5-chloro-N-[(1RS,2SR)-2-(4-fluorophenyl)-2-hydroxy-1-[4-(trifluoromethyl)benzyl]ethyl]naphthalene-1-carboxamide

• 分子结构分类: 有机化合物 - 苯丙烷和聚酮 - 直链 1,3-二芳基丙烷
• 英文名称: 5-chloro-N-[(1RS,2SR)-2-(4-fluorophenyl)-2-hydroxy-1-[4-(trifluoromethyl)benzyl]ethyl]naphthalene-1-carboxamide
• 英文别名: 5-chloro-N-[1-(4-fluorophenyl)-1-hydroxy-3-[4-(trifluoromethyl)phenyl]propan-2-yl]naphthalene-1-carboxamide
• 化学式: C₂₇H₂₀ClF₄NO₂
• 分子量: 501.908
• InChiKey: RLYCZVSKMKPHMD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.9
• 重原子数：
  35
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.15
• 拓扑面积：
  49.3
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为产物：
  描述：

  (1RS,2SR)-2-amino-1-(4-fluorophenyl)-3-[4-(trifluoromethyl)phenyl]propan-1-ol 、 5-氯-1-萘酸 在 1-羟基苯并三唑 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 乙腈 为溶剂， 以85%的产率得到5-chloro-N-[(1RS,2SR)-2-(4-fluorophenyl)-2-hydroxy-1-[4-(trifluoromethyl)benzyl]ethyl]naphthalene-1-carboxamide
  参考文献：
  名称：

  EP1362846

  摘要：

  公开号：

文献信息

• [EN] BENZOTHIAZOLE AND THIAZOLE'5,5-B!PYRIDINE COMPOSITIONS AND THEIR USE AS UBIQUITIN LIGASE INHIBITORS<br/>[FR] COMPOSITIONS DE BENZOTHIAZOLE ET DE THIAZOLE'5,5-B!PYRIDINE ET LEUR UTILISATION COMME INHIBITEURS DE L'UBIQUITINE LIGASE
  申请人：RIGEL PHARMACEUTICALS INC

  公开号：WO2005037845A1

  公开（公告）日：2005-04-28

  This invention describes compounds and pharmaceutical compositions useful as ubiquitin agent inhibitors. The compounds and pharmaceutical compositions of the invention are useful as inhibitors of the biochemical pathways of organisms in which ubiquitination is involved. The invention also comprises the use of the compounds and pharmaceutical compositions of the invention for the treatment of conditions that require inhibition of ubiquitination. Furthermore, the invention comprises methods of inhibiting ubiquitination in a cell comprising contacting a cell in which inhibition of ubiquitination is desired with a pharmaceutical composition according to the invention.

  这项发明描述了化合物和制药组合物，作为泛素代理抑制剂。该发明的化合物和制药组合物作为抑制泛素化参与的生物化学途径的抑制剂是有用的。该发明还包括使用该发明的化合物和制药组合物治疗需要抑制泛素化的情况。此外，该发明还包括通过使用该发明的制药组合物接触需要抑制泛素化的细胞来抑制细胞内泛素化的方法。
• Aminoethanol derivatives
  申请人：——

  公开号：US20040127574A1

  公开（公告）日：2004-07-01

  The present invention provides a pharmaceutical agent having cholesteryl ester transfer protein inhibitory action and useful as a blood lipid lowering agent and the like. The present invention relates to a compound represented by the formula 1 wherein Ar 1 is an aromatic ring group optionally having substituents, Ar 2 is an aromatic ring group having substituents, OR″ is an optionally protected hydroxyl group, R is an acyl group, R′ is a hydrogen atom or a hydrocarbon group optionally having substituents, or a salt thereof, and a pharmaceutical composition containing a compound of the formula (I) or a salt thereof or a prodrug thereof.

  本发明提供了一种具有胆固醇酯转移蛋白抑制作用的药物剂，可用作降低血脂等方面的药物。本发明涉及一种由式1表示的化合物，其中Ar1是一个带有取代基的芳香环基团，Ar2是一个带有取代基的芳香环基团，OR″是一个可选保护的羟基，R是一个酰基，R′是一个氢原子或一个可选带有取代基的碳氢基团，或其盐，以及含有式(I)的化合物或其盐或前药的药物组合物。
• AMINOETHANOL DERIVATIVES
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1362846A1

  公开（公告）日：2003-11-19

  The present invention provides a pharmaceutical agent having cholesteryl ester transfer protein inhibitory action and useful as a blood lipid lowering agent and the like. The present invention relates to a compound represented by the formula wherein Ar1 is an aromatic ring group optionally having substituents, Ar2 is an aromatic ring group having substituents, OR'' is an optionally protected hydroxyl group, R is an acyl group, R' is a hydrogen atom or a hydrocarbon group optionally having substituents, or a salt thereof, and a pharmaceutical composition containing a compound of the formula (I) or a salt thereof or a prodrug thereof.

  本发明提供了一种具有胆固醇酯转移蛋白抑制作用的药剂，可用作降血脂药等。本发明涉及一种由式表示的化合物 其中 Ar1 是可选具有取代基的芳香环基，Ar2 是可选具有取代基的芳香环基，OR''是可选保护的羟基，R 是酰基，R'是氢原子或可选具有取代基的烃基，或其盐，以及含有式（I）化合物或其盐或其原药的药物组合物。
• BENZOTHIAZOLE AND THIAZOLE'5,5-B!PYRIDINE COMPOSITIONS AND THEIR USE AS UBIQUITIN LIGASE INHIBITORS
  申请人：Rigel Pharmaceuticals, Inc.

  公开号：EP1680431A1

  公开（公告）日：2006-07-19
• US6982348B2
  申请人：——

  公开号：US6982348B2

  公开（公告）日：2006-01-03