2-(Pyridazin-3-yloxy)ethylamine | 403860-23-1

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 2-(Pyridazin-3-yloxy)ethylamine
• 英文别名: 2-(3-pyridazinyloxy)ethanamine；2-pyridazin-3-yloxyethanamine
• CAS: 403860-23-1
• 化学式: C₆H₉N₃O
• 分子量: 139.157
• InChiKey: YCBSRVPSWOLVMV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  10
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  61
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  3,6-二氯哒嗪 、 C.I.酸性橙108 在 5%-palladium/activated carbon sodium hydride 、 盐酸 、 氢气 作用下， 以 xylene 为溶剂， 反应 15.33h， 生成 2-(Pyridazin-3-yloxy)ethylamine
  参考文献：
  名称：

  Bicyclic pyrrolyl amides as glucogen phosphorylase inhibitors

  摘要：

  杂环酰胺衍生物的化学式（I）：其中—X-Y-Z-选择自—S—CR4═CR5—，—CR4═CR5—S—，—O—CR4═CR5—，—CR4═CR5—O—，—N═CR4—S—，—S—CR4═N—，—NR6—CR4═CR5—和—CR4═CR5—NR6—；或其药学上可接受的盐或体内可水解酯；（附带条件）；具有糖原磷酸化酶抑制活性，因此在治疗与糖原磷酸化酶活性增加相关的疾病状态中具有价值。描述了制备所述杂环酰胺衍生物和含有它们的药物组合物的方法。

  公开号：

  US20030232875A1

文献信息

• Novel Indoline Compounds
  申请人：LEBRETON Luc

  公开号：US20080119465A1

  公开（公告）日：2008-05-22

  Sulfonylindoline compounds of formula I, wherein R1 through R4, Y and Z have defined meanings, a process for preparation of such compounds, and the use as pharmaceutically active substances, particularly for the treatment or inhibition of neurodegeneration, cardiovascular disease, inflammatory disease, hypercholesterolemia, dyslipidemia, obesity or diabetes.

  公式I的磺胺基吲哚化合物，其中R1至R4，Y和Z具有定义的含义，一种制备这种化合物的过程，以及用作药用活性物质，特别用于治疗或抑制神经退行性疾病、心血管疾病、炎症性疾病、高胆固醇血症、血脂异常、肥胖或糖尿病。
• COMPOUNDS FOR TREATING DISORDERS SENSITIVE TO SEROTONINERGIC REGULATION CONTROLLED BY THE 5-HT1A RECEPTORS
  申请人：Neurolixis

  公开号：EP3260452A1

  公开（公告）日：2017-12-27

  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。
• 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。
• BICYCLIC PYRROLYL AMIDES AS GLUCOGEN PHOSPHORYLASE INHIBITORS
  申请人：AstraZeneca AB

  公开号：EP1317459A1

  公开（公告）日：2003-06-11
• NOUVEAUX COMPOSES DE L'INDOLINE
  申请人：LABORATOIRES FOURNIER S.A.

  公开号：EP1885695A2

  公开（公告）日：2008-02-13