2-(4-pyridyl)ethyl thiolbenzoate | 105163-73-3

• 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-pyridyl)ethyl thiolbenzoate
• 英文别名: S-(2-pyridin-4-ylethyl) benzenecarbothioate
• CAS: 105163-73-3
• 化学式: C₁₄H₁₃NOS
• 分子量: 243.329
• InChiKey: LNJQIJWQNORNDQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  17
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.14
• 拓扑面积：
  55.3
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-(4-pyridyl)ethyl thiolbenzoate 、 碘甲烷 以 丙酮 为溶剂， 反应 24.0h， 以96%的产率得到2-(1-methyl-4-pyridinio)ethyl thiolbenzoate iodide
  参考文献：
  名称：

  2-(4-Pyridyl)ethyl as a protective group for sulfur functionality

  摘要：

  DOI：

  10.1021/jo00375a029
• 作为产物：
  描述：

  4-吡啶乙硫醇盐酸盐 、 苯乙酰氯 在 sodium ethanolate 作用下， 以 乙醇 为溶剂， 反应 140.0h， 以49%的产率得到2-(4-pyridyl)ethyl thiolbenzoate
  参考文献：
  名称：

  2-(4-Pyridyl)ethyl as a protective group for sulfur functionality

  摘要：

  DOI：

  10.1021/jo00375a029

文献信息

• METHOD OF SCREENING REMEDY FOR DIABETES
  申请人：YAMANOUCHI PHARMACEUTICAL CO. LTD.

  公开号：EP1338651A1

  公开（公告）日：2003-08-27

  A convenient screening tool and a convenient screening method for obtaining an agent for treating diabetes, a pharmaceutical composition for treating diabetes, and a process for manufacturing the pharmaceutical composition are disclosed. The screening tool is a G protein-coupled receptor, a variation functionally equivalent thereto, or a homologous polypeptide thereof which promotes insulin secretion under a high glucose concentration by activation, or cells transformed with an expression vector comprising a polynucleotide encoding the above polypeptide and expressing the polypeptide.

  本发明公开了一种方便的筛选工具和一种方便的筛选方法，用于获得一种治疗糖尿病的药物、一种治疗糖尿病的药物组合物以及一种制造该药物组合物的工艺。 筛选工具是一种 G 蛋白偶联受体、其功能等同的变体或其同源多肽，这种多肽在高葡萄糖浓度下通过活化促进胰岛素分泌，或者是用包含编码上述多肽的多核苷酸的表达载体转化的细胞，并表达上述多肽。
• METHOD OF SCREENING INSULIN CONTENT ENHANCER
  申请人：YAMANOUCHI PHARMACEUTICAL CO., LTD.

  公开号：EP1538217A1

  公开（公告）日：2005-06-08

  A screening tool for an agent for promoting insulin production and/or an agent for increasing insulin content, wherein the tool is a G protein-coupled receptor exhibiting an activity of promoting insulin production by activation, or a cell expressing the polypeptide, is disclosed. Further, a method for screening an agent for promoting insulin production and/or an agent for increasing insulin content, comprising the steps of bringing the cell or a cell membrane thereof into contact with a substance to be tested, and analyzing whether or not the polypeptide is activated, is disclosed. The screening tool and the screening method are useful in screening a substance which increases insulin content and prevents and/or treats diabetes. Furthermore, a novel agent for increasing insulin content comprising as an active ingredient a substance obtained by the screening, is disclosed.

  本发明公开了一种促进胰岛素分泌的制剂和/或增加胰岛素含量的制剂的筛选工具，其中该工具是表现出通过激活促进胰岛素分泌活性的G蛋白偶联受体，或表达多肽的细胞。此外，还公开了一种用于筛选促进胰岛素分泌的制剂和/或增加胰岛素含量的制剂的方法，该方法包括以下步骤：使细胞或其细胞膜与待测物质接触，并分析多肽是否被激活。 该筛选工具和筛选方法有助于筛选出一种能增加胰岛素含量、预防和/或治疗糖尿病的物质。 此外，还公开了一种增加胰岛素含量的新型制剂，其活性成分包括通过筛选获得的物质。
• Process for manufacturing a pharmaceutical composition for treating diabetes
  申请人：Astellas Pharma Inc.

  公开号：EP1770159A1

  公开（公告）日：2007-04-04

  A process for manufacturing a pharmaceutical composition for treating diabetes, comprising the steps of: bringing a cell or a cell membrane into contact with a compound to be tested; analyzing whether or not a polypeptide is activated; and preparing a formulation containing the analyzed substance.

  一种治疗糖尿病的药物组合物的生产工艺，包括以下步骤：使细胞或细胞膜与待测化合物接触；分析多肽是否被激活；制备含有被分析物质的制剂。
• Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP-1 level
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP1808168A1

  公开（公告）日：2007-07-18

  The present invention concerns combination of an amount of a GPR1 19 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-I level in a subject over that provided by the amount of the GPR1 19 agonist or the amount of the DPP-FV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-I level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-I secretagogues.

  本发明涉及一定量的 GPR1 19 激动剂与一定量的二肽基肽酶 IV (DPP-IV) 抑制剂的组合，从而使该组合在降低受试者血糖水平或提高血 GLP-I 水平方面的效果优于单独使用一定量的 GPR1 19 激动剂或 DPP-FV 抑制剂所提供的效果，以及使用这种组合治疗或预防糖尿病及其相关病症或通过提高血 GLP-I 水平而改善的病症。 本发明还涉及使用 G 蛋白偶联受体筛选 GLP-I 促泌剂。
• Combination therapy for the treatment of diabetes and conditions related thereto and for the treatment of conditions ameliorated by increasing a blood GLP-1 level
  申请人：Arena Pharmaceuticals, Inc.

  公开号：EP2116235A1

  公开（公告）日：2009-11-11

  The present invention concerns combination of an amount of a GPR1 19 agonist with an amount of a dipeptidyl peptidase IV (DPP-IV) inhibitor such that the combination provides an effect in lowering a blood glucose level or in increasing a blood GLP-I level in a subject over that provided by the amount of the GPR1 19 agonist or the amount of the DPP-FV inhibitor alone and the use of such a combination for treating or preventing diabetes and conditions related thereto or conditions ameliorated by increasing a blood GLP-I level. The present invention also relates to the use of a G protein-coupled receptor to screen for GLP-I secretagogues.

  本发明涉及一定量的 GPR1 19 激动剂与一定量的二肽基肽酶 IV (DPP-IV) 抑制剂的组合，从而使该组合在降低受试者血糖水平或提高血 GLP-I 水平方面的效果优于单独使用一定量的 GPR1 19 激动剂或 DPP-FV 抑制剂所提供的效果，以及使用这种组合治疗或预防糖尿病及其相关病症或通过提高血 GLP-I 水平而改善的病症。 本发明还涉及使用 G 蛋白偶联受体筛选 GLP-I 促泌剂。

表征谱图