(R)-Topotecan

• 分子结构分类: 有机化合物 - 生物碱及其衍生物 - 喜树碱
• 英文名称: (R)-Topotecan
• 英文别名: (19R)-8-[(dimethylamino)methyl]-19-ethyl-7,19-dihydroxy-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaene-14,18-dione
• 化学式: C₂₃H₂₃N₃O₅
• 分子量: 421.4
• InChiKey: UCFGDBYHRUNTLO-HSZRJFAPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  31
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.347
• 拓扑面积：
  103
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• [EN] A PRODRUG PLATFORM USEFUL TO DELIVER AMINES, AMIDES AND PHENOLS<br/>[FR] PLATE-FORME DE PROMÉDICAMENTS UTILE POUR ADMINISTRER DES AMINES, DES AMIDES ET DES PHÉNOLS
  申请人：SHANGHAI CHANGCHENGYIYAOKEJI COMPANY LTD

  公开号：WO2021032075A1

  公开（公告）日：2021-02-25

  Provided herein is a prodrug platform useful to deliver pharmaceutically active amines, amides and phenols and their use in the diagnosis, prevention and/or treatment of various diseases. Compared with the parent drug (e.g., Gemcitabine), the prodrugs show a significant overall safety improvement (therapeutic index (TI) improvement), especially in liver.

  本文提供了一种用于传递药用活性胺、酰胺和酚的前药平台，以及它们在诊断、预防和/或治疗各种疾病中的用途。与母药（例如吉西他滨）相比，前药在整体安全性方面表现出明显改善（疗效指数（TI）改善），尤其是在肝脏方面。
• Water-Soluble Polymer Conjugates of Topotecan
  申请人：Gu Xuyuan

  公开号：US20140371258A1

  公开（公告）日：2014-12-18

  Provided herein are water-soluble polymer conjugates of topotecan, along with compositions comprising the conjugates and related methods of making and using the same.

  本文提供了水溶性聚合物结合拓扑替康的化合物，以及包含这些结合物的组合物和相关的制备和使用方法。
• [EN] ANTI-CANCER NUCLEAR HORMONE RECEPTOR-TARGETING COMPOUNDS<br/>[FR] COMPOSÉS CIBLANT DES RÉCEPTEURS HORMONAUX NUCLÉAIRES ANTICANCÉREUX
  申请人：NUVATION BIO INC

  公开号：WO2022204184A1

  公开（公告）日：2022-09-29

  The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.

  该披露涉及从核类固醇受体结合物中衍生出的抗癌化合物，包括含有相同化合物的产品，以及它们的使用和制备方法。
• A PRODRUG PLATFORM USEFUL TO DELIVER AMINES, AMIDES AND PHENOLS
  申请人：Shanghai ChangChengYiYaokeji Company Limited

  公开号：US20220281904A1

  公开（公告）日：2022-09-08

  A prodrug platform is useful to deliver pharmaceutically active amines, amides and phenols and their use in the diagnosis, prevention and/or treatment of various diseases. Compared with the parent drug (e.g., Gemcitabine), the prodrugs show a significant overall safety improvement (therapeutic index (TI) improvement), especially in liver. The prodrugs can treat several diseases, including, for example, cancer, metabolic disease, viral infection, immunological disease, neurologic disease, and blood disease.
• [EN] WATER-SOLUBLE POLYMER CONJUGATES OF TOPOTECAN<br/>[FR] CONJUGUÉS POLYMÈRES HYDROSOLUBLES DE TOPOTÉCAN
  申请人：NEKTAR THERAPEUTICS

  公开号：WO2012083197A1

  公开（公告）日：2012-06-21

  Provided herein are water-soluble polymer conjugates of topotecan, along with compositions comprising the conjugates and related methods of making and using the same.