N-(7-amino-2-oxoheptan-3-yl)-2-(methylamino)-3-phenylpropanamide

• 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: N-(7-amino-2-oxoheptan-3-yl)-2-(methylamino)-3-phenylpropanamide
• 化学式: C₁₇H₂₇N₃O₂
• 分子量: 305.4
• InChiKey: WHTHFIUFRRKCHB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.1
• 重原子数：
  22
• 可旋转键数：
  10
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.53
• 拓扑面积：
  84.2
• 氢给体数：
  3
• 氢受体数：
  4

文献信息

• SPECIFIC SITES FOR MODIFYING ANTIBODIES TO MAKE IMMUNOCONJUGATES
  申请人：Novartis AG

  公开号：EP3960767A2

  公开（公告）日：2022-03-02

  The present application provides specific sites for modifying antibodies or antibody fragments by replacing at least one native amino acid in the constant region of a parental antibody or antibody fragment with cysteine, which can be used as a site of attachment for a payload or linker-payload combination. In one embodiment, the antibodies are modified with cysteines at positions 152 and 375 of the heavy chain constant region, as defined by EU numbering format. In another embodiment, the antibodies are modified with cysteines at position 360 of the heavy chain constant region, and position 107 of the kappa light chain constant region, as defined by EU numbering format.

  本申请通过用半胱氨酸取代亲代抗体或抗体片段恒定区中的至少一个原生氨基酸，提供了修饰抗体或抗体片段的特定位点，这些位点可用作有效载荷或连接子-有效载荷组合的连接位点。在一个实施方案中，抗体在重链恒定区的 152 位和 375 位被半胱氨酸修饰，如欧盟编号格式所定义。在另一个实施方案中，抗体在重链恒定区的 360 位和 kappa 轻链恒定区的 107 位被半胱氨酸修饰，如欧盟编号格式所定义。
• CYTOTOXIC PEPTIDES AND CONJUGATES THEREOF
  申请人：GEIERSTANGER Bernhard Hubert

  公开号：US20160311853A1

  公开（公告）日：2016-10-27

  Disclosed herein are novel cytotoxic peptides of formula (I) as described herein: and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel cytotoxic peptide linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.
• AURISTATIN DERIVATIVES AND CONJUGATES THEREOF
  申请人：Geierstanger Bernhard Hubert

  公开号：US20170121282A1

  公开（公告）日：2017-05-04

  Disclosed herein are novel compounds of formula (I) as described herein: and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel compound linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.
• ANTIBODY CONJUGATES COMPRISING TOLL-LIKE RECEPTOR AGONIST
  申请人：CORTEZ Alex

  公开号：US20170121421A1

  公开（公告）日：2017-05-04

  Provided herein are antibody conjugates comprising toll-like receptor agonists and the use of such conjugates for the treatment of cancer. In some embodiments, the conjugates comprise anti-HER2 antibodies.
• AMATOXIN DERIVATIVES AND CONJUGATES THEREOF AS INHIBITORS OF RNA POLYMERASE
  申请人：Grunewald Jan

  公开号：US20170355731A1

  公开（公告）日：2017-12-14

  The invention disclosed herein relates to cytotoxic cyclic peptides of Formula (I), methods of inhibiting RNA polymerase with such cyclic peptides, immunoconjugates comprising such cyclic peptides (i.e Antibody Drug Conjugates), pharmaceutical compositions comprising such cyclic peptides immunoconjugates, compositions comprising such cyclic peptides immunoconjugates with a therapeutic co-agent and methods of treatment using such cyclic peptides immunoconjugates: