ethyl 2-[[[2-[[[4-(3-methoxypropoxy)-3-methyl-2-pyridyl]methyl]sulfinyl]-1H-benzimidazol-1-yl]carbonyl](methyl)amino]ethyl carbonate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并咪唑类
• 英文名称: ethyl 2-[[[2-[[[4-(3-methoxypropoxy)-3-methyl-2-pyridyl]methyl]sulfinyl]-1H-benzimidazol-1-yl]carbonyl](methyl)amino]ethyl carbonate
• 英文别名: ethyl 2-[[[2-[[[4-(3-methoxypropoxy)-3-methyl-pyridin-2-yl)methyl]sulfinyl]-1H-benzimidazol-1-yl]carbonyl](methyl)amino]ethyl carbonate；ethyl 2-[[[2-[[[4-(3-methoxypropoxy)-3-methyl-pyridin-2-yl]methyl]sulfinyl]-1H-benzimidazol-1-yl]carbonyl](methyl)amino]ethyl carbonate；Ethyl 2-[[2-[[4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methylsulfinyl]benzimidazole-1-carbonyl]-methylamino]ethyl carbonate
• 化学式: C₂₅H₃₂N₄O₇S
• 分子量: 532.618
• InChiKey: MHGFGKWCSQFPCR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  37
• 可旋转键数：
  14
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  141
• 氢给体数：
  0
• 氢受体数：
  10

反应信息

• 作为产物：
  描述：

  2-[(ethoxycarbonyl)(methyl)amino]ethyl ethyl carbonate 在 4-二甲氨基吡啶 、 三乙胺 、 三氯氧磷 作用下， 以 四氢呋喃 、 乙腈 为溶剂， 反应 113.0h， 生成 ethyl 2-[[[2-[[[4-(3-methoxypropoxy)-3-methyl-2-pyridyl]methyl]sulfinyl]-1H-benzimidazol-1-yl]carbonyl](methyl)amino]ethyl carbonate
  参考文献：
  名称：

  CONTROLLED RELEASE PREPARATION

  摘要：

  提供了一种受控释放制剂，其中活性成分的释放受到控制，通过在胃肠道内停留或缓慢迁移来延长时间释放活性成分，采用胶囊化片剂、颗粒或细颗粒的方式，其中活性成分的释放受到控制，并且使用了一种凝胶形成聚合物。所述的片剂、颗粒或细颗粒在含有活性成分的核心颗粒上形成了一个受控释放的涂层。

  公开号：

  US20160128945A1

文献信息

• [EN] PRODRUGS OF IMIDAZOLE DERIVATIVES, FOR USE AS PROTON PUMP INHIBITORS IN THE TREATMENT OF E.G. PEPTIC ULCERS<br/>[FR] PROMEDICAMENTS DE DERIVES D'IMIDAZOLE SERVANT D'INHIBITEURS DE POMPE A PROTONS DANS LE TRAITEMENT DE L'ULCERE GASTRO-DUODENAL
  申请人：TAKEDA CHEMICAL INDUSTRIES LTD

  公开号：WO2003105845A1

  公开（公告）日：2003-12-24

  An imidazole compound represented by the formula (I), a salt thereof and a compound of the formula (V), which is one of the intermediates thereof. wherein each symbol is as defined in the present specification. The compound of the present invention shows a superior anti-ulcer activity, a gastric acid secretion inhibitory action, a mucosa-protecting action, an anti-Helicobacter pylori action and the like. Since it shows low toxicity, the compound is useful as a pharmaceutical product.

  一种以化学式(I)表示的咪唑化合物，其盐以及化学式(V)的化合物，后者是其中的一种中间体。其中，每个符号如本说明书中所定义。本发明的化合物表现出优越的抗溃疡活性、抑制胃酸分泌作用、保护粘膜作用、抗幽门螺杆菌作用等。由于其低毒性，该化合物可用作药物产品。
• Drug composition having active ingredient adhered at high concentration to spherical core
  申请人：Yoneyama Shuji

  公开号：US20060159760A1

  公开（公告）日：2006-07-20

  Granule, fine particle or tablet of excellent leaching property, comprising a drug active ingredient in high content realized by forming a layer containing drug active ingredient on core particles through a combination of a method of dispersing and adhering an active ingredient while spraying or adding a binder with a method of spraying or adding a solution or suspension wherein an active ingredient and a binder are contained so as to effect adhesion. Further, there are provided a drug composition containing such a granule, fine particle or tablet and a process for producing the same.

