[4-(3-aminophenyl)thiazol-2-ylthio]-N-[1-(3,4-dichlorobenzyl)piperidin-4-yl]acetamide | 474968-36-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: [4-(3-aminophenyl)thiazol-2-ylthio]-N-[1-(3,4-dichlorobenzyl)piperidin-4-yl]acetamide
• 英文别名: 2-[[4-(3-aminophenyl)-1,3-thiazol-2-yl]sulfanyl]-N-[1-[(3,4-dichlorophenyl)methyl]piperidin-4-yl]acetamide
• CAS: 474968-36-0
• 化学式: C₂₃H₂₄Cl₂N₄OS₂
• 分子量: 507.508
• InChiKey: SPVNYKPZOPUTIZ-UHFFFAOYSA-N

物化性质

• 密度：
  1.43±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.5
• 重原子数：
  32
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  125
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  [4-(3-aminophenyl)thiazol-2-ylthio]-N-[1-(3,4-dichlorobenzyl)piperidin-4-yl]acetamide 在 2-二甲氨基吡啶 、 乙酸酐 作用下， 以 二氯甲烷 为溶剂， 反应 1.0h， 生成 [4-(3-acetylamidephenyl)thiazol-2-ylthio]-N-[1-(3,4-dichlorobenzyl)piperidin-4-yl]acetamide
  参考文献：
  名称：

  3,4-Dihalobenzylpiperidine derivatives and their medical use

  摘要：

  公开号：

  EP1389616B1

文献信息

• Novel benzylpiperidine compound
  申请人：——

  公开号：US20040158071A1

  公开（公告）日：2004-08-12

  The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. 1 wherein each symbol is as defined in the specification.

  本发明的目的是提供一种具有基于趋化因子抑制活性的治疗效果的化合物，作为口服药物而言，具有令人满意的药物品质。本发明人发现以下苯基哌啶衍生物（式（1））具有趋化因子抑制活性。进一步的深入研究成功增强了该化合物的趋化因子抑制活性和血液稳定性，从而完成了本发明。式中每个符号如说明书中所定义。
• NOVEL BENZYLPIPERIDINE COMPOUND
  申请人：Mitsubishi Pharma Corporation

  公开号：EP1389616A1

  公开（公告）日：2004-02-18

  The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. wherein each symbol is as defined in the specification.

  本发明的目的是提供一种具有基于趋化因子抑制活性的治疗效果的化合物，该化合物作为口服药物是令人满意的。 本发明者发现以下苄基哌啶衍生物（式（1））具有趋化因子抑制活性。通过进一步深入研究，成功地提高了本化合物的趋化因子抑制活性和在血液中的稳定性，并完成了本发明。 其中各符号如说明书中所定义。
• US7115635B2
  申请人：——

  公开号：US7115635B2

  公开（公告）日：2006-10-03
• [EN] METHODS AND COMPOSITIONS FOR THE TREATMENT AND/OR PREVENTION OF BOWEL DISORDERS<br/>[FR] PROCÉDÉS ET COMPOSITIONS POUR LE TRAITEMENT ET/OU LA PRÉVENTION DE TROUBLES INTESTINAUX
  申请人：VICTORIA UNIVERSITY

  公开号：WO2014075124A1

  公开（公告）日：2014-05-22

  The present invention relates to methods for the treatment and/or prevention of bowel disorders. The methods and compositions disclosed herein are useful in treatment and prevention of inflammatory bowel disease.
• 3,4-Dihalobenzylpiperidine derivatives and their medical use
  申请人：Mitsubishi Tanabe Pharma Corporation

  公开号：EP1389616B1

  公开（公告）日：2011-07-27