N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide | 219963-52-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二嗪烷类
• 英文名称: N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide
• 英文别名: SB 357134
• CAS: 219963-52-7
• 化学式: C₁₇H₁₈Br₂FN₃O₃S
• 分子量: 523.221
• InChiKey: BLWHAZZXRHTFJE-UHFFFAOYSA-N

物化性质

• 沸点：
  607.1±65.0 °C(Predicted)
• 密度：
  1.701±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  27
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  79
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  1-(2-甲氧苯基)哌嗪 在 吡啶 、 氯磺酸 、 氢氧化钾 、 N,N-二异丙基乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 、 1,2-二氯乙烷 为溶剂， 反应 40.0h， 生成 N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide
  参考文献：
  名称：

  Phenyl benzenesulfonamides are novel and selective 5-HT6 antagonists: identification of N-(2,5-dibromo-3-fluorophenyl)-4-methoxy-3-piperazin-1-ylbenzenesulfonamide (SB-357134)

  摘要：

  Substituted N-phenyl-4-methoxy-3-piperazin-1-ylbenzenesulfonamides and conformationally restricted analogues have been identified as high affinity and selective 5-HT6 antagonists. Compounds from this series had a range of pharmacokinetic profiles in rat and in general there was a correlation between clearance and CNS penetration. Based on its overall biological profile 2 (SB-357134) was selected for further pre-clinical evaluation. (C) 2000 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(00)00597-7

文献信息

• [EN] AMINO ARYLSULFONAMIDE COMPOUNDS AND THEIR USE AS 5-HT6 LIGANDS FIELD OF INVENTION<br/>[FR] COMPOSÉS D'AMINOARYLSULFONAMIDE ET LEUR UTILISATION COMME LIGANDS DE 5-HT6
  申请人：SUVEN LIFE SCIENCES LTD

  公开号：WO2009053997A1

  公开（公告）日：2009-04-30

  The present invention relates to novel amino arylsulfonamide compounds of the formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them: The present invention also relates to a process for the preparation of above said novel compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The compounds of the invention are useful in the treatment of various disorders that are related to 5-HT6 receptor functions. Specifically, the compounds of this invention are also useful in the treatment of various CNS disorders, hematological disorders, eating disorders, obesity, anxiety, depression, diseases associated with pain, respiratory diseases, gastrointestinal, cardiovascular diseases and cancer.

  本发明涉及一种新型氨基芳基磺酰胺化合物的公式(I)，其衍生物，其立体异构体，其药学上可接受的盐以及含有它们的药学上可接受的组合物：本发明还涉及制备上述新型化合物、其衍生物、其立体异构体、其药学上可接受的盐以及含有它们的药学上可接受的组合物的方法。本发明的化合物在治疗与5-HT6受体功能相关的各种疾病方面具有用途。具体而言，本发明的化合物还可用于治疗各种中枢神经系统疾病、血液学疾病、进食障碍、肥胖、焦虑、抑郁、与疼痛有关的疾病、呼吸系统疾病、消化系统疾病、心血管疾病和癌症。
• AMINO ARYLSULFONAMIDE COMPOUNDS AND THEIR USE AS 5-HT6 LIGANDS
  申请人：Ramakrishna Nirogi Venkata Satya

  公开号：US20100216861A1

  公开（公告）日：2010-08-26

  The present invention relates to novel amino arylsulfonamide compounds of the formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them: The present invention also relates to a process for the preparation of above said novel compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The compounds of the invention are useful in the treatment of various disorders that are related to 5-HT 6 receptor functions. Specifically, the compounds of this invention are also useful in the treatment of various CNS disorders, hematological disorders, eating disorders, obesity, anxiety, depression, diseases associated with pain, respiratory diseases, gastrointestinal, cardiovascular diseases and cancer.

  本发明涉及一种新型氨基芳基磺酰胺化合物的公式（I），它们的衍生物，立体异构体，其药用可接受盐和含有它们的药用可接受组合物：本发明还涉及上述新型化合物的制备方法，它们的衍生物，立体异构体，其药用可接受盐和含有它们的药用可接受组合物。本发明的化合物在治疗与5-HT6受体功能相关的各种疾病方面具有用途。具体来说，本发明的化合物也在治疗各种中枢神经系统疾病，血液疾病，进食障碍，肥胖，焦虑，抑郁，与疼痛有关的疾病，呼吸系统疾病，胃肠道疾病，心血管疾病和癌症方面具有用途。
• [EN] SUBSTITUTED INDOLYL COMPOUNDS AND THEIR USE AS 5-HT6 LIGANDS<br/>[FR] COMPOSÉS INDOLYLE SUBSTITUÉS ET LEUR UTILISATION EN TANT QUE LIGANDS DE 5-HT6
  申请人：SUVEN LIFE SCIENCES LTD

  公开号：WO2009034581A1

  公开（公告）日：2009-03-19

  The present invention relates to novel substituted indolyl compounds of formula (I), their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, their derivatives, their stereoisomers, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions containing them. This invention also relates to the novel intermediates involved therein and process of their preparation. These compounds are useful in the treatment of various disorders that are related to 5-HT6 receptor functions.

  本发明涉及公式（I）的新型取代吲哚基化合物，其衍生物，其立体异构体，其药学上可接受的盐和含有它们的药学上可接受的组合物。本发明还涉及上述新型化合物，其衍生物，其立体异构体，其药学上可接受的盐和含有它们的药学上可接受的组合物的制备方法。本发明还涉及其中涉及的新型中间体及其制备方法。这些化合物在治疗与5-HT6受体功能相关的各种疾病中有用。
• [EN] N-(3,5-DICHLORO-2-METHOXYPHENYL)-4-METHOXY-3-PIPERAZIN-1-YL-BENZENESULFONAMIDE<br/>[FR] N-(3,5-DICHLORO-2-METHOXYPHENYL)-4-METHOXY-3-PIPERAZIN-1-YL-BENZENESULFONAMIDE
  申请人：SMITHKLINE BEECHAM PLC

  公开号：WO2002018358A1

  公开（公告）日：2002-03-07

  The invention relates to a novel sulfonamide compound having pharmacological activity, a process for its preparation, to compositions containing the same and to its use in the treatment of various disorders, particularly CNS disorders.

  本发明涉及一种具有药理活性的新型磺酰胺化合物，其制备方法，含有该化合物的组合物以及在治疗各种疾病，特别是中枢神经系统疾病方面的应用。
• N-(3,5-dichloro-2-methoxyphenyl)-4-methoxy-3-piperazin-1-yl-benzenesulfonamide
  申请人：——

  公开号：US20040034036A1

  公开（公告）日：2004-02-19

  The invention relates to a novel sulfonamide compound having pharmacological activity, a process for its preparation, to compositions containing the same and to its use in the treatment of various disorders, particularly CNS disorders.

  该发明涉及一种具有药理活性的新型磺酰胺化合物，其制备过程，含有该化合物的组合物以及其在治疗各种疾病，特别是中枢神经系统疾病中的应用。