(+/-)-7-[(7-chloro-2,4(1H,3H)-quinazolinedione-3-yl)sulfonyl]-2-oxo-1H,3H-quinoline-3-carboxylic acid | 259536-85-1

• 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
• 英文名称: (+/-)-7-[(7-chloro-2,4(1H,3H)-quinazolinedione-3-yl)sulfonyl]-2-oxo-1H,3H-quinoline-3-carboxylic acid
• 英文别名: (+/-)-7-[(7-Chloro-2,4 (1H,3H)-Quinazolinedion-3-yl)Sulfonyl]-2-oxo-1H,3H-Quinoline-3-Carboxylic acid；7-[(7-chloro-2,4-dioxo-1H-quinazolin-3-yl)sulfonyl]-2-oxo-3,4-dihydro-1H-quinoline-3-carboxylic acid
• CAS: 259536-85-1
• 化学式: C₁₈H₁₂ClN₃O₇S
• 分子量: 449.828
• InChiKey: MSBQLTQSAOWQIM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  30
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  158
• 氢给体数：
  3
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  (+/-)-3-t-butoxycarbonyl-2-oxo-1H,3H-quinoline-7-sulfonamide 、 benzyl 4-chloro-2-N-phenoxycarbonylanthranilate 生成 (+/-)-7-[(7-chloro-2,4(1H,3H)-quinazolinedione-3-yl)sulfonyl]-2-oxo-1H,3H-quinoline-3-carboxylic 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

• PREVENTIVE OR THERAPEUTIC DRUGS FOR FIBROSIS CONTAINING CHYMASE INHIBITORS AS THE ACTIVE INGREDIENT
  申请人：——

  公开号：US20020183338A1

  公开（公告）日：2002-12-05

  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): 1 or a pharmaceutically acceptable salt thereof is included therein.

  一种预防或治疗皮肤或各种内脏纤维化的药物，含有一种作为有效成分的针对钠胃蛋白酶抑制剂，是一种无副作用、安全的药物，可抑制病情的进展，预防并改善并发症的发展，并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用盐。
• Quinazoline derivatives and pharmaceutical applications thereof
  申请人：Fukami Harukazu

  公开号：US20050148608A1

  公开（公告）日：2005-07-07

  A quinazoline derivative having formula (1) and a pharmacrutically acceptable salt thereof: wherein the ring A represents an aryl group. which derivative has a chymase inhibitory activity and suppresses the exacerbation of cascular permeability induced by chymase, and a pharmaceutical composition containing the same as an essential ingredient. These compounds are useful for treatment of allergic diseases, rheumatic diseases, and cardiac and circulatory system diseases which are due to the abnormal exacerbation of Angiotensin II production.

  具有公式（1）的喹唑啉衍生物及其药学上可接受的盐：其中环A代表芳基基团。该衍生物具有抑制胰蛋白酶活性并抑制由胰蛋白酶诱导的血管通透性加剧的作用，并包含其作为必要成分的药物组合物。这些化合物对于治疗过敏性疾病、风湿性疾病以及由血管紧张素II产生异常加剧引起的心脏和循环系统疾病非常有用。
• 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。
• 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。
• PREVENTIVE OR THERAPEUTIC DRUGS FOR VARIOUS EOSINOPHILIA-RELATED DISEASES CONTAINING CHYMASE INHIBITORS AS THE ACTIVE INGREDIENT
  申请人：SUNTORY LIMITED

  公开号：EP1174151A1

  公开（公告）日：2002-01-23

  A medicament for the prevention or treatment of diseases involving an increase of eosinophils having a chymase inhibitor, as its effective ingredient, which is a safe medicament for the prevention or treatment of diseases accompanied with an increase in eosinophils, which suppresses the progress of the condition, prevents progress 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.

  一种用于预防或治疗涉及嗜酸性粒细胞增加的疾病的药物，以糜蛋白酶抑制剂为有效成分，是一种用于预防或治疗伴有嗜酸性粒细胞增加的疾病的安全药物，可抑制病情发展，防止并发症的发生，提高患者的生活质量，其中包括具有式（I）的喹唑啉衍生物： 或其药学上可接受的盐。