(E)-4-(1-hydroxypyrrolidin-2-yl)-2-methyl-4-oxobut-2-enamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: (E)-4-(1-hydroxypyrrolidin-2-yl)-2-methyl-4-oxobut-2-enamide
• 化学式: C₉H₁₄N₂O₃
• 分子量: 198.22
• InChiKey: OVPOZNHLVUXVFP-AATRIKPKSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.1
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  83.6
• 氢给体数：
  2
• 氢受体数：
  4

文献信息

• Minimally toxic prodrugs
  申请人：LIFE SCIENCES RESEARCH PARTNERS VZW

  公开号：US10076576B2

  公开（公告）日：2018-09-18

  The present invention relates to the field of oligopeptide prodrugs that are intended for the treatment of cancer. The selectivity of these prodrugs requires the presence of an (oligo)peptidic moiety and/or a protective capping group to ensure the prodrug stability in blood. It further in particular relates to the exemplary oligopeptidic moiety ALGP and to prodrugs comprising it. In particular it also relates to the capping group phosphonoacetyl and to prodrugs comprising this capping group.

  本发明涉及用于治疗癌症的寡肽原药领域。这些原药的选择性要求存在一个（寡）肽分子和/或一个保护性封端基团，以确保原药在血液中的稳定性。本发明还特别涉及示例性低聚肽分子 ALGP 以及包含该分子的原药。特别还涉及封端基团膦酰乙酰基和包含该封端基团的原药。
• MINIMALLY TOXIC PRODRUGS
  申请人：Life Sciences Research Partners VZW

  公开号：EP2938360A2

  公开（公告）日：2015-11-04
• [EN] MINIMALLY TOXIC PRODRUGS<br/>[FR] PROMÉDICAMENTS MINIMALEMENT TOXIQUES
  申请人：LIFE SCIENCES RES PARTNERS VZW

  公开号：WO2014102312A2

  公开（公告）日：2014-07-03

  The present invention relates to the field of oligopeptide prodrugs that are intended for the treatment of cancer. The selectivity of these prodrugs requires the presence of an (oligo)peptidic moiety and/or a protective capping group to ensure the prodrug stability in blood.. It further in particular relates to the exemplary oligopeptidic moiety ALGP and to prodrugs comprising it. In particular it also relates to the capping group phosphonoacetyl and to prodrugs comprising this capping group.
• [EN] COMPOUNDS COMPRISING A TETRAPEPTIDIC MOIETY<br/>[FR] COMPOSÉS COMPRENANT UNE FRACTION TÉTRAPEPTIDIQUE
  申请人：[en]COBIORES NV

  公开号：WO2022167664A1

  公开（公告）日：2022-08-11

  The present invention relates to the field of compounds intended for the treatment of cancer. Selectivity of these compounds is gained through the presence of a specific tetrapeptidic moiety allowing selective release of the drug. The drug in particular is a cytostatic, cytotoxic, or anti-cancer drug. A protective capping group can be introduced to ensure stability of the compound in blood. The tetrapeptidic moieties provide to prodrug compounds a selectivity index of at least 2 for at least 2 different types of cancers (compared to normal cells).