2-[(5-Fluoropyridin-2-yl)oxy]ethanamine | 1247202-90-9

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-[(5-Fluoropyridin-2-yl)oxy]ethanamine
• 英文别名: 2-((5-Fluoropyridin-2-yl)oxy)ethan-1-amine；2-(5-fluoropyridin-2-yl)oxyethanamine
• CAS: 1247202-90-9
• 化学式: C₇H₉FN₂O
• 分子量: 156.16
• InChiKey: VTQGEXCRGJRXET-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  11
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  48.1
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Novel Benzyl Sulfonamide Derivatives Useful As MOGAT-2 Inhibitors
  申请人：Eli Lilly and Company

  公开号：US20130197039A1

  公开（公告）日：2013-08-01

  The present invention provides compounds of Formula below: and analogues thereof where the various substituent groups, R1, R2, R3, R4, R5 A, and X are described herein; or a pharmaceutical salt thereof; a method of treating a condition such as hypertriglyceridemia and a process for preparing the compounds.

  本发明提供以下式的化合物及其类似物，其中各种取代基团R1、R2、R3、R4、R5、A和X如本文所述；或其药用盐；一种治疗高甘油三酯血症等疾病的方法；以及制备这些化合物的方法。
• Compounds for treating disorders sensitive to serotoninergic regulation controlled by the 5-HT1A receptors
  申请人：NEUROLIXIS

  公开号：US10562853B2

  公开（公告）日：2020-02-18

  The invention concerns compounds that possess a high affinity at 5-HT1A receptors and an agonist efficacy, as measured by Emax values from a cellular activation assay, that is higher than that of the compounds described in prior art. The capacity of the compounds of the invention to activate an effector protein complex is higher than that the most efficacious agonist described in prior art. Compounds of the invention also exhibit an exceptionally high selectivity (Ki ratio greater than 1000-fold) with respect, in particular, to dopamine D2 receptors and adrenergic receptors of the alpha1 subtype. This selectivity which constitutes a great advantage since it means that the compounds will avoid inducing (central and peripheral) effects associated with activating or inhibiting such receptors.

  本发明所涉及的化合物对 5-HT1A 受体具有高亲和力，并且根据细胞活化实验的 Emax 值衡量，其激动剂功效高于现有技术中所述的化合物。本发明化合物激活效应蛋白复合物的能力高于现有技术中最有效的激动剂。本发明的化合物还具有极高的选择性（Ki 比值大于 1000 倍），特别是对多巴胺 D2 受体和α1 亚型肾上腺素能受体。这种选择性具有很大的优势，因为它意味着本发明的化合物可以避免引起与激活或抑制这些受体相关的（中枢和外周）效应。
• BENZYL SULFONAMIDE DERIVATIVES USEFUL AS MOGAT-2 INHIBITORS
  申请人：Eli Lilly and Company

  公开号：EP2809651B1

  公开（公告）日：2016-06-29
• COMPOUNDS FOR TREATING DISORDERS SENSITIVE TO SEROTONINERGIC REGULATION CONTROLLED BY THE 5-HT1A RECEPTORS
  申请人：Neurolixis

  公开号：EP3475268A1

  公开（公告）日：2019-05-01
• US8575352B2
  申请人：——

  公开号：US8575352B2

  公开（公告）日：2013-11-05