6-(Ethylphenylsulfamoyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid cycloheptylamide

• 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: 6-(Ethylphenylsulfamoyl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid cycloheptylamide
• 英文别名: N-cycloheptyl-6-[ethyl(phenyl)sulfamoyl]-4-oxo-1H-quinoline-3-carboxamide
• 化学式: C₂₅H₂₉N₃O₄S
• mdl: MFCD15109818
• 分子量: 467.6
• InChiKey: OGVDEAPJBRGQIE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  33
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  104
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Modulators of Cystic Fibrosis Transmembrane Conductance Regulator
  申请人：VERTEX PHARMACEUTICALS INCORPORATED

  公开号：US20160095858A1

  公开（公告）日：2016-04-07

  The present invention features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R 1 , R 2 , R 3 , W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.

  本发明涉及一种具有以下化学式I的化合物： 或其药用可接受的盐，其中R 1 ，R 2 ，R 3 ，W，X，Y，Z，n，o，p和q在此处定义，用于治疗CFTR介导的疾病，如囊性纤维化。本发明还涉及药物组合物、治疗方法和相关工具包。
• [EN] MODULATORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR<br/>[FR] MODULATEURS DU RÉGULATEUR DE LA CONDUCTANCE TRANSMEMBRANAIRE DE LA FIBROSE KYSTIQUE
  申请人：VERTEX PHARMA

  公开号：WO2017173274A1

  公开（公告）日：2017-10-05

  The present disclosure features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, W, X, Z, n, p, and Rings A and B are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present disclosure also features pharmaceutical compositions, method of treating, and kits thereof.

  本公开涉及一种具有化学式I的化合物：或其药用可接受的盐，其中R1、R2、W、X、Z、n、p以及环A和环B在此处被定义，用于治疗CFTR介导的疾病，如囊性纤维化。本公开还涉及药物组合物、治疗方法以及相关工具包。
• Compositions and methods for treating disorders associated with salt or fluid retention
  申请人：Ironwood Pharmaceuticals, Inc.

  公开号：EP2671584A2

  公开（公告）日：2013-12-11

  Methods for reducing the risk of or treating a disorder associated with fluid and/or salt retention in a patient are described. The methods include administering to the patient an agent selected from: a) an agent that reduces sodium absorption in the intestine; b) an agent that increases anion secretion in the intestine; or c) an agent that both reduces sodium absorption in the intestine and increases anion secretion in the intestine.

  本文描述了降低患者发生与体液和/或盐潴留有关的疾病的风险或治疗这种疾病的方法。这些方法包括向患者施用选自以下几种的制剂：a) 减少肠道钠吸收的制剂；b) 增加肠道阴离子分泌的制剂；或 c) 既减少肠道钠吸收又增加肠道阴离子分泌的制剂。
• Modulators of cystic fibrosis transmembrane conductance regulator
  申请人：Vertex Pharmaceuticals Incorporated

  公开号：US10258624B2

  公开（公告）日：2019-04-16

  The present invention features a compound of formula I: or a pharmaceutically acceptable salt thereof, where R1, R2, R3, W, X, Y, Z, n, o, p, and q are defined herein, for the treatment of CFTR mediated diseases, such as cystic fibrosis. The present invention also features pharmaceutical compositions, method of treating, and kits thereof.

  本发明的特征是一种式 I 的化合物： 或其药学上可接受的盐，其中 R1、R2、R3、W、X、Y、Z、n、o、p 和 q 在本文中定义，用于治疗 CFTR 介导的疾病，如囊性纤维化。本发明还包括药物组合物、治疗方法及其试剂盒。
• Methods for increasing CFTR activity
  申请人：THE UAB RESEARCH FOUNDATION

  公开号：US10300052B2

  公开（公告）日：2019-05-28

  The present disclosure provides compounds effective in increasing mucociliary clearance in a subject. In one embodiment, the compounds are of the general formula I. The present disclosure further shows that such compounds are effective in increasing activation of the CFTR, thereby increasing mucociliary clearance in the subject. The present disclosure further shows that such compounds are effective in increasing the depth of ASL, thereby increasing mucociliary clearance in the subject. In one embodiment of each of the foregoing, the subject is free from congenital or genetic defect in the cellular mucociliary clearance apparatus and/or acquired abnormality in the cellular mucociliary clearance apparatus.

  本公开提供了能有效提高受试者粘膜清除率的化合物。在一个实施方案中，化合物为通式 I。本公开进一步表明，此类化合物能有效增加 CFTR 的活化，从而增加受试者的粘液纤毛清除率。本公开进一步表明，此类化合物能有效增加 ASL 深度，从而增加受试者的粘液纤毛清除率。在上述各项的一个实施方案中，受试者没有细胞粘液纤毛清除装置的先天或遗传缺陷和/或细胞粘液纤毛清除装置的后天异常。