1-(2'-Imidazolyl)-5-methyl-2-(1H) pyridone | 53427-92-2

• 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: 1-(2'-Imidazolyl)-5-methyl-2-(1H) pyridone
• 英文别名: 1-(1H-imidazol-2-yl)-5-methylpyridin-2-one
• CAS: 53427-92-2
• 化学式: C₉H₉N₃O
• 分子量: 175.19
• InChiKey: HNLISHZVCXNFPW-UHFFFAOYSA-N

物化性质

• 沸点：
  475.4±28.0 °C(Predicted)
• 密度：
  1.304±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  49
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  2-羟基-5-甲基嘧啶 、 2-氯咪唑 以82%的产率得到1-(2'-Imidazolyl)-5-methyl-2-(1H) pyridone
  参考文献：
  名称：

  5-Methyl-1-phenyl-2-(1H)-pyridone compositions and methods of use

  摘要：

  描述了一种含有活性成分5-甲基-1-苯基-2-(1H)-吡啶酮的新型镇痛、退烧、抗炎组合物。这种组合物还被发现能显著降低血清尿酸和葡萄糖水平，并对人类和其他哺乳动物的多种上呼吸道疾病治疗有效。皮肤状况如皮炎和毒葛也可以通过这种药物缓解。含有5-甲基-1-苯基-2-(1H)-吡啶酮的组合物在口服时不引起刺激，在应用于特定靶组织时也没有显著的刺激或其他后遗症。

  公开号：

  US03974281A1

文献信息

• Macrocyclic compounds as inhibitors of viral replication
  申请人：Blatt M. Lawrence

  公开号：US20050267018A1

  公开（公告）日：2005-12-01

  The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

  该实施例提供了一般式I-XIX的化合物，以及包括药物组合在内的组合物，其中包括一种主体化合物。该实施例还提供了治疗方法，包括治疗黄病毒感染的方法，包括丙型肝炎病毒感染的方法和治疗肝纤维化的方法，这些方法通常涉及向需要的个体施用一种主体化合物或组合物的有效量。
• MACROCYCLIC COMPOUNDS AS INHIBITORS OF VIRAL REPLICATION
  申请人：BLATT LAWRENCE M.

  公开号：US20090286843A1

  公开（公告）日：2009-11-19

  The embodiments provide compounds of the general formulas I-XIX, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating flaviviral infection, including hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.

  该实施例提供了一般式I-XIX的化合物，以及包括药物组合物在内的组合物。该实施例还提供了治疗方法，包括治疗黄热病毒感染的方法，包括丙型肝炎病毒感染的方法和治疗肝纤维化的方法，通常涉及向需要治疗的个体施用所述化合物或组合物的有效量。
• Aerosol pirfenidone and pyridone analog compounds and uses thereof
  申请人：Avalyn Pharma Inc.

  公开号：US10028966B2

  公开（公告）日：2018-07-24

  Disclosed herein are formulations of pirfenidone or pyridone analog compounds for aerosolization and use of such formulations for aerosol administration of pirfenidone or pyridone analog compounds for the prevention or treatment of various fibrotic and inflammatory diseases, including disease associated with the lung, heart, kidney, liver, eye and central nervous system. In some embodiments, pirfenidone or pyridone analog compound formulations and delivery options described herein allow for efficacious local delivery of pirfenidone or pyridone analog compound. Compositions include all formulations, kits, and device combinations described herein. Methods include inhalation procedures, indications and manufacturing processes for production and use of the compositions described.

  本文公开了用于气雾化的吡非尼酮或吡啶酮类似物化合物制剂，以及使用此类制剂气雾给药吡非尼酮或吡啶酮类似物化合物以预防或治疗各种纤维化和炎症性疾病，包括与肺、心、肾、肝、眼和中枢神经系统有关的疾病。在某些实施方案中，本文所述的吡非尼酮或吡啶酮类似化合物制剂和给药方案可实现吡非尼酮或吡啶酮类似化合物的有效局部给药。组合物包括本文所述的所有制剂、试剂盒和装置组合。方法包括用于生产和使用所述组合物的吸入程序、适应症和生产工艺。
• Aerosol pirfenidone and pyridone analog compound and uses thereof
  申请人：Avalyn Pharma Inc.

  公开号：US11071741B2

  公开（公告）日：2021-07-27

  Disclosed herein are formulations of pirfenidone or pyridone analog compounds for aerosolization and use of such formulations for aerosol administration of pirfenidone or pyridone analog compounds for the prevention or treatment of various fibrotic and inflammatory diseases, including disease associated with the lung, heart, kidney, liver, eye and central nervous system. In some embodiments, pirfenidone or pyridone analog compound formulations and delivery options described herein allow for efficacious local delivery of pirfenidone or pyridone analog compound. Compositions include all formulations, kits, and device combinations described herein. Methods include inhalation procedures, indications and manufacturing processes for production and use of the compositions described.

  本文公开了用于气雾化的吡非尼酮或吡啶酮类似物化合物制剂，以及使用此类制剂气雾给药吡非尼酮或吡啶酮类似物化合物以预防或治疗各种纤维化和炎症性疾病，包括与肺、心、肾、肝、眼和中枢神经系统有关的疾病。在某些实施方案中，本文所述的吡非尼酮或吡啶酮类似化合物制剂和给药方案可实现吡非尼酮或吡啶酮类似化合物的有效局部给药。组合物包括本文所述的所有制剂、试剂盒和装置组合。方法包括用于生产和使用所述组合物的吸入程序、适应症和生产工艺。
• Compositions and methods for treating viral infections
  申请人：Blatt M Lawrence

  公开号：US20060198823A1

  公开（公告）日：2006-09-07

  The present invention provides methods of treating a virus infection, and methods of reducing viral load, or reducing the time to viral clearance, or reducing morbidity or mortality in the clinical outcomes, in patients suffering from a coronavirus infection. The present invention further provides methods of reducing the risk that an individual will develop a pathological virus infection, that has clinical sequelae. The methods generally involve administering a therapeutically effective amount of a Type I or Type III interferon receptor agonist and a Type II interferon receptor agonist for the treatment of a virus infection, and co-administering an amount of an additional non-pirfenidone/pirfenidone analog agent effective to reduce or eliminate the occurrence or severity of side effects normally associated with the administration of the interferon receptor agonists.

  本发明提供了治疗病毒感染的方法，以及降低冠状病毒感染患者的病毒载量，或缩短病毒清除时间，或降低临床结果中的发病率或死亡率的方法。本发明进一步提供了降低个体发生病理性病毒感染风险的方法，这种病毒感染会产生临床后遗症。这些方法一般包括施用治疗有效量的Ⅰ型或Ⅲ型干扰素受体激动剂和Ⅱ型干扰素受体激动剂来治疗病毒感染，并同时施用一定量的额外的非pirfenidone/pirfenidone类似物制剂，以有效减少或消除通常与施用干扰素受体激动剂相关的副作用的发生或严重程度。