5-ethyl-6-methyl-2-phenylpyrimidin-4-ol

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 5-ethyl-6-methyl-2-phenylpyrimidin-4-ol
• 英文别名: 5-ethyl-4-methyl-2-phenyl-1H-pyrimidin-6-one
• 化学式: C₁₃H₁₄N₂O
• 分子量: 214.267
• InChiKey: AEWJPVBBGFZTTJ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  16
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  41.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5-ethyl-6-methyl-2-phenylpyrimidin-4-ol 在 三氯氧磷 作用下， 生成 2-phenyl-5-ethyl-6-methyl-4-chloropyrimidine
  参考文献：
  名称：

  Discovery of selective PDE4B inhibitors

  摘要：

  In this study the first PDE4B selective inhibitor is described. Optimization of lead 2-arylpyrimidine derivatives afforded a series of potent PDE4B inhibitors with >100-fold selectivity over the PDE4D isozyme. With a good pharmacokinetic profile, a selected compound exhibited potent anti-inflammatory effects in vivo and showed less emesis compared with Cilomilast. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.04.121
• 作为产物：
  描述：

  5-ethyl-6-methyl-2-phenyl-1,3-oxazin-4-one 、 氨 以100%的产率得到
  参考文献：
  名称：

  GRASSI, G.;FOTI, F.;RISITANO, F., J. CHEM. RES. SYNOP., 1983, N 4, 102-103

  摘要：

  DOI：

文献信息

• [EN] NURR1:RXR ACTIVATING COMPOUNDS FOR SIMULTANEOUS TREATMENT OF SYMPTOMS AND PATHOLOGY OF PARKINSON'S DISEASE<br/>[FR] COMPOSÉS ACTIVANT NURR1:RXR POUR LE TRAITEMENT SIMULTANÉ DES SYMPTÔMES ET DE LA PATHOLOGIE DE LA MALADIE DE PARKINSON
  申请人：VASSILATIS DEMETRIOS K

  公开号：WO2017068070A1

  公开（公告）日：2017-04-27

  The invention provides a series of substituted aryl pyrimidine compounds and the use of these compounds as therapeutics to treat or prevent neurodegenerative disorders, including Parkinson's disease. Compounds of the invention are also able to treat the symptoms of such diseases and therefore represent a new treatment modality for ameliorating chronic and acute conditions. The compounds of the invention are capable of selectively potentiating the activity of the Nurr1:RXRα heterodimer, and are able to treat diseases or conditions associated with aberrant Nurr1:RXRα function. The invention further provides methods for treating neurodegenerative disorders by administration of Nurr1:RXRα activating agents.

  这项发明提供了一系列取代芳基嘧啶化合物，并利用这些化合物作为治疗剂来治疗或预防神经退行性疾病，包括帕金森病。该发明的化合物还能够治疗这些疾病的症状，因此代表了一种新的治疗方式，用于改善慢性和急性病症。该发明的化合物能够选择性地增强Nurr1:RXRα异源二聚体的活性，并能够治疗与异常Nurr1:RXRα功能相关的疾病或病症。该发明还提供了通过给予Nurr1:RXRα激活剂来治疗神经退行性疾病的方法。
• Nurr1:RXR activating compounds for simultaneous treatment of symptoms and pathology of Parkinson's disease
  申请人：Vassilatis Demetrios K.

  公开号：US10946019B2

  公开（公告）日：2021-03-16

  The invention provides a series of substituted aryl pyrimidine compounds and the use of these compounds as therapeutics to treat or prevent neurodegenerative disorders, including Parkinson's disease. Compounds of the invention are also able to treat the symptoms of such diseases and therefore represent a new treatment modality for ameliorating chronic and acute conditions. The compounds of the invention are capable of selectively potentiating the activity of the Nurr1:RXRα heterodimer, and are able to treat diseases or conditions associated with aberrant Nurr1:RXRα function. The invention further provides methods for treating neurodegenerative disorders by administration of Nurr1:RXRα activating agents.

  本发明提供了一系列取代芳基嘧啶化合物，并将这些化合物用作治疗或预防神经退行性疾病（包括帕金森病）的药物。本发明的化合物还能治疗此类疾病的症状，因此是一种改善慢性和急性疾病的新治疗方式。本发明的化合物能够选择性地增强Nurr1:RXRα异二聚体的活性，能够治疗与Nurr1:RXRα功能异常相关的疾病或病症。本发明进一步提供了通过施用 Nurr1:RXRα 激活剂治疗神经退行性疾病的方法。
• Pinner, Chemische Berichte, 1889, vol. 22, p. 1610
  作者：Pinner

  DOI：——

  日期：——
• Pinner, Die Imidoaether und ihre Derivate <Berlin 1892>, S. 253
  作者：Pinner

  DOI：——

  日期：——
• NURR1:RXR ACTIVATING COMPOUNDS FOR SIMULTANEOUS TREATMENT OF SYMPTOMS AND PATHOLOGY OF PARKINSON'S DISEASE
  申请人：Vassilatis, Demetrios K.

  公开号：EP3365329B1

  公开（公告）日：2022-03-30