1-Methanesulfonyl-3-(4-phenoxyphenyl)-1H-pyrazole | 299206-37-4

• 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: 1-Methanesulfonyl-3-(4-phenoxyphenyl)-1H-pyrazole
• 英文别名: 1-methylsulfonyl-3-(4-phenoxyphenyl)pyrazole
• CAS: 299206-37-4
• 化学式: C₁₆H₁₄N₂O₃S
• 分子量: 314.365
• InChiKey: ROEHLBUICRNXHR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  22
• 可旋转键数：
  4
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  69.6
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  甲基磺酰氯 、 3-[4-phenoxyphenyl]pyrazole 以 吡啶 、 水 为溶剂， 反应 16.0h， 以Column chromatography afforded 152 mg (91%) of the title compound as white solid, mp 136° C的产率得到1-Methanesulfonyl-3-(4-phenoxyphenyl)-1H-pyrazole
  参考文献：
  名称：

  Aryl substituted pyrazoles, imidazoles, oxazoles, thiazoles and pyrroles, and the use thereof

  摘要：

  本发明涉及具有式I:1的化合物或其药学上可接受的盐、前药或溶剂，其中Het和R5-R13在规范中设定。本发明还涉及使用式I的化合物治疗全身和局部缺血后的神经损伤，治疗或预防神经退行性疾病，如肌萎缩侧索硬化症（ALS），以及治疗、预防或改善急性或慢性疼痛，作为抗耳鸣剂、抗癫痫药物、抗躁郁药物、局部麻醉剂、抗心律失常药物以及治疗或预防糖尿病神经病变的药物。

  公开号：

  US20030069292A1

文献信息

• Aryl substituted pyrazoles, and pyrroles, and the use thereof
  申请人：Euro-Celtique S.A.

  公开号：US06414011B1

  公开（公告）日：2002-07-02

  This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R13 are set in the specification. The invention also is directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

  这项发明涉及具有以下化学式I的化合物： 或其药学上可接受的盐、前药或溶剂化合物，其中Het和R5-R13在规范中设置。该发明还涉及化合物I的用途，用于治疗全脑和局部缺血后的神经损伤，用于治疗或预防神经退行性疾病，如肌萎缩侧索硬化症（ALS），以及用于治疗、预防或改善急性或慢性疼痛，作为抗耳鸣剂，作为抗癫痫药，作为抗躁郁药，作为局部麻醉药，作为抗心律失常药，以及用于治疗或预防糖尿病性神经病变。
• Aryl-substituted pyrazoles, imidazoles, oxazoles, thiazoles and pyrroles as anticonvulsants
  申请人：EURO-CELTIQUE S.A.

  公开号：EP2266960A2

  公开（公告）日：2010-12-29

  Aryl Substituted Pyrazoles, Imidazoles, Oxazoles, Thiazoles and Pyrroles, and the Use Thereof This invention relates to compounds having formula (I) or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R13 are set in the specification. The invention also is directed to the use of compounds of formula (I) for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

  芳基取代的吡唑、咪唑、噁唑、噻唑和吡咯及其用途 本发明涉及具有式（I）的化合物或其药学上可接受的盐、原药或溶液，其中 Het 和 R5-R13 在说明书中列出。本发明还涉及式（I）化合物在以下方面的用途：治疗全局性和局灶性缺血后的神经元损伤；治疗或预防神经退行性疾病，如肌萎缩性脊髓侧索硬化症（ALS）；治疗、预防或改善急性或慢性疼痛；抗耳鸣剂；抗惊厥剂；抗躁狂抑制剂；局部麻醉剂；抗心律失常剂；以及治疗或预防糖尿病神经病变。
• Sodium channel blocker compositions and the use thereof
  申请人：——

  公开号：US20020037926A1

  公开（公告）日：2002-03-28

  Methods of treating or preventing chronic pain or convulsion are disclosed by administering to an animal a sodium channel blocker and at least one of gabapentin and pregabalin. Also disclosed are pharmaceutical compositions and kits for the treatment or prevention of chronic pain or convulsion.

  本发明公开了通过向动物施用钠通道阻滞剂以及加巴喷丁和普瑞巴林中的至少一种来治疗或预防慢性疼痛或抽搐的方法。还公开了用于治疗或预防慢性疼痛或抽搐的药物组合物和试剂盒。
• Dispersible formulation of an anti-inflammatory agent
  申请人：Britten Jean Nancy

  公开号：US20050004098A1

  公开（公告）日：2005-01-06

  A method is provided for treatment and/or prevention of an inflammatory condition in a fluid-containing organ having a natural exterior orifice, such as the udder of a milk-producing animal or an ear of a subject. The invention also relates to a dispersible pharmaceutical composition suitable for infusion into the organ according to the method of the invention, and a process for preparing such a composition.

  本发明提供了一种方法，用于治疗和/或预防具有天然外部孔口的含液器官的炎症，例如产奶动物的乳房或受试者的耳朵。本发明还涉及一种适用于根据本发明方法注入器官的可分散药物组合物，以及制备这种组合物的工艺。
• SODIUM CHANNEL BLOCKER COMPOSITIONS AND THE USE THEREOF
  申请人：Euro-Celtique S.A.

  公开号：EP1169060A1

  公开（公告）日：2002-01-09