2,5-Dioxopyrrolidin-1-yl 3-(2-hydroxyethoxy)propanoate | 123502-58-9

• 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: 2,5-Dioxopyrrolidin-1-yl 3-(2-hydroxyethoxy)propanoate
• 英文别名: (2,5-dioxopyrrolidin-1-yl) 3-(2-hydroxyethoxy)propanoate
• CAS: 123502-58-9
• 化学式: C₉H₁₃NO₆
• 分子量: 231.2
• InChiKey: PXQHLLVZZMVCNV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.7
• 重原子数：
  16
• 可旋转键数：
  7
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.67
• 拓扑面积：
  93.1
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• NOVEL CONJUGATES, PREPARATION THEREOF, AND THERAPEUTIC USE THEREOF
  申请人：BOUCHARD Hervé

  公开号：US20120225089A1

  公开（公告）日：2012-09-06

  Provided herein are cryptophycin conjugates and compositions containing them. Methods of making and using such compounds also are provided.

  本发明提供了隐藻素偶联物及其包含它们的组合物。还提供了制备和使用此类化合物的方法。
• POLYETHYLENE GLYCOLATED SUPEROXIDE DISMUTASE MIMETICS
  申请人：Salvemini Daniela

  公开号：US20080318917A1

  公开（公告）日：2008-12-25

  Compounds and methods for utilizing compounds comprising a superoxide dismutase mimetic covalently linked to polyethylene glycol. Methods are also provided for preparing a superoxide dismutase mimetic covalently linked to a polyethylene glycol, the methods comprising reacting an activated polyethylene glycol with a superoxide, dismutase mimetic, or alternatively, reacting a superoxide dismutase mimetic with an activated polyethylene glycol. A method is also provided for preventing or treating a disease or disorder in which superoxide anions are implicated, comprising administering to a subject in need thereof, a therapeutically effective amount of a compound comprising a superoxide dismutase mimetic covalently linked to a polyethylene glycol. Methods of determining the safety and efficacy of the compounds ere also provided. Methods for determining the safety and efficacy can include methods in lab animals and humans.

  化合物和利用化合物的方法，包括将超氧化物歧化酶类似物共价连接到聚乙二醇中。还提供了制备超氧化物歧化酶类似物共价连接到聚乙二醇的方法，其中包括将活化聚乙二醇与超氧化物歧化酶类似物反应，或者将超氧化物歧化酶类似物与活化聚乙二醇反应。还提供了一种方法，用于预防或治疗超氧阴离子参与的疾病或紊乱，包括向需要治疗的受体注射含有超氧化物歧化酶类似物共价连接到聚乙二醇的化合物的治疗有效剂量。还提供了确定化合物安全性和有效性的方法。确定安全性和有效性的方法可以包括在实验动物和人类中进行的方法。
• BIOMOLECULE POLYMER CONJUGATES AND METHODS FOR MAKING THE SAME
  申请人：Chilkoti Ashutosh

  公开号：US20110294189A1

  公开（公告）日：2011-12-01

  Methods for producing biomolecule-polymer conjugates, such as polypeptide-polymer conjugates, include attachment of an initiator agent to a biomolecule and in situ polymerization of a polymer from defined sites on the biomolecule. The conjugates may have desirable pharmacological properties and may be used therapeutically.

  生物分子 - 聚合物共轭物的制备方法，例如多肽 - 聚合物共轭物，包括将起始剂附加到生物分子上，并从生物分子上的定义位置原位聚合聚合物。这些共轭物可能具有理想的药理学特性，并可用于治疗。
• POLYMER CONJUGATES OF THERAPEUTIC PEPTIDES
  申请人：NEKTAR THERAPEUTICS

  公开号：US20160022828A1

  公开（公告）日：2016-01-28

  The invention provides peptides that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the peptide not attached to the water-soluble oligomer.

  本发明提供了通过共价结合水溶性寡聚体进行化学修饰的肽。本发明的结合物在通过任何一种给药途径进行给药时，表现出与未附着水溶性寡聚体的肽不同的特征。
• Method for preparation of site-specific protein conjugates
  申请人：PR Pharmaceuticals Inc.

  公开号：EP2599502A2

  公开（公告）日：2013-06-05

  The invention is directed to a single-step method for rapidly and efficiently preparing protein-polymer conjugates, including an insulin-polymer conjugate. According to the method of the present invention, a protein and hydrophilic polymer are contacted in the presence of at least one organic solvent and at least one metal chelator, under conditions that promote the formation of a conjugate of the protein and polymer. Thus, the invention is directed to the site-specific modification of selected proteins, such as insulin, with poly(ethylene glycol) at residue PheB 1. The invention also provides a pharmaceutical formulation for encapsulating the conjugate in a biodegradable polymer.

  本发明涉及一种快速高效制备蛋白质-聚合物共轭物（包括胰岛素-聚合物共轭物）的一步法。根据本发明的方法，蛋白质和亲水性聚合物在至少一种有机溶剂和至少一种金属螯合剂的存在下接触，其条件是促进蛋白质和聚合物共轭物的形成。因此，本发明的目的是在残基 PheB 1 处用聚乙二醇对选定的蛋白质（如胰岛素）进行位点特异性修饰。 本发明还提供了一种将共轭物封装在生物可降解聚合物中的药物制剂。