2,5-吡咯烷二酮,1-[[[(1-甲基乙基)氨基]羰基]氧代]- | 18484-44-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 中文名称: 2,5-吡咯烷二酮,1-[[[(1-甲基乙基)氨基]羰基]氧代]-
• 英文名称: O-succinimidyl N-isopropylcarbamate
• 英文别名: isopropyl-N-succinimidyl carbamate；isopropyl-N-succimidyl carbamate；N-Isopropylcarbamoyloxy-succinimid；(2,5-dioxopyrrolidin-1-yl) N-propan-2-ylcarbamate
• CAS: 18484-44-1
• 化学式: C₈H₁₂N₂O₄
• 分子量: 200.194
• InChiKey: KHAMNADHIXZMMY-UHFFFAOYSA-N

物化性质

• 熔点：
  142-143 °C
• 密度：
  1.29±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.62
• 拓扑面积：
  75.7
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2,5-吡咯烷二酮,1-[[[(1-甲基乙基)氨基]羰基]氧代]- 、 t-Boc-Met-Ile-Phe-Leu-OMe 生成 N-isopropylureido-Met-Ile-Phe-Leu-OMe
  参考文献：
  名称：

  Met-Ile-Phe-Leu derivatives: full and partial agonists of human neutrophil formylpeptide receptors

  摘要：

  The biological action of a series of Met-Ile-Phe-Leu analogues was analyzed on human neutrophils. to evaluate their ability to interact with formylpeptide receptors and to induce the related neutrophil responses. Three in vitro assays were carried out: receptor binding, chemotaxis and superoxide anion release. Our results demonstrate that formyl-Met-Ile-Phe-Leu derivatives act as more potent full agonists than formyl-Met-Leu-Phe, the tripeptide normally used as a model chemoattractant for the study of cell functions. On the other hand, the presence of N-ureidoisopropyl substituent in tetrapeptides imparts weak partial agonist properties. It has furthermore been demonstrated that the C-terminal methyl esterification or amination weakly influences the properties of tetrapeptide homologues. Finally, t-Boc-Met-Ile-Phe-Leu derivatives do not appear able to interact with formylpeptide receptors. (C) 2001 Elsevier Science B.V. All rights reserved.

  DOI：

  10.1016/s0014-2999(00)00908-0
• 作为产物：
  描述：

  N-羟基丁二酰亚胺 、 异氰酸异丙酯 在 三乙胺 作用下， 以 四氢呋喃 为溶剂， 生成 2,5-吡咯烷二酮,1-[[[(1-甲基乙基)氨基]羰基]氧代]-
  参考文献：
  名称：

  Pirrung, Michael C.; Chen, Jrlung, Journal of the American Chemical Society, 1995, vol. 117, # 4, p. 1240 - 1245

  摘要：

  DOI：

文献信息

• [EN] AURISTATIN DERIVATIVES AND CONJUGATES THEREOF<br/>[FR] DÉRIVÉS D'AURISTATINE ET CONJUGUÉS DE CEUX-CI
  申请人：NOVARTIS AG

  公开号：WO2015189791A1

  公开（公告）日：2015-12-17

  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.

  本文披露了如下所述的化合物(I)的新颖化合物，以及在制备免疫结合物（即抗体药物结合物）中使用这些肽的用途。本文还描述了包括这种新颖化合物与抗原结合基团（如抗体）连接的免疫结合物（即抗体药物结合物），这些免疫结合物可用于治疗细胞增殖性疾病。该发明还提供了包括这些免疫结合物的药物组合物，包括与治疗性辅助剂一起的免疫结合物的组合物，以及使用这些免疫结合物和组合物治疗细胞增殖性疾病的方法。
• [EN] AMATOXIN DERIVATIVES AND CONJUGATES THEREOF AS INHIBITORS OF RNA POLYMERASE<br/>[FR] DÉRIVÉS D'AMATOXINE ET LEURS CONJUGUÉS À UTILISER EN TANT QU'INHIBITEURS DE L'ARN POLYMÉRASE
  申请人：NOVARTIS AG

  公开号：WO2017191579A1

  公开（公告）日：2017-11-09

  The invention disclosed herein relates to cytotoxic cyclic peptides of Formula (A), 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.

  本发明涉及公式（A）的细胞毒性环肽，以及利用这些环肽抑制RNA聚合酶的方法，包括这些环肽的免疫结合物（即抗体药物结合物），包含这些环肽免疫结合物的药物组合物，含有这些环肽免疫结合物和治疗性辅助剂的组合物，以及利用这些环肽免疫结合物进行治疗的方法。
• Cytotoxic peptides and conjugates thereof
  申请人：NOVARTIS AG

  公开号：US10392421B2

  公开（公告）日：2019-08-27

  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.

  本文公开了如本文所述的式 (I) 的新型细胞毒性肽： 以及使用这种肽制造免疫结合剂（即抗体药物结合剂）的方法 本发明还描述了免疫结合剂（即抗体药物结合剂），其包含与抗原结合分子（如抗体）连接的这种新型细胞毒性肽；其中这种免疫结合剂可用于治疗细胞增殖性疾病。本发明进一步提供了包含这些免疫共轭物的药物组合物、包含这些免疫共轭物与治疗共用试剂的组合物，以及使用这些免疫共轭物和组合物治疗细胞增殖障碍的方法。
• Amatoxin derivatives and conjugates thereof as inhibitors of RNA polymerase
  申请人：NOVARTIS AG

  公开号：US10464969B2

  公开（公告）日：2019-11-05

  The invention disclosed herein relates to cytotoxic cyclic peptides of Formula (A), 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:

  本发明涉及式（A）的细胞毒性环肽、用这种环肽抑制 RNA 聚合酶的方法、包含这种环肽的免疫结合剂（即抗体药物结合剂）、包含这种环肽免疫结合剂的药物组合物、包含这种环肽免疫结合剂与治疗共用试剂的组合物以及使用这种环肽免疫结合剂的治疗方法：
• Cyclic dinucleotide
  申请人：TAKEDA PHARMACEUTICAL COMPANY LIMITED

  公开号：US10980825B2

  公开（公告）日：2021-04-20

  The present disclosure provides a compound having a STING agonistic activity, which may be expected to be useful as an agent for the prophylaxis or treatment of STING-related diseases. The present disclosure relates to a compound represented by the formula (I): wherein each symbol is as defined in the description, or a salt thereof.

  本公开提供了一种具有 STING 激动活性的化合物，该化合物有望用作预防或治疗 STING 相关疾病的药物。 本公开涉及一种由式（I）表示的化合物： 其中各符号如描述中所定义，或其盐类。