(Z)-N²,Nω,Nω'-tris(tert-butoxycarbonyl)arginine

• 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: (Z)-N²,Nω,Nω'-tris(tert-butoxycarbonyl)arginine
• 英文别名: Boc-Arg(Boc)-OH；5-[bis[(2-methylpropan-2-yl)oxycarbonylamino]methylideneamino]-2-[(2-methylpropan-2-yl)oxycarbonylamino]pentanoic acid
• 化学式: C₂₁H₃₈N₄O₈
• 分子量: 474.555
• InChiKey: BGOFOVHACSQSIE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  33
• 可旋转键数：
  14
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.76
• 拓扑面积：
  165
• 氢给体数：
  4
• 氢受体数：
  9

反应信息

• 作为反应物：
  描述：

  (Z)-N²,Nω,Nω'-tris(tert-butoxycarbonyl)arginine 在 四氯化锡 作用下， 以 乙酸乙酯 为溶剂， 反应 3.0h， 以81%的产率得到N^α-Boc-arginine hydrochloride
  参考文献：
  名称：

  Total deprotection of N,N′-bis(tert-butoxycarbonyl)guanidines using SnCl4

  摘要：

  The total deprotection of N,N'-bis-Boc guanidines using SnCl4 proceeds smoothly in ethyl acetate at room temperature and leads to the easily isolable corresponding guanidinium chlorides. (C) 1997 Published by Elsevier Science Ltd.

  DOI：

  10.1016/s0040-4039(97)10148-4

文献信息

• [EN] CONJUGATE COMPOUNDS FOR THE DEGRADATION OF RAF<br/>[FR] COMPOSÉS CONJUGUÉS POUR LA DÉGRADATION DE RAF
  申请人：ZAMBONI CHEM SOLUTIONS INC

  公开号：WO2020168172A1

  公开（公告）日：2020-08-20

  The present disclosure provides, inter alia, RAF-Degrading Conjugate Compounds that are useful in the treatment of cancer and other RAF related diseases. Also provided are, pharmaceutical compositions, methods of treatment, and kits comprising a RAF-Degrading Conjugate Compound.

  本公开提供了用于治疗癌症和其他与RAF相关疾病的RAF降解共轭化合物。还提供了药物组合物、治疗方法和包含RAF降解共轭化合物的试剂盒。
• TOPICAL OCULAR DRUG DELIVERY
  申请人：The Regents of the University of Colorado, a body corporate

  公开号：US20130190324A1

  公开（公告）日：2013-07-25

  The present invention provides compositions and methods for increasing the delivery (i.e., bioavailability) of a compound to an ocular cell. Such compositions and methods can be used to treat an ocular clinical condition. Typically, increased bioavailability or delivery of the compound to ocular cells is achieved by utilizing a membrane transporter.

  本发明提供了增加化合物输送到眼细胞（即生物利用度）的组合物和方法。这些组合物和方法可用于治疗眼部临床疾病。通常，通过利用膜转运蛋白实现将化合物输送到眼细胞的生物利用度或输送量增加。
• [EN] MODULATION OF IMMUNE CELLS<br/>[FR] MODULATION DE CELLULES IMMUNITAIRES
  申请人：OCTAGON THERAPEUTICS INC

  公开号：WO2021155277A1

  公开（公告）日：2021-08-05

  Disclosed are immune cell-selective small molecule IMPDH inhibitor compounds and methods of their synthesis and use to treat proliferative disorders.

  本发明涉及免疫细胞选择性小分子IMPDH抑制剂化合物及其合成和用于治疗增殖性疾病的方法。
• BARETTIN AND DERIVATIVES THEREOF FOR MEDICAL USE, IN PARTICULAR FOR THE TREATMENT OF DISEASES RELATED TO OXIDATIVE STRESS OR INFLAMMATION, AND FOR PRESERVING OR WASHING ORGANS
  申请人：ABC Bioscience AS

  公开号：US20160039796A1

  公开（公告）日：2016-02-11

  The compounds of formula (I) herein include barettin and derivatives thereof, or any pharmaceutically acceptable salt thereof for use as a medicament. Further the compounds may be used for the treatment of diseases related to oxidative stress and the treatment of inflammatory diseases; for the cosmetic treatment of skin aging; in a solution for the preservation and/or washing of organs; and as a food and/or feed additive.

  公式（I）的化合物包括barettin及其衍生物，或任何医药上可接受的盐，用作药物。此外，这些化合物可用于治疗与氧化应激相关的疾病和炎症性疾病的治疗；用于皮肤老化的美容治疗；在溶液中用于器官的保存和/或清洗；以及作为食品和/或饲料添加剂。
• Discovery of Norbornene as a Novel Hydrophobic Tag Applied in Protein Degradation
  作者：Shaowen Xie、Feiyan Zhan、Jingjie Zhu、Yuan Sun、Huajian Zhu、Jie Liu、Jian Chen、Zheying Zhu、Dong‐Hua Yang、Zhe‐Sheng Chen、Hong Yao、Jinyi Xu、Shengtao Xu

  DOI：10.1002/anie.202217246

  日期：2023.3.20

  A novel norbornene-based hydrophobic tag was developed that expands the clinical potential of targeted protein degradation technologies. The degrader Hyt-9, which was obtained by connecting an ALK ligand with norbornene, exhibited potent antiproliferative and degradative activities in vitro and in vivo. Furthermore, norbornene could be used to degrade EZH2 when tagged with the EZH2 inhibitor tazemetostat

  开发了一种新型的基于降冰片烯的疏水标签，扩大了靶向蛋白质降解技术的临床潜力。通过连接 ALK 配体和降冰片烯获得的降解剂Hyt-9在体外和体内表现出有效的抗增殖和降解活性。此外，当在降解剂Hyt-13中标记 EZH2 抑制剂他泽美司他时，降冰片烯可用于降解 EZH2 。