1H-Pyrrole-2,5-dione, 1-(2-propoxyethyl)- | 1260092-54-3

• 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: 1H-Pyrrole-2,5-dione, 1-(2-propoxyethyl)-
• 英文别名: 1-(2-propoxyethyl)pyrrole-2,5-dione
• CAS: 1260092-54-3
• 化学式: C₉H₁₃NO₃
• 分子量: 183.2
• InChiKey: OCWJSCIZFINQEI-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  13
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.56
• 拓扑面积：
  46.6
• 氢给体数：
  0
• 氢受体数：
  3

文献信息

• Antibody drug conjugate, intermediate, preparation method, pharmaceutical composition and uses thereof
  申请人：XDCEXPLORER (SHANGHAI) CO., LTD.

  公开号：US10449258B2

  公开（公告）日：2019-10-22

  Disclosed are an antibody drug conjugate IB, which uses ether linkages for connection, and improves the water solubility, stability and cytotoxicity in vivo and in intro, and an intermediate, a pharmaceutical composition, and uses of the antibody drug conjugate. The antibody drug conjugate has simple synthetic steps and a high yield.

  披露了一种抗体药物偶联物IB，它使用醚键连接，提高了体内和体外的水溶性、稳定性和细胞毒性，以及一种中间体、药物组合物和抗体药物偶联物的用途。该抗体药物偶联物具有简单的合成步骤和高产率。
• NOVEL OPTICAL LABELING MOLECULES FOR PROTEOMICS AND OTHER BIOLOGICAL ANALYSES
  申请人：DRATZ Edward

  公开号：US20100252433A1

  公开（公告）日：2010-10-07

  The invention relates to compositions and methods useful in the labeling and identification of changes in protein levels, changes in enzyme activity, and changes in protein modification. The invention provides for highly soluble optical labeling molecules which are optionally cleavable after separation of mixtures of labeled proteins into components. These optical labeling molecules find utility in a variety of applications, including use in the field of proteomics.

  本发明涉及用于标记和识别蛋白质水平变化、酶活性变化和蛋白质修饰变化的组合物和方法。本发明提供了高度溶解的光学标记分子，这些分子在将标记蛋白质的混合物分离成组分后可选择性地被裂解。这些光学标记分子在各种应用中具有实用性，包括在蛋白质组学领域的应用。
• METHOD FOR PREPARING ANTIBODY-DRUG CONJUGATE INTERMEDIATE BY MEANS OF ACID METHOD AND APPLICATION THEREOF
  申请人：Mabplex International, Ltd.

  公开号：EP3828196A1

  公开（公告）日：2021-06-02

  Provided is a method for producing an antibody-drug conjugate intermediate by addition of acid. An acid additive is used to convert the monomethyl auristatin derivative into a salt thereof to participate in the reaction. The addition of the acid additive can significantly improve the yield of the final product. In addition, the low price of the acid additive greatly reduces the production cost of the final ADC product. Moreover, the method of the present invention adopts a one-step preparation process, in addition to a higher yield of the final product, not only reducing the cost of the consumables, labor, equipment, site, raw materials and the like in the production, but also greatly reducing the production of the waste liquid, and thus reducing production costs and improving production efficiency, and making the method suitable for industrial large-scale production.

  本发明提供了一种通过加酸生产抗体-药物共轭中间体的方法。使用酸添加剂将单甲基金丝桃素衍生物转化为其盐，以参与反应。添加酸添加剂可显著提高最终产品的产量。此外，酸添加剂价格低廉，大大降低了 ADC 最终产品的生产成本。而且，本发明方法采用一步制备工艺，除了最终产品收率较高外，不仅降低了生产中的耗材、人工、设备、场地、原料等成本，还大大减少了废液的产生，从而降低了生产成本，提高了生产效率，适合工业化大规模生产。
• Splicing modulator antibody-drug conjugates and methods of use
  申请人：EISAI R&D MANAGEMENT CO., LTD.

  公开号：US11352348B2

  公开（公告）日：2022-06-07

  Linker-drug compounds and antibody-drug conjugates that bind to human oncology targets are disclosed. The linker-drug compounds and antibody-drug conjugates comprise a splicing modulator drug moiety. The disclosure further relates to methods and compositions for use in the treatment of neoplastic disorders by administering the antibody-drug conjugates provided herein. In an embodiment, the splicing modulator comprises a pladienolide or a pladienolide derivative.

  本发明公开了与人类肿瘤靶点结合的连接子药物化合物和抗体药物共轭物。连接子-药物化合物和抗体-药物共轭物包含剪接调节剂药物分子。本发明进一步涉及通过施用本文提供的抗体-药物共轭物治疗肿瘤性疾病的方法和组合物。在一个实施方案中，剪接调节剂包括pladienolide或pladienolide衍生物。
• PEG CONJUGATES OF NK4
  申请人：BRANDT Michael

  公开号：US20080085857A1

  公开（公告）日：2008-04-10

  The present invention provides a conjugate consisting essentially of a NK4 molecule and a polyethylene glycol group having a molecular weight of from about 20 to about 40 kDa. The invention also provides a composition in which the monoPEGylated conjugates comprise at least 90% of the total of pegylated NK4 molecules and unpegylated NK4 molecules in the composition. Also provided is a composition in which the monoPEGylated conjugates comprise conjugates in which the PEG groups are attached to groups randomly selected from the lysine side chains of NK4 molecules and the N-terminal amino groups of NK4 molecules. A method for the treatment of cancer by administering 1 to 30 mg monoPEGylated NK4 per kg per day is further provided.