4-oxo-N-[2-(propan-2-ylamino)ethyl]pentanamide

• 分子结构分类: 有机化合物 - 脂质和类脂质分子 - 脂肪酰基
• 英文名称: 4-oxo-N-[2-(propan-2-ylamino)ethyl]pentanamide
• 化学式: C₁₀H₂₀N₂O₂
• 分子量: 200.28
• InChiKey: DJJSXHPWWJODLZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  14
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  58.2
• 氢给体数：
  2
• 氢受体数：
  3

文献信息

• BIODEGRADABLE POLYETHYLENE GLYCOL BASED WATER-INSOLUBLE HYDROGELS
  申请人：Ascendis Pharma A/S

  公开号：EP3782649A1

  公开（公告）日：2021-02-24

  The invention relates to a process for the preparation of a hydrogel prodrug, comprising the steps of (a) providing a reactive biodegradable hydrogel, wherein said hydrogel comprises backbone moieties which are linked together through crosslinker moieties, each crosslinker moiety being terminated by at least two hydrolytically degradable bonds, and wherein from a branching core 3 to 16 linear PEG-based polymeric chains extend and wherein one terminus of said polymeric chains is connected to the branching core and the other to a hyperbranched dendritic moiety; wherein each said hyperbranched dendritic moiety has at least 3 branchings and at least 4 reactive functional groups; (b) conjugating a prodrug linker to a biologically active moiety, resulting in a biologically active moiety-prodrug linker conjugate; and (c) reacting the biologically active moiety-prodrug linker conjugate from step (b) with the reactive functional groups of the hydrogel of step (a). The invention further relates to a hydrogel prodrug obtainable from the process.

  本发明涉及一种制备水凝胶原药的工艺，包括以下步骤 (a) 提供一种活性生物可降解水凝胶，其中所述水凝胶包括通过交联剂分子连接在一起的骨架分子、每个交联剂分子以至少两个可水解降解键为端基，其中从分支核心延伸出 3 至 16 条线性 PEG 基聚合物链，所述聚合物链的一个端基与分支核心相连，另一个端基与超支化树枝状分子相连；其中每个所述超支化树枝状分子具有至少 3 个分支和至少 4 个活性官能团；(b) 将原药连接体与生物活性分子共轭，得到生物活性分子-原药连接体共轭物；以及 (c) 将步骤(b)中的生物活性分子-原药连接体共轭物与步骤(a)中水凝胶的活性官能团反应。本发明还涉及一种可从该工艺中获得的水凝胶原药。
• Prodrug comprising a drug-linker conjugate
  申请人：Ascendis Pharma A/S

  公开号：EP2596805B1

  公开（公告）日：2021-10-27
• PRODRUG COMPRISING A SELF-CLEAVABLE LINKER
  申请人：Ascendis Pharma A/S

  公开号：EP2237799B1

  公开（公告）日：2019-04-10
• DRY GROWTH HORMONE COMPOSITION TRANSIENTLY LINKED TO A POLYMER CARRIER
  申请人：ASCENDIS PHARMA ENDOCRINOLOGY DIVISION A/S

  公开号：EP2512450B1

  公开（公告）日：2018-02-07
• PROTEIN CARRIER-LINKED PRODRUGS
  申请人：Ascendis Pharma A/S

  公开号：EP2741782B1

  公开（公告）日：2020-05-06