1-[(2-Sulfanylpropanoyl)oxy]pyrrolidine-2,5-dione | 68181-18-0

• 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: 1-[(2-Sulfanylpropanoyl)oxy]pyrrolidine-2,5-dione
• 英文别名: (2,5-dioxopyrrolidin-1-yl) 2-sulfanylpropanoate
• CAS: 68181-18-0
• 化学式: C₇H₉NO₄S
• 分子量: 203.22
• InChiKey: HGCBPBZRTKWGLY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  13
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.57
• 拓扑面积：
  64.7
• 氢给体数：
  1
• 氢受体数：
  5

文献信息

• [EN] AMATOXIN DERIVATIVES AND CONJUGATES THEREOF AS INHIBITORS OF RNA POLYMERASE<br/>[FR] DÉRIVÉS D'AMATOXINE ET LEURS CONJUGUÉS À UTILISER EN TANT QU'INHIBITEURS DE L'ARN POLYMÉRASE
  申请人：NOVARTIS AG

  公开号：WO2017191579A1

  公开（公告）日：2017-11-09

  The invention disclosed herein relates to cytotoxic cyclic peptides of Formula (A), methods of inhibiting RNA polymerase with such cyclic peptides, immunoconjugates comprising such cyclic peptides (i.e Antibody Drug Conjugates), pharmaceutical compositions comprising such cyclic peptides immunoconjugates, compositions comprising such cyclic peptides immunoconjugates with a therapeutic co-agent and methods of treatment using such cyclic peptides immunoconjugates.

  本发明涉及公式（A）的细胞毒性环肽，以及利用这些环肽抑制RNA聚合酶的方法，包括这些环肽的免疫结合物（即抗体药物结合物），包含这些环肽免疫结合物的药物组合物，含有这些环肽免疫结合物和治疗性辅助剂的组合物，以及利用这些环肽免疫结合物进行治疗的方法。
• Disulfur bridge linkers for conjugation of a cell-binding molecule
  申请人：Suzhou M-Conj Biotech Co., Ltd.

  公开号：US10322104B2

  公开（公告）日：2019-06-18

  The present invention relates to novel disulfur bridge linkers containing hydrazine used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking a pair of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.

  本发明涉及新型含肼二硫桥连接体，用于通过桥接细胞结合分子上的一对硫醇，将化合物/细胞毒剂与细胞结合分子特异性连接。本发明还涉及制造这种连接体的方法、使用这种连接体制造均相共轭物的方法，以及应用这种共轭物治疗癌症、感染和自身免疫性疾病的方法。
• Cytotoxic agents and conjugates thereof
  申请人：POLYTHERICS LIMITED

  公开号：US10654873B2

  公开（公告）日：2020-05-19

  Provided herein are novel maytansinoid compounds of general formula I. Also provided herein are conjugates comprising the compounds linked to a binding protein via a linker, and conjugating reagents comprising the compounds attached via a linker to at least one functional group capable of reacting with a binding protein. Also provided herein are pharmaceutical compositions comprising the compounds and conjugates, therapeutic methods and uses involving the compounds and conjugates, for example in cancer therapy, and novel synthetic processes.

  本文提供了通式 I 的新型 maytansinoid 化合物。本文还提供了包含通过连接体与结合蛋白连接的化合物的共轭物，以及包含通过连接体与至少一个能与结合蛋白反应的官能团连接的化合物的共轭试剂。本文还提供了包含化合物和共轭物的药物组合物、涉及化合物和共轭物的治疗方法和用途（例如在癌症治疗中）以及新型合成工艺。
• CROSSLINKED GELS COMPRISING POLYALKYLENEIMINES, AND THEIR USES AS MEDICAL DEVICES
  申请人：HyperBranch Medical Technology, Inc.

  公开号：US20170049924A1

  公开（公告）日：2017-02-23

  One aspect of the present invention generally relates to methods of sealing a wound or tissue plane or filling a void splace. In a preferred embodiment, the wound is an ophthalmic, pleural or dural wound. In certain instances, the compositions used to seal the wound or tissue plane comprises a polyalkyleneimine. In a preferred embodiment, the polyalkyleneimine is polyethyleneimine. Treatment of the polyethyleneimine with a cross-linking reagent causes the polyethyleneimine polymers to polymerize forming a seal. In certain instances, the cross-linking reagent is a polyethylene glycol having reactive terminal groups. In certain instances, the reactive terminal groups are activated esters, such as N-hydroxy succinimide ester. In certain instances, the reactive terminal groups are isocyanates. In certain instances, the polyethyleneimine has a lysine, cysteine, isocysteine or other nucleophilic group attached to the periphery of the polymer. In certain instances, the polyethyleneimine is mixed with a second polymer, such as a polyethylene glycol containing nucleophilic groups. In certain instances, the compositions used to seal the wound or tissue plane are formed by reacting a polyalkyleneimine bearing electrophilic groups with a cross-linking reagent containing nucleophilic groups. In certain instances, the electrophilic groups on the polyalkyleneimine are activated esters, such as N-hydroxy succinimide ester. In certain instances, the compositions used to seal the wound or tissue plane are formed by reacting a polyalkyleneimine bearing photopolymerizable groups with ultraviolet or visible light. Compositions used to seal the wound which contain PEI or a derivative of PEI are found to adhere tightly to the tissue. Other aspects of the present invention relate to methods of filling a void of a patient or adhering tissue. In certain instances, the methods use a polyalkyleneimine. In a preferred embodiment, the polyalkyleneimine is polyethyleneimine. Another aspect of the present invention relates to a polymeric composition formed by exposing a polyalkyleneimine to an activated polyalkylene glycol. In certain instances, the composition is attached to mammalian tissue.
• DISULFUR BRIDGE LINKERS FOR CONJUGATION OF A CELL-BINDING MOLECULE
  申请人：Suzhou M-Conj Biotech Co., Ltd.

  公开号：US20170209595A1

  公开（公告）日：2017-07-27

  The present invention relates to novel disulfur bridge linkers containing hydrazine used for the specific conjugation of compounds/cytotoxic agents to a cell-binding molecule, through bridge linking a pair of thiols on the cell-binding molecule. The invention also relates to methods of making such linkers, and of using such linkers in making homogeneous conjugates, as well as of application of the conjugates in treatment of cancers, infections and autoimmune disorders.