2-(4-Aminobenzyl)-3,5-dioxo-1,2,4-oxadiazolidine | 258856-29-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-(4-Aminobenzyl)-3,5-dioxo-1,2,4-oxadiazolidine
• 英文别名: 2-(4-aminobenzyl)-1,2,4-oxadiazolidine-3,5-dione；2-[(4-aminophenyl)methyl]-1,2,4-oxadiazolidine-3,5-dione
• CAS: 258856-29-0
• 化学式: C₉H₉N₃O₃
• 分子量: 207.189
• InChiKey: PACCEMKMBYNXDI-UHFFFAOYSA-N

物化性质

• 密度：
  1.475±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  84.7
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  2-(4-Aminobenzyl)-3,5-dioxo-1,2,4-oxadiazolidine 、 2-[(3'-formyl-2,2'-dimethylbiphenyl-4-yl)oxy]ethyl acetate 在 溶剂黄146 、 三乙酰氧基硼氢化钠 、 sodium methylate 作用下， 以 甲醇 为溶剂， 反应 68.0h， 生成 sodium 2-[4-({[4'-(2-hydroxyethoxy)-2,2'-dimethylbiphenyl-3-yl]methyl}amino)benzyl]-3,5-dioxo-1,2,4-oxadiazolidin-4-ide
  参考文献：
  名称：

  EP2216330

  摘要：

  公开号：
• 作为产物：
  描述：

  N-hydroxy-N-(4-nitrobenzyl)urea 、 氯甲酸乙酯 在 palladium-carbon sodium hydroxide 作用下， 以 四氢呋喃 、 乙醇 、 水 为溶剂， 以17%的产率得到2-(4-Aminobenzyl)-3,5-dioxo-1,2,4-oxadiazolidine
  参考文献：
  名称：

  Benzothiepin derivatives, process for the preparation of the same and uses thereof

  摘要：

  本发明提供了一种化合物，其通式为：其中环A为可选择性取代的苯环；R1为可选择性取代的非芳香性杂环基团；R2和R3各自独立地为氢原子或可选择性取代的烃基团；n为0至3的整数；或其盐，这些化合物作为药物具有促进骨形成和软骨形成的效果。本发明涉及一种胺化合物，该化合物具有优异的抑制淀粉样β蛋白产生和/或分泌的效果，以及其制备和应用。特别是，它对于预防和/或治疗例如神经退行性疾病、淀粉样血管病、由脑血管障碍引起的神经紊乱等具有显著效果。

  公开号：

  US06355672B1

文献信息

• Oxadiazolidinedione compound
  申请人：Astellas Pharma Inc.

  公开号：US07968552B2

  公开（公告）日：2011-06-28

  A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided. It was found that an oxadiazolidinedione compound which is characterized by the possession of a benzyl or the like substituent binding to the cyclic group via a linker at the 2-position of the oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof, has excellent GPR40 agonist action. In addition, since the oxadiazolidinedione compound of the present invention showed excellent insulin secretion promoting action and blood glucose level-lowering action, it is useful as an insulin secretion promoter or an agent for preventing/treating diabetes.

  提供了一种可用作药物的化合物，特别是胰岛素分泌促进剂或用于预防/治疗与GPR40相关的疾病，例如糖尿病等。发现一种噁唑烷二酮化合物，其特征在于在噁唑烷二酮环的2位通过连接基与环状基团结合的苄基或类似基团，或其药学上可接受的盐具有优异的GPR40激动剂作用。此外，由于本发明的噁唑烷二酮化合物显示出优异的胰岛素分泌促进作用和降低血糖水平的作用，因此它可用作胰岛素分泌促进剂或预防/治疗糖尿病的药物。
• OXADIAZOLIDINEDIONE COMPOUND
  申请人：Negoro Kenji

  公开号：US20100267775A1

  公开（公告）日：2010-10-21

  A pharmaceutical agent having GPR40 receptor agonistic action, particularly a compound which is useful as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus. The present inventors have examined a compound having GPR40 receptor agonistic action, confirmed that an oxadiazolidinedione compound which has a substituent such as a benzyl group, etc. linked with a substituent such as a phenyl group, etc. through a linker at the 2-position of an oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof has an excellent GPR40 agonistic activity, and thus completed the invention. The oxadiazolidinedione compound has excellent insulin secretagogue action and anti-hyperglycemic action, and therefore can be used as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus.

