methyl 1-(2,6-dimethylphenyl)-6-oxo-1,6-dihydro-3-pyridinecarboxylate | 887307-27-9

• 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: methyl 1-(2,6-dimethylphenyl)-6-oxo-1,6-dihydro-3-pyridinecarboxylate
• 英文别名: methyl 1-(2,6-dimethylphenyl)-6-oxo-1,6-dihydropyridine-3-carboxylate；Methyl 1-(2,6-dimethylphenyl)-6-oxo-1,6-dihydropyridine-3-carboxylate；methyl 1-(2,6-dimethylphenyl)-6-oxopyridine-3-carboxylate
• CAS: 887307-27-9
• 化学式: C₁₅H₁₅NO₃
• 分子量: 257.289
• InChiKey: BDZCNAACKXGHFS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  19
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  46.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  methyl 1-(2,6-dimethylphenyl)-6-oxo-1,6-dihydro-3-pyridinecarboxylate 在 二异丁基氢化铝 作用下， 以 四氢呋喃 为溶剂， 反应 6.5h， 生成 methyl 1-(2,6-dimethylphenyl)-6-oxo-1,4,5,6-tetrahydropyridine-3-carboxylate
  参考文献：
  名称：

  EP2011788

  摘要：

  公开号：
• 作为产物：
  描述：

  香豆灵酸甲酯 、 2,6-二甲基苯胺 在 sodium hydride 作用下， 以 四氢呋喃 为溶剂， 反应 4.0h， 生成 methyl 1-(2,6-dimethylphenyl)-6-oxo-1,6-dihydro-3-pyridinecarboxylate
  参考文献：
  名称：

  WO2007/40208

  摘要：

  公开号：

文献信息

• Nitrogenous Heterocyclic Compound and Pharmaceutical Use Thereof
  申请人：Nakai Hisao

  公开号：US20070265308A1

  公开（公告）日：2007-11-15

  The present invention relates to a compound that has p38 MAP kinase inhibitory activity useful as drug medicine, represented by the general formula (I): wherein all the symbols are as defined in the description, or its salt, N-oxide or solvate, or a prodrug thereof. Further, there are provided a process for producing the same and usage thereof. The compound of the general formula (I) has a p38 MAP kinase inhibitory activity and is useful for the prevention and/or treatment of diseases in which an abnormal production of cytokine, such as inflammatory cytokine or chemokine, or an over-reaction thereto would be instrumental in the cause and aggravation of pathologic condition thereof, namely, cytokine-mediated diseases, for example, inflammatory diseases, respiratory diseases, circulatory diseases, central nervous diseases, etc.

  本发明涉及一种具有p38 MAP激酶抑制活性的化合物，可用作药物，其通式表示为（I）：其中所有符号如描述中所定义，或其盐，N-氧化物或溶剂合物，或其前药。此外，还提供了其生产方法和用途。通式（I）的化合物具有p38 MAP激酶抑制活性，并可用于预防和/或治疗细胞因子异常产生的疾病，例如炎性细胞因子或趋化因子，或对其过度反应会导致病理状况恶化的细胞因子介导疾病，例如炎症性疾病、呼吸系统疾病、循环系统疾病、中枢神经系统疾病等。
• NITROGEN-CONTAINING HETEROCYCLIC COMPOUND AND PHARMACEUTICAL APPLICATION THEREOF
  申请人：NAKAI Hisao

  公开号：US20100063104A1

  公开（公告）日：2010-03-11

  It is intended to provide a compound represented by the formula (I): wherein all the symbols are as defined in the description; which has a p38 MAP kinase inhibitory activity, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. The compound of the invention is useful for preventing or treating a disease in which the abnormal production of a cytokine such as an inflammatory cytokine or a chemokine or overreaction to them is considered to be involved in the cause and aggravation of pathological conditions, in other words, an inflammatory disease, a respiratory disease, a cardiovascular disease, a central nervous system disease or the like, which is a cytokine-mediated disease.

