2-(1H-咪唑-4-基甲基)-8H-茚并[1,2-d]噻唑单富马酸酯 | 159081-22-8

• 分子结构分类: 有机化合物 - 苯类化合物
• 中文名称: 2-(1H-咪唑-4-基甲基)-8H-茚并[1,2-d]噻唑单富马酸酯
• 英文名称: 2-(4-imidazolylmethyl)-8H-indeno[1,2-d]thiazole
• 英文别名: 2-(1H-imidazol-4-ylmethyl)-8H-indeno[1,2-d]thiazole；8H-Indeno(1,2-d)thiazole, 2-(1H-imidazol-4-ylmethyl)-；2-(1H-imidazol-5-ylmethyl)-4H-indeno[1,2-d][1,3]thiazole
• CAS: 159081-22-8
• 化学式: C₁₄H₁₁N₃S
• 分子量: 253.327
• InChiKey: SWXJBBYBDXFMGG-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.8
• 重原子数：
  18
• 可旋转键数：
  2
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  69.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  2-溴-1-茚满酮 、 4(5)-(2-amino-2-thioxoethyl)imidazole hydrochloride 在 乙酸乙酯 、 氯仿 、 碳酸氢钠 、 氯化钠 、 magnesium sulfate 作用下， 以 异丙醇 为溶剂， 反应 0.5h， 以0.12 g (32%) of 2-(4-imidazolylmethyl)-8H-indeno[1,2-d]thiazole was obtained的产率得到2-(1H-咪唑-4-基甲基)-8H-茚并[1,2-d]噻唑单富马酸酯
  参考文献：
  名称：

  Condensed thiazole derivative, production process thereof and

  摘要：

  提供了作为5-HT.sub.3受体激动剂有用的缩合噻唑衍生物，可以用以下公式(I)或其药学上可接受的盐来表示，其制备过程和药物组成物如下： ##STR1## 其中R，A，L.sub.1，L.sub.2，L和R.sup.1-R.sup.6在此定义，Im表示以下公式的一个基团： ##STR2##

  公开号：

  US05565479A1

文献信息

• NOVEL CONDENSED THIAZOLE DERIVATIVE, PROCESS FOR PRODUCING THE SAME, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP0666263A1

  公开（公告）日：1995-08-09

  A condensed thiazole derivative useful as a 5-HT₃ receptor agonist, represented by general formula (I), a pharmaceutically acceptable salt thereof, a process for producing the same, and a pharmaceutical composition containing the same, wherein R represents hydrogen, halogen, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, nitro, amino, cyano or protected hydroxy; A represents a benzene or naphthalene ring; one of L₁ and L₂ represents a mere bond while the other then represents: (a) linear or branched lower alkylene which may be interrupted by oxygen or sulfur, (b) oxygen or sulfur, or (c) lower alkenylene; L represents a mere bond, or linear or branched lower alkylene; Im represents α or β; R¹, R² and R³ may be the same or different from one another and each represents hydrogen or lower alkyl; and R⁴, R⁵ and R⁶ may be the same or different from one another and each represents hydrogen or lower alkyl.

  一种可用作 5-HT₃ 受体激动剂的缩合噻唑衍生物，由通式(I)、其药学上可接受的盐、生产该衍生物的工艺以及含有该衍生物的药物组合物表示，其中 R 代表氢、卤素、羟基、低级烷氧基、羧基、低级烷氧基羰基、硝基、氨基、氰基或受保护的羟基；A 代表苯环或萘环； L₁ 和 L₂ 中的一个代表单纯的键，而另一个则代表(a) 可被氧或硫打断的直链或支链低级亚烷基，(b) 氧或硫，或 (c) 低级烯基；L 代表纯键，或直链或支链低级亚烷基；Im 代表 α 或 β；R¹、R² 和 R³ 可彼此相同或不同，且各自代表氢或低级烷基；以及 R⁴、R⁵ 和 R⁶ 可彼此相同或不同，且各自代表氢或低级烷基。
• Compositions useful for treating gastrointestinal motility disorders
  申请人：Landau B. Steven

  公开号：US20050059704A1

  公开（公告）日：2005-03-17

  The present invention relates to method of treating a gastrointestinal motility disorder in a subject in need of treatment comprising coadministering to said subject a first amount of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof; and a second amount of at least one gastric acid suppressing agent (e.g., a proton pump inhibitor, an H 2 receptor antagonist or a pharmaceutically acceptable salt, hydrate or solvate thereof; or an acid pump antagonist or pharmaceutically acceptable salt, hydrate or solvate thereof) wherein the first and second amounts together comprise a therapeutically effective amount. In particular, the method is for treating GERD, including nocturnal GERD. The invention further relates to a method of treating nocturnal GERD comprising administering to a subject in need thereof a therapeutically effective amount of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof. The invention further relates to a method of increasing esophageal motility in a subject in need thereof. The method of increasing esophageal motility can be achieved by administration of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof. The coadministration can also be used to increase esophageal motility.

  本发明涉及治疗需要治疗的受试者胃肠道运动紊乱的方法，包括向所述受试者联合施用第一种量的具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液；以及第二种量的至少一种胃酸抑制剂（如质子泵抑制剂、H 2 受体拮抗剂或其药学上可接受的盐、水合物或溶液；或酸泵拮抗剂或其药学上可接受的盐、水合物或溶液），其中第一和第二量共同构成治疗有效量。特别是，该方法用于治疗胃食管反流病，包括夜间胃食管反流病。本发明进一步涉及一种治疗夜间胃食管反流病的方法，该方法包括向有需要的受试者施用治疗有效量的具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液。本发明进一步涉及一种增加需要者食管蠕动的方法。增加食管蠕动的方法可通过给予具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液。联合给药也可用于增加食管运动。
• Compositions useful for increasing lower esophageal sphincter pressure
  申请人：Landau B. Steven

  公开号：US20060189648A1

  公开（公告）日：2006-08-24

  The present invention relates to a method of increasing the pressure of the lower esophageal sphincter in a subject in need thereof comprising administering to said subject a specified amount of a compound having 5-HT 3 receptor agonist activity or a pharmaceutically acceptable salt, hydrate or solvate thereof. The subject in need of treatment is suffering from GERD, including nocturnal GERD.

  本发明涉及一种增加有需要的受试者食管下括约肌压力的方法，包括向所述受试者施用指定量的具有 5-HT 3 受体激动剂活性的化合物或其药学上可接受的盐、水合物或溶液。需要治疗的受试者患有胃食管反流病，包括夜间胃食管反流病。
• COMPOSITIONS USEFUL FOR TREATING GASTROINTESTINAL MOTILITY DISORDERS
  申请人：Dynogen Pharmaceuticals Inc.

  公开号：EP1663313A2

  公开（公告）日：2006-06-07
• Compositions and methods for treating gastrointestinal hypomotility and associated disorders
  申请人：Ashburn T. Ted

  公开号：US20070010543A1

  公开（公告）日：2007-01-11

  This invention relates to methods for treating, preventing and/or managing GI hypomotility or a disorder associated with GI hypomotility in a subject including administering to the subject two compounds, where the first compound is a 5HT 3 agonist and where the combination of the two compounds results in an increase in GI motility. Also provided are compositions and kits for use in methods of the invention.