1-(2-methoxyethyl)-N,N.2-trimethyl-8-phenyl-1,6,7,8-tetrahydrochromeno[7,8-d]imidazole-5-carboxamide

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 黄酮类化合物
• 英文名称: 1-(2-methoxyethyl)-N,N.2-trimethyl-8-phenyl-1,6,7,8-tetrahydrochromeno[7,8-d]imidazole-5-carboxamide
• 英文别名: 1-(2-Methoxyethyl)-N,N,2-trimethyl-8-phenyl-1,6,7,8-tetrahydrochromeno[7,8-d]imidazole-5-carboxamide；1-(2-methoxyethyl)-N,N,2-trimethyl-8-phenyl-7,8-dihydro-6H-pyrano[2,3-e]benzimidazole-5-carboxamide
• 化学式: C₂₃H₂₇N₃O₃
• 分子量: 393.486
• InChiKey: QSSLNCOGGSGPGR-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3
• 重原子数：
  29
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.39
• 拓扑面积：
  56.6
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为产物：
  描述：

  1-(2-methoxyethyl)-2-methyl-8-phenyl-1,6,7,8-tetrahydrochromeno[7,8-d]imidazole-5-carboxylic acid 、 盐酸二甲胺 在 O-(1H-benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate 、 三乙胺 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 12.0h， 以100%的产率得到1-(2-methoxyethyl)-N,N.2-trimethyl-8-phenyl-1,6,7,8-tetrahydrochromeno[7,8-d]imidazole-5-carboxamide
  参考文献：
  名称：

  WO2008/35195

  摘要：

  公开号：

文献信息

• Benzimidazole Derivatives as Selective Acid Pump Inhibitors
  申请人：Koike Hiroki

  公开号：US20100048532A1

  公开（公告）日：2010-02-25

  This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R 1 , R 2 , R 3 , R 4 , A and E are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the method of treatment and the use, comprising such compounds for the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), laryngopharyngeal reflux disease, peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori , dyspepsia, functional dyspepsia, Zolliπger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, cancer, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.

  本发明涉及式（I）的化合物或其药学上可接受的盐，其中：R1、R2、R3、R4、A和E分别如本文所述或其药学上可接受的盐，并含有此类化合物的组合物以及治疗和使用的方法，包括使用此类化合物治疗由酸泵拮抗活性介导的疾病，例如但不限于胃肠疾病、胃食管疾病、胃食管反流病（GERD）、喉咙咽部反流病、消化性溃疡、胃溃疡、十二指肠溃疡、NSAID引起的溃疡、胃炎、幽门螺杆菌感染、消化不良、功能性消化不良、Zolliπger-Ellison综合症、非侵蚀性反流病（NERD）、内脏疼痛、癌症、烧心、恶心、食管炎、吞咽困难、过多唾液、气道疾病或哮喘等病症。
• Benzimidazole derivatives as selective acid pump inhibitors
  申请人：Koike Hiroki

  公开号：US08466166B2

  公开（公告）日：2013-06-18

  This invention relates to compounds of the formula (I): or a pharmaceutically acceptable salt thereof, wherein: R1, R2, R3, R4, A and E are each as described herein or a pharmaceutically acceptable salt, and compositions containing such compounds and the method of treatment and the use, comprising such compounds for the treatment of a condition mediated by acid pump antagonistic activity such as, but not limited to, as gastrointestinal disease, gastroesophageal disease, gastroesophageal reflux disease (GERD), laryngopharyngeal reflux disease, peptic ulcer, gastric ulcer, duodenal ulcer, NSAID-induced ulcers, gastritis, infection of Helicobacter pylori, dyspepsia, functional dyspepsia, Zolliπger-Ellison syndrome, non-erosive reflux disease (NERD), visceral pain, cancer, heartburn, nausea, esophagitis, dysphagia, hypersalivation, airway disorders or asthma.

