4-bromo-3-chloro-N-(thiazol-2-yl)benzenesulfonamide | 1104807-01-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4-bromo-3-chloro-N-(thiazol-2-yl)benzenesulfonamide
• 英文别名: 4-bromo-3-chloro-N-(1,3-thiazol-2-yl)benzenesulfonamide
• CAS: 1104807-01-3
• 化学式: C₉H₆BrClN₂O₂S₂
• 分子量: 353.648
• InChiKey: VZDDFMRLWYZCHN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.1
• 重原子数：
  17
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  95.7
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-bromo-3-chloro-N-(thiazol-2-yl)benzenesulfonamide 、 1-(1-甲基-1H-吡唑)-乙胺 在 tris-(dibenzylideneacetone)dipalladium(0) 、 sodium t-butanolate 、 2-二-叔丁膦基-2',4',6'-三异丙基联苯 作用下， 以 甲苯 为溶剂， 反应 72.0h， 以5%的产率得到3-chloro-4-((1-(1-methyl-1H-pyrazol-4-yl)ethyl)amino)-N-(thiazol-2-yl)benzenesulfonamide
  参考文献：
  名称：

  BENZENESULFONAMIDE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS

  摘要：

  这项发明涉及苯磺酰胺化合物，作为其立体异构体、对映异构体、互变异构体或它们的混合物；或其药学上可接受的盐、溶剂合物或前药，用于治疗与电压门控钠通道相关的疾病或症状，如癫痫和/或癫痫发作障碍。

  公开号：

  US20180162868A1
• 作为产物：
  描述：

  2-氨基噻唑 、 4-溴-3-氯苯磺酰氯 在 吡啶 作用下， 以 二氯甲烷 为溶剂， 反应 16.0h， 以58%的产率得到4-bromo-3-chloro-N-(thiazol-2-yl)benzenesulfonamide
  参考文献：
  名称：

  BENZENESULFONAMIDE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS

  摘要：

  这项发明涉及苯磺酰胺化合物，作为其立体异构体、对映异构体、互变异构体或它们的混合物；或其药学上可接受的盐、溶剂合物或前药，用于治疗与电压门控钠通道相关的疾病或症状，如癫痫和/或癫痫发作障碍。

  公开号：

  US20180162868A1

文献信息

• SODIUM CHANNEL INHIBITORS
  申请人：Fulp Alan Bradley

  公开号：US20090023740A1

  公开（公告）日：2009-01-22

  Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.

  提供了在通过抑制电压门控钠通道中的钠离子通量来治疗疾病方面有用的化合物、组合物和方法。更具体地，本发明提供了取代磺胺基的化合物、包含这些化合物的组合物，以及使用这些化合物或组合物治疗中枢或外周神经系统疾病的方法，特别是通过阻断与所示疾病的发作或复发相关的钠通道来治疗疼痛和慢性疼痛。本发明的化合物、组合物和方法特别适用于通过抑制电压门控钠通道中的离子通量来治疗神经病理性或炎症性疼痛。
• Sodium channel inhibitors
  申请人：Icagen Inc.

  公开号：US08124610B2

  公开（公告）日：2012-02-28

  Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.

  本发明提供了一种通过抑制电压门控钠通道中的钠离子流来治疗疾病的化合物、组合物和方法。具体而言，本发明提供了取代磺酰胺的化合物、包含这些化合物的组合物以及使用这些化合物或组合物治疗中枢或外周神经系统疾病，尤其是疼痛和慢性疼痛的方法，通过阻断与所述疾病的发生或复发有关的钠通道。本发明的化合物、组合物和方法特别适用于通过抑制电压门控钠通道中的离子流来治疗神经病理性或炎性疼痛。
• Benzenesulfonamide compouds and their use as therapeutic agents
  申请人：Xenon Pharmaceuticals Inc.

  公开号：US11174268B2

  公开（公告）日：2021-11-16

  This invention is directed to benzenesulfonamide compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment of diseases or conditions associated with voltage-gated sodium channels, such as epilepsy and/or epileptic seizure disorders.

  本发明涉及苯磺酰胺化合物，作为其立体异构体、对映体、同系物或其混合物；或其药学上可接受的盐、溶液剂或原药，用于治疗与电压门控钠通道相关的疾病或病症，如癫痫和/或癫痫发作性疾病。
• US8124610B2
  申请人：——

  公开号：US8124610B2

  公开（公告）日：2012-02-28
• [EN] SODIUM CHANNEL INHIBITORS<br/>[FR] INHIBITEURS DES CANAUX SODIQUES
  申请人：ICAGEN INC

  公开号：WO2009012242A2

  公开（公告）日：2009-01-22

  Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted sulfonamides, compos i-tiona comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel. Formula (II)