4,5-Dihydro-6-(pyridin-4-yl)-pyridazin-3(2H)-one | 70670-55-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪类
• 英文名称: 4,5-Dihydro-6-(pyridin-4-yl)-pyridazin-3(2H)-one
• 英文别名: 4,5-dihydro-6-(4-pyridinyl)-3(2H)-pyridazinone；4,5-Dihydro-6-(4-pyridyl)-pyridazin-3(2H)-one；3-pyridin-4-yl-4,5-dihydro-1H-pyridazin-6-one
• CAS: 70670-55-2
• 化学式: C₉H₉N₃O
• 分子量: 175.19
• InChiKey: FBOQGQULUAPQCC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.22
• 拓扑面积：
  54.4
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  4,5-Dihydro-6-(pyridin-4-yl)-pyridazin-3(2H)-one 生成 6-(吡啶-4-基)吡嗪-3(2H)-酮
  参考文献：
  名称：

  LESHER, G. Y.;DICKINSON, W. B.

  摘要：

  DOI：
• 作为产物：
  描述：

  4-(pyridin-4-yl)-4-oxobutanenitrile 生成 4,5-Dihydro-6-(pyridin-4-yl)-pyridazin-3(2H)-one
  参考文献：
  名称：

  LESHER, G. Y.;DICKINSON, W. B.

  摘要：

  DOI：

文献信息

• Heterocyclic compound and cardiotonic agent containing the same as
  申请人：Zenyaku Kogyo Kabushiki Kaisha

  公开号：US05446042A1

  公开（公告）日：1995-08-29

  The present invention relates to a novel heterocyclic compound having excellent positive inotropic effect as cardiotonic agent and suppressing increase of heart rate and a cardiotonic agent containing the novel heterocyclic compound as active component.

  本发明涉及一种具有优异正性肌力效应的新型杂环化合物，作为心力衰竭药物具有卓越的正性肌力效应，并抑制心率增加，以及包含该新型杂环化合物作为活性成分的心力衰竭药物。
• 4-Amino-6-(pyridinyl)-3(2H)-pyridazinones and their use as cardiotonics
  申请人：Sterling Drug Inc.

  公开号：US04305943A1

  公开（公告）日：1981-12-15

  4-Amino-2-R-6-PY-3(2H)-pyridazinones (I) or salts thereof, which are useful as cardiotonics, where R is hydrogen, lower-alkyl or lower-hydroxyalkyl, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substituents are prepared by: (a) reaction of 2-R-6-PY-3(2H)-pyridazinone (II) with hydrazine; (b) conversion from 2,3-dihydro-2-R-3-oxo-6-PY-4-pyridazinecarboxamide (III); or, (c) conversion form 2,3-dihydro-2-R-3-oxo-6-PY-4-pyridazinecarboxylic acid hydrazide (IV). Also shown are: the use of I or salts as cardiotonic agents; and, the preparation of intermediates.

  4-氨基-2-R-6-PY-3(2H)-吡啶并嗪酮(I)或其盐，可用作心力衰竭药物，其中R为氢、低烷基或低羟基烷基，PY为4-或3-吡啶基或带有一个或两个低烷基取代基的4-或3-吡啶基，通过以下方法制备：(a) 2-R-6-PY-3(2H)-吡啶并嗪酮(II)与肼的反应；(b) 从2,3-二氢-2-R-3-氧代-6-PY-4-吡啶并嗪甲酰胺(III)转化而来；或(c) 从2,3-二氢-2-R-3-氧代-6-PY-4-吡啶并嗪羧酸肼酰肼(IV)转化而来。还显示了：将I或其盐用作心力衰竭药物；以及中间体的制备。
• 3-Hydrazino-6-(pyridinyl) pyridazines and cardiotonic use thereof
  申请人：Sterling Drug Inc.

