5-chloro-2-(2-methoxyphenyl)-4H-benzo[d][1,3]oxazin-4-one | 1234707-34-6

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并恶嗪类
• 英文名称: 5-chloro-2-(2-methoxyphenyl)-4H-benzo[d][1,3]oxazin-4-one
• 英文别名: 5-chloro-2-(2'-methoxylphenyl)-4H-benzo[d][1,3]oxazin-4-one；5-chloro-2-(2-methoxyphenyl)-3,1-benzoxazin-4-one
• CAS: 1234707-34-6
• 化学式: C₁₅H₁₀ClNO₃
• 分子量: 287.702
• InChiKey: JUUQBMMWWLBTLH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  20
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  47.9
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  2-氨基-6-氯苯甲酸 、 甲氧基苯甲酰氯 在 吡啶 作用下， 反应 24.0h， 以49%的产率得到5-chloro-2-(2-methoxyphenyl)-4H-benzo[d][1,3]oxazin-4-one
  参考文献：
  名称：

  Synthesis and evaluation of benzoxazinone derivatives on activity of human neutrophil elastase and on hemorrhagic shock-induced lung injury in rats

  摘要：

  A new series of benzoxazinone analogs were designed, synthesized, and assayed to determine their effects on superoxide anion generation and neutrophil elastase (NE) release in formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP)-activated human neutrophils. Of these, compounds 6-10 showed a potent dual inhibitory effect on NE release and superoxide anion generation. In contrast, compounds 11-15 exhibited highly selective and potent inhibitory activities on NE release. These results indicate that the inhibitory activity on NE release in FMLP-activated human neutrophils depended on the position of chloro-substituent in the A ring. On the other hand, 13 significantly attenuated the increase in myeloperoxidase (MPO) activity and edema in the lung of rats after trauma-hemorrhagic shock. Therefore, these compounds could be developed as new NE inhibitors. (c) 2010 Elsevier Masson SAS. All rights reserved.

  DOI：

  10.1016/j.ejmech.2010.03.046

文献信息

• BENZOXAZINONE COMPOUND, METHOD FOR PRODUCING THE SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
  申请人：Hsieh Pei-Wen

  公开号：US20110319611A1

  公开（公告）日：2011-12-29

  A benzoxazinone compound having the following formula (I): wherein one of R 1 and R 2 is H, and the other of R 1 and R 2 is a halogen group, and R 1 and R 2 cannot be the same at the same time; and R 3 , R 4 , R 5 , R 6 , and R 7 are independently selected from the group consisting of H, a halogen group, a C 1 -C 4 alkyl group, and a C 1 -C 4 alkoxyl group.

  具有以下式子(I)的苯并噁唑酮化合物：其中R1和R2中的一个是H，另一个是卤素基团，且R1和R2不能同时相同；R3、R4、R5、R6和R7分别独立地选自H、卤素基团、C1-C4烷基和C1-C4烷氧基组成的群。
• Methods and pharmaceutical compositions for the treatment of bacterial infections in patients suffering from cirrhosis
  申请人：INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE)

  公开号：US10201536B2

  公开（公告）日：2019-02-12

  The present invention relates to methods and pharmaceutical compositions for the treatment of bacterial infections in patients suffering from cirrhosis. In particular, the present invention relates to a method of treating bacterial infection in a patient suffering from cirrhosis comprising administering to the patient a therapeutically effective amount of a TLR7 and/or TLR8 agonist.

  本发明涉及治疗肝硬化患者细菌感染的方法和药物组合物。特别是，本发明涉及一种治疗肝硬化患者细菌感染的方法，包括向患者施用治疗有效量的TLR7和/或TLR8激动剂。
• METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF BACTERIAL INFECTIONS IN PATIENTS SUFFERING FROM CIRRHOSIS
  申请人：INSERM (INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE)

  公开号：US20180140597A1

  公开（公告）日：2018-05-24

  The present invention relates to methods and pharmaceutical compositions for the treatment of bacterial infections in patients suffering from cirrhosis. In particular, the present invention relates to a method of treating bacterial infection in a patient suffering from cirrhosis comprising administering to the patient a therapeutically effective amount of a TLR7 and/or TLR8 agonist.
• [EN] METHODS AND COMPOSITIONS FOR THE TREATMENT OF A CHAGAS DISEASE<br/>[FR] MÉTHODES ET COMPOSITIONS POUR LE TRAITEMENT DE LA MALADIE DE CHAGAS
  申请人：BIOMED VALLEY DISCOVERIES

  公开号：WO2014186623A2

  公开（公告）日：2014-11-20

  The present invention provides, inter alia, methods for treating or ameliorating the effects of a Chagas disease. The methods include administering to a subject in need thereof an effective amount of a first active agent selected from the group consisting of a histamine-H1-receptor antagonist, a selective neutrophil elastase inhibitor, an ergot alkaloid derivative, an inhibitor of 3 β-hydroxysteroid dehydrogenase, a reversible acetylcholinesterase inhibitor, a protease inhibitor, an aldosterone antagonist, a naphthoquinone, and combinations thereof, and a second active agent, which is benznidazole. Also provided are compositions for treating or ameliorating the effects of a Chagas disease. The compositions include azelastine and benznidazole in amounts effective to treat or ameliorate the effect of a Chagas disease and a pharmaceutically acceptable carrier.
• Synthesis and evaluation of benzoxazinone derivatives on activity of human neutrophil elastase and on hemorrhagic shock-induced lung injury in rats
  作者：Pei-Wen Hsieh、Huang-Ping Yu、Yi-Ju Chang、Tsong-Long Hwang

  DOI：10.1016/j.ejmech.2010.03.046

  日期：2010.7

  A new series of benzoxazinone analogs were designed, synthesized, and assayed to determine their effects on superoxide anion generation and neutrophil elastase (NE) release in formyl-L-methionyl-L-leucyl-L-phenylalanine (FMLP)-activated human neutrophils. Of these, compounds 6-10 showed a potent dual inhibitory effect on NE release and superoxide anion generation. In contrast, compounds 11-15 exhibited highly selective and potent inhibitory activities on NE release. These results indicate that the inhibitory activity on NE release in FMLP-activated human neutrophils depended on the position of chloro-substituent in the A ring. On the other hand, 13 significantly attenuated the increase in myeloperoxidase (MPO) activity and edema in the lung of rats after trauma-hemorrhagic shock. Therefore, these compounds could be developed as new NE inhibitors. (c) 2010 Elsevier Masson SAS. All rights reserved.