ethylene glycol | 1415329-07-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: ethylene glycol
• 英文别名: NHPI-PEG1-C2-NHS ester；(2,5-dioxopyrrolidin-1-yl) 3-[2-(1,3-dioxoisoindol-2-yl)oxyethoxy]propanoate
• CAS: 1415329-07-5
• 化学式: C₁₇H₁₆N₂O₈
• 分子量: 376.323
• InChiKey: OJAHTLFPOOGMOQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  27
• 可旋转键数：
  9
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.35
• 拓扑面积：
  120
• 氢给体数：
  0
• 氢受体数：
  8

反应信息

• 作为反应物：
  描述：

  ethylene glycol 、 4-((S)-2-((S)-2-amino-3-methylbutanamido)-5-ureidopentanamido)benzyl ((S)-1-(((S)-1-(((3R,4S,5S)-3-methoxy-1-((S)-2-((1R,2R)-1-methoxy-2-methyl-3-oxo-3-(((S)-2-phenyl-1-(thiazol-2-yl)ethyl)amino)propyl)pyrrolidin-1-yl)-5-methyl-1-oxoheptan-4-yl)(methyl)amino)-3-methyl-1-oxobutan-2-yl)amino)-3-methyl-1-oxobutan-2-yl)(methyl)carbamate 以 N,N-二甲基甲酰胺 为溶剂， 反应 16.0h， 生成 [4-[[(2S)-5-(carbamoylamino)-2-[[(2S)-2-[3-[2-(1,3-dioxoisoindol-2-yl)oxyethoxy]propanoylamino]-3-methylbutanoyl]amino]pentanoyl]amino]phenyl]methyl N-[(2S)-1-[[(2S)-1-[[(3R,4S,5S)-3-methoxy-1-[(2S)-2-[(1R,2R)-1-methoxy-2-methyl-3-oxo-3-[[(1S)-2-phenyl-1-(1,3-thiazol-2-yl)ethyl]amino]propyl]pyrrolidin-1-yl]-5-methyl-1-oxoheptan-4-yl]-methylamino]-3-methyl-1-oxobutan-2-yl]amino]-3-methyl-1-oxobutan-2-yl]-N-methylcarbamate
  参考文献：
  名称：

  [EN] COMPOSITIONS CONTAINING, METHODS INVOLVING, AND USES OF NON-NATURAL AMINO ACID LINKED DOLASTATIN DERIVATIVES
  [FR] COMPOSITIONS CONTENANT DES DÉRIVÉS DE DOLASTATINE LIÉS À DES ACIDES AMINÉS NON NATUREL

  摘要：

  披露的是非天然氨基酸和杜洛司他汀类似物，其中包括至少一种非天然氨基酸，以及制造这种非天然氨基酸和多肽的方法。杜洛司他汀类似物可以包括广泛的可能性功能，但通常至少具有一个肟、羰基、二羰基和/或羟基胺基团。还披露了在翻译后进一步修改的非天然氨基酸杜洛司他汀类似物，实施这种修改的方法，以及纯化这种杜洛司他汀类似物的方法。通常，修改后的杜洛司他汀类似物至少包括一个肟、羰基、二羰基和/或羟基胺基团。进一步披露了使用这样的非天然氨基酸杜洛司他汀类似物和修改后的非天然氨基酸杜洛司他汀类似物的方法，包括治疗、诊断和其他生物技术应用。

  公开号：

  WO2012166560A1
• 作为产物：
  描述：

  3-(2-羟基乙氧基)丙酸叔丁酯 在 盐酸 、 偶氮二甲酸二异丙酯 、 N,N'-二环己基碳二亚胺 、 三苯基膦 作用下， 以 四氢呋喃 、 1,4-二氧六环 为溶剂， 反应 2.0h， 生成 ethylene glycol
  参考文献：
  名称：

  [EN] ANTI-CD70 ANTIBODY DRUG CONJUGATES
  [FR] CONJUGUÉS DE MÉDICAMENT ANTICORPS ANTI-CD70

  摘要：

  本发明涉及抗CD70抗体以及包含至少一个非天然编码氨基酸的抗体药物偶联物。在此公开了具有一个或多个非天然编码氨基酸的αCD70抗体，并且进一步公开了抗体药物偶联物，其中本发明的αCD70抗体与一个或多个毒素偶联。进一步还公开了使用此类非天然氨基酸抗体药物偶联物的方法，包括治疗、诊断和其他生物技术应用。

  公开号：

  WO2013192360A1

文献信息

• [EN] PROSTATE-SPECIFIC MEMBRANE ANTIGEN ANTIBODY DRUG CONJUGATES<br/>[FR] CONJUGUÉS ANTICORPS-MÉDICAMENT D'ANTIGÈNE MEMBRANAIRE SPÉCIFIQUE À LA PROSTATE
  申请人：AMBRX INC

  公开号：WO2013185117A1

  公开（公告）日：2013-12-12

  This invention relates to prostate-specific membrane antigen (PSMA) antibodies and antibody drug conjugates comprising at least one non-naturally-encoded amino acid. Disclosed herein are αPSMA antibodies with one or more non-naturally encoded amino acids and further disclosed are antibody drug conjugates wherein the αPSMA antibodies of the invention are conjugated to one or more toxins. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid antibody drug conjugates, dolastatin analogs, and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology uses.