  本发明旨在提供一种由公式（I）表示的化合物：其中所有符号如描述中所定义的；其具有p38 MAP激酶抑制活性，其盐，其N-氧化物，其溶剂合物或其前药。本发明的化合物可用于预防或治疗疾病，其中被认为异常产生细胞因子如炎症性细胞因子或趋化因子或对它们过度反应与病理情况的发生和加重有关，换句话说，是细胞因子介导的疾病，例如炎症性疾病，呼吸系统疾病，心血管疾病，中枢神经系统疾病或类似疾病。
• Nitrogen-containing heterocyclic compound and pharmaceutical application thereof
  申请人：Ono Pharmaceuticals Co., Ltd.

  公开号：US07968572B2

  公开（公告）日：2011-06-28

  It is intended to provide a compound represented by the formula (I): wherein all the symbols are as defined in the description; which has a p38 MAP kinase inhibitory activity, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. The compound of the invention is useful for preventing or treating a disease in which the abnormal production of a cytokine such as an inflammatory cytokine or a chemokine or overreaction to them is considered to be involved in the cause and aggravation of pathological conditions, in other words, an inflammatory disease, a respiratory disease, a cardiovascular disease, a central nervous system disease or the like, which is a cytokine-mediated disease.

  本发明旨在提供一种由公式（I）表示的化合物：其中所有符号如描述中所定义的；该化合物具有p38 MAP激酶抑制活性，其盐，其N-氧化物，其溶剂化物或其前药。本发明的化合物可用于预防或治疗疾病，其中细胞因子的异常产生，如炎性细胞因子或趋化因子，或对它们的过度反应被认为是病理情况的原因和恶化，换句话说，是一种细胞因子介导的疾病，如炎症性疾病，呼吸系统疾病，心血管疾病，中枢神经系统疾病或类似疾病。
• Oxadiazolidinedione compound
  申请人：Astellas Pharma Inc.

  公开号：US07968552B2

  公开（公告）日：2011-06-28

  A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided. It was found that an oxadiazolidinedione compound which is characterized by the possession of a benzyl or the like substituent binding to the cyclic group via a linker at the 2-position of the oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof, has excellent GPR40 agonist action. In addition, since the oxadiazolidinedione compound of the present invention showed excellent insulin secretion promoting action and blood glucose level-lowering action, it is useful as an insulin secretion promoter or an agent for preventing/treating diabetes.

  提供了一种可用作药物的化合物，特别是胰岛素分泌促进剂或用于预防/治疗与GPR40相关的疾病，例如糖尿病等。发现一种噁唑烷二酮化合物，其特征在于在噁唑烷二酮环的2位通过连接基与环状基团结合的苄基或类似基团，或其药学上可接受的盐具有优异的GPR40激动剂作用。此外，由于本发明的噁唑烷二酮化合物显示出优异的胰岛素分泌促进作用和降低血糖水平的作用，因此它可用作胰岛素分泌促进剂或预防/治疗糖尿病的药物。
• Oxadiazolidinedione Compound
  申请人：Negoro Kenji

  公开号：US20090186909A1

  公开（公告）日：2009-07-23

  [Problem] A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided. [Means for resolution] It was found that an oxadiazolidinedione compound which is characterized by the possession of a benzyl or the like substituent binding to the cyclic group via a linker at the 2-position of the oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof, has excellent GPR40 agonist action. In addition, since the oxadiazolidinedione compound of the present invention showed excellent insulin secretion promoting action and blood glucose level-lowering action, it is useful as an insulin secretion promoter or an agent for preventing/treating diabetes.

  【问题】提供一种可用作药物的化合物，特别是胰岛素分泌促进剂或用于预防/治疗涉及GPR40的疾病，如糖尿病等。 【解决方法】发现一种氧代唑烷二酮化合物，其特征在于在氧代唑烷二酮环的2位通过连接基与环上的苯甲基或类似取代基结合，或其药学上可接受的盐具有优异的GPR40激动剂作用。此外，由于本发明的氧代唑烷二酮化合物表现出良好的胰岛素分泌促进作用和降低血糖水平的作用，因此它可用作胰岛素分泌促进剂或预防/治疗糖尿病的药物。