5-methoxy-2-morpholin-4-yl-pyridin-4-ylamine | 848579-82-8

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 5-methoxy-2-morpholin-4-yl-pyridin-4-ylamine
• 英文别名: 5-methoxy-2-morpholin-4-ylpyridin-4-amine
• CAS: 848579-82-8
• 化学式: C₁₀H₁₅N₃O₂
• 分子量: 209.248
• InChiKey: DZWMLVOTHCAMFI-UHFFFAOYSA-N

物化性质

• 沸点：
  446.3±45.0 °C(Predicted)
• 密度：
  1.214±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.2
• 重原子数：
  15
• 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：
  60.6
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  5-methoxy-2-morpholin-4-yl-pyridin-4-ylamine 、 苯甲酰基异硫氰酸酯 以 丙酮 为溶剂， 反应 1.5h， 以66%的产率得到1-benzoyl-3-(5-methoxy-2-morpholin-4-yl-pyridin-4-yl)-thiourea
  参考文献：
  名称：

  Thiazolopyridine

  摘要：

  本发明涉及式I的化合物，其中R1和R2如下所述。这些化合物对A2A受体具有高亲和力，并对A1和A3受体具有良好的选择性。这些化合物在治疗阿尔茨海默病、抑郁症、帕金森病和注意力缺陷多动障碍等方面具有用途。

  公开号：

  US20050065151A1
• 作为产物：
  描述：

  甲醇 、 5-iodo-2-morpholin-4-yl-pyridin-4-ylamine 在 copper(l) iodide 、 1,10-菲罗啉 caesium carbonate 作用下， 反应 0.5h， 以50%的产率得到5-methoxy-2-morpholin-4-yl-pyridin-4-ylamine
  参考文献：
  名称：

  Thiazolopyridine

  摘要：

  本发明涉及式I的化合物，其中R1和R2如下所述。这些化合物对A2A受体具有高亲和力，并对A1和A3受体具有良好的选择性。这些化合物在治疗阿尔茨海默病、抑郁症、帕金森病和注意力缺陷多动障碍等方面具有用途。

  公开号：

  US20050065151A1

文献信息

• THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS
  申请人：F. HOFFMANN-LA ROCHE AG

  公开号：EP1670805A1

  公开（公告）日：2006-06-21
• US7273865B2
  申请人：——

  公开号：US7273865B2

  公开（公告）日：2007-09-25
• [EN] THIAZOLOPYRIDINE DERIVATIVES AS ADENOSINE RECEPTOR LIGANDS<br/>[FR] DERIVES DE THIAZOLOPYRIDINE EN TANT QUE LIGANDS DU RECEPTEUR D'ADENOSINE
  申请人：HOFFMANN LA ROCHE

  公开号：WO2005028484A1

  公开（公告）日：2005-03-31

  The present invention relates to compounds of the general formula (I) wherein R1 is morpholin-4-yl, phenyl or tetrahydropyran-4-yl; R2 is -(CH2)n-aryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of halogen, lower alkoxy, lower alkyl, -(CH2)n NR’R', -0 (CH2)n-O -lower alkyl, or -(CH2)n-heterocyclyl, or is heteroaryl, unsubstituted or substituted by one or more substituents, selected from the group consisting of lower alkyl, lower alkoxy, -(CH2)n NR'R', -(CH2)n-heterocyclyl, which is optionally substituted by hydroxy or lower alkoxy, or is -(CH2)n-heterocyclyl, optionally substituted by one or more substituents selected from the group consisting of -(CH2)n,-OH, -(CH2)n-O-lower alkyl or lower alkyl, or is -(CH2)n-cycloalkyl, or is - (CH2)n,-O -lower alkyl, or is NR'R’’, or is benzo[1,3]dioxole, 2-methyl-l-oxo-2,8-diaza-spiro[4,5] decane, 2-oxa-5-aza­bicyclo [2.2.1]heptane or I-oxa-8-aza-spiro[4.5]decane; R',R' are independently from each other lower alkyl, - (CH2)n ,-O -lower alkyl or cycloalkyl, optionally substituted by hydroxy; n is 0, 1 or 2; and to pharmaceutically acceptable acid addition salts thereof. These compounds may be used in the control or prevention of illnesses based on the modulation of the adenosine system, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, neuroprotection, schizophrenia, anxiety, pain, respiration deficits, depression, drug addiction, such as amphetamine, cocaine, opioids, ethanol, nicotine, cannabinoids, or against asthma, allergic responses, hypoxia, ischaernia, seizure and substance abuse. Furthermore, compounds of the present invention may be useful as sedatives, muscle relaxants, antipsychotics, antiepileptics, anticonvulsants and cardiaprotective agents for disorders such as coronary artery disease and heart failure. The most preferred indications in accordance with the present invention are those which include disorders of the central nervous system, for example the treatment or prevention of Alzheimer's disease, certain depressive disorders, drug addiction, neuroprotection and Parkinson's disease as well as ADHD.
• Thiazolopyridine
  申请人：Norcross David Roger

  公开号：US20050065151A1

  公开（公告）日：2005-03-24

  The present invention relates to compounds of formula I wherein R 1 and R 2 are described hereinbelow. These compounds have high affinity to A 2A receptors and good selectivity to A 1 and A 3 receptors. These compounds are useful, inter alia, in the treatment of Alzheimer's disease, depression, Parkinson's disease and ADHD.

  本发明涉及式I的化合物，其中R1和R2如下所述。这些化合物对A2A受体具有高亲和力，并对A1和A3受体具有良好的选择性。这些化合物在治疗阿尔茨海默病、抑郁症、帕金森病和注意力缺陷多动障碍等方面具有用途。