2-(2-oxo-2-(4-(3-oxo-3-(2-oxoazetidin-1-yl)propyl)phenylamino)ethoxy)acetic acid | 1024602-85-4

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 内酰胺类
• 英文名称: 2-(2-oxo-2-(4-(3-oxo-3-(2-oxoazetidin-1-yl)propyl)phenylamino)ethoxy)acetic acid
• 英文别名: ((4-[3-Oxo-3-(2-oxo-azetidin-1-yl)-propyl]-phenylcarbamoyl)-methoxy)-acetic acid；2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetic acid
• CAS: 1024602-85-4
• 化学式: C₁₆H₁₈N₂O₆
• 分子量: 334.329
• InChiKey: UKFWCNWTULOBSF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  24
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  113
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  2-(2-oxo-2-(4-(3-oxo-3-(2-oxoazetidin-1-yl)propyl)phenylamino)ethoxy)acetic acid 在 N,N'-二异丙基碳二亚胺 作用下， 以 四氢呋喃 、 N,N-二甲基甲酰胺 为溶剂， 生成 N-[2-[2-[2-(2-hydroxyethoxy)ethoxy]ethoxy]ethyl]-2-[2-oxo-2-[4-[3-oxo-3-(2-oxoazetidin-1-yl)propyl]anilino]ethoxy]acetamide
  参考文献：
  名称：

  Development of a long acting human growth hormone analog suitable for once a week dosing

  摘要：

  Human growth hormone was conjugated to a carrier aldolase antibody, using a novel linker by connecting a disulphide bond in growth hormone to a lysine-94 amine located on the Fab arm of the antibody. The resulting CovX body showed reduced affinity towards human growth hormone receptor, reduced cell-based activity, but improved pharmacodynamic properties. We have demonstrated that this CovX-body, given once a week, showed comparable activity as growth hormone given daily in an in vivo hypophysectomized rat model. (c) 2012 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2012.11.104
• 作为产物：
  描述：

  3-(4-硝基苯基)丙酸 在 正丁基锂 、 氯化亚砜 、 palladium 10% on activated carbon 、 氢气 作用下， 以 四氢呋喃 为溶剂， -70.0~25.0 ℃ 、68.95 kPa 条件下， 反应 3.25h， 生成 2-(2-oxo-2-(4-(3-oxo-3-(2-oxoazetidin-1-yl)propyl)phenylamino)ethoxy)acetic acid
  参考文献：
  名称：

  PROCESSES FOR PREPARING PEPTIDE CONJUGATES AND LINKERS

  摘要：

  本发明提供了一种制备5b式化合物的方法，以及其中间体，以及用于制备这些类似化合物的新型化合物类。

  公开号：

  US20150031108A1

文献信息

• CYTOTOXIC PEPTIDES AND ANTIBODY DRUG CONJUGATES THEREOF
  申请人：PFIZER INC.

  公开号：US20130129753A1

  公开（公告）日：2013-05-23

  The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.

  本发明涉及细胞毒性五肽，其抗体药物偶联物，以及使用它们治疗癌症的方法。
• GLUCAGON-LIKE PROTEIN-1 RECEPTOR (GLP-1R) AGONIST COMPOUNDS
  申请人：BRADSHAW Curt W.

  公开号：US20090098130A1

  公开（公告）日：2009-04-16

  The present invention provides GA targeting compounds which comprise GA targeting agent-linker conjugates linked to a combining site of an antibody. Various uses of the compounds are provided, including methods to prevent or treat diabetes or diabetes-related conditions.

  本发明提供了包括连接到抗体结合位点的GA靶向剂-连接剂共轭物的GA靶向化合物。提供了化合物的各种用途，包括预防或治疗糖尿病或与糖尿病相关的疾病的方法。
• ANTI-ANGIOGENIC COMPOUNDS
  申请人：Bradshaw Curt

  公开号：US20080166364A1

  公开（公告）日：2008-07-10

  The present invention provides AA targeting compounds which comprise AA targeting agent-linker conjugates which are linked to a combining site of an antibody. Various uses of the compounds are provided, including methods to treat disorders connected to abnormal angiogenesis.

  本发明提供了包括与抗体的结合位点连接的AA靶向剂-连接剂共轭物的AA靶向化合物。提供了化合物的各种用途，包括治疗与异常血管生成相关的疾病的方法。
• Anti-Angiogenic Compounds
  申请人：Bradshaw Curt W.

  公开号：US20080152660A1

  公开（公告）日：2008-06-26

  The present invention provides AA targeting compounds which comprise AA targeting agent-linker conjugates which are linked to a combining site of an antibody. Various uses of the compounds are provided, including methods to treat disorders connected to abnormal angiogenesis.

  本发明提供了AA靶向化合物，其中包括与抗体结合位点连接的AA靶向剂-连接剂共轭物。提供了化合物的各种用途，包括治疗与异常血管生成有关的疾病的方法。
• METHODS OF TREATING A DISEASE OR CONDITION ASSOCIATED WITH ABNORMAL ANGIOGENESIS
  申请人：Bradshaw Curt

  公开号：US20120301431A1

  公开（公告）日：2012-11-29

  The present invention provides methods of treating (including preventing) a disease or condition associated with abnormal angiogenesis in a subject include administering a therapeutically effective amount of an AA targeting compound of the invention to the subject. The AA targeting compounds comprise AA targeting agent-linker conjugates which are linked to a combining site of an antibody.

  本发明提供了用于治疗（包括预防）与受试者中异常血管生成相关的疾病或症状的方法，包括向受试者施用本发明的AA靶向化合物的治疗有效量。AA靶向化合物包括AA靶向剂-连接剂偶联物，其与抗体的结合位点相连。