  该文描述了一种具有良好浸出性的颗粒、细粒或片剂，其中包含高含量的药物活性成分，通过将药物活性成分形成在核心颗粒上的一层，通过将活性成分分散和粘附的方法与喷雾或添加粘合剂的方法相结合，或通过添加含有活性成分和粘合剂的溶液或悬浮液以实现粘附。此外，还提供了一种含有这种颗粒、细粒或片剂的药物组成物和制备该药物组成物的方法。
• Controlled release preparation
  申请人：Akiyama Yohko

  公开号：US20060013868A1

  公开（公告）日：2006-01-19

  A controlled release preparation wherein the release of active ingredient is controlled, which releases an active ingredient for an extended period of time by staying or slowly migrating in the gastrointestinal tract, is provided by means such as capsulating a tablet, granule or fine granule wherein the release of active ingredient is controlled and a gel-forming polymer. Said tablet, granule or fine granule has a release-controlled coating-layer formed on a core particle containing an active ingredient.

  提供一种控制释放制剂，其中活性成分的释放受控制，通过将其包裹在胶囊、颗粒或细颗粒中，以及使用凝胶形成聚合物等手段，使其在胃肠道中停留或缓慢迁移，从而延长活性成分的释放时间。该胶囊、颗粒或细颗粒在含有活性成分的核心粒子上形成了释放控制的涂层层。
• Controlled release composition
  申请人：Nagahara Naoki

  公开号：US20060177509A1

  公开（公告）日：2006-08-10

  The present invention provides a controlled release composition showing release of an active ingredient (proton pump inhibitor) controlled in two or more steps at different release rates, which contains 1) a release-controlled part A capable of controlling release of the active ingredient to occur at a predetermined rate, 2) a release-controlled part B capable of controlling release of the active ingredient to occur at a predetermined rate lower than the release rate of the release-controlled part A, and where necessary, 3) a release-controlled part C capable of controlling release of the active ingredient to occur at a predetermined rate faster than the release rate of the release-controlled part B, wherein the release of the active ingredient from the release-controlled part B precedes the release of the active ingredient from the release-controlled part A (when release-controlled part C is contained, the release of the active ingredient from the release-controlled part C precedes the release of the active ingredient from the release-controlled part B).

  本发明提供了一种控制释放组合物，该组合物显示出活性成分（质子泵抑制剂）在不同的释放速率下控制释放，其中包括1）能够控制活性成分以预定速率释放的释放控制部分A，2）能够控制活性成分以比释放控制部分A更低的预定速率释放的释放控制部分B，必要时还包括3）能够控制活性成分以比释放控制部分B更快的预定速率释放的释放控制部分C，其中活性成分从释放控制部分B的释放先于从释放控制部分A的释放（当包含释放控制部分C时，从释放控制部分C的释放先于从释放控制部分B的释放）。
• Prodrugs of imidazole derivatives, for use as proton pump inhibitors in the treatment of e.g. peptic ulcers
  申请人：Kamiyama Keiji

  公开号：US20050222210A1

  公开（公告）日：2005-10-06

  An imidazole compound represented by the formula (I), a salt thereof and a compound of the formula (V), which is one of the intermediates thereof. wherein each symbol is as defined in the present specification. The compound of the present invention shows a superior anti-ulcer activity, a gastric acid secretion inhibitory action, a mucosa-protecting action, an anti- Helicobacter pylori action and the like. Since it shows low toxicity, the compound is useful as a pharmaceutical product.

  本发明提供了一种以式(I)表示的咪唑化合物及其盐和式(V)的中间体之一的化合物，其中每个符号如本说明书所定义。该发明的化合物表现出优异的抗溃疡活性、抑制胃酸分泌作用、保护粘膜作用、抗幽门螺杆菌作用等。由于其毒性低，该化合物可用作制药产品。