ethyl N-(4,5,7-trifluorobenzothiazol-2-yl)methyl-N-cyclopropylsuccinamate | 166172-88-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并噻唑类
• 英文名称: ethyl N-(4,5,7-trifluorobenzothiazol-2-yl)methyl-N-cyclopropylsuccinamate
• 英文别名: Ethyl 4-[cyclopropyl-[(4,5,7-trifluoro-1,3-benzothiazol-2-yl)methyl]amino]-4-oxobutanoate
• CAS: 166172-88-9
• 化学式: C₁₇H₁₇F₃N₂O₃S
• 分子量: 386.395
• InChiKey: JLBIQRMDWNXPLN-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  26
• 可旋转键数：
  8
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.47
• 拓扑面积：
  87.7
• 氢给体数：
  0
• 氢受体数：
  8

文献信息

• SUCCINAMIC ACID COMPOUND, PROCESS FOR PRODUCING THE SAME, AND USE THEREOF
  申请人：Senju Pharmaceutical Co., Ltd.

  公开号：EP0719767A1

  公开（公告）日：1996-07-03

  Provision of a succinamic acid compound of the formula (1) wherein R1 is an alkyl or a lower alkenyl and R2 is an optionally esterified carboxyl, a pharmaceutically acceptable salt thereof, an agent for the prophylaxis and/or treatment of the complications of diabetes, comprising, as an active ingredient, the succinamic acid compound or a pharmaceutically acceptable salt thereof, an aldose reductase inhibitor comprising, as an active ingredient, the succinamic acid compound or a pharmaceutically acceptable salt thereof, and a method for producing the succinamic acid compound or a pharmaceutically acceptable salt thereof. The novel succinamic acid compounds of the formula (1) of the present invention and pharmaceutically acceptable salts thereof have a strong aldose reductase inhibitory activity in mammals such as human, and show superior safety. Hence, they are useful as pharmaceutical agents for the treatment of the complications of diabetes such as faulty union of corneal injury, cataract, neurosis, retinopathy and nephropathy, in particular, cataract and neurosis. According to the production method of the present invention, efficient production of such useful compounds of the present invention can be provided.

  提供式（1）的琥珀酰胺酸化合物 其中 R1 是烷基或低级烯基，R2 是任选酯化的羧基，其药学上可接受的盐；一种预防和/或治疗糖尿病并发症的制剂，其活性成分包括琥珀酰胺酸化合物或其药学上可接受的盐；一种醛糖还原酶抑制剂，其活性成分包括琥珀酰胺酸化合物或其药学上可接受的盐；以及一种生产琥珀酰胺酸化合物或其药学上可接受的盐的方法。本发明式（1）的新型琥珀肟酸化合物及其药学上可接受的盐在哺乳动物（如人类）体内具有很强的醛糖还原酶抑制活性，并显示出优越的安全性。因此，它们可作为药物制剂用于治疗糖尿病并发症，如角膜损伤的错误结合、白内障、神经衰弱、视网膜病变和肾病，特别是白内障和神经衰弱。根据本发明的生产方法，可以高效生产本发明的此类有用化合物。
• US5688818A
  申请人：——

  公开号：US5688818A

  公开（公告）日：1997-11-18