2-苯基[1,3]噁唑并[4,5-c]喹啉-4(5H)-酮 | 132198-53-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 中文名称: 2-苯基[1,3]噁唑并[4,5-c]喹啉-4(5H)-酮
• 英文名称: 2-phenyloxazolo[4,5-c]quinolin-4(5H)-one
• 英文别名: 2-Phenyl-oxazolo(4,5-c)quinolin-4-one；2-phenyl-5H-[1,3]oxazolo[4,5-c]quinolin-4-one
• CAS: 132198-53-9
• 化学式: C₁₆H₁₀N₂O₂
• 分子量: 262.268
• InChiKey: WEVBZMVDUUWBJH-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.9
• 重原子数：
  20
• 可旋转键数：
  1
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  55.1
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-溴-N,N-二甲基乙胺氢溴酸盐 、 2-苯基[1,3]噁唑并[4,5-c]喹啉-4(5H)-酮 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 以39%的产率得到5-(2-(dimethylamino)ethyl)-2-phenyloxazolo[4,5-c]quinolin-4(5H)-one
  参考文献：
  名称：

  恶唑并[4,5-c]-喹啉酮类似物作为新型白细胞介素33抑​​制剂的合理设计、合成和评价

  摘要：

  的恶唑并[4,5-C] -喹啉酮类似物7  Ç是白细胞介素33的第一小分子抑制剂，其结合至IL-33和ST2的在2D NMR研究的接口和白细胞介素的强抑制证明-6 在人类肥大细胞中产生。

  DOI：

  10.1002/asia.202100896
• 作为产物：
  描述：

  2-苯基-4-噁唑羧酸 在 palladium diacetate 、 (benzotriazo-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate 、 caesium carbonate 、 三乙胺 、 三苯基膦 作用下， 以 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 反应 3.0h， 生成 2-苯基[1,3]噁唑并[4,5-c]喹啉-4(5H)-酮
  参考文献：
  名称：

  Synthesis of 2-Aryl-oxazolo[4,5-c]quinoline-4(5H)-ones and 2-Aryl-thiazolo[4,5-c]quinoline-4(5H)-ones

  摘要：

  graphicsNovel and highly efficient syntheses of oxazolo[4,5-c]quinoline-4(5H)-ones (1) and thiazolo[4,5-c]quinoline-4(5H)-ones (2) from ethyl 2-chlorooxazole-4-carboxylate (4) and ethyl 2-bromo-5-chlorothiazole-4-carboxylate (13), respectively, are described.

  DOI：

  10.1021/ol0350285

文献信息

• NOVEL QUINOLINONE DERIVATIVE AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING ALLERGIC DISEASES SUCH AS ASTHMA OR ATOPIC DERMATITIS INCLUDING THE QUINOLINONE DERIVATIVE AS ACTIVE INGREDIENT
  申请人：Korea University Research and Business Foundation, Sejong Campus

  公开号：US20200140457A1

  公开（公告）日：2020-05-07

  The present invention relates to anovel quinolinone derivative compound that regulates intracellular signal transduction mediated by TSLP and IL-33 to exhibit efficacy in preventing or treating allergic diseases such as asthma or atopic dermatitis. The quinolinone derivative compound of the present invention can effectively suppress inflammatory responses of allergic diseases such as asthma or atopic dermatitis. The present invention also relates to a pharmaceutical composition including the quinolinone derivative compound. The pharmaceutical composition of the present invention can be used to fundamentally prevent or treat various allergic and asthmatic diseases.

  本发明涉及一种新型喹诺酮衍生物化合物，通过调节由TSLP和IL-33介导的细胞内信号传导，以在预防或治疗哮喘或特应性皮炎等过敏疾病中发挥功效。本发明的喹诺酮衍生物化合物可以有效抑制哮喘或特应性皮炎等过敏疾病的炎症反应。本发明还涉及包括喹诺酮衍生物化合物的药物组合物。本发明的药物组合物可用于根本预防或治疗各种过敏和哮喘疾病。
• NOVEL QUINOLINONE DERIVATIVE AND PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING ALLERGIC DISEASE SUCH AS ASTHMA OR ATOPY COMPRISING SAME AS ACTIVE INGREDIENT
  申请人：Korea University Research and Business Foundation, Sejong Campus

  公开号：EP3567044A1

  公开（公告）日：2019-11-13

  The present invention relates to a novel quinolinone derivative compound that regulates intracellular signal transduction mediated by TSLP and IL-33 to exhibit efficacy in preventing or treating allergic diseases such as asthma or atopic dermatitis. The quinolinone derivative compound of the present invention can effectively suppress inflammatory responses of allergic diseases such as asthma or atopic dermatitis. The present invention also relates to a pharmaceutical composition including the quinolinone derivative compound. The pharmaceutical composition of the present invention can be used to fundamentally prevent or treat various allergic and asthmatic diseases.

  本发明涉及一种新型喹啉酮衍生物化合物，该化合物可调节由 TSLP 和 IL-33 介导的细胞内信号转导，从而在预防或治疗哮喘或特应性皮炎等过敏性疾病方面发挥功效。 本发明的喹啉酮衍生物化合物可有效抑制哮喘或特应性皮炎等过敏性疾病的炎症反应。 本发明还涉及一种包括喹啉酮衍生物化合物的药物组合物。 本发明的药物组合物可用于从根本上预防或治疗各种过敏性疾病和哮喘疾病。
• Quinolinone derivative and pharmaceutical composition for preventing or treating allergic diseases such as asthma or atopic dermatitis including the quinolinone derivative as active ingredient
  申请人：Azcuris Co., Ltd.

  公开号：US11168094B2

  公开（公告）日：2021-11-09

  The present invention relates to a novel quinolinone derivative compound that regulates intracellular signal transduction mediated by TSLP and IL-33 to exhibit efficacy in preventing or treating allergic diseases such as asthma or atopic dermatitis. The quinolinone derivative compound of the present invention can effectively suppress inflammatory responses of allergic diseases such as asthma or atopic dermatitis. The present invention also relates to a pharmaceutical composition including the quinolinone derivative compound. The pharmaceutical composition of the present invention can be used to fundamentally prevent or treat various allergic and asthmatic diseases.

  本发明涉及一种新型喹啉酮衍生物化合物，该化合物可调节由 TSLP 和 IL-33 介导的细胞内信号转导，从而在预防或治疗哮喘或特应性皮炎等过敏性疾病方面发挥功效。本发明的喹啉酮衍生物化合物可有效抑制哮喘或特应性皮炎等过敏性疾病的炎症反应。本发明还涉及一种包括喹啉酮衍生物化合物的药物组合物。本发明的药物组合物可用于从根本上预防或治疗各种过敏性疾病和哮喘疾病。
• 4-Hydroxy-2-quinolones. 36. Synthesis of 2-R-oxazolo[4,5-c]quinolin-4(5H)-ones
  作者：I. V. Ukrainets、S. G. Taran、L. V. Sidorenko、O. V. Gorokhova、A. V. Turov

  DOI：10.1007/bf02320336

  日期：1997.11
• US5182290A
  申请人：——

  公开号：US5182290A

  公开（公告）日：1993-01-26