3-(4-Iminopentylsulfanyl)-1-methylpyrrolidine-2,5-dione

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: 3-(4-Iminopentylsulfanyl)-1-methylpyrrolidine-2,5-dione
• 英文别名: 3-(4-iminopentylsulfanyl)-1-methylpyrrolidine-2,5-dione
• 化学式: C₁₀H₁₆N₂O₂S
• 分子量: 228.31
• InChiKey: XOLOYGWEVJGGIZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  15
• 可旋转键数：
  5
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.7
• 拓扑面积：
  86.5
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• COMPLEX COMPRISING LIGAND AND CEACAM5 ANTIBODY FAB FRAGMENT
  申请人：Astellas Pharma Inc.

  公开号：EP3909606A1

  公开（公告）日：2021-11-17

  Provided is a conjugate comprising a ligand, a spacer, and a peptide linker useful for an in-vivo diagnostic drug and internal radiation therapy, using an anti-human CEACAM5 antibody Fab fragment whose binding activity is not attenuated even by labeling with a metal, a fluorescent dye, or the like. A conjugate comprising an anti-human CEACAM5 antibody Fab fragment and a ligand, the fragment comprising a heavy chain fragment including a heavy chain variable region consisting of a specific amino acid sequence and a light chain including a light chain variable region consisting of a specific amino acid sequence, or a conjugate comprising a ligand, a spacer, and a peptide linker, wherein the binding activity thereof is not attenuated even by labeling with a metal, a fluorescent dye, or the like, can be used as a diagnostic composition and/or a pharmaceutical composition.

  本发明提供了一种由配体、间隔物和多肽连接体组成的共轭物，可用于体内诊断药物和体内放射治疗，该共轭物使用抗人CEACAM5抗体Fab片段，即使用金属、荧光染料等标记，其结合活性也不会减弱。由抗人 CEACAM5 抗体 Fab 片段和配体组成的共轭物，该片段包括重链片段（其中包括由特定氨基酸序列组成的重链可变区）和轻链片段（其中包括由特定氨基酸序列组成的轻链可变区），或由配体、间隔物和肽连接体组成的共轭物，其结合活性即使用金属、荧光染料等标记也不会减弱，可用作诊断组合物和/或药物组合物。
• COMPLEX COMPRISING LIGAND, SPACER, PEPTIDE LINKER, AND BIOMOLECULE
  申请人：Astellas Pharma Inc.

  公开号：EP3909608A1

  公开（公告）日：2021-11-17

  Provided is a conjugate comprising a ligand, a spacer, and a peptide linker useful for an in-vivo diagnostic drug and internal radiation therapy, using an anti-human MUC1 antibody Fab fragment whose binding activity is not attenuated even by labeling with a metal, a fluorescent dye, or the like. A conjugate comprising 3arm DOTA, a specific spacer, a specific peptide linker, and a biomolecule including an anti-human MUC1 antibody Fab fragment, wherein the binding activity thereof is not attenuated even by labeling with a metal, a fluorescent dye, or the like, can be used as a diagnostic composition and/or a pharmaceutical composition.

  本发明提供了一种由配体、间隔物和肽链连接物组成的共轭物，该共轭物可用于体内诊断药物和体内放射治疗，使用的抗人MUC1抗体Fab片段即使用金属、荧光染料或类似物标记，其结合活性也不会减弱。由 3arm DOTA、特异性间隔物、特异性肽连接物和包括抗人 MUC1 抗体 Fab 片段的生物大分子组成的共轭物可用作诊断组合物和/或药物组合物。
• US20140271465A1
  申请人：——

  公开号：US20140271465A1

  公开（公告）日：2014-09-18
• COMPLEX HAVING ANTI-HUMAN MUC1 ANTIBODY FAB FRAGMENT, PEPTIDE LINKER AND/OR LIGAND
  申请人：Astellas Pharma Inc.

  公开号：US20210340276A1

  公开（公告）日：2021-11-04

  Provided are a conjugate comprising an anti-human MUC1 antibody Fab fragment and a peptide linker and/or a ligand, a composition for diagnosis and/or a pharmaceutical composition comprising the conjugate, a method for diagnosing and/or treating a cancer using the conjugate, and the like. In the conjugate used, the anti-human MUC1 antibody Fab fragment is bound to the ligand via the peptide linker or the like.
• CONJUGATE COMPRISING LIGAND, SPACER, PEPTIDE LINKER, AND BIOMOLECULE
  申请人：ASTELLAS PHARMA INC.

  公开号：US20220105194A1

  公开（公告）日：2022-04-07

  Provided is a conjugate comprising a ligand, a spacer, and a peptide linker useful for an in-vivo diagnostic drug and internal radiation therapy, using an anti-human MUC1 antibody Fab fragment whose binding activity is not attenuated even by labeling with a metal, a fluorescent dye, or the like. A conjugate comprising 3arm DOTA, a specific spacer, a specific peptide linker, and a biomolecule including an anti-human MUC1 antibody Fab fragment, wherein the binding activity thereof is not attenuated even by labeling with a metal, a fluorescent dye, or the like, can be used as a diagnostic composition and/or a pharmaceutical composition.