N-(5-chlorothiazol-2-yl)-6-fluoro-1-((1,2,3,4-tetrahydroisoquinolin-8-yl)methyl)-1H-indazole-5-sulfonamide | 1608479-60-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: N-(5-chlorothiazol-2-yl)-6-fluoro-1-((1,2,3,4-tetrahydroisoquinolin-8-yl)methyl)-1H-indazole-5-sulfonamide
• 英文别名: N-(5-chloro-1,3-thiazol-2-yl)-6-fluoro-1-(1,2,3,4-tetrahydroisoquinolin-8-ylmethyl)indazole-5-sulfonamide
• CAS: 1608479-60-2
• 化学式: C₂₀H₁₇ClFN₅O₂S₂
• 分子量: 477.971
• InChiKey: OJFGKCLKLHOZNY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.5
• 重原子数：
  31
• 可旋转键数：
  5
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.2
• 拓扑面积：
  126
• 氢给体数：
  2
• 氢受体数：
  8

文献信息

• [EN] N-SUBSTITUTED INDAZOLE SULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS<br/>[FR] COMPOSÉS INDAZOLE SULFONAMIDE N-SUBSTITUÉS AYANT UNE ACTIVITÉ SÉLECTIVE DANS LES CANAUX SODIQUES POTENTIEL-DÉPENDANTS
  申请人：MERCK SHARP & DOHME

  公开号：WO2014066491A1

  公开（公告）日：2014-05-01

  Disclosed are compounds of Formula AA and Formula AB: wherein "Heteroaryl-1", RA1, RA2, RB1, and RC are defined herein, which novel compounds have properties for blocking Nav 1.7 ion channels found in peripherial and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formulae AA and AB or their salts, and methods of treating neuropathic pain disorders using the same.

  本发明涉及AA式和AB式化合物：其中“杂环芳基-1”，RA1、RA2、RB1和RC的定义如本文中所述，这些新型化合物具有阻止周围和交感神经元中发现的Nav 1.7离子通道的特性。还描述了包含AA式和AB式化合物或其盐的制药配方，并且使用它们治疗神经病理性疼痛障碍的方法。
• BENZOXAZOLINONE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS
  申请人：Merck Sharp & Dohme Corp.

  公开号：US20150252034A1

  公开（公告）日：2015-09-10

  Disclosed are compounds of Formula A: Formula A, or a salt thereof, wherein “Het”, R a , and R b are defined herein, which have properties for blocking Na v 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating neuropathic pain disorders using the same.

  本发明涉及A式化合物：A式，或其盐，其中“Het”，Ra和Rb的定义在此处，具有阻断外周和交感神经元中发现的Nav1.7离子通道的特性。还描述了包含A式化合物或其盐的药物制剂，以及使用它们治疗神经病理性疼痛障碍的方法。
• N-SUBSTITUTED INDAZOLE SULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS
  申请人：Merck Sharp & Dohme Corp.

  公开号：US20150284389A1

  公开（公告）日：2015-10-08

  Disclosed are compounds of Formula A A and Formula A B : wherein “Heteroaryl-1”, R A1 , R A2 , R B1 , and R C are defined herein, which novel compounds have properties for blocking Na 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formulae A A and A B or their salts, and methods of treating neuropathic pain disorders using the same.

  本发明涉及式AA和式AB的化合物：其中“Heteroaryl-1”，RA1，RA2，RB1和RC在此定义，这些新型化合物具有阻断周围和交感神经元中发现的Na 1.7离子通道的特性。还描述了包含式AA和AB或其盐的制药配方，以及使用它们治疗神经病理性疼痛障碍的方法。
• US9388179B2
  申请人：——

  公开号：US9388179B2

  公开（公告）日：2016-07-12