2-(4-fluoro-phenyl)-imidazo[1,2-a]pyridine-6-carboxylic acid amide | 733-02-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 2-(4-fluoro-phenyl)-imidazo[1,2-a]pyridine-6-carboxylic acid amide
• 英文别名: 2-(4-fluoro-phenyl)-imidazo[1,2-a]pyridine-6-carboxylic acid amide；2-(4-fluorophenyl)imidazo[1,2-a]pyridine-6-carboxamide；2-<4-Fluor-phenyl>-5-aminoformyl-pyrimidazol
• CAS: 733-02-8
• 化学式: C₁₄H₁₀FN₃O
• 分子量: 255.251
• InChiKey: DXQZQRYCHCVGOB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 重原子数：
  19
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  60.4
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  聚合甲醛 、 2-(4-fluoro-phenyl)-imidazo[1,2-a]pyridine-6-carboxylic acid amide 在 sodium acetate 、 溶剂黄146 、 碳酸氢铵 作用下， 以 水 、 乙腈 为溶剂， 反应 2.0h， 生成 2-(4-fluorophenyl)-3-(hydroxymethyl)imidazo[1,2-a]pyridine-6-carboxamide
  参考文献：
  名称：

  [EN] IMIDAZOPYRIDINE COMPOUNDS
  [FR] COMPOSÉS IMIDAZOPYRIDINES

  摘要：

  这项发明涉及式(I)的化合物及其药学上可接受的盐和溶剂化合物，这些化合物是SSAO活性的抑制剂。该发明还涉及包含这些化合物的药物组合物，以及利用这些化合物治疗或预防抑制SSAO活性有益的医疗状况，如炎症性疾病和免疫紊乱。

  公开号：

  WO2010064020A1
• 作为产物：
  描述：

  6-氨基烟酰胺 、 2-溴-4'-氟苯乙酮 在 sodium hydroxide 作用下， 以 乙醇 为溶剂， 生成 2-(4-fluoro-phenyl)-imidazo[1,2-a]pyridine-6-carboxylic acid amide
  参考文献：
  名称：

  [EN] IMIDAZOPYRIDINE COMPOUNDS
  [FR] COMPOSÉS IMIDAZOPYRIDINES

  摘要：

  这项发明涉及式(I)的化合物及其药学上可接受的盐和溶剂化合物，这些化合物是SSAO活性的抑制剂。该发明还涉及包含这些化合物的药物组合物，以及利用这些化合物治疗或预防抑制SSAO活性有益的医疗状况，如炎症性疾病和免疫紊乱。

  公开号：

  WO2010064020A1

文献信息

• Imidazo[1,2-a]pyridines and their use as pharmaceuticals
  申请人：sanofi-aventis

  公开号：EP1964840A1

  公开（公告）日：2008-09-03

  Imidazo[1,2-a]pyridines and their use as pharmaceuticals The present invention relates to derivatives of imidazo[1,2-a]pyridines of the formula (I), in which R, R1 to R4 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of the formula I, to pharmaceutical compositions comprising them, and to the use of compounds of the formula I for the manufacture of a medicament for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

  咪唑[1,2-a]吡啶及其作为药物的用途。本发明涉及咪唑[1,2-a]吡啶衍生物的公式(I)，其中R、R1至R4和n具有声明中指示的含义，这些衍生物调节内皮型一氧化氮(NO)合酶的转录，并且是有价值的药理活性化合物。具体来说，公式I的化合物上调内皮型NO合酶酶的表达，并可应用于需要增加该酶的表达或增加NO水平或正常化降低的NO水平的情况。该发明还涉及公式I化合物的制备方法，包括它们的药物组合物，以及公式I化合物用于制造刺激内皮型NO合酶表达或治疗各种疾病的药物，包括心血管疾病如动脉粥样硬化、血栓形成、冠状动脉疾病、高血压和心脏功能不全等。
• IMIDAZO[1,2-a]PYRIDINES AND THEIR USE AS PHARMACEUTICALS
  申请人：ZOLLER Gerhard

  公开号：US20100113412A1

  公开（公告）日：2010-05-06

  The present invention relates to derivatives of imidazo[1,2-a]pyridines of formula I, in which R, R1 to R4 and n have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired. The invention further relates to processes for the preparation of compounds of formula I, to pharmaceutical compositions comprising them, and to the use of compounds of formula I for the stimulation of the expression of endothelial NO synthase or for the treatment of various diseases including cardiovascular disorders such as atherosclerosis, thrombosis, coronary artery disease, hypertension and cardiac insufficiency, for example.

  本发明涉及公式I的咪唑[1,2-a]吡啶衍生物，其中R、R1至R4和n具有所述权利要求中所示的含义，这些衍生物调节内皮型一氧化氮（NO）合酶的转录，并且是有价值的药理活性化合物。具体地，公式I的化合物上调内皮型NO合酶的表达，并可应用于需要增加该酶的表达或增加NO水平或恢复降低的NO水平的情况。本发明还涉及制备公式I的化合物的方法，包括它们的制药组合物，以及使用公式I的化合物刺激内皮型NO合酶的表达或治疗各种疾病，包括心血管疾病，如动脉粥样硬化、血栓形成、冠状动脉疾病、高血压和心脏衰竭等。
• Imidazopyridine Compounds
  申请人：Nilsson Marianne

  公开号：US20120010188A1

  公开（公告）日：2012-01-12

  The invention relates to compounds of formula (I): and their pharmaceutically acceptable salts and solvates, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.

  本发明涉及公式（I）的化合物及其药学上可接受的盐和溶剂化物，它们是SSAO活性抑制剂。本发明还涉及包含这些化合物的药物组合物和使用这些化合物治疗或预防抑制SSAO活性有益的医疗条件，例如炎症性疾病和免疫紊乱。
• IMIDAZOPYRIDINE COMPOUNDS
  申请人：Proximagen Limited

  公开号：US20150239905A1

  公开（公告）日：2015-08-27

  The invention relates to compounds of formula (I): and their pharmaceutically acceptable salts and solvates, which are inhibitors of SSAO activity. The invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the treatment or prevention of medical conditions wherein inhibition of SSAO activity is beneficial, such as inflammatory diseases and immune disorders.

  本发明涉及式(I)的化合物及其药学上可接受的盐和溶剂，它们是SSAO活性的抑制剂。本发明还涉及包含这些化合物的制药组合物以及使用这些化合物治疗或预防抑制SSAO活性有益的医疗状况，例如炎症性疾病和免疫障碍。
• IMIDAZO[1,2-A]PYRIDINES AND THEIR USE AS PHARMACEUTICALS
  申请人：Sanofi-Aventis

  公开号：EP2129375A1

  公开（公告）日：2009-12-09