  公开号：US04304775A1

  公开（公告）日：1981-12-08

  3-Hydrazino-6-PY-pyridazine or pharmaceutically-acceptable acid-addition salt thereof is useful as a cardiotonic agent, where PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substitutents. 6-PY-3-pyridazinol is prepared by reacting 6-PY-3-pyridazinol with a chlorinating agent to produce 3-chloro-6-PY-pyridazine and reacting said 3-chloro compound with hydrazine to produce said 3-hydrazino compound. 3-Hydrazino-6-PY-pyridazine or pharmaceutically-acceptable acid-addition salt thereof is disclosed as the active component in cardiotonic compositions for increasing cardiac contractility and in the method for increasing cardiac contractility in a patient requiring such treatment. The novel intermediate 3-chloro-6-PY-pyridazine is prepared as noted above.

  3-肼基-6-PY-吡啶嗪或其药学上可接受的酸加成盐在心脏强心剂中有用，其中PY是4-或3-吡啶基或4-或3-吡啶基有一个或两个较低烷基取代基。通过将6-PY-3-吡啶嗪与氯化剂反应以产生3-氯-6-PY-吡啶嗪，再将所述3-氯化合物与肼反应以产生所述3-肼基化合物来制备6-PY-3-吡啶醇。本发明披露了3-肼基-6-PY-吡啶嗪或其药学上可接受的酸加成盐作为增加心脏收缩力的心脏强心剂组成物的活性成分，并用于增加需要此类治疗的患者的心脏收缩力的方法。新型中间体3-氯-6-PY-吡啶嗪如上所述制备。
• Cardiotonic use of 4,5-dihydro-6-(4-pyridinyl)-3(2H)-pyridazinones
  申请人：Sterling Drug Inc.

  公开号：US04486431A1

  公开（公告）日：1984-12-04

  4,5-Dihydro-4-R-6-(4-pyridinyl)-3(2H)-pyridazinone (IA) or pharmaceutically-acceptable acid-addition salt thereof, where R is hydrogen or methyl, is shown as the active component in cardiotonic composition and method for increasing cardiac contractility in a patient requiring such treatment. Also shown is the preparation of IA by reacting a lower-alkyl 2-R-4-(BN)-4-cyano-4-(4-pyridinyl)butanoate with hydrazine, where R is hydrogen or methyl, and BN is 4-morpholinyl, 1-piperidinyl or 1-pyrrolidinyl.

  4,5-二氢-4-R-6-(4-吡啶基)-3(2H)-吡啶嗪酮(IA)或其药学上可接受的酸加成盐，其中R为氢或甲基，被证明是心脏强心剂组合物和增加需要此类治疗的患者心脏收缩力的方法中的活性成分。还展示了通过将较低烷基2-R-4-(BN)-4-氰基-4-(4-吡啶基)丁酸酯与肼反应制备IA的方法，其中R为氢或甲基，BN为4-吗啡啉基，1-哌啶基或1-吡咯烷基。
• 6-(Pyridinyl)-3(2H)-pyridazinones and their use as cardiotonics
  申请人：Sterling Drug Inc.

  公开号：US04304777A1

  公开（公告）日：1981-12-08

  2-R-6-PY-3(2H)-pyridazinones (I) or salts thereof, which are useful as cardiotonics, where R is hydrogen, lower-alkyl or lower-hydroxyalkyl, and PY is 4- or 3-pyridinyl or 4- or 3-pyridinyl having one or two lower-alkyl substituents, are prepared by reacting 2-R-4,5-dihydro-6-PY-3(2H)-pyridazinone with a dehydrogenating agent. Also shown are: cardiotonic compositions and a method for increasing cardiac contractility using I or salts; and, the preparation of the corresponding intermediate 4,5-dihydro compounds.

  2-R-6-PY-3(2H)-pyridazinones（I）或其盐，可用作心脏强心剂，其中R为氢，低烷基或低羟基烷基，PY为4-或3-吡啶基或具有一个或两个低烷基取代基的4-或3-吡啶基，通过将2-R-4,5-二氢-6-PY-3（2H）-吡啶嗪与脱氢剂反应制备而成。还显示了：使用I或盐的心脏强心剂组合物和增加心脏收缩力的方法；以及相应的中间体4,5-二氢化合物的制备。