6-(8-chloro-10,11-dihydro-5H-dibenzo[b,f]azepin-2-yl)picolinamide

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯氮卓类
• 英文名称: 6-(8-chloro-10,11-dihydro-5H-dibenzo[b,f]azepin-2-yl)picolinamide
• 英文别名: 6-(3-chloro-6,11-dihydro-5H-benzo[b][1]benzazepin-8-yl)pyridine-2-carboxamide
• 化学式: C₂₀H₁₆ClN₃O
• 分子量: 349.82
• InChiKey: DHGZFNINOOBXHZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.2
• 重原子数：
  25
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  68
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  亚氨基二苄 在 bis-triphenylphosphine-palladium(II) chloride 、 (1,1'-bis(diphenylphosphino)ferrocene)palladium(II) dichloride 、 N-氯代丁二酰亚胺 、 N-溴代丁二酰亚胺(NBS) 、 potassium acetate 、 silica gel 、 sodium carbonate 作用下， 以 1,4-二氧六环 、 乙二醇二甲醚 、 乙醇 、 氯仿 、 水 为溶剂， 反应 31.5h， 生成 6-(8-chloro-10,11-dihydro-5H-dibenzo[b,f]azepin-2-yl)picolinamide
  参考文献：
  名称：

  Dibenzazepines and dibenzoxazepines as sodium channel blockers

  摘要：

  We have identified two related series of dibenzazepine and dibenzoxazepine sodium channel blockers, which showed good potency on Na(v)1.7 in FLIPR- based and electrophysiological functional assays. (C) 2014 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2014.11.025

文献信息

• DIBENZAZEPINE DERIVATIVES AND USE THEREOF
  申请人：Purdue Pharma L.P.

  公开号：US20150175569A1

  公开（公告）日：2015-06-25

  The present disclosure provides dibenzazepine derivatives having Formula I or I(A): and the pharmaceutically acceptable salts and solvates thereof, wherein R 3a , R 3b , R 6 , V 1 , V 2 , Z 1 , Z 2 , Z 3 , and G are defined as set forth in the specification. The present disclosure is also directed to the use of the compounds of Formula I or I(A), and the pharmaceutically acceptable salts or solvates thereof, to treat a disorder responsive to the blockade of one or more sodium channels. In one embodiment, the compounds of the present disclosure are useful for treating pain.

  本公开提供具有化学式I或I(A)的二苯并蒽啉衍生物及其药学上可接受的盐和溶剂化合物，其中R3a、R3b、R6、V1、V2、Z1、Z2、Z3和G的定义如规范中所述。本公开还涉及使用化合物I或I(A)及其药学上可接受的盐或溶剂化合物来治疗对阻断一个或多个钠通道敏感的疾病。在一个实施例中，本公开的化合物对治疗疼痛有用。
• Dibenzazepine derivatives and use thereof
  申请人：Purdue Pharma L.P.

  公开号：US10125113B2

  公开（公告）日：2018-11-13

  The present disclosure provides dibenzazepine derivatives having Formula I or I(A): and the pharmaceutically acceptable salts and solvates thereof, wherein R3a, R3b, R6, V1, V2, Z1, Z2, Z3, and G are defined as set forth in the specification. The present disclosure is also directed to the use of the compounds of Formula I or I(A), and the pharmaceutically acceptable salts or solvates thereof, to treat a disorder responsive to the blockade of one or more sodium channels. In one embodiment, the compounds of the present disclosure are useful for treating pain.

  本公开提供了具有式 I 或 I(A)的二苯并氮杂卓衍生物： 及其药学上可接受的盐和溶液，其中 R3a、R3b、R6、V1、V2、Z1、Z2、Z3 和 G 的定义如说明书所述。本公开还涉及式 I 或 I(A)化合物及其药学上可接受的盐或溶解物用于治疗对阻断一种或多种钠通道有反应的紊乱。在一个实施方案中，本公开的化合物可用于治疗疼痛。
• US9695144B2
  申请人：——

  公开号：US9695144B2

  公开（公告）日：2017-07-04
• Dibenzazepines and dibenzoxazepines as sodium channel blockers
  作者：Stephen M. Lynch、Laykea Tafesse、Kevin Carlin、Parijat Ghatak、Donald J. Kyle

  DOI：10.1016/j.bmcl.2014.11.025

  日期：2015.1

  We have identified two related series of dibenzazepine and dibenzoxazepine sodium channel blockers, which showed good potency on Na(v)1.7 in FLIPR- based and electrophysiological functional assays. (C) 2014 Elsevier Ltd. All rights reserved.