1-(2-吡啶基)-1,2-乙二胺 | 115464-35-2

• 分子结构分类: 有机化合物 - 有机氮化合物
• 中文名称: 1-(2-吡啶基)-1,2-乙二胺
• 英文名称: 2-(1,2-diaminoethyl)pyridine
• 英文别名: 1-(Pyridin-2-yl)ethane-1,2-diamine；1-pyridin-2-ylethane-1,2-diamine
• CAS: 115464-35-2
• 化学式: C₇H₁₁N₃
• 分子量: 137.184
• InChiKey: COSJCAMRRQYRRD-UHFFFAOYSA-N

物化性质

• 沸点：
  277.9±25.0 °C(Predicted)
• 密度：
  1?+-.0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -1.2
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  64.9
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  1-(2-吡啶基)-1,2-乙二胺 、 Boc-L-Phe-L-His-(3S,4S)-Sta-L-Leu-OCH3 生成 tert-butyl N-[(2S)-1-[[(2S)-1-[[(3S,4S)-1-[[(2S)-1-[(2-amino-2-pyridin-2-ylethyl)amino]-4-methyl-1-oxopentan-2-yl]amino]-3-hydroxy-6-methyl-1-oxoheptan-4-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]carbamate
  参考文献：
  名称：

  Renin inhibitors containing hydrophilic groups. Tetrapeptides with enhanced aqueous solubility and nanomolar potency

  摘要：

  Nineteen tetrapeptides containing statine (Sta) and 4-amino-5-cyclohexyl-3-hydroxypentanoic acid (ACHPA) were prepared. Solubility measurements of these compounds were carried out in H2O and in pH 7.4 phosphate buffer solution, and their partition coefficients were determined in a 1:1 1-octanol/sodium phosphate-citric acid buffer system. The tetrapeptides were tested in vitro for their ability to inhibit porcine, canine, and human plasma renins. Four compounds, 6, 12, 14, and 20, were potent inhibitors against all renins tested (IC50 = 10(-9) M). Compound 12 was administered orally to dogs and substantially inhibited plasma renin activity for up to 5 h. The addition of polar groups to the C-terminus of Sta- and ACHPA-containing tetrapeptides renders them soluble in aqueous milieu and provides a valuable tool with which to examine the role of the renin-angiotensin system in physiological and pathological circumstances.

  DOI：

  10.1021/jm00118a009
• 作为产物：
  描述：

  2-氯吡啶 、 乙二胺 在 sodium hydroxide 、 氯仿 、 Sodium sulfate-III 作用下， 反应 16.0h， 生成 1-(2-吡啶基)-1,2-乙二胺
  参考文献：
  名称：

  Aminoalkyl-pyrazinones and-pyridones as thrombin inhibitors

  摘要：

  本发明涉及式(I)的化合物，其中A，B，X，R1，R2，G，R3，D和E的含义如描述和权利要求中所述。所述化合物可用作凝血剂。本发明还涉及其制备和用作药物的用途。

  公开号：

  US20070099927A1

文献信息

• [EN] BENZOPYRANE AND IMIDAZOLE DERIVATIVES USEFUL FOR THE STABILIZATION OF AMYLOIDOGENIC IMMUNOGLOBULIN LIGHT CHAINS<br/>[FR] DÉRIVÉS DE STABILISATION DE BENZOPYRANE ET D'IMIDAZOLE UTILISÉS POUR LA STABILISATION DE CHAÎNES LÉGÈRES D'IMMUNOGLOBULINES AMYLOÏDOGÉNIQUES
  申请人：SCRIPPS RESEARCH INST

  公开号：WO2020205683A1

  公开（公告）日：2020-10-08

  In immunoglobulin light chain amyloidosis (AL), the unique antibody light chain (LC) protein that is secreted by monoclonal plasma cells in each patient misfolds and/or aggregates, a process leading to organ degeneration. For treating AL patients, such as those with substantial cardiac involvement who have difficulty tolerating existing chemotherapy regimens, provided herein are small molecule compounds of Formula Ia, Formula Ib, and Formula II that are kinetic stabilizers of the native dimeric structure of full-length LCs, which compounds can slow or stop the amyloidogenicity cascade at its origin.

  在免疫球蛋白轻链淀粉样变性（AL）中，每位患者体内由单克隆浆细胞分泌的独特抗体轻链（LC）蛋白会错误折叠和/或聚集，导致器官退化的过程。为了治疗AL患者，例如那些存在严重心脏受累且难以耐受现有化疗方案的患者，本文提供了化学式Ia、化学式Ib和化学式II的小分子化合物，这些化合物是全长LC的动力学稳定剂，可以减缓或停止淀粉样生成性级联反应的起源。
• [EN] BENZOIMIDAZOLE DERIVATIVES AND GLYCOGEN SYNTHASE KINASE-3 BETA INHIBITORS CONTAINING THE SAME<br/>[FR] DÉRIVÉS DE BENZIMIDAZOLE ET INHIBITEURS DE GLYCOGÈNE SYNTHASE KINASE-3-BÊTA CONTENANT CEUX-CI
  申请人：ONCOTHERAPY SCIENCE INC

  公开号：WO2010014794A1

  公开（公告）日：2010-02-04

  Benzoimidazole Derivatives are provided. The compounds of the present invention are useful for Glycogen Synthase Kinase-3 Beta Inhibitors.

  苯并咪唑衍生物已提供。本发明的化合物对于糖原合成酶激酶-3β抑制剂是有用的。
• Ligands of Integrin Receptors
  申请人：Geneste Herve

  公开号：US20080221082A1

  公开（公告）日：2008-09-11

  The invention relates to the use of cyclic compounds as ligands of integrin receptors, in particular as ligands of the α V β 3 integrin receptor, the novel compounds themselves, their use, and pharmaceutical preparations comprising these compounds.

  本发明涉及将环状化合物用作整合素受体的配体，特别是用作αVβ3整合素受体的配体，以及这些新化合物本身、它们的用途和包含这些化合物的制药制剂。
• Substituted 2H-[1,2,4]Triazolo[4,3-A]Pyrazines as Gsk-3 Inhibitors
  申请人：Benbow William John

  公开号：US20070249612A1

  公开（公告）日：2007-10-25

  The invention relates to compounds of formula (I) prodrugs thereof, and the pharmaceutically acceptable salts of the compounds and prodrugs, wherein R a , R b , R 1 and R 2 are as defined herein; pharmaceutical compositions thereof; and uses thereof.

  本发明涉及公式(I)化合物及其前药、所述化合物和前药的药学上可接受的盐，其中Ra、Rb、R1和R2如本文所定义；药物组合物；以及其用途。
• Benzoimidazole Derivatives and Glycogen Synthase Kinase-3 Beta Inhibitors Containing the Same
  申请人：Ohtani Mitsuaki

  公开号：US20110190351A1

  公开（公告）日：2011-08-04

  Benzoimidazole Derivatives are provided. The compounds of the present invention are useful for Glycogen Synthase Kinase-3 Beta Inhibitors.

  本发明提供苯并咪唑衍生物。本发明的化合物可用作糖原合成酶激酶-3β抑制剂。