3-[N-(5-Ethyl-2-methoxy-6-methyl-pyridin-3-ylmethyl)-amino]-5-ethyl-6-methyl-2(1H)-pyridinone | 139547-89-0

• 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: 3-[N-(5-Ethyl-2-methoxy-6-methyl-pyridin-3-ylmethyl)-amino]-5-ethyl-6-methyl-2(1H)-pyridinone
• 英文别名: 3-[N-(5-Ethyl-2-methoxy-6-methyl-3-pyridylmethyl)-amino]-5-ethyl-6-methyl-2(1H)-pyridinone；3-[N-[(5-Ethyl-2-methoxy-6-methyl-3-pyridyl)methyl]amino]-5-ethyl-6-methylpyridin-2(1H)-one；5-ethyl-3-[(5-ethyl-2-methoxy-6-methylpyridin-3-yl)methylamino]-6-methyl-1H-pyridin-2-one
• CAS: 139547-89-0
• 化学式: C₁₈H₂₅N₃O₂
• 分子量: 315.415
• InChiKey: IUKVADMYSQZSIH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  23
• 可旋转键数：
  6
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  63.2
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  3-氨基-5-乙基-6-甲基-2(1H)-吡啶酮 、 2-methoxy-5-ethyl-6-methylnicotinaldehyde 在 sodium tetrahydroborate 、 溶剂黄146 作用下， 生成 3-[N-(5-Ethyl-2-methoxy-6-methyl-pyridin-3-ylmethyl)-amino]-5-ethyl-6-methyl-2(1H)-pyridinone
  参考文献：
  名称：

  合成和评估2-吡啶酮衍生物作为特定的HIV-1逆转录酶抑制剂。3.3-氨基吡啶-2（1H）-1的吡啶基和苯基类似物。

  摘要：

  在努力开发新型的非核苷，特定的人类免疫缺陷病毒1型（HIV-1）逆转录酶（RT）抑制剂时，一系列3-[（（吡啶甲基））]和3-[（（苯基甲基））] [-2]合成了吡啶酮衍生物，并测试了其对HIV-1 RT的抑制活性。更有效的化合物在吡啶基和苯环上具有2'-甲氧基和4'-和/或5'-脂族取代基。还评估了几种更有效的化合物在MT-4细胞培养物中的抗病毒活性。从这一系列化合物中，3- [N-[（5-乙基-2-甲氧基-6-甲基-3-吡啶基）甲基]氨基] -5-乙基-6-甲基吡啶-2（1H）-一（6选择）进行临床评估。

  DOI：

  10.1021/jm00054a009

文献信息

• Synergism of HIV reverse transcriptase inhibitors
  申请人：MERCK & CO. INC.

  公开号：EP0484071A3

  公开（公告）日：1992-11-25

  The combination of certain aminopyridones and anti-HIV nucleoside analogs has been found to synergistically inhibit HIV reverse transcriptase. This combination is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a combination of compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in further combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.

  已发现某些氨基吡啶酮类化合物与抗HIV核苷类类似物协同抑制HIV反转录酶。该组合在预防或治疗HIV感染以及治疗艾滋病方面具有用途，无论是作为化合物的组合、药学上可接受的盐、药物组成成分，还是与其他抗病毒药物、抗感染药物、免疫调节剂、抗生素或疫苗进一步组合与否。还描述了治疗艾滋病的方法以及预防或治疗HIV感染的方法。
• [EN] USE OF BHAP COMPOUNDS IN COMBINATION WITH OTHER NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS FOR THE TREATMENT OF HIV INFECTION<br/>[FR] UTILISATION DE COMPOSES BHAP EN COMBINAISON AVEC D'AUTRES INHIBITEURS DE LA TRANSCRIPTASE INVERSE NON-NUCLEOSIDIQUES DANS LE TRAITEMENT DES INFECTIONS A VIH
  申请人：THE UPJOHN COMPANY

  公开号：WO1994009781A1

  公开（公告）日：1994-05-11

  (EN) The present invention are methods of treating a HIV positive human which comprises (1) administering to the HIV positive individual a sensitizingly effective amount of a SENSITIZING HIV-1 INHIBITOR until increased sensitivity to a NON-NUCLEOSIDE HIV TREATMENT DRUG develops, (2) administering to the HIV positive individual an effective amount of a NON-NUCLEOSIDE HIV TREATMENT DRUG. An alternative method is a method of treating a HIV positive human which comprises administering to the HIV positive individual a sensitizingly effective amount of one or more SENSITIZING HIV-1 INHIBITOR concurrently with an effective amount of a NON-NUCLEOSIDE HIV TREATMENT DRUG.(FR) La présente invention se rapporte à des procédés de traitement d'un patient séropositif consistant à (1) administrer au patient séropositif une dose efficace sensibilisante d'un inhibiteur du VIH-1 sensibilisant jusqu'à ce qu'une sensibilité accrue à un médicament non-nucléosidique traitant le VIH se développe, (2) administrer au patient séropositif une dose efficace d'un médicament non-nucléosidique traitant le VIH. Une autre variante du procédé de traitement d'un patient séropositif consiste à administrer au patient séropositif une dose efficace sensibilisante d'un ou de plusieurs inhibiteurs du VIH sensibilisants, en même temps qu'une dose efficace d'un médicament non-nucléosidique traitant le VIH.

  本发明涉及治疗艾滋病毒（HIV）阳性人群的方法，包括：（1）向HIV阳性个体施用足够的敏感性HIV-1抑制剂，直到对非核苷类HIV治疗药物产生增加敏感性，（2）向HIV阳性个体施用足够的非核苷类HIV治疗药物。另一种方法是同时向HIV阳性个体施用足够的一种或多种敏感性HIV-1抑制剂和足够的非核苷类HIV治疗药物。
• Inhibitors of HIV reverse transcriptase
  申请人：MERCK & CO. INC.

  公开号：EP0462800A2

  公开（公告）日：1991-12-27

  Novel pyridones inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by IV are also described.

  新型吡啶酮类药物可抑制艾滋病病毒逆转录酶，可用于预防或治疗艾滋病病毒感染和治疗艾滋病，可作为化合物、药学上可接受的盐、药物组合成分，无论是否与其他抗病毒药、抗感染药、免疫调节剂、抗生素或疫苗联合使用。还描述了治疗艾滋病的方法和预防或治疗 IV 感染的方法。
• 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。