  本发明涉及式(I)的化合物或其药学上可接受的盐，其中：R1、R2、R3、R4、A和E均如本文所述或其药学上可接受的盐，以及含有这些化合物的组合物、治疗方法和使用，包括用于治疗酸泵拮抗活性介导的疾病，例如但不限于胃肠疾病、胃食管疾病、胃食管反流病(GERD)、喉咙咽反流病、消化性溃疡、胃溃疡、十二指肠溃疡、NSAID引起的溃疡、胃炎、幽门螺杆菌感染、消化不良、功能性消化不良、佐利-埃利森综合征、非侵蚀性反流病(NERD)、脏器疼痛、癌症、烧心、恶心、食管炎、吞咽困难、多口水、气道疾病或哮喘。
• ACID PUMP ANTAGONIST FOR TREATMENT OF DISEASES ASSOCIATED WITH ABNORMAL GASTROINTESTINAL MOVEMENT
  申请人：RaQualia Pharma Inc

  公开号：EP2452680A1

  公开（公告）日：2012-05-16

  The present invention relates to a use of a compound having an acid pump antagonistic activity, a pharmaceutically acceptable salt thereof or a pharmaceutical composition thereof for the manufacture of a medicament for prevention or treatment of diseases in which abnormal gastrointestinal motility is involved. In addition, the present invention relates to the method of prevention or treatment including administering to a human or animal. The compound, the pharmaceutically acceptable salt thereof, or pharmaceutical compositions containing them, may be used in combination with one or more second active agent. Further, the present invention relates to pharmaceutical compositions and kits comprising a compound having an acid pump antagonistic activity or a pharmaceutically acceptable salt thereof for the prevention or treatment of said diseases.

  本发明涉及一种具有酸泵拮抗活性的化合物、其药学上可接受的盐或其药物组合物的用途，用于制造预防或治疗胃肠道运动异常疾病的药物。此外，本发明还涉及预防或治疗方法，包括给人或动物用药。本发明的化合物、其药学上可接受的盐或含有它们的药物组合物可与一种或多种第二活性剂结合使用。此外，本发明还涉及包含具有酸泵拮抗活性的化合物或其药学上可接受的盐的药物组合物和试剂盒，用于预防或治疗上述疾病。
• TABLET
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP3329921A1

  公开（公告）日：2018-06-06

  The present invention provides a tablet showing high stability of the active ingredients (potassium-competitive acid blocker and acetylsalicylic acid) and stably and rapidly expressing the pharmacological effects of the active ingredients after administration. The present invention provides a tablet containing an inner core and an outer layer, wherein the inner core is an enteric-coated tablet containing acetylsalicylic acid, and the outer layer contains a potassium-competitive acid blocker free of enteric coating.

  本发明提供了一种有效成分（钾竞争性酸阻滞剂和乙酰水杨酸）稳定性高的片剂，服用后可稳定、快速地发挥有效成分的药理作用。 本发明提供了一种含有内芯和外层的片剂，其中内芯是含有乙酰水杨酸的肠溶衣片剂，外层含有不含肠溶衣的钾竞争性酸阻滞剂。
• Tablet
  申请人：Takeda Pharmaceutical Company Limited

  公开号：US10835541B2

  公开（公告）日：2020-11-17

  The present invention provides a tablet showing high stability of the active ingredients (potassium-competitive acid blocker and acetylsalicylic acid) and stably and rapidly expressing the pharmacological effects of the active ingredients after administration. The present invention provides a tablet containing an inner core and an outer layer, wherein the inner core is an enteric-coated tablet containing acetylsalicylic acid, and the outer layer contains a potassium-competitive acid blocker free of enteric coating.

  本发明提供了一种有效成分（钾竞争性酸阻滞剂和乙酰水杨酸）稳定性高的片剂，服用后可稳定、快速地发挥有效成分的药理作用。 本发明提供了一种包含内核和外层的片剂，其中内核为含有乙酰水杨酸的肠溶衣片剂，外层含有不含肠溶衣的钾竞争性酸阻滞剂。