7-benzyl-8-(6-hydroxymethyl-[1,4]diazepan-1-yl)-1,3-dimethyl-3,7-dihydropurine-2,6-dione | 389059-99-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并嘧啶类
• 英文名称: 7-benzyl-8-(6-hydroxymethyl-[1,4]diazepan-1-yl)-1,3-dimethyl-3,7-dihydropurine-2,6-dione
• 英文别名: 7-benzyl-8-[6-(hydroxymethyl)-1,4-diazepan-1-yl]-1,3-dimethylpurine-2,6-dione
• CAS: 389059-99-8
• 化学式: C₂₀H₂₆N₆O₃
• 分子量: 398.465
• InChiKey: RRLWFBZULYMFIM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  29
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  93.9
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  7-benzyl-8-chloro-1,3-dimethyl-1,3,7-trihydropurine-2,6-dione 在 potassium carbonate 作用下， 以 甲醇 、 二氯甲烷 、 N,N-二甲基甲酰胺 为溶剂， 以1%的产率得到7-benzyl-8-(6-hydroxymethyl-[1,4]diazepan-1-yl)-1,3-dimethyl-3,7-dihydropurine-2,6-dione
  参考文献：
  名称：

  Heterocyclic compounds, which are inhibitors of the enzyme DPP-IV

  摘要：

  本发明涉及治疗活性和选择性抑制剂酶DPP-IV，包含该化合物的药物组合物以及利用这些化合物制造用于治疗与DPP-IV使蛋白质失活有关的疾病的药物，例如2型糖尿病和肥胖症，以及治疗与DPP-IV使蛋白质失活有关的疾病的方法，例如2型糖尿病和肥胖症。

  公开号：

  US20020161001A1

文献信息

• SUSTAINED RELEASE PREPARATION
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1537880A1

  公开（公告）日：2005-06-08

  The sustained-release preparation of the present invention, which contains a dipeptidyl peptidase IV inhibitor and a hydrophilic polymer, can appropriately inhibit the DPP-IV activity, and is superior in convenience or compliance.

  本发明的缓释制剂含有二肽基肽酶 IV 抑制剂和亲水性聚合物，可以适当抑制 DPP-IV 的活性，在方便性或顺应性方面更胜一筹。
• Heterocyclic compounds that are inhibitors of the enzyme DPP-IV
  申请人：NOVO NORDISK A/S

  公开号：EP1561752A1

  公开（公告）日：2005-08-10

  The present invention relates to therapeutically active and selective inhibitors of the enzyme DPP-IV, pharmaceutical compositions comprising the compounds and the use of such compounds for and the manufacture of medicaments for treating diseases that are associated with proteins which are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity, as well as methods for treating diseases that are associated with proteins which are subject to inactivation by DPP-IV, such as type 2 diabetes and obesity.

  本发明涉及具有治疗活性和选择性的DPP-IV酶抑制剂、包含这些化合物的药物组合物、使用这些化合物治疗与DPP-IV灭活的蛋白质有关的疾病（如2型糖尿病和肥胖症）的药物以及治疗与DPP-IV灭活的蛋白质有关的疾病（如2型糖尿病和肥胖症）的方法。
• CONTROLLED RELEASE COMPOSITION
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1607088A1

  公开（公告）日：2005-12-21

  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释组合物，其活性成分（质子泵抑制剂）的释放可通过两个或多个步骤以不同的释放速率进行控制，该组合物包含 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) 能控制活性成分以低于释放控制部分 A 的释放速率的预定速率释放的释放控制部分 B，必要时， 3) 能控制活性成分以快于释放控制部分 B 的释放速率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 的释放先于活性成分从释放控制部分 A 的释放（当包含释放控制部分 C 时，活性成分从释放控制部分 C 的释放先于活性成分从释放控制部分 B 的释放）。
• REMEDY FOR DIABETES
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1671649A1

  公开（公告）日：2006-06-21

  An agent for treating diabetes with sulfonylurea secondary failure which comprises a dipeptidyl peptidase IV inhibitor. The agent of the present invention is an agent for treating diabetes with sulfonylurea secondary failure showing excellent insulin-secreting and hypoglycemic effects on even diabetic patients on whom a sulfonylurea compound or a fast-acting insulin secretagogue has no insulin-secreting effect and therefore no sufficient hypoglycemic effect.

  一种包含二肽基肽酶 IV 抑制剂的磺酰脲继发性失效糖尿病治疗剂。本发明的制剂是一种用于治疗磺酰脲类继发性失效糖尿病的制剂，甚至对磺酰脲类化合物或速效胰岛素促泌剂没有胰岛素分泌作用因而没有足够降血糖作用的糖尿病患者也有很好的胰岛素分泌和降血糖作用。
• Sustained release preparation
  申请人：Akiyama Yohko

  公开号：US20060039974A1

  公开（公告）日：2006-02-23

  The sustained-release preparation of the present invention, which contains a dipeptidyl peptidase IV inhibitor and a hydrophilic polymer, can appropriately inhibit the DPP-IV activity, and is superior in convenience or compliance.

  本发明的缓释制剂含有二肽基肽酶 IV 抑制剂和亲水性聚合物，可以适当抑制 DPP-IV 的活性，在方便性或顺应性方面更胜一筹。