolobenzodiazepine monomer and dimer prodrugs having a glutathione-activated disulfide prodrug moiety, a DT-diaphorase-activated quinone prodrug moiety or a reactive oxygen species-activated aryl boronic acid or aryl boronic ester prodrug moiety. The invention further relates to pyrrolobenzodiazepine prodrug dimer-antibody conjugates.

  这项发明涉及具有谷胱甘肽活化二硫键前药基团、DT-二氢呋喃酮酶活化醌前药基团或活化氧化物种的芳基硼酸或芳基硼酯前药基团的吡咯苯并二氮杂环烷单体和二聚体前药。该发明还涉及吡咯苯并二氮杂环烷前药二聚体-抗体共轭物。
• [EN] HINDERED DISULFIDE DRUG CONJUGATES<br/>[FR] CONJUGUÉS MÉDICAMENTEUX À PONT DISULFURE ENCOMBRÉ
  申请人：GENENTECH INC

  公开号：WO2017064675A1

  公开（公告）日：2017-04-20

  The invention relates generally to disulfide drug conjugates wherein a linker comprising a sulfur-bearing carbon atom substituted with at least one hydrocarbyl or substituted hydrocarbyl is conjugated by a disulfide bond to a cysteine sulfur atom of a targeting carrier, and wherein the linker is further conjugated to a drug moiety. The invention further relates to activated linker-drug conjugates suitable for conjugation to a targeting carrier by a disulfide bond. The invention further relates to methods for preparing hindered disulfide drug conjugates.

  该发明一般涉及二硫键药物偶联物，其中含有至少一个被至少一个碳氢化合物或取代碳氢化合物所取代的含硫碳原子的连接剂通过二硫键与靶向载体的半胱氨酸硫原子偶联，并且连接剂进一步与药物部分偶联。该发明进一步涉及适合通过二硫键与靶向载体偶联的活化连接剂-药物偶联物。该发明还进一步涉及制备受阻二硫键药物偶联物的方法。
• Hindered disulfide drug conjugates
  申请人：Genentech, Inc.

  公开号：US10729738B2

  公开（公告）日：2020-08-04

  The invention relates generally to disulfide drug conjugates wherein a linker comprising a sulfur-bearing carbon atom substituted with at least one hydrocarbyl or substituted hydrocarbyl is conjugated by a disulfide bond to a cysteine sulfur atom of a targeting carrier, and wherein the linker is further conjugated to a drug moiety. The invention further relates to activated linker-drug conjugates suitable for conjugation to a targeting carrier by a disulfide bond. The invention further relates to methods for preparing hindered disulfide drug conjugates.

  本发明一般涉及二硫化物药物共轭物，其中由至少一个烃基或取代烃基取代的含硫碳原子组成的连接体通过二硫键与靶向载体的半胱氨酸硫原子共轭，并且连接体进一步与药物分子共轭。 本发明进一步涉及适合通过二硫键与靶向载体共轭的活化连接体-药物共轭物。 本发明进一步涉及制备受阻二硫化物药物共轭物的方法。
• HINDERED DISULFIDE DRUG CONJUGATES
  申请人：Genentech, Inc.

  公开号：EP3362100B1

  公开（公告）日：2022-06-22
• PYRROLOBENZODIAZEPINE PRODRUGS AND ANTIBODY CONJUGATES THEREOF
  申请人：GENENTECH, INC.

  公开号：US20190175749A1

  公开（公告）日：2019-06-13

  The invention relates generally to pyrrolobenzodiazepine monomer and dimer prodrugs having a glutathione-activated disulfide prodrug moiety, a DT-diaphorase-activated quinone prodrug moiety or a reactive oxygen species-activated aryl boronic acid or aryl boronic ester prodrug moiety. The invention further relates to pyrrolobenzodiazepine prodrug dimer-antibody conjugates.