(2S)-2,6-diamino-5-hydroxyhexanoic acid;hydrochloride

• 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: (2S)-2,6-diamino-5-hydroxyhexanoic acid;hydrochloride
• 化学式: C6H15ClN2O3
• 分子量: 198.65
• InChiKey: MJXVOTKVFFAZQJ-YKXIHYLHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -1.08
• 重原子数：
  12
• 可旋转键数：
  5
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.83
• 拓扑面积：
  110
• 氢给体数：
  5
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  碳酸氢钠 、 (2S)-2,6-diamino-5-hydroxyhexanoic acid;hydrochloride 、 N-benzyloxycarbonyloxy-5-norbornene-2,3-dicarboximide 在 乙腈 、 盐酸 、 乙酸乙酯 、 sodium hydroxide 、 50W-2X 、 吡啶 、 水 作用下， 以 水 、 乙腈 为溶剂， 反应 2.25h， 以to give III (1.24 g, 0.0042 mol, 33%)的产率得到N-Benzyloxycarbonyl-5-hydroxylysine
  参考文献：
  名称：

  N-carboxymethyl substituted lysyl and .alpha.-(.epsilon.-aminoalkyl)

  摘要：

  分子式为：##STR1##其中R.sup.2为--(CH.sub.2).sub.k --X--(CH.sub.2).sub.j --NHR.sup.3；其中k为0至3，j为1或2；X为F或OH；R.sup.3为氢；低碳基或低芳基烷基，可被羟基，羧基，氨基甲酰或羧基烷氧基取代；或酰基；以及其药学上可接受的盐；是抑制血管紧张素I转化酶的抑制剂，可用作降压剂。

  公开号：

  US04602002A1

文献信息

• [EN] INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND/OR TRYPTOPHAN 2,3-DIOXYGENASE<br/>[FR] INHIBTEURS DE L'INDOLÉAMINE 2,3-DIOXYGÉNASE ET/OU DU TRYPTOPHANE DIOXYGÉNASE
  申请人：IDORSIA PHARMACEUTICALS LTD

  公开号：WO2019034725A1

  公开（公告）日：2019-02-21

  The present invention relates to compounds of Formula (I) inhibiting indoleamine 2,3-dioxygenase (IDO) and/or tryptophan 2,3-dioxygenase (TDO) enzymes. Further, their synthesis and their use as medicaments in inter alia cancer is disclosed.

  这项发明涉及抑制吲哚胺 2,3-二氧化酶（IDO）和/或色氨酸 2,3-二氧化酶（TDO）酶的化合物（I）的公式。此外，还披露了它们的合成以及它们在包括癌症在内的药物中的用途。
• Therapeutic and diagnostic domain 1 beta2GP1 polypeptides and methods of using same
  申请人：Marquis M. David

  公开号：US20050004351A1

  公开（公告）日：2005-01-06

  The present invention provides domain 1 β 2 GPI polypeptides, polynucleotides encoding these polypeptides, mimetics of these polypeptides, and methods using domain 1 β 2 GPI polypeptides and mimetics. Domain 1 of β 2 GPI has been shown to bind to anti-cardiolipin (β 2 GPI-dependent antiphospholipid) antibodies, which are associated with several pathologies, such as thrombosis and fetal loss. The domain 1 β 2 GPI polypeptides may be used to detect β 2 GPI-dependent antiphospholipid antibodies in a sample. The invention further provides methods of inducing tolerance using these domain 1 β 2 GPI polypeptides.

  本发明提供了1区β2GPI多肽、编码这些多肽的多核苷酸、这些多肽的类似物以及使用1区β2GPI多肽和类似物的方法。已经证明β2GPI的1区能够结合抗心磷脂（β2GPI依赖性抗磷脂抗体），这些抗体与多种病理学如血栓形成和胎儿流产有关。1区β2GPI多肽可用于检测样品中的β2GPI依赖性抗磷脂抗体。本发明还提供了使用这些1区β2GPI多肽诱导耐受的方法。
• LYSINE COMPOUNDS AND THEIR USE IN SITE- AND CHEMOSELECTIVE MODIFICATION OF PEPTIDES AND PROTEINS
  申请人：Ovaa Huib

  公开号：US20120135913A1

  公开（公告）日：2012-05-31

  The present invention concerns new thiolysine and selenolysine compounds that can be used as building blocks for peptides and proteins, providing ligation handles for site- and chemoselective modification of said peptides and proteins. In particular, the invention provides. In particular, the invention provides (the use of) the compounds 5-thiolysine (also referred to as δ-thiolysine); 4-thiolysine (also referred to as γ-thiolysine); 5-selenolysine (also referred to as δ-selenolysine) and 4-selenolysine (also referred to as γ-selenolysine). The positioning of the thiol or selenol group at the respective carbon atom allows for a very efficient intramolecular transfer reaction to take place after conjugation with a selected ligand, and the thiol or selenol group may subsequently be removed using reported procedures, thereby restoring the native lysine structure, or be used as an additional conjugation handle. The methodology is fast and gives well-defined material.

  本发明涉及新的巯基赖氨酸和硒基赖氨酸化合物，可用作肽和蛋白质的构建块，为所述肽和蛋白质的位点和化学选择性修饰提供连接手柄。具体而言，本发明提供了化合物5-巯基赖氨酸（也称为δ-巯基赖氨酸）；4-巯基赖氨酸（也称为γ-巯基赖氨酸）；5-硒基赖氨酸（也称为δ-硒基赖氨酸）和4-硒基赖氨酸（也称为γ-硒基赖氨酸）的使用。将巯基或硒基团位于相应的碳原子上，可在与所选配体共轭后发生非常高效的分子内转移反应，巯基或硒基团随后可使用已知的程序去除，从而恢复天然的赖氨酸结构，或用作额外的连接手柄。该方法快速且给出明确的材料。
• Method for Producing cis-5-hydroxy-2-piperidinecarboxylic Acid Derivative, and Method for Purifying cis-5-hydroxy-2-piperidinecarboxylic Acid
  申请人：API CORPORATION

  公开号：US20150239906A1

  公开（公告）日：2015-08-27

  The present invention aims to provide a method for purifying cis-5-hydroxy-2-piperidinecarboxylic acid with high purity, and a method for producing its derivative. The present invention provides a method for producing a cis-5-hydroxy-2-piperidinecarboxylic acid derivative, which method comprises a step of converting cis-5-hydroxy-2-piperidinecarboxylic acid into a compound(s) of Formula (1) and/or Formula (2) (wherein R 1 represents a protective group for an amino group, and R2 represents a C 1 -C 6 alkyl group), and a method for purifying cis-5-hydroxy-2-piperidinecarboxylic acid.

  本发明旨在提供一种高纯度纯化顺式-5-羟基-2-哌啶羧酸的方法，以及其衍生物的生产方法。本发明提供了一种生产顺式-5-羟基-2-哌啶羧酸衍生物的方法，该方法包括将顺式-5-羟基-2-哌啶羧酸转化为式（1）和/或式（2）化合物的步骤（其中R1代表氨基的保护基，R2代表C1-C6烷基），以及一种纯化顺式-5-羟基-2-哌啶羧酸的方法。
• Peptide-mediated delivery of immunoglobulins across the blood-brain barrier
  申请人：Mayo Foundation for Medical Education and Research

  公开号：US10072065B2

  公开（公告）日：2018-09-11

  Provided herein are materials and methods for delivering immunoglobulins (e.g. therapeutic immunoglobulins) across the blood-brain barrier.

  本文提供了穿过血脑屏障递送免疫球蛋白（如治疗性免疫球蛋白）的材料和方法。