  本发明涉及前列腺特异性膜抗原（PSMA）抗体及包含至少一个非天然编码氨基酸的抗体药物偶联物。公开了具有一个或多个非天然编码氨基酸的αPSMA抗体，以及进一步公开了抗体药物偶联物，其中本发明的αPSMA抗体与一个或多个毒素偶联。还公开了非天然氨基酸多拉司汀类似物，这些类似物在翻译后进一步修饰，以及实现这些修饰的方法和纯化这些多拉司汀类似物的方法。通常，修饰的多拉司汀类似物包括至少一个肟、羰基、二羰基和/或羟基胺基团。进一步公开了使用此类非天然氨基酸抗体药物偶联物、多拉司汀类似物和修饰的非天然氨基酸多拉司汀类似物的方法，包括治疗、诊断和其他生物技术用途。
• COMPOSITIONS CONTAINING, METHODS INVOLVING, AND USES OF NON-NATURAL AMINO ACID LINKED DOLASTATIN DERIVATIVES
  申请人：Ambrx, Inc.

  公开号：EP3470413A2

  公开（公告）日：2019-04-17

  Disclosed herein are non-natural amino acids and dolastatin analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The dolastatin analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid dolastatin analogs and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology use.

  本文公开了包括至少一种非天然氨基酸的非天然氨基酸和多拉他汀类似物，以及制造这种非天然氨基酸和多肽的方法。多拉他汀类似物可包括多种可能的官能团，但通常具有至少一个肟基、羰基、二羰基和/或羟胺基团。本文还公开了经翻译后进一步修饰的非天然氨基酸多拉他汀类似物、进行此类修饰的方法以及纯化此类多拉他汀类似物的方法。通常，修饰的多拉他汀类似物包括至少一个肟基、羰基、二羰基和/或羟胺基团。进一步公开的是使用此类非天然氨基酸多拉他汀类似物和修饰的非天然氨基酸多拉他汀类似物的方法，包括治疗、诊断和其它生物技术用途。
• Anti-CD70 antibody drug conjugates
  申请人：Ambrx, Inc.

  公开号：US10208123B2

  公开（公告）日：2019-02-19

  This invention relates to anti-CD70 antibodies and antibody drug conjugates comprising at least one non-naturally-encoded amino acid. Disclosed herein are αCD70 antibodies with one or more non-naturally encoded amino acids and further disclosed are antibody drug conjugates wherein the αCD70 antibodies of the invention are conjugated to one or more toxins. Further disclosed are methods for using such non-natural amino acid antibody drug conjugates, including therapeutic, diagnostic, and other biotechnology uses.

  本发明涉及包含至少一个非天然编码氨基酸的抗 CD70 抗体和抗体药物共轭物。本发明公开了含有一个或多个非天然编码氨基酸的αCD70抗体，并进一步公开了抗体药物共轭物，其中本发明的αCD70抗体与一种或多种毒素共轭。进一步公开了使用这种非天然氨基酸抗体药物共轭物的方法，包括治疗、诊断和其他生物技术用途。
• Prostate-specific membrane antigen antibody drug conjugates
  申请人：Ambrx, Inc.

  公开号：US10800856B2

  公开（公告）日：2020-10-13

  This invention relates to prostate-specific membrane antigen (PSMA) antibodies and antibody drug conjugates comprising at least one non-naturally-encoded amino acid. Disclosed herein are αPSMA antibodies with one or more non-naturally encoded amino acids and further disclosed are antibody drug conjugates wherein the αPSMA antibodies of the invention are conjugated to one or more toxins. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid antibody drug conjugates, dolastatin analogs, and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology uses.

  本发明涉及前列腺特异性膜抗原（PSMA）抗体和包含至少一个非天然编码氨基酸的抗体药物共轭物。本发明公开了含有一个或多个非天然编码氨基酸的αPSMA抗体，并进一步公开了抗体药物共轭物，其中本发明的αPSMA抗体与一种或多种毒素共轭。本文还公开了经翻译后进一步修饰的非天然氨基酸多拉他汀类似物、进行此类修饰的方法以及纯化此类多拉他汀类似物的方法。通常，修饰的多拉他汀类似物包括至少一个肟基、羰基、二羰基和/或羟胺基团。进一步公开的是使用此类非天然氨基酸抗体药物共轭物、多拉他汀类似物和修饰的非天然氨基酸多拉他汀类似物的方法，包括治疗、诊断和其它生物技术用途。
• Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
  申请人：Ambrx, Inc.

  公开号：US10954270B2

  公开（公告）日：2021-03-23

  Disclosed herein are non-natural amino acids and dolastatin analogs that include at least one non-natural amino acid, and methods for making such non-natural amino acids and polypeptides. The dolastatin analogs can include a wide range of possible functionalities, but typically have at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Also disclosed herein are non-natural amino acid dolastatin analogs that are further modified post-translationally, methods for effecting such modifications, and methods for purifying such dolastatin analogs. Typically, the modified dolastatin analogs include at least one oxime, carbonyl, dicarbonyl, and/or hydroxylamine group. Further disclosed are methods for using such non-natural amino acid dolastatin analogs and modified non-natural amino acid dolastatin analogs, including therapeutic, diagnostic, and other biotechnology use.

  本文公开了包括至少一种非天然氨基酸的非天然氨基酸和多拉他汀类似物，以及制造这种非天然氨基酸和多肽的方法。多拉他汀类似物可包括多种可能的官能团，但通常具有至少一个肟基、羰基、二羰基和/或羟胺基团。本文还公开了经翻译后进一步修饰的非天然氨基酸多拉他汀类似物、进行此类修饰的方法以及纯化此类多拉他汀类似物的方法。通常，修饰的多拉他汀类似物包括至少一个肟基、羰基、二羰基和/或羟胺基团。进一步公开的是使用此类非天然氨基酸多拉他汀类似物和修饰的非天然氨基酸多拉他汀类似物的方法，包括治疗、诊断和其它生物技术用途。