11-methoxy-3,6,9-trioxaundecanyl N-succinimidyl carbonate | 147912-03-6

• 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: 11-methoxy-3,6,9-trioxaundecanyl N-succinimidyl carbonate
• 英文别名: m-PEG4-succinimidyl carbonate；(2,5-dioxopyrrolidin-1-yl) 2-[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]ethyl carbonate
• CAS: 147912-03-6
• 化学式: C₁₄H₂₃NO₉
• 分子量: 349.338
• InChiKey: UCHQKIQOBVMTDI-UHFFFAOYSA-N

物化性质

• 沸点：
  433.0±55.0 °C(Predicted)
• 密度：
  1.26±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1
• 重原子数：
  24
• 可旋转键数：
  15
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.79
• 拓扑面积：
  110
• 氢给体数：
  0
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  11-methoxy-3,6,9-trioxaundecanyl N-succinimidyl carbonate 生成 N-((11-Methoxy-3,6,9-trioxaundecanyloxy)carbonyl)-L-leucine N-hydroxysuccinimide ester
  参考文献：
  名称：

  LISSENCEPHALY THERAPEUTIC AGENT

  摘要：

  公开号：

  EP2647386B1
• 作为产物：
  描述：

  四乙基乙二醇单甲酯 生成 11-methoxy-3,6,9-trioxaundecanyl N-succinimidyl carbonate
  参考文献：
  名称：

  LISSENCEPHALY THERAPEUTIC AGENT

  摘要：

  公开号：

  EP2647386B1

文献信息

• [EN] ALPHA-KETOAMIDE DERIVATIVE, AND PRODUCTION METHOD AND USE THEREOF<br/>[FR] DERIVE D'ALPHA-CETOAMIDE, SON PROCEDE DE PRODUCTION ET D'UTILISATION
  申请人：SENJU PHARMA CO

  公开号：WO2005056519A1

  公开（公告）日：2005-06-23

  The present invention provides a compound represented by the formula (I): (INSERT CHEMICAL FORMULA) (wherein R1 is a lower alkyl substituted by a lower alkoxy or a heterocyclic group, or a heterocyclic group; R2 is a lower alkyl optionally substituted by a phenyl; and R3 is a lower alkyl optionally substituted by a halogen, a lower alkoxy or a phenyl, or a fused polycyclic hydrocarbon group), which is well absorbed orally, exhibits durability of good blood level and has potent calpain inhibitory activity.

  本发明提供了一种化合物，其化学式表示为（I）：（插入化学式）（其中R1是由低烷基取代的低烷氧基或杂环基，或者是杂环基；R2是可选择地由苯基取代的低烷基；R3是可选择地由卤素、低烷氧基或苯基取代的低烷基，或者是融合的多环碳氢基），该化合物在口服后被很好地吸收，表现出良好的血液水平持久性，并具有强大的钙蛋白酶抑制活性。
• COMPOSITION FOR TREATMENT AND/OR PREVENTION OF PERIPHERAL NERVE DISORDER
  申请人：OSAKA CITY UNIVERSITY

  公开号：US20190314320A1

  公开（公告）日：2019-10-17

  The present invention provides a means for treating and/or preventing peripheral nerve disorder by facilitating regeneration of peripheral nerves. Specifically, the present invention provides a composition for treating and/or preventing peripheral nerve disorder comprising a compound represented by the general formula (I): wherein R 1 is lower alkyl substituted with lower alkoxy, lower alkyl substituted with a heterocyclic group, a heterocyclic group, or a group represented by the formula (IIa): R 4 O—R 5  m (IIa) wherein R 4 is lower alkyl, R 5 is lower alkylene, and m is an integer of 1 to 6; R 2 is lower alkyl optionally substituted with phenyl; and R 3 is lower alkyl optionally substituted with halogen, lower alkoxy, or phenyl; condensed polycyclic hydrocarbon; or hydrogen.

  本发明提供了一种治疗和/或预防外周神经障碍的方法，通过促进外周神经再生。具体地，本发明提供了一种用于治疗和/或预防外周神经障碍的组合物，包括由通式（I）表示的化合物： 其中R1为与低烷氧基取代的低烷基，与杂环基取代的低烷基，杂环基，或由式（IIa）表示的基团： R4O—R5m（IIa） 其中R4为低烷基，R5为低烷基烯，m为1至6的整数； R2为可选择地取代苯基的低烷基；和 R3为可选择地取代卤素，低烷氧基，或苯基的低烷基；缩合多环碳氢化合物；或氢。
• Fatty acid formulations for oral delivery of proteins and peptides, and uses thereof
  申请人：Radhakrishnan Balasingam