  一种具有GPR40受体激动作用的药物，特别是一种可用作胰岛素分泌剂或预防和/或治疗糖尿病的药物。本发明人研究了一种具有GPR40受体激动作用的化合物，确认了一种氧杂二唑烷环的2位上有一个连接着苯基等取代基的连接基的苯甲基等取代基的氧杂二唑烷酮化合物，或其药学上可接受的盐具有优异的GPR40激动活性，从而完成了本发明。氧杂二唑烷酮化合物具有优异的胰岛素分泌剂作用和抗高血糖作用，因此可用作胰岛素分泌剂或预防和/或治疗糖尿病的药物。
• Oxadiazolidinedione Compound
  申请人：Negoro Kenji

  公开号：US20090186909A1

  公开（公告）日：2009-07-23

  [Problem] A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided. [Means for resolution] It was found that an oxadiazolidinedione compound which is characterized by the possession of a benzyl or the like substituent binding to the cyclic group via a linker at the 2-position of the oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof, has excellent GPR40 agonist action. In addition, since the oxadiazolidinedione compound of the present invention showed excellent insulin secretion promoting action and blood glucose level-lowering action, it is useful as an insulin secretion promoter or an agent for preventing/treating diabetes.

  【问题】提供一种可用作药物的化合物，特别是胰岛素分泌促进剂或用于预防/治疗涉及GPR40的疾病，如糖尿病等。 【解决方法】发现一种氧代唑烷二酮化合物，其特征在于在氧代唑烷二酮环的2位通过连接基与环上的苯甲基或类似取代基结合，或其药学上可接受的盐具有优异的GPR40激动剂作用。此外，由于本发明的氧代唑烷二酮化合物表现出良好的胰岛素分泌促进作用和降低血糖水平的作用，因此它可用作胰岛素分泌促进剂或预防/治疗糖尿病的药物。
• BENZOTHIEPIN DERIVATIVES, PROCESS FOR THE PREPARATION OF THE SAME AND USES THEREOF
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1103552A1

  公开（公告）日：2001-05-30

  The invention provides compounds of the formula: wherein the ring A is an optionally substituted benzene ring; R1 is an optionally substituted non-aromatic heterocyclic group; R2 and R3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0 - 3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.

  本发明提供了如下式的化合物： 其中，环 A 是任选取代的苯环；R1 是任选取代的非芳香杂环基团；R2 和 R3 独立地是氢原子或任选取代的烃基；n 是 0 - 3 的整数；或其盐，可用作具有促进成骨作用和促进软骨作用的药物。 本发明涉及一种在抑制淀粉样蛋白-b 的产生和/或分泌方面具有卓越效果的胺类化合物及其生产和使用方法。特别是，它对预防和/或治疗神经退行性疾病、淀粉样血管病、脑血管疾病引起的神经系统疾病等有效。
• Benzothiepine derivatives, their production and use
  申请人：——

  公开号：US20020128308A1

  公开（公告）日：2002-09-12

  The invention provides compounds of the formula: 1 wherein the ring A is an optionally substituted benzene ring; R 1 is an optionally substituted non-aromatic heterocyclic group; R 2 and R 3 are independently hydrogen atom or an optionally substituted hydrocarbon group; n is an integer of 0-3; or salts thereof, which are useful as medicines having an osteogenesis promoting effect and chondrogensis promoting effect. The present invention relates to an amine compound having an excellent effect of inhibiting production and/or secretion of amyloid-b protein, a production and use thereof. Especially, it is effective for preventing and/or treating, for example, neurodegenerative diseases, amyloid angiopathy, neurological disorders caused by cerebrovascular disorders, and so forth.

  本发明提供了以下式子的化合物： 1 其中环 A 是任选取代的苯环； R 1 是任选取代的非芳香杂环基团； R 2 和 R 3 独立地为氢原子或任选取代的烃基；n 为 0-3 的整数；或其盐，可用作具有促进成骨作用和促进软骨作用的药物。 本发明涉及一种具有良好抑制淀粉样蛋白-b 生成和/或分泌效果的胺类化合物及其生产和使用方法。特别是，它对预防和/或治疗神经退行性疾病、淀粉样血管病、脑血管疾病引起的神经紊乱等有效。