[2-Hydroxy-2-(1-hydroxybutan-2-yloxy)ethyl] 5-oxo-5-(2-sulfanylethylamino)pentanoate

• 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: [2-Hydroxy-2-(1-hydroxybutan-2-yloxy)ethyl] 5-oxo-5-(2-sulfanylethylamino)pentanoate
• 英文别名: [2-hydroxy-2-(1-hydroxybutan-2-yloxy)ethyl] 5-oxo-5-(2-sulfanylethylamino)pentanoate
• 化学式: C₁₃H₂₅NO₆S
• 分子量: 323.41
• InChiKey: VEUBUGRMHZQXOM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  21
• 可旋转键数：
  13
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.85
• 拓扑面积：
  106
• 氢给体数：
  4
• 氢受体数：
  7

文献信息

• PROTEIN-POLYMER-DRUG CONJUGATES
  申请人：Mersana Therapeutics, Inc.

  公开号：US20160220696A1

  公开（公告）日：2016-08-04

  Auristatin compounds and conjugates thereof are provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -L D -D, the protein based recognition-molecule being connected to the polymeric carrier by L P . Each occurrence of D is independently an Auristatin compound. L D and L P are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

  本文提供了Auristatin化合物及其共轭物。该共轭物包括一种基于蛋白质的识别分子（PBRM）和一种聚合物载体，该聚合物载体被取代了一个或多个-LD-D，其中，基于蛋白质的识别分子通过LP连接到聚合物载体上。每个D的出现都是独立的Auristatin化合物。LD和LP是连接治疗剂和PBRM到聚合物载体的连接物。还公开了用于与PBRM共轭形成聚合物-药物-PBRM共轭物的聚合物支架，以及包含共轭物的组合物，其制备方法以及使用共轭物或其组合物治疗各种疾病的方法。
• TUBULYSIN COMPOUNDS AND CONJUGATES THEREOF
  申请人：Mersana Therapeutics, Inc.

  公开号：US20160022829A1

  公开（公告）日：2016-01-28

  A tubulysin compound conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -L D -D, the protein based recognition-molecule being connected to the polymeric carrier by L P . Each occurrence of D is independently a tubulysin compound having a molecular weight≦5 kDa. L D and L P are distinct linkers connecting the tubulysin compound and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer-tubulysin compound-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.

  本文提供了一种管芽菌素化合物结合物。该结合物包括一种基于蛋白质的识别分子（PBRM）和一种聚合物载体，该聚合物载体被取代了一个或多个-LD-D，其中，基于蛋白质的识别分子通过LP连接到聚合物载体上。每个D的出现独立地是分子量≦5 kDa的管芽菌素化合物。LD和LP是连接管芽菌素化合物和PBRM分别到聚合物载体的不同连接物。还公开了用于与PBRM结合形成聚合物-管芽菌素化合物-PBRM结合物的聚合物支架，包括结合物的组合物，其制备方法以及使用结合物或其组合物治疗各种疾病的方法。
• US9770519B2
  申请人：——

  公开号：US9770519B2

  公开（公告）日：2017-09-26
• [EN] PROTEIN-POLYMER-DRUG CONJUGATES<br/>[FR] CONJUGUÉS PROTÉINE-POLYMÈRE-MÉDICAMENT
  申请人：MERSANA THERAPEUTICS INC

  公开号：WO2014093394A1

  公开（公告）日：2014-06-19

  A drug conjugate is provided herein. The conjugate comprises a protein based recognition-molecule (PBRM) and a polymeric carrier substituted with one or more -LD-D, the protein based recognition-molecule being connected to the polymeric carrier by Lp. Each occurrence of D is independently a therapeutic agent having a molecular weight < 5 kDa. LD and Lp are linkers connecting the therapeutic agent and PBRM to the polymeric carrier respectively. Also disclosed are polymeric scaffolds useful for conjugating with a PBRM to form a polymer- drug-PBRM conjugate described herein, compositions comprising the conjugates, methods of their preparation, and methods of treating various disorders with the conjugates or their compositions.