3-甲基-1,2,3,4-四氢吡啶并[2,3-b]吡嗪-2-酮 | 74983-04-3

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 3-甲基-1,2,3,4-四氢吡啶并[2,3-b]吡嗪-2-酮
• 英文名称: 3-Methyl-1,2,3,4-tetrahydro-pyrido<2,3-b>pyrazin-2-on
• 英文别名: 3,4-dihydro-3-methylpyrido<2,3-b>pyrazin-2(1H)-one；3-methyl-3,4-dihydro-1H-pyrido<2,3-b>pyrazin-2-one；3-methyl-3,4-dihydro-1H-pyrido[2,3-b]pyrazin-2-one；3-methyl-3,4-dihydropyrido[2,3-b]pyrazin-2(1H)-one；3-methyl-1H,2H,3H,4H-pyrido[2,3-b]pyrazin-2-one
• CAS: 74983-04-3
• 化学式: C₈H₉N₃O
• mdl: MFCD18836844
• 分子量: 163.179
• InChiKey: RJOLRYKVHJWYEN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.6
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.25
• 拓扑面积：
  54
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  3-甲基-1,2,3,4-四氢吡啶并[2,3-b]吡嗪-2-酮 在 sodium hydroxide 、 双氧水 作用下， 以 水 为溶剂， 反应 10.0h， 以1.2 g的产率得到3-methyl-1H-pyrido<2,3-b>pyrazin-2-one
  参考文献：
  名称：

  [EN] PYRIDINE COMPOUNDS AND USES THEREOF
  [FR] COMPOSÉS DE PYRIDINE ET LEURS UTILISATIONS

  摘要：

  本发明涉及式(I)的吡啶化合物。该发明的不同方面涉及包括所述化合物的药物组合物以及将该化合物用作治疗神经和精神疾病的治疗剂。

  公开号：

  WO2013034761A1
• 作为产物：
  描述：

  N-(3-nitro-2-pyridyl)-α-alanine 在 铁粉 、 溶剂黄146 作用下， 反应 1.5h， 以1.4 g的产率得到3-甲基-1,2,3,4-四氢吡啶并[2,3-b]吡嗪-2-酮
  参考文献：
  名称：

  [EN] PYRIDINE COMPOUNDS AND USES THEREOF
  [FR] COMPOSÉS DE PYRIDINE ET LEURS UTILISATIONS

  摘要：

  本发明涉及式(I)的吡啶化合物。该发明的不同方面涉及包括所述化合物的药物组合物以及将该化合物用作治疗神经和精神疾病的治疗剂。

  公开号：

  WO2013034761A1

文献信息

• HETEROCYCLIC COMPOUND
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP2873669A1

  公开（公告）日：2015-05-20

  The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.

  本发明提供一种具有PDE2A选择性抑制作用的化合物，可用作预防或治疗精神分裂症、阿尔茨海默病等疾病的药剂。本发明是一种由式（1）表示的化合物：其中每个符号如规范中所述，或其盐。
• Pyridine Compounds and Uses Thereof
  申请人：Jorgensen Morten

  公开号：US20140235645A1

  公开（公告）日：2014-08-21

  The present invention is directed to pyridine compounds of Formula (I). Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds as therapeutic agents treating neurological and psychiatric disorders.

  本发明涉及式(I)的吡啶化合物。发明的不同方面涉及包含所述化合物的制药组合物以及将该化合物用作治疗神经系统和精神障碍的治疗剂。
• Nitrogenated heterocyclic compound
  申请人：Takeda Pharmaceutical Company Limited

  公开号：US10017508B2

  公开（公告）日：2018-07-10

  The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.

  本发明提供了一种具有 PDE2A 选择性抑制作用的化合物，该化合物可作为预防或治疗精神分裂症、阿尔茨海默病等的药物。 本发明是一种由式（1）表示的化合物： 其中各符号如说明书所述，或其盐类。
• 2-Phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides as nonbenzodiazepine anticonvulsants and anxiolytics
  作者：Bruce E. Tomczuk、C. R. Taylor、L. Meredith Moses、Deborah B. Sutherland、Young S. Lo、David N. Johnson、William B. Kinnier、Brian F. Kilpatrick

  DOI：10.1021/jm00114a007

  日期：1991.10

  A series of 2-phenyl-3H-imidazo[4,5-b]pyridine-3-acetamides were designed and synthesized as non-benzodiazepine anxiolytics based on a molecular disconnection of a typical 1,4-benzodiazepine (BZD). A number of these compounds showed submicromolar potency in a [H-3]benzodiazepine binding assay in vitro and good potency in protecting rodents against pentylenetetrazole-induced seizures. Compound 84 appears to be a selective anticonvulsant (pentylenetetrazole) agent when tested against a profile of chemically and electrically induced seizures in mice. In addition, compound 148 appears to be a selective anxiolytic/hypnotic agent on the basis of biochemical and pharmacological characterization. It appears to be a full BZD agonist as assessed by GABA shift ratio and to be effective in punishment and nonpunishment animal models of anxiety. In addition, it shows a lower side-effect profile than diazepam as assessed by rotorod neurotoxicity and potentiation of ethanol-induced sleep time in mice. The chemistry and structure-activity relationships of this series is discussed.
• NITROGENATED HETEROCYCLIC COMPOUND
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP2848618B1

  公开（公告）日：2018-03-14