1-[3-(morpholin-4-yl)pyridin-4-yl]methanamine | 1149585-84-1

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 1-[3-(morpholin-4-yl)pyridin-4-yl]methanamine
• 英文别名: (3-Morpholin-4-ylpyridin-4-yl)methanamine
• CAS: 1149585-84-1
• 化学式: C₁₀H₁₅N₃O
• 分子量: 193.249
• InChiKey: RAKFRLAUASGAIS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.5
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  51.4
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-[3-(morpholin-4-yl)pyridin-4-yl]methanamine 、 6-(4-chlorophenyl)-pyrazine-2-carbonyl chloride 在 三乙胺 作用下， 以 二氯甲烷 为溶剂， 反应 3.0h， 以60%的产率得到N-((3-morpholinopyridin-4-yl)methyl)-6-(4-chlorophenyl)-pyrazine-2-carboxamide
  参考文献：
  名称：

  Discovery and biological evaluation of potent, selective, orally bioavailable, pyrazine-based blockers of the Nav1.8 sodium channel with efficacy in a model of neuropathic pain

  摘要：

  Na(v)1.8 (also known as PN3) is a tetrodotoxin-resistant (TTx-r) voltage-gated sodium channel (VGSC) that is highly expressed on small diameter sensory neurons. It has been implicated in the pathophysiology of inflammatory and neuropathic pain, and we envisioned that selective blockade of Na(v)1.8 would be analgesic, while reducing adverse events typically associated with non-selective VGSC blocking therapeutic agents. Herein, we describe the preparation and characterization of a series of 6-aryl-2-pyrazinecarboxamides, which are potent blockers of the human Na(v)1.8 channel and also block TTx-r sodium currents in rat dorsal root ganglia (DRG) neurons. Selected derivatives display selectivity versus human Na(v)1.2. We further demonstrate that an example from this series is orally bioavailable and produces antinociceptive activity in vivo in a rodent model of neuropathic pain following oral administration. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmc.2010.09.057
• 作为产物：
  描述：

  3-chloro-5-(morpholin-4-yl)pyridin-4-ylcarbonitrile 在 palladium 10% on activated carbon 氢气 作用下， 以 甲醇 为溶剂， 反应 6.0h， 以99%的产率得到1-[3-(morpholin-4-yl)pyridin-4-yl]methanamine
  参考文献：
  名称：

  [EN] PYRIDAZINONE DERIVATIVES AND USE THEREOF AS P2X7 RECEPTOR INHIBITORS
  [FR] DÉRIVÉS DE PYRIDAZINONE ET LEUR UTILISATION COMME INHIBITEURS DU RÉCEPTEUR P2X7

  摘要：

  翻译结果为：新型的哒嗪酮化合物，其化学公式为(I)，能够抑制嘌呤能P2X7受体，并对预防、治疗和改善炎症性和免疫性疾病有益。

  公开号：

  WO2009057827A1

文献信息

• PYRIDAZINONE COMPOUNDS AND P2X7 RECEPTOR INHIBITORS
  申请人：Shigeta Yukihiro

  公开号：US20100286390A1

  公开（公告）日：2010-11-11

  Novel pyridazinone compounds of formula (I), which inhibit the purinergic P2X7 receptor and are useful for prevention, therapy and improvement of inflammatory and immunological diseases.

  化合物(I)是一种新型的吡啶并嗪酮化合物，可以抑制嘌呤能P2X7受体，因此可用于预防、治疗和改善炎症和免疫性疾病。
• Ferroportin inhibitors
  申请人：Vifor (International) AG

  公开号：US10364239B2

  公开（公告）日：2019-07-30

  The invention relates to novel compounds of the general formula (A-I), with Het-2 being an optionally substituted bicyclic heteroaryl of the formula (AA) pharmaceutical compositions comprising them and the use thereof as medicaments, in particular for the use as ferroportin inhibitors, more particularly for the use in the prophylaxis and/or treatment of diseases caused by a lack of hepcidin or iron metabolism disorders, such as particularly iron overload states such as in particular thalassemia and hemochromatosis.

  本发明涉及通式(A-I)的新型化合物，其中Het-2为通式(AA)的任选取代的双环杂芳基。本发明涉及由这些化合物组成的药物组合物及其作为药物的用途，特别是作为铁皮质素抑制剂的用途，尤其是用于预防和/或治疗由缺乏铁皮质素或铁代谢紊乱引起的疾病，如特别是铁过载状态，如地中海贫血症和血色病。
• PYRIDAZINONE DERIVATIVES AND USE THEREOF AS P2X7 RECEPTOR INHIBITORS
  申请人：Nissan Chemical Industries, Ltd.

  公开号：EP2203429A1

  公开（公告）日：2010-07-07
• FERROPORTIN INHIBITORS
  申请人：Vifor (International) AG

  公开号：EP3364967A2

  公开（公告）日：2018-08-29
• NOVEL FERROPORTIN INHIBITORS
  申请人：Vifor (International) AG

  公开号：EP3365339A1

  公开（公告）日：2018-08-29