N-Cyclopropyl-1-[3-(3-pyridinylethynyl)phenyl]-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide | 500355-45-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: N-Cyclopropyl-1-[3-(3-pyridinylethynyl)phenyl]-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide
• 英文别名: N-cyclopropyl-4-oxo-1-(3-(2-(pyridin-3-yl)ethynyl)phenyl)-1,4-dihydro-1,8-naphthyridine-3-carboxamide；N-cyclopropyl-4-oxo-1-[3-(2-pyridin-3-ylethynyl)phenyl]-1,8-naphthyridine-3-carboxamide
• CAS: 500355-45-3
• 化学式: C₂₅H₁₈N₄O₂
• 分子量: 406.444
• InChiKey: JQKSFYBCJSWDGS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  31
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  75.2
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  N-Cyclopropyl-1-(3-ethynylphenyl)-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide 生成 N-Cyclopropyl-1-[3-(3-pyridinylethynyl)phenyl]-1,4-dihydro[1,8]naphthyridin-4-one-3-carboxamide
  参考文献：
  名称：

  Alkyne-aryl phosphodiesterase-4 inhibitors

  摘要：

  由公式(I)表示的化合物： 1 或其药用可接受的盐，是磷酸二酯酶4抑制剂，用于治疗哮喘和炎症。

  公开号：

  US20030114478A1

文献信息

• NOVEL SALT 628
  申请人：Briggner Lars-Erik

  公开号：US20100216843A1

  公开（公告）日：2010-08-26

  6-Methyl-5-(1-methyl-1H-pyrazol-5-yl)-N-[5-(methylsulfonyl)pyridin-2-yl]methyl}-2-oxo-1-[3-(trifluoromethyl)phenyl]-1,2-dihydropyridine-3-carboxamide 4-methylbenzenesulfonate and a novel crystalline form thereof are disclosed together with processes for preparing such salt and form, pharmaceutical compositions comprising such a salt and form, and the methods of treatment using such a salt and form.

  6-甲基-5-(1-甲基-1H-吡唑-5-基)-N-[5-(甲磺酰基)吡啶-2-基]甲基}-2-氧代-1-[3-(三氟甲基)苯基]-1,2-二氢吡啶-3-羧酰胺 4-甲基苯磺酸盐及其一种新的结晶形式，以及制备这种盐和形式的方法，包含这种盐和形式的药物组合物，以及使用这种盐和形式进行治疗的方法。
• Alternative Forms of the Phosphodiesterase-4 Inhibitor N-Cyclopropyl-1--4-Oxo-1,4-Dihydro-1,8-Naphthyridine-3-Carboxyamide
  申请人：Clas Sophie-Dorothee

  公开号：US20110245290A1

  公开（公告）日：2011-10-06

  The present invention is directed to alternative forms of the title phosphodiesterase 4 inhibitor which has the structural formula shown immediately below:

  本发明涉及选择性磷酸二酯酶4抑制剂的替代形式，其结构式如下所示：
• [EN] ALTERNATIVE FORMS OF THE PHOSPHODIESTERASE-4 INHIBITOR N-CYCLOPROPYL-1-{3-[(1-OXIDOPRYIDIN-3-YL)ETHYNYL]PHENYL}-4-OXO-1,4-DIHYDRO-1,8-NAPHTHYRIDINE-3-CARBOXYAMIDE<br/>[FR] FORMES ALTERNATIVES DU N-CYCLOPROPYL-1-{3-[(1-OXIDOPRYIDIN-3-YL)ETHYNYL]PHENYL}-4-OXO-1,4-DIHYDRO-1,8-NAPHTHYRIDINE-3-CARBOXYAMIDE, UN INHIBITEUR DE PHOSPHODIESTERASE DE TYPE 4
  申请人：MERCK FROSST CANADA LTD

  公开号：WO2005105084A1

  公开（公告）日：2005-11-10

  The present invention is directed to alternative forms of the title phosphodiesterase 4 inhibitor which has the structural formula shown immediately below: Compound IX

  本发明涉及磷酸二酯酶4抑制剂的替代形式，其结构式如下所示：化合物IX。
• Use of phosphodiesterase-4 inhibitors as enhancers of cognition
  申请人：Dube Daniel

  公开号：US20060040981A1

  公开（公告）日：2006-02-23

  The present invention is directed to a method of enhancing cognition in a healthy subject comprising administering a safe cognition enhancing amount of a phosphodiesterase-4 inhibitor. In particular, this invention is directed to a method of enhancing memory, learning, retention, recall, awareness and judgement in health subjects comprising administering a safe and effective amount of a phosphodiesterase-4 inhibitor.

  本发明涉及一种增强健康受试者认知能力的方法，包括给予安全的磷酸二酯酶-4抑制剂增强认知能力的剂量。特别地，本发明涉及一种增强健康受试者记忆、学习、保留、回忆、意识和判断力的方法，包括给予安全有效的磷酸二酯酶-4抑制剂的剂量。
• Use of pde4 inhibitors as adjunct therapy for psychiatric disorders
  申请人：Scolnick M. Edward

  公开号：US20060069115A1

  公开（公告）日：2006-03-30

  The use of a PDE4 inhibitor in conjunction with psychotherapy provides enhanced therapeutic results in the treatment of psychiatric disorders including, for example, specific phobias, panic disorders, anxiety disorders including posttraumatic stress disorders, and obsessive-compulsive disorder.

  在治疗精神障碍，例如特定恐惧症、惊恐障碍、包括创伤后应激障碍和强迫症的焦虑障碍中，与心理治疗同时使用PDE4抑制剂可以提供增强的治疗效果。