1-(5-Aethoxycarbonyl-2-thienyl)aethanol | 34878-43-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 噻吩类
• 英文名称: 1-(5-Aethoxycarbonyl-2-thienyl)aethanol
• 英文别名: 5-(1-hydroxy-ethyl)-thiophene-2-carboxylic acid ethyl ester；(R,S)-5-(1-hydroxy-ethyl)-thiophene-2-carboxylic acid ethyl ester；ethyl 5-(1-hydroxyethyl)thiophene-2-carboxylate
• CAS: 34878-43-8
• 化学式: C₉H₁₂O₃S
• 分子量: 200.258
• InChiKey: HIMNWYYVXHTXSW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  13
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  74.8
• 氢给体数：
  1
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  1-(5-Aethoxycarbonyl-2-thienyl)aethanol 在 二苯基膦叠氮化物 、 1,8-二氮杂双环[5.4.0]十一碳-7-烯 作用下， 以 甲苯 为溶剂， 反应 15.5h， 生成 ethyl 5-(1-azidoethyl)thiophene-2-carboxylate
  参考文献：
  名称：

  EP2172447

  摘要：

  公开号：

文献信息

• AMIDE COMPOUND
  申请人：Nozawa Eisuke

  公开号：US20110144153A1

  公开（公告）日：2011-06-16

  [Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided. [Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.

  【问题】提供一种化合物，该化合物可用作药物组合物的活性成分，例如用于治疗慢性肾衰竭和/或糖尿病肾病的药物组合物。 【解决方法】本发明人对具有EP4受体拮抗活性的化合物进行了广泛的研究，并确认本发明的酰胺化合物具有EP4受体拮抗活性，从而完成了本发明。本发明的酰胺化合物具有EP4受体拮抗活性，可用作预防和/或治疗各种EP4相关疾病的药物组合物的活性成分，例如慢性肾衰竭和/或糖尿病肾病等。
• Glucagon receptor antagonists, preparation and therapeutic uses
  申请人：Eli Lilly and Company

  公开号：US08084489B2

  公开（公告）日：2011-12-27

  The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have glucagon receptor antagonist or inverse agonist activity, as well as methods of using these compounds and intermediates and methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising N compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

  本发明揭示了一种新的化合物式(I)或其药学上可接受的盐，该化合物具有胰高血糖素受体拮抗剂或反向激动剂活性，以及使用这些化合物的方法和制备这些化合物的中间体和方法。在另一实施例中，本发明揭示了包括化合物式(I)的N种药物组合物，以及使用它们治疗糖尿病和其他胰高血糖素相关代谢障碍等方法。
• Glucagon Receptor Antagonists, Preparation and Therapeutic Uses
  申请人：Chappell Mark Donald

  公开号：US20100137417A1

  公开（公告）日：2010-06-03

  The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof which have glucagon receptor antagonist or inverse agonist activity, as well as methods of using these compounds and intermediates and methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising N compounds of Formula (I) as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

  本发明揭示了公式（I）的新化合物或其药学上可接受的盐，具有胰高血糖素受体拮抗剂或反向激动剂活性，以及使用这些化合物的方法，以及制备这些化合物的中间体和方法。在另一种实施方式中，本发明揭示了包含公式（I）的N个化合物的药物组合物，以及使用它们治疗糖尿病和其他胰高血糖素相关代谢紊乱等方法。
• Amide compound
  申请人：Nozawa Eisuke

  公开号：US08598355B2

  公开（公告）日：2013-12-03

  [Problems] A compound, which is useful as an active ingredient of a pharmaceutical composition, for example, a pharmaceutical composition for treating chronic renal failure and/or diabetic nephropathy, is provided. [Solving Means] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic activity, and confirmed that the amide compound of the present invention has an EP4 receptor antagonistic activity, thereby completing the present invention. The amide compound of the present invention has an EP4 receptor antagonistic activity, and can be used as an active ingredient of a pharmaceutical composition for preventing and/or treating various EP4-related diseases, for example, chronic renal failure and/or diabetic nephropathy, and the like.

  【问题】提供一种化合物，该化合物可用作药物组合物的活性成分，例如用于治疗慢性肾功能衰竭和/或糖尿病肾病的药物组合物。 【解决方法】本发明人对具有EP4受体拮抗活性的化合物进行了广泛的研究，并确认本发明的酰胺化合物具有EP4受体拮抗活性，从而完成了本发明。本发明的酰胺化合物具有EP4受体拮抗活性，可用作预防和/或治疗各种与EP4相关的疾病的药物组合物的活性成分，例如慢性肾功能衰竭和/或糖尿病肾病等。
• AMIDE COMPOUNDS
  申请人：Nozawa Eisuke

  公开号：US20110028463A1

  公开（公告）日：2011-02-03

  [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.

  【问题】提供一种可用作治疗慢性肾功能不全或糖尿病肾病的药物化合物。 【解决问题的方法】本发明者对具有EP4受体拮抗作用的化合物进行了广泛的研究，结果发现具有羧酸基或其等效物的各种酰胺衍生物表现出优异的EP4受体拮抗作用，从而完成了本发明。由于本发明的化合物具有优异的EP4受体拮抗作用，因此可用作预防和/或治疗慢性肾功能不全或糖尿病肾病的药物。