5,7-dichloro-1,8-naphthyridin-2-ol | 210642-96-9

• 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: 5,7-dichloro-1,8-naphthyridin-2-ol
• 英文别名: 5,7-Dichloro-1,8-naphthyridin-2(1H)-one；5,7-dichloro-1H-1,8-naphthyridin-2-one
• CAS: 210642-96-9
• 化学式: C₈H₄Cl₂N₂O
• 分子量: 215.039
• InChiKey: AHHBDALNEHKPGT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  42
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  5,7-dichloro-1,8-naphthyridin-2-ol 在 三乙胺 、 三氯氧磷 作用下， 反应 25.5h， 生成 Ethyl 4-(4,7-dichloro-1,8-naphthyridin-2-yl)piperazine-1-carboxylate
  参考文献：
  名称：

  Synthesis of 1,8-naphthyridine derivatives: Potential antihypertensive agents — Part VII

  摘要：

  A series of 2-(carbethoxypiperazinyl)- and 2-piperazinyl-1,8-naphthyridine derivatives, variously substituted, have been synthesized and pharmacologically investigated for their antihypertensive activity. Some of them exhibited a significant and prolonged decrease of the mean arterial pressure (MAP) on spontaneously hypertensive rats. For this series of compounds, on the basis of the pharmacological results obtained, no structure-activity relationship can be deduced at this time. Moreover, the most active and representative compounds 11b, 12a and 16b were investigated by means of in vitro pharmacological functional studies and in vivo, as diuretic agents, to determine a possible mechanism of the antihypertensive activity, which is unknown for the moment. (C) Elsevier, Paris.

  DOI：

  10.1016/s0223-5234(98)80014-7
• 作为产物：
  描述：

  2,6-二氨基吡啶 在 三氟乙酸 、 sodium nitrite 、 三氯氧磷 作用下， 以 二苯醚 为溶剂， 反应 38.5h， 生成 5,7-dichloro-1,8-naphthyridin-2-ol
  参考文献：
  名称：

  [EN] COMPOUNDS AND METHODS FOR INHIBITING mTOR
  [FR] COMPOSÉS ET PROCÉDÉS D'INHIBITION DE MTOR

  摘要：

  揭示了具有作为 mTOR 抑制剂活性的化合物。这些化合物具有以下结构（I），包括立体异构体、药用可接受的盐和前药，其中 R1、R2、R3、R4 和 A 如本文所定义。还公开了与制备和使用这些化合物相关的方法，以及包含这些化合物的药物组合物。

  公开号：

  WO2017031427A1

文献信息

• [EN] COMPOUNDS AND METHODS FOR INHIBITING mTOR<br/>[FR] COMPOSÉS ET PROCÉDÉS D'INHIBITION DE MTOR
  申请人：3-V BIOSCIENCES INC

  公开号：WO2017031427A1

  公开（公告）日：2017-02-23

  Compounds having activity as mTOR inhibitors are disclosed. The compounds have the following structure (I) including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

  揭示了具有作为 mTOR 抑制剂活性的化合物。这些化合物具有以下结构（I），包括立体异构体、药用可接受的盐和前药，其中 R1、R2、R3、R4 和 A 如本文所定义。还公开了与制备和使用这些化合物相关的方法，以及包含这些化合物的药物组合物。
• NOVEL COMPOUNDS
  申请人：BOEHM JEFFREY CHARLES

  公开号：US20090239897A1

  公开（公告）日：2009-09-24

  Novel substituted 1,5,7-trisubstituted-1,8-napthyridin-2(1H)-one compounds; 1,5,7 trisubstituted-1,6-napthyridine-2-(1H)-one compounds and 1,5,7-trisubstituted quinoline-2(1H)-one compounds, processes for the preparation thereof, the use thereof in treating CSBP/p38 kinase mediated diseases and pharmaceutical compositions for use in such therapy.

  小说替代了1,5,7-三取代-1,8-萘啶-2（1H）-酮化合物; 1,5,7-三取代-1,6-萘啶-2-（1H）-酮化合物和1,5,7-三取代喹啉-2（1H）-酮化合物，其制备方法，用于治疗CSBP / p38激酶介导的疾病，并用于此类治疗的制药组合物。
• US7550480B2
  申请人：——

  公开号：US7550480B2

  公开（公告）日：2009-06-23
• Synthesis of 1,8-naphthyridine derivatives: Potential antihypertensive agents — Part VII
  作者：Pier Luigi Ferrarini、Claudio Mori、Muwaffag Badawneh、Vincenzo Calderone、Lorella Calzolari、Tiziana Loffredo、Enrica Martinotti、Giuseppe Saccomanni

  DOI：10.1016/s0223-5234(98)80014-7

  日期：1998.6

  A series of 2-(carbethoxypiperazinyl)- and 2-piperazinyl-1,8-naphthyridine derivatives, variously substituted, have been synthesized and pharmacologically investigated for their antihypertensive activity. Some of them exhibited a significant and prolonged decrease of the mean arterial pressure (MAP) on spontaneously hypertensive rats. For this series of compounds, on the basis of the pharmacological results obtained, no structure-activity relationship can be deduced at this time. Moreover, the most active and representative compounds 11b, 12a and 16b were investigated by means of in vitro pharmacological functional studies and in vivo, as diuretic agents, to determine a possible mechanism of the antihypertensive activity, which is unknown for the moment. (C) Elsevier, Paris.