3,5-diamino-6-chloro-N-[8-[4-[[6-[(2S)-2-hydroxybutoxy]naphthalen-2-yl]methoxy]benzoyl]-1,3,8-triazaspiro[4.5]dec-2-en-2-yl]pyrazine-2-carboxamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: 3,5-diamino-6-chloro-N-[8-[4-[[6-[(2S)-2-hydroxybutoxy]naphthalen-2-yl]methoxy]benzoyl]-1,3,8-triazaspiro[4.5]dec-2-en-2-yl]pyrazine-2-carboxamide
• 化学式: C₃₄H₃₇ClN₈O₅
• 分子量: 673.2
• InChiKey: HDCKQVPQOSHPHM-DEOSSOPVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4
• 重原子数：
  48
• 可旋转键数：
  10
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.32
• 拓扑面积：
  190
• 氢给体数：
  5
• 氢受体数：
  10

文献信息

• TREATING DISEASES MEDIATED BY BLOCKADE OF THE EPITHELIAL SODIUM CHANNEL WITH PYRAZINE-2-CARBOXAMIDE DERIVATIVES
  申请人：Bhalay Gurdip

  公开号：US20140171421A1

  公开（公告）日：2014-06-19

  A compound of Formula I in free or salt or solvate form, where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 and R 11 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

  式I的化合物以自由形式、盐形式或溶剂形式存在，其中R1、R2、R3、R4、R5、R6、R7、R8、R9、R10和R11的含义如规范中所示，可用于治疗对上皮钠通道阻滞有反应的疾病。还描述了含有这些化合物的制药组合物和制备这些化合物的过程。
• Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases
  申请人：Vertex Pharmaceuticals Incorporated

  公开号：US20140329814A2

  公开（公告）日：2014-11-06

  The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.

  本发明涉及制药组合物，包括上皮钠通道活性抑制剂与至少一种ABC转运蛋白调节剂化合物，该化合物为公式A、公式B、公式C或公式D。本发明还涉及该制药组合物的制药配方，以及使用该组合物治疗CFTR介导的疾病，特别是囊性纤维化的方法。