N-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methylleucine

• 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-[(9H-fluoren-9-ylmethoxy)carbonyl]-N-methylleucine
• 英文别名: 2-[9H-fluoren-9-ylmethoxycarbonyl(methyl)amino]-4-methylpentanoic acid
• 化学式: C₂₂H₂₅NO₄
• 分子量: 367.4
• InChiKey: BUJQSIPFDWLNDC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  27
• 可旋转键数：
  7
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  66.8
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• [EN] ELONGATION FACTOR 1-ALPHA INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DU FACTEUR D'ALLONGEMENT 1-ALPHA ET LEURS UTILISATIONS
  申请人：UNIV CALIFORNIA

  公开号：WO2021158899A1

  公开（公告）日：2021-08-12

  Disclosed herein, inter alia, are compounds for inhibiting Elongation Factor 1-alpha and uses thereof.

  本公开的内容包括用于抑制Elongation Factor 1-alpha的化合物及其用途。
• METHOD FOR THE SYNTHESIS OF CYCLIC DEPSIPEPTIDES
  申请人：Bayer Animal Health GmbH

  公开号：EP3480195A1

  公开（公告）日：2019-05-08

  The present invention relates to a method for the synthesis of cyclic depsipeptides, in particular emodepside, involving specific carboxylic acid group protecting tags: TAG is preferably: wherein m is ≥ 15 to ≤ 25, p is ≥ 8 to ≤ 18 and q is ≥ 15 to ≤ 25.

  本发明涉及一种合成环状脱氢肽的方法，特别是合成emodepside的方法，涉及特定的羧酸保护标签。标签最好是：其中m为≥15至≤25，p为≥8至≤18，q为≥15至≤25。
• MACROCYCLIC COMPOUNDS FOR INHIBITION OF TUMOR NECROSIS FACTOR ALPHA
  申请人：Lee Jinbo

  公开号：US20100152099A1

  公开（公告）日：2010-06-17

  The invention provides macrocyclic compounds and methods for their synthesis and use. In particular, the invention provides macrocyclic compounds that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.

  该发明提供了大环化合物及其合成和使用方法。具体而言，该发明提供了调节肿瘤坏死因子α活性和/或用于治疗医学状况（如类风湿性关节炎、银屑病和哮喘）的大环化合物。
• CYCLIC PEPTIDE COMPOUND HAVING HIGH MEMBRANE PERMEABILITY, AND LIBRARY CONTAINING SAME
  申请人：Chugai Seiyaku Kabushiki Kaisha

  公开号：EP3636807A1

  公开（公告）日：2020-04-15

  The present inventors have found that when screening for cyclic peptide compounds that can specifically bind to a target molecule, the use of a library including cyclic peptide compounds having a long side chain in the cyclic portion can improve the hit rate for cyclic peptide compounds that can specifically bind to the target molecule. Meanwhile, the present inventors have found that tryptophan and tyrosine residues, which have conventionally been used in oral low molecular-weight pharmaceuticals and are amino acid residues having an indole skeleton or a hydroxyphenyl group, are not suitable for peptides intended to attain high membrane permeability.

  本发明人发现，在筛选能与目标分子特异性结合的环肽化合物时，使用包括环状部分具有长侧链的环肽化合物库，可以提高能与目标分子特异性结合的环肽化合物的命中率。同时，本发明者发现色氨酸和酪氨酸残基不适合用于旨在获得高膜渗透性的肽，这两种残基通常用于口服低分子量药物，是具有吲哚骨架或羟基苯基的氨基酸残基。
• Gelatinase inhibitors and use thereof
  申请人：Iproteos S.L

  公开号：US10414797B2

  公开（公告）日：2019-09-17

  New gelatinase inhibitors, processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy and/or prophylaxis of conditions wherein inhibition of gelatinases is useful such as epilepsy, schizophrenia, Alzheimer disease, autism (in particular associated to fragile X syndrome), mental retardation, mood disorders such as bipolar disorders, depression, vascular diseases such as ischemic stroke and atherosclerosis, inflammatory diseases such as multiple sclerosis, rheumatoid arthritis and inflammatory bowel disease, drug addiction, neuropathic pain, lung diseases such as asthma and chronic obstructive pulmonary disease, cancer and sepsis.

  新的明胶酶抑制剂、其制备工艺、包含它们的药物组合物，以及它们在治疗和/或预防明胶酶抑制剂有用的疾病中的用途，如癫痫、精神分裂症、阿尔茨海默病、自闭症（特别是与脆性X综合征有关的疾病）、精神发育迟滞、情绪障碍（如双相情感障碍）、抑郁症、血管疾病（如缺血性中风和动脉粥样硬化）、炎症性疾病（如多发性硬化症、类风湿关节炎）、情绪障碍，如躁郁症、抑郁症；血管疾病，如缺血性中风和动脉粥样硬化；炎症性疾病，如多发性硬化症、类风湿性关节炎和炎症性肠病；药物成瘾；神经性疼痛；肺部疾病，如哮喘和慢性阻塞性肺病；癌症和败血症。