4-[((N-maleimidomethyl)cyclohexanecarboxamido)methyl]cyclohexanecarboxylic acid

• 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: 4-[((N-maleimidomethyl)cyclohexanecarboxamido)methyl]cyclohexanecarboxylic acid
• 英文别名: 4-[[[4-[(2,5-Dioxopyrrol-1-yl)methyl]cyclohexanecarbonyl]amino]methyl]cyclohexane-1-carboxylic acid
• 化学式: C₂₀H₂₈N₂O₅
• 分子量: 376.453
• InChiKey: SGJRPSKVMWKVEF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.7
• 拓扑面积：
  104
• 氢给体数：
  2
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-[((N-maleimidomethyl)cyclohexanecarboxamido)methyl]cyclohexanecarboxylic acid 、 喜树碱 在 4-二甲氨基吡啶 、 1,2-二氯乙烷 、 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 18.08h， 生成 20-O-BCH-camptothecin
  参考文献：
  名称：

  WO2007/113687

  摘要：

  公开号：
• 作为产物：
  描述：

  4-(N-马来酰亚胺基甲基)环己烷-1-羧酸琥珀酰亚胺酯 、 tranexamic acid 以 水 、 N,N-二甲基甲酰胺 为溶剂， 反应 4.08h， 生成 4-[((N-maleimidomethyl)cyclohexanecarboxamido)methyl]cyclohexanecarboxylic acid
  参考文献：
  名称：

  WO2007/113687

  摘要：

  公开号：

文献信息

• CAMPTOTHECIN-CELL PENETRATING PEPTIDE CONJUGATES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
  申请人：Drais Pharmaceuticals, Inc.

  公开号：EP1998809B1

  公开（公告）日：2014-06-25
• CAMPTOTHECIN-PEPTIDE CONJUGATES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
  申请人：Michel Matthieu

  公开号：US20100015136A1

  公开（公告）日：2010-01-21

  The present invention relates to a novel compound of use in the improved delivery of therapeutic drug agents into target cells or tissues, composition comprising the same and uses thereof. The compound is more specifically a conjugate of a peptide moiety and a camptothecin, a derivative or analog thereof which provides numerous benefits, including enhancement in terms of aqueous solubility, pharmacokinetics and tissue distribution, enlargement of the therapeutic index, and limitation of the inter-patient metabolic variability, as well as improvement of delivery of the biologically active ingredient to the target cells or tissues.
• CAMPTOTHEAN-PEPTIDE CONJUGATES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
  申请人：DRAIS PHARMACEUTICALS, INC.

  公开号：US20130244956A1

  公开（公告）日：2013-09-19

  The present invention relates to a novel compound of use in the improved delivery of therapeutic drug agents into target cells or tissues, composition comprising the same and uses thereof. The compound is more specifically a conjugate of a peptidic moiety and a camptothecin, a derivative or analog thereof which provides numerous benefits, including enhancement in terms of aqueous solubility, pharmacokinetics and tissue distribution, enlargement of the therapeutic index, and limitation of the inter-patient metabolic variability, as well as improvement of delivery of the biologically active ingredient to the target cells or tissues.
• US8410045B2
  申请人：——

  公开号：US8410045B2

  公开（公告）日：2013-04-02
• [EN] CAMPTOTHECIN-PEPTIDE CONJUGATES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME<br/>[FR] CONJUGUÉS DE CAMPTOTHÉCINE ET DE PEPTIDE ET COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
  申请人：DIATOS SA

  公开号：WO2007113687A2

  公开（公告）日：2007-10-11

  [EN] The present invention relates to a novel compound of use in the improved delivery of therapeutic drug agents into target cells or tissues, composition comprising the same and uses thereof. The compound is more specifically a conjugate of a peptidic moiety and a camptothecin, a derivative or analog thereof which provides numerous benefits, including enhancement in terms of aqueous solubility, pharmacokinetics and tissue distribution, enlargement of the therapeutic index, and limitation of the inter-patient metabolic variability, as well as improvement of delivery of the biologically active ingredient to the target cells or tissues.
  [FR] La présente invention concerne l'utilisation d'un nouveau composé permettant une meilleure administration d'agents médicamenteux thérapeutiques à des cellules ou tissus cibles, de même que des compositions contenant ledit composé et ses utilisations. Le composé est plus spécifiquement un conjugué d'un groupement peptidique et d'une camptothécine, un dérivé, ou un analogue de celui-ci, qui offre de nombreux avantages, incluant une amélioration en termes d'hydrosolubilité, de pharmacocinétique et de distribution tissulaire, une élévation de l'indice thérapeutique, et une limitation de la variabilité métabolique parmi les patients. L'invention concerne également l'amélioration de l'administration du principe biologiquement actif aux cellules ou tissus cibles.