4-Amino-8-(4-chlorophenyl)-7-methylpyrazolo[5,1-c][1,2,4]triazine-3-carboxylic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 英文名称: 4-Amino-8-(4-chlorophenyl)-7-methylpyrazolo[5,1-c][1,2,4]triazine-3-carboxylic acid
• 英文别名: 4-amino-8-(4-chlorophenyl)-7-methylpyrazolo[5,1-c][1,2,4]triazine-3-carboxylic acid
• 化学式: C₁₃H₁₀ClN₅O₂
• 分子量: 303.7
• InChiKey: GEDLMDOYDCEYCY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  21
• 可旋转键数：
  2
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  106
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• [EN] SMALL MOLECULE CFTR CORRECTORS<br/>[FR] CORRECTEURS DE CFTR À PETITES MOLÉCULES
  申请人：DISCOVERYBIOMED INC

  公开号：WO2014081820A1

  公开（公告）日：2014-05-30

  Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of rescuing halide efflux in a cell, correcting a processing defect of a delF508-CFTR protein in a cell, and correcting functional delF508-CFTR chloride channels in a cell are also provided.

  提供了一种能有效拯救卤化物外流、delF508-CFTR蛋白加工以及细胞顶端功能氯离子输运的新型CFTR校正化合物。还提供了治疗蛋白质折叠障碍（例如囊性纤维化）的方法。这些方法包括给予CFTR校正化合物或其药用盐或前药。还提供了在细胞中拯救卤化物外流、纠正细胞中delF508-CFTR蛋白的加工缺陷以及纠正细胞中功能性delF508-CFTR氯通道的方法。
• SMALL MOLECULE CFTR CORRECTORS
  申请人：DISCOVERYBIOMED, INC.

  公开号：US20150299206A1

  公开（公告）日：2015-10-22

  Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of rescuing halide efflux in a cell, correcting a processing defect of a delF508-CFTR protein in a cell, and correcting functional delF508-CFTR chloride channels in a cell are also provided.
• US9676779B2
  申请人：——

  公开号：US9676779B2

  公开（公告）日：2017-06-13