(S)-3-(3,5-difluoro-phenyl)-N-{1-[3-(pyrazin-2-yloxy)-phenyl]-ethyl}-acrylamide | 694511-22-3

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 肉桂酸及其衍生物
• 英文名称: (S)-3-(3,5-difluoro-phenyl)-N-{1-[3-(pyrazin-2-yloxy)-phenyl]-ethyl}-acrylamide
• 英文别名: (E)-3-(3,5-difluorophenyl)-N-[(1S)-1-(3-pyrazin-2-yloxyphenyl)ethyl]prop-2-enamide
• CAS: 694511-22-3
• 化学式: C₂₁H₁₇F₂N₃O₂
• 分子量: 381.382
• InChiKey: OYFZNQOCEVPMAB-GJBLVYBDSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  28
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  64.1
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• Pyridinyl, pyrimidinyl and pyrazinyl amides as potassium channel openers
  申请人：——

  公开号：US20040102449A1

  公开（公告）日：2004-05-27

  The present invention provides novel heterocyclic amides and related derivatives having the general Formula I 1 wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , A, B and Z are as defined in the specification, or a nontoxic pharmaceutically acceptable salt, solvate or hydrate thereof which are openers or activators of KCNQ potassium channels. The present invention also provides pharmaceutical compositions comprising said heterocyclic amides and to the method of treatment of disorders sensitive to KCNQ potassium channel opening activity such as migraine or a migraine attack, bipolar disorders, epilepsy, acute and chronic pain and anxiety.

  本发明提供了具有一般式I1的新型杂环酰胺和相关衍生物，其中R1、R2、R3、R4、R5、R6、A、B和Z如规范中所定义，或其无毒药学上可接受的盐、溶剂或水合物，它们是KCNQ钾通道的开放剂或激活剂。本发明还提供了包括上述杂环酰胺的药物组合物以及对于对KCNQ钾通道开放活性敏感的疾病的治疗方法，如偏头痛或偏头痛发作、双相障碍、癫痫、急性和慢性疼痛和焦虑。
• Crystal forms of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4(3-ethynyl-phenyl)-1methyl-1h-quinolin-2-one, 2,3,-dihydroxybutanedioate salts and method of production
  申请人：Lyssikatos P. Joseph

  公开号：US20050020836A1

  公开（公告）日：2005-01-27

  The invention relates to crystal forms of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1H-quinolin-2-one, 2,3-dihydroxy butanedioate salts having the formula shown below: and to pharmaceutical compositions containing the above compound, methods of treating hyperproliferative diseases, such as cancers, in mammals, especially humans by administering the above compound, and to methods of preparing the crystal forms of the above compound and related compounds.

  本发明涉及以下化合物的晶体形式，其为6-[(4-氯苯基)-羟基-(3-甲基-3H-咪唑-4-基)-甲基]-4-(3-乙炔基-苯基)-1-甲基-1H-喹啉-2-酮，2,3-二羟基丁二酸盐，其化学式如下： 本发明还涉及含上述化合物的制药组合物，通过给哺乳动物，特别是人类，注射上述化合物治疗增生性疾病，如癌症的方法，以及制备上述化合物及相关化合物的晶体形式的方法。
• US6900210B2
  申请人：——

  公开号：US6900210B2

  公开（公告）日：2005-05-31