4-[(7-chloro-2,4(1H,3H)-quinazolinedione-3-yl)sulfonyl]salicylic acid

• 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: 4-[(7-chloro-2,4(1H,3H)-quinazolinedione-3-yl)sulfonyl]salicylic acid
• 英文别名: 4-[(7-chloro-2,4 (1H,3H)-quinazolinedion-3-yl)sulfonyl]salicylic Acid；4-[(7-chloro-2,4-dioxo-1H-quinazolin-3-yl)sulfonyl]-2-hydroxybenzoic acid
• 化学式: C₁₅H₉ClN₂O₇S
• 分子量: 396.765
• InChiKey: VQGGMADIEHAKNW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  26
• 可旋转键数：
  3
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  150
• 氢给体数：
  3
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  4-[(7-chloro-2,4(1H,3H)-quinazolinedione-3-yl)sulfonyl]salicylic acid 在 sodium hydroxide 作用下， 以 四氢呋喃 、 水 为溶剂， 生成 4-[(7-chloro-2,4(1H,3H)-quinazolinedione-3-yl)sulfonyl]salicylic acid monosodium salt
  参考文献：
  名称：

  Quinazoline derivatives and pharmaceutical applications thereof

  摘要：

  一种具有化学式（1）的喹唑啉衍生物及其药用盐：其中环A代表芳基，该衍生物具有针对钳酶的抑制活性，可抑制钳酶诱导的血管通透性加剧，并且含有该衍生物作为主要成分的药物组合物。这些化合物可用于治疗由于Angiotensin II产生异常加剧而导致的过敏性疾病、风湿性疾病以及心脏和循环系统疾病。

  公开号：

  US06867214B1
• 作为产物：
  描述：

  methyl 4-chloro-2-phenoxycarbonyl-aminobenzoate 、 4-t-butoxycarbonyl-3-hydroxybenzenesulfonamide 生成 4-[(7-chloro-2,4(1H,3H)-quinazolinedione-3-yl)sulfonyl]salicylic acid
  参考文献：
  名称：

  Medicament for prevention and treatment of dermatitis having chymase inhibitor as effective ingredient

  摘要：

  一种安全且无副作用的药物，用于预防或治疗表现为双相炎症反应的皮炎或由重复暴露于抗原引起的皮炎，该药物抑制病情进展并改善患者的生活质量，其中包括一种喹唑啉衍生物，其具有公式（I）或（II）或其药学上可接受的盐作为有效成分，用于治疗表现为双相炎症反应的皮炎或由重复暴露于抗原引起的皮炎。

  公开号：

  US20020183339A1

文献信息

• Medicament for prevention and treatment of dermatitis having chymase inhibitor as effective ingredient
  申请人：——

  公开号：US20020183339A1

  公开（公告）日：2002-12-05

  A medicament safe and free from side effects, for the prevention or treatment of dermatitis exhibiting a biphasic inflammation reaction or dermatitis induced by repeated exposure to an antigen, which suppresses the progress of the condition and improves the quality of life of the patient, which medicament treats dermatitis exhibiting a biphasic inflammation reaction or dermatitis induced by repeated exposure to an antigen by including a quiazoline derivative having the formula (I) or (II) or its pharmaceutically acceptable salt as an effective ingredient: 1

  一种安全且无副作用的药物，用于预防或治疗表现为双相炎症反应的皮炎或由重复暴露于抗原引起的皮炎，该药物抑制病情进展并改善患者的生活质量，其中包括一种喹唑啉衍生物，其具有公式（I）或（II）或其药学上可接受的盐作为有效成分，用于治疗表现为双相炎症反应的皮炎或由重复暴露于抗原引起的皮炎。
• METHOD OF TREATING DERMATITIS COMPRISING ADMINISTERING A CHYMASE INHIBITOR
  申请人：Fukami Harukazu

  公开号：US20100029695A1

  公开（公告）日：2010-02-04

  A medicament safe and free from side effects, for the prevention or treatment of dermatitis exhibiting a biphasic inflammation reaction or dermatitis induced by repeated exposure to an antigen, which suppresses the progress of the condition and improves the quality of life of the patient, which medicament treats dermatitis exhibiting a biphasic inflammation reaction or dermatitis induced by repeated exposure to an antigen by including a quiazoline derivative having the formula (I) or (II) or its pharmaceutically acceptable salt as an effective ingredient:

  一种安全且无副作用的药物，用于预防或治疗表现为双相炎症反应的皮炎或由重复接触抗原引起的皮炎，该药物抑制疾病的进展并改善患者的生活质量。该药物通过将具有公式（I）或（II）的喹唑啉衍生物或其药学上可接受的盐作为有效成分来治疗表现为双相炎症反应的皮炎或由重复接触抗原引起的皮炎。
• Preventive or therapeutic drugs for fibrosis containing chymase inhibitors as the active ingredient
  申请人：Suntory Limited

  公开号：US06500835B2

  公开（公告）日：2002-12-31

  A medicament for the prevention or treatment containing a chymase inhibitor, as an effective component, which is a side effect-free, safe medicament for prevention or treatment of fibrosis of the skin or various viscera which suppresses the progression of the condition, prevents the progression of complications, and improves the quality of life of the patient, wherein a quinazoline derivative having the formula (I): or a pharmaceutically acceptable salt thereof is included therein.

  一种药物，用于预防或治疗纤维化，其有效成分为一种无副作用、安全的基质酶抑制剂，可抑制病情进展，预防并发症的进展，提高患者的生活质量。其中包括具有以下结构式（I）的喹唑啉衍生物或其药学上可接受的盐。
• Method of treating dermatitis comprising administering a chymase inhibitor
  申请人：Asubio Pharma Co., Ltd.

  公开号：US07618977B2

  公开（公告）日：2009-11-17

  Medicaments for the treatment of dermatitis exhibiting a biphasic inflammation reaction or dermatitis induced by repeated exposure to an antigen, having quinazolidone derivatives of formula I or II that are herein defined, are disclosed.

  本文揭示了用公式I或II所定义的喹唑酮衍生物治疗表现为双相炎症反应或由重复暴露于抗原引起的皮炎的药物。
• INHIBITORS AGAINST VASCULAR LIPID DEPOSITION CONTAINING CHYMASE-INHIBITING SUBSTANCES
  申请人：SUNTORY LIMITED

  公开号：EP1142586A1

  公开（公告）日：2001-10-10

  There is provided a preventive or therapeutic agent for diseases accompanied by abnormal vascular function in which lipid deposition in the blood vessel is involved, said agent comprising a chymase inhibitor as an active ingredient. As the chymase inhibitor, a quinazoline derivative represented by the following formula is used. In the above formula, the ring A represents an aromatic ring.

  本发明提供了一种预防或治疗剂，用于治疗伴有血管功能异常的疾病，其中涉及血管中的脂质沉积，所述制剂包括作为活性成分的糜蛋白酶抑制剂。 作为糜蛋白酶抑制剂，使用了由下式表示的喹唑啉衍生物。 在上式中，环 A 代表芳香环。