5-methyl-1-(2'-methylphenyl)-2(1H)-pyridone

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 5-methyl-1-(2'-methylphenyl)-2(1H)-pyridone
• 英文别名: 5-Methyl-1-(2-methylphenyl)pyridin-2-one
• 化学式: C₁₃H₁₃NO
• 分子量: 199.252
• InChiKey: VYXSRCVSKXRDAN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  15
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  20.3
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  2-羟基-5-甲基嘧啶 、 2-甲基苯硼酸 在 copper diacetate 吡啶 作用下， 以 二氯甲烷 为溶剂， 以50%的产率得到5-methyl-1-(2'-methylphenyl)-2(1H)-pyridone
  参考文献：
  名称：

  COMPOUNDS AND METHODS FOR TREATING INFLAMMATORY AND FIBROTIC DISORDERS

  摘要：

  公开了用于治疗炎症和纤维化疾病的化合物和方法，包括用活性化合物调节应激活化蛋白激酶（SAPK）系统的方法，其中活性化合物对p38 MAPK的抑制效力较低；并且其中接触是在SAPK调节浓度下进行的，该浓度对化合物抑制p38 MAPK的抑制浓度百分比较低。还公开了吡非尼酮的衍生物和类似物，它们可用于调节应激活化蛋白激酶（SAPK）系统。

  公开号：

  US20090318455A1

文献信息

• 1-(SUBSTITUTED PHENYL)-5- METHYL- 2 - (1H) PYRIDONE IN THE MANUFACTURE OF MEDICAMENTS FOR TREATING FIBROSIS IN ORGANS OR TISSUES
  申请人：Xiangya Hospital of Central South University

  公开号：EP1878428A1

  公开（公告）日：2008-01-16

  The use of 1-(substituted phenyl)-5-methyl-2-(1H) pyridone in the manufacture of medicaments for treating fibrosis in organs or tissues. It indicates that 1-(substituted phenyl)-5-methyl-2-(1H) pyridone can inhibit the cells produced by various ECM, and their effect is higher than pirfenidone. Therefore, this tpye of compounds can be used as active ingredient for preparing the antifibrotic agent in organs and tissues.

  将 1-(取代苯基)-5-甲基-2-(1H)吡啶酮用于制造治疗器官或组织纤维化的药物。研究表明，1-（取代苯基）-5-甲基-2-（1H）吡啶酮能抑制由各种 ECM 产生的细胞，其效果高于吡非尼酮。因此，这类化合物可作为制备器官和组织抗纤维化剂的活性成分。
• Composition and Method for Treating Fibrotic Diseases
  申请人：Tao Jian Li

  公开号：US20070203203A1

  公开（公告）日：2007-08-30

  The present invention discloses 5-methyl-1-(substituted phenyl)-2(1H)-pyridones have enhanced anti-fibrotic activities than 5-methyl-1-(non-substituted phenyl)-2(1H)-pyridones. An representative example of 5-methyl-(1-substituted phenyl)-2(1H)-pyridones is 1-(3′-fluorophenyl)-5-methyl-2(1H)-pyridone. Accordingly, there are provided compositions comprising one or more compounds selected from the group consisting of 5-methyl-1-(substituted phenyl)-2(1H)-pyridones and methods of using the same to treat or prevent fibrosis diseases.
• COMPOSITION AND METHOD FOR TREATING FIBROTIC DISEASES
  申请人：TAO Li Jian

  公开号：US20090258911A1

  公开（公告）日：2009-10-15

  The present invention discloses 5-methyl-1-(substituted phenyl)-2(1H)-pyridones have enhanced anti-fibrotic activities than 5-methyl-1-(non-substituted phenyl)-2(1H)-pyridones. An representative example of 5-methyl-(1-substituted phenyl)-2(1H)-pyridones is 1-(3′-fluorophenyl)-5-methyl-2(1H)-pyridone. Accordingly, there are provided compositions comprising one or more compounds selected from the group consisting of 5-methyl-1-(substituted phenyl)-2(1H)-pyridones and methods of using the same to treat or prevent fibrosis diseases.
• COMPOSITION AND METHOD FOR TREATING PROTEINURIA
  申请人：SHI Yuenian Eric

  公开号：US20100099719A1

  公开（公告）日：2010-04-22

  The present invention discloses 5-methyl-1-(substituted phenyl)-2(1H)-pyridones having the ability to reduce proteinuria and for treating kidney diseases. The ability to reduce proteinuria has a renoprotective effect for slowing the progression of kidney diseases. A representative example of 5-methyl-(1-substituted phenyl)-2(1H)-pyridones is 1-(3′-fluorophenyl)-5-methyl-2(1H)-pyridone, AKF-PD. Accordingly, the present invention provides compositions comprising one or more compounds selected from the group consisting of 5-methyl-1-(substituted phenyl)-2(1H)-pyridones and methods of using the same to treat proteinuria and kidney diseases.
• METHODS FOR TREATING ACUTE MYOCARDIAL INFARCTIONS AND ASSOCIATED DISORDERS
  申请人：Olgin Jeff

  公开号：US20100190731A1

  公开（公告）日：2010-07-29

  The invention relates to methods of treating patients who have suffered an acute myocardial infarction (AMI) with a therapeutic that has anti-fibrotic effects, for example, pirfenidone and analogs thereof.