5-氯-1,8-萘啶-2(1h)-酮 | 250264-28-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 5-氯-1,8-萘啶-2(1h)-酮
• 英文名称: 2-hydroxy-5-chloro-1,8-naphthyridine
• 英文别名: 5-chloro-1H-1,8-naphthyridin-2-one
• CAS: 250264-28-9
• 化学式: C₈H₅ClN₂O
• 分子量: 180.593
• InChiKey: DIHDSAINCRHSHA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.2
• 重原子数：
  12
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  42
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  5-氯-1,8-萘啶-2(1h)-酮 在 sodium hydroxide 、 sodium hydride 作用下， 以 乙醇 、 N,N-二甲基甲酰胺 为溶剂， 反应 40.0h， 生成 1-Methyl-5-piperazin-1-yl-1H-[1,8]naphthyridin-2-one
  参考文献：
  名称：

  Synthesis of 1,8-naphthyridine derivatives: potential antihypertensive agents – Part VIII

  摘要：

  A series of (ethoxycarbonylpiperazinyl)- and piperazinyl-1,8-naphthyridine derivatives, variously substituted, has been synthesized and pharmacologically investigated for anthihypertensive activity. Some of them exhibited a significant and prolonged decrease of the mean arterial pressure (MAP) on spontaneously hypertensive rats. On the basis of the pharmacological results, no structure-activity relationship can be deduced at this time. Moreover, the most active compound 4e, was investigated by means of in vitro pharmacological functional studies and in vivo, as a diuretic agent, to determine a possible mechanism of the antihypertensive activity, which results in a probably non-competitive antagonism against alpha(1), vascular adrenoceptors. This mechanism was also shown by the compounds 8 and 13. (C) Elsevier, Paris.

  DOI：

  10.1016/s0223-5234(99)80099-3
• 作为产物：
  描述：

  2-amino-5-chloro-1,8-naphthyridine 在 硫酸 、 sodium nitrite 、 ammonium hydroxide 作用下， 反应 4.0h， 以70%的产率得到5-氯-1,8-萘啶-2(1h)-酮
  参考文献：
  名称：

  Synthesis of 1,8-naphthyridine derivatives: potential antihypertensive agents – Part VIII

  摘要：

  A series of (ethoxycarbonylpiperazinyl)- and piperazinyl-1,8-naphthyridine derivatives, variously substituted, has been synthesized and pharmacologically investigated for anthihypertensive activity. Some of them exhibited a significant and prolonged decrease of the mean arterial pressure (MAP) on spontaneously hypertensive rats. On the basis of the pharmacological results, no structure-activity relationship can be deduced at this time. Moreover, the most active compound 4e, was investigated by means of in vitro pharmacological functional studies and in vivo, as a diuretic agent, to determine a possible mechanism of the antihypertensive activity, which results in a probably non-competitive antagonism against alpha(1), vascular adrenoceptors. This mechanism was also shown by the compounds 8 and 13. (C) Elsevier, Paris.

  DOI：

  10.1016/s0223-5234(99)80099-3

文献信息

• Novel compounds
  申请人：Boehm Charles Jeffrey

  公开号：US20060211727A1

  公开（公告）日：2006-09-21

  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，制备这些化合物的方法，将其用于治疗CSBP / p38激酶介导的疾病以及用于此类治疗的制药组合物。
• 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。
• Bicyclic compounds with kinase inhibitory activity
  申请人：Calderwood F. Emily

  公开号：US20070149533A1

  公开（公告）日：2007-06-28

  The present invention provides novel bicyclic compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

  本发明提供了一种新颖的双环化合物，可用作蛋白激酶抑制剂。本发明还提供了包括本发明化合物的制药组合物以及使用该组合物治疗各种疾病的方法。
• NAPHTHYRIDINONES AS PROTEIN KINASE INHIBITORS
  申请人：Xiao Yufang

  公开号：US20110269758A1

  公开（公告）日：2011-11-03

  Naphthyridinone derivative compounds that inhibit Aurora kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed Aurora kinases such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.

  本发明揭示了抑制Aurora激酶酶的萘啶酮衍生物化合物，以及包含这些化合物的制药组合物和合成这些化合物的方法。这些化合物在治疗由未调节和/或扰动的Aurora激酶引起的增殖性疾病中具有实用性，如癌症、银屑病、病毒和细菌感染、炎症性和自身免疫性疾病。
• プロテインキナーゼ阻害剤としてのナフチリジノン
  申请人：メルク パテント ゲゼルシャフト ミット ベシュレンクテル ハフツング

  公开号：JP2011526912A

  公开（公告）日：2011-10-20

  オーロラ・キナーゼ酵素を阻害するナフチリジノン誘導体化合物が、これらの化合物を含んでなる医薬組成物及びこれらの化合物の合成方法と共に開示される。かかる化合物には、癌、乾癬、ウイルスや細菌の感染症、炎症性疾患及び自己免疫疾患などの無秩序な及び／又は障害のあるオーロラ・キナーゼに起因する増殖性疾患の処置における有用性がある。

  本研究公开了抑制极光激酶的萘啶酮衍生物化合物，以及含有这些化合物的药物组合物和合成这些化合物的方法。这些化合物可用于治疗由极光激酶紊乱和/或受损引起的增殖性疾病，如癌症、牛皮癣、病毒和细菌感染、炎症性疾病和自身免疫性疾病。