  公开号：US20060018874A1

  公开（公告）日：2006-01-26

  Fatty acid compositions for administration of of pharmaceutical agents, such as proteins and peptides, protein and peptide conjugates, and/or cation-polypeptide conjugate complexes. In particular, the invention provides a solid pharmaceutical composition formulated for oral administration by ingestion, having from about 0.1 to about 75% w/w fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent. Further, the invention provides a liquid pharmaceutical composition formulated for oral administration by ingestion, comprising: from about 0.1 to about 10% w/v fatty acid component, where the fatty acid component comprises saturated or unsaturated C4, C5, C6, C7, C8, C9, C10, C11, or C12 fatty acids and/or salts of such fatty acids; and a therapeutic agent.

  脂肪酸组成物用于制备药物，例如蛋白质和肽，蛋白质和肽共轭物以及/或阳离子-多肽共轭物复合物的给药。特别地，本发明提供了一种固体制剂，用于经口摄入口服，其含有约0.1至约75％w/w的脂肪酸成分，其中所述脂肪酸成分包括饱和或不饱和的C4，C5，C6，C7，C8，C9，C10，C11或C12脂肪酸和/或这些脂肪酸的盐；以及治疗剂。此外，本发明提供了一种液体制剂，用于经口摄入口服，包括：约0.1至约10％w/v的脂肪酸成分，其中所述脂肪酸成分包括饱和或不饱和的C4，C5，C6，C7，C8，C9，C10，C11或C12脂肪酸和/或这些脂肪酸的盐；以及治疗剂。
• Cation complexes of insulin compound conjugates, formulations and uses thereof
  申请人：Radhakrishnan Balasingam

  公开号：US20060019873A1

  公开（公告）日：2006-01-26

  An insulin compound coupled to a modifying moiety having a formula: —X—R 1 —Y-PAG-Z-R  (Formula VI) where, X, Y and Z are independently selected linking groups and each is optionally present, and X, when present, is coupled to the insulin compound by a covalent bond, either R 1 or R 2 is is a lower alkyl, optionally including a carbonyl group, and when R 1 is a lower alkyl, R 2 is a capping group, and PAG is a linear or branched carbon chain incorporating one or more alkalene glycol moieties, and optionally incorporating one or more additional moieties selected from the group consisting of —S—, —O—, —N—, and —C(O)—, and where the modifying moiety has a maximum number of 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, or 25 heavy atoms.

  一种胰岛素化合物，与具有以下式的修饰基偶联：—X—R1—Y-PAG-Z-R（VI式）其中，X、Y和Z是独立选择的连接基，每个都可以选择存在，且当X存在时，它通过共价键与胰岛素化合物偶联，R1或R2是较低的烷基，可以包括一个羰基基团，当R1是较低的烷基时，R2是一个端基，PAG是一种线性或支链碳链，包括一个或多个碱基二醇基团，并且可以包括从以下组中选择的一个或多个附加基团：—S—、—O—、—N—和—C（O）—，其中修饰基最多有3、4、5、6、7、8、9、10、11、12、13、14、15、16、17、18、19、20、21、22、23、24或25个重原子。
• Cation complexes of insulin compund conjugates, formulation and uses thereof
  申请人：Radhakrishnan Balasingam

  公开号：US20060019874A1

  公开（公告）日：2006-01-26

  The invention provides a complex including a cation and an insulin compound conjugate. The insulin compound conjugate includes insulin compound, such as human insulin or an analog thereof, conjugated to a modifying moiety, such as a polyethylene glycol moiety. The invention also includes solids and pharmaceutical compositions including such complexes, methods of making such complexes, and methods of using such complexes in the treatment of insulin compound deficiencies and other ailments. Further, the invention includes novel insulin compound conjugates and modifying moieties for use in making novel insulin compound conjugates. The invention also includes fatty acid compositions for administration of pharmaceutical agents, such as the novel insulin compound conjugates, and/or the cation-insulin compound conjugate complexes of the invention.

  本发明提供了一种包括阳离子和胰岛素化合物共轭物的复合物。胰岛素化合物共轭物包括胰岛素化合物，如人类胰岛素或其类似物，与修饰基团，如聚乙二醇基团结合。本发明还包括包括这种复合物的固体和制药组合物，制备这种复合物的方法以及使用这种复合物治疗胰岛素化合物缺乏和其他疾病的方法。此外，本发明还包括用于制备新型胰岛素化合物共轭物的新型胰岛素化合物共轭物和修饰基团。本发明还包括用于给药的脂肪酸组合物，例如用于给药本发明的新型胰岛素化合物共轭物和/或阳离子-胰岛素化合物共轭物复合物的制药剂。