N-(4-甲基-2-吡啶基)-1,2-乙二胺 | 526184-60-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 中文名称: N-(4-甲基-2-吡啶基)-1,2-乙二胺
• 英文名称: 2-(2-aminoethylamino)-4-methylpyridine
• 英文别名: N'-(4-methyl-2-pyridyl)ethane-1,2-diamine；N-(4-methylpyridin-2-yl)ethane-1,2-diamine；N'-(4-methylpyridin-2-yl)ethane-1,2-diamine
• CAS: 526184-60-1
• 化学式: C₈H₁₃N₃
• 分子量: 151.211
• InChiKey: POLFZJFTWICAOV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  11
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  50.9
• 氢给体数：
  2
• 氢受体数：
  3

安全信息

• 海关编码：
  2933399090

反应信息

• 作为反应物：
  描述：

  N-(4-甲基-2-吡啶基)-1,2-乙二胺 在 sodium hydride 、 三乙胺 、 lithium hexamethyldisilazane 作用下， 以 四氢呋喃 、 二氯甲烷 、 mineral oil 为溶剂， 反应 36.17h， 生成 tert-butyl N-(4-methyl-2-pyridyl)-N-[2-[[(E)-3,3,3-trifluoroprop-1-enyl]sulfonylamino]ethyl]carbamate
  参考文献：
  名称：

  [EN] HETEROARYL COMPOUNDS WITH A-CYCLIC BRIDGING UNIT
  [FR] COMPOSÉS HÉTÉROARYLES À UNITÉ DE PONTAGE CYCLIQUE

  摘要：

  这项发明涉及某些杂环芳基化合物，可用作药物，更具体地用作治疗动物的药物。该药物可用于治疗寄生虫感染，如蠕虫感染，以及由这些感染引起的寄生虫病的治疗。该发明还涉及利用这些化合物制备药物和治疗方法，包括将这些化合物给需要治疗的动物。该发明还涉及包含这些化合物的药物组合物和试剂盒。

  公开号：

  WO2013144179A1
• 作为产物：
  描述：

  2-氯-4-甲基吡啶 、 乙二胺 反应 18.0h， 生成 N-(4-甲基-2-吡啶基)-1,2-乙二胺
  参考文献：
  名称：

  Discovery of Aminoglycoside Mimetics by NMR-Based Screening of Escherichia coli A-site RNA

  摘要：

  A method is described for the NMR-based screening for the discovery of aminoglycoside mimetics that bind to Escherichia coli A-site RNA. Although aminoglycosides are clinically useful, they exhibit high nephrotoxicity and ototoxicity, and their overuse has led to the development of resistance to important microbial pathogens. To identify a new series of aminoglycoside mimetics that could potentially overcome the problems associated with toxicities and resistance development observed with the aminoglycosides, we have prepared large quantities of E. coli 16 S A-site RNA and conducted an NMR-based screening of our compound library in search for small-molecule RNA binders against this RNA target. From these studies, several classes of compounds were identified as initial hits with binding affinities in the range of 70 muM to 3 mM. Lead optimization through synthetic modifications of these initial hits led to the discovery of several small-molecule aminoglycoside mimetics that are structurally very different from the known aminoglycosides. Structural models of the A-site RNA/ligand complexes were prepared and compared to the three-dimensional structures of the RNA/aminoglycoside complexes.

  DOI：

  10.1021/ja021354o

文献信息

• [EN] PRMT5 INHIBITORS CONTAINING A DIHYDRO- OR TETRAHYDROISOQUINOLINE AND USES THEREOF<br/>[FR] INHIBITEURS DE LA PRMT5 CONTENANT UNE DIHYDRO- OU TÉTRAHYDRO-ISOQUINOLÉINE ET LEURS UTILISATIONS
  申请人：EPIZYME INC

  公开号：WO2014100730A1

  公开（公告）日：2014-06-26

  Described herein are compounds of Formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5- mediated disorders are also described.

  本文描述了式（A）的化合物，其药学上可接受的盐以及药物组合物。本发明的化合物对抑制PRMT5活性是有用的。还描述了利用这些化合物治疗PRMT5介导的疾病的方法。
• [EN] COMPOUNDS AND USES THEREOF<br/>[FR] COMPOSÉS ET LEURS UTILISATIONS
  申请人：FOGHORN THERAPEUTICS INC

  公开号：WO2019152437A1

  公开（公告）日：2019-08-08

  The present disclosure features compounds useful for the treatment of BAF complex-related disorders.

  本公开涉及用于治疗BAF复合物相关疾病的化合物。
• [EN] PRMT5 INHIBITORS AND USES THEREOF<br/>[FR] INHIBITEURS DE PRMT5 ET LEURS UTILISATIONS
  申请人：EPIZYME INC

  公开号：WO2014100734A1

  公开（公告）日：2014-06-26

  Described herein are compounds of formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.

  本文描述了式（A）的化合物，其药学上可接受的盐以及药物组成物。本发明的化合物对抑制PRMT5活性是有用的。还描述了利用这些化合物治疗PRMT5介导的疾病的方法。
• PRMT5 INHIBITORS AND USES THEREOF
  申请人：Epizyme, Inc.

  公开号：US20140329794A1

  公开（公告）日：2014-11-06

  Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.

  本文描述了公式（I）的化合物，其药学上可接受的盐以及其制药组合物。本发明的化合物可用于抑制PRMT5活性。还描述了使用这些化合物治疗PRMT5介导的疾病的方法。
• HETEROARYL COMPOUNDS WITH A-CYCLIC BRIDGING UNIT
  申请人：Intervet Inc.

  公开号：US20150057279A1

  公开（公告）日：2015-02-26

  This invention relates to certain heteroaryl compounds which may be used as medicaments, more specifically as medicaments for treating animals. The medicament can be used for the treatment of parasitic infections such as helminth infections and the treatment of parasitosis caused by such infections. This invention also relates to uses of the compounds to make medicaments and treatments comprising the administration of the compounds to animals in need of the treatments. This invention also relates to pharmaceutical compositions and kits comprising the compounds.

  本发明涉及某些杂环芳基化合物，可用作药物，更具体地用作治疗动物的药物。该药物可用于治疗寄生虫感染，如蠕虫感染和由此类感染引起的寄生虫病的治疗。本发明还涉及使用该化合物制备药物和治疗，包括将该化合物给需要治疗的动物。本发明还涉及包含该化合物的制药组合物和试剂盒。