1-[4-(2,4-Dichlorophenyl)sulfanylphenyl]ethanone | 1289207-60-8

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 1-[4-(2,4-Dichlorophenyl)sulfanylphenyl]ethanone
• CAS: 1289207-60-8
• 化学式: C₁₄H₁₀Cl₂OS
• 分子量: 297.205
• InChiKey: WJQNJKVPOHYPNK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.9
• 重原子数：
  18
• 可旋转键数：
  3
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.07
• 拓扑面积：
  42.4
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  1-[4-(2,4-Dichlorophenyl)sulfanylphenyl]ethanone 在 间氯过氧苯甲酸 作用下， 以 二氯甲烷 为溶剂， 生成
  参考文献：
  名称：

  The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors

  摘要：

  In this communication, human 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) inhibitory activities of a novel series of diarylsulfones are described. Optimization of this series resulted in several highly potent 11b-HSD1 inhibitors with excellent pharmacokinetic (PK) properties. Compound (S)-25 showed excellent efficacy in a non-human primate ex vivo pharmacodynamic model. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.09.097
• 作为产物：
  描述：

  2,4-dichlorodiphenylsulfide 、 乙酰氯 在 三溴化铝 作用下， 以 二硫化碳 为溶剂， 生成 1-[4-(2,4-Dichlorophenyl)sulfanylphenyl]ethanone
  参考文献：
  名称：

  The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors

  摘要：

  In this communication, human 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) inhibitory activities of a novel series of diarylsulfones are described. Optimization of this series resulted in several highly potent 11b-HSD1 inhibitors with excellent pharmacokinetic (PK) properties. Compound (S)-25 showed excellent efficacy in a non-human primate ex vivo pharmacodynamic model. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2010.09.097

文献信息

• [EN] ARYLBENZYLPIPERIDINE COMPOUNDS<br/>[FR] COMPOSÉS D'ARYLBENZYLPIPÉRIDINE
  申请人：LUNDBECK & CO AS H

  公开号：WO2007114916A2

  公开（公告）日：2007-10-11

  [EN] This invention is directed to arylbenzylpiperidine compounds which are ligands at the MCHl receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression comprising administering to the subject a therapeutically effective amount of a compound of the subject invention. This invention further provides a method of treating a subject suffering from anxiety comprising administering to the subject a therapeutically effective amount of a compound of the subject invention. This invention also provides a method of treating a subject suffering from obesity comprising administering to the subject a therapeutically effective amount of a compound of the subject invention. Furthermore, the present invention is directed to the use of a compound of the subject invention for the manufacture of a medicament for treating a subject suffering from depression, anxiety or obesity.
  [FR] La présente invention concerne des composés d'arylbenzylpipéridine constituant des ligands au niveau du récepteur MCHI. L'invention propose une composition pharmaceutique comprenant une quantité thérapeutiquement suffisante d'un composé de l'invention et un excipient pharmaceutiquement admis. L'invention concerne également un procédé permettant de traiter un sujet soufrant de dépression, par administration d'une quantité thérapeutiquement efficace d'un composé de l'invention. L'invention concerne aussi un procédé permettant de traiter un sujet soufrant d'anxiété, par administration d'une quantité thérapeutiquement efficace d'un composé de l'invention. L'invention concerne en outre un procédé permettant de traiter un sujet soufrant d'obésité, par administration d'une quantité thérapeutiquement efficace d'un composé de l'invention. Enfin, l'invention concerne l'utilisation d'un composé de l'invention pour la fabrication d'un médicament pour le traitement d'un sujet souffrant de dépression, d'anxiété ou d'obésité.
• The synthesis and SAR of novel diarylsulfone 11β-HSD1 inhibitors
  作者：Xuelei Yan、Zhulun Wang、Athena Sudom、Mario Cardozo、Michael DeGraffenreid、Yongmei Di、Pingchen Fan、Xiao He、Juan C. Jaen、Marc Labelle、Jinsong Liu、Ji Ma、Dustin McMinn、Shichang Miao、Daqing Sun、Liang Tang、Hua Tu、Stefania Ursu、Nigel Walker、Qiuping Ye、Jay P. Powers

  DOI：10.1016/j.bmcl.2010.09.097

  日期：2010.12

  In this communication, human 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1) inhibitory activities of a novel series of diarylsulfones are described. Optimization of this series resulted in several highly potent 11b-HSD1 inhibitors with excellent pharmacokinetic (PK) properties. Compound (S)-25 showed excellent efficacy in a non-human primate ex vivo pharmacodynamic model. (C) 2010 Elsevier Ltd. All rights reserved.