N-((1RS,2SR)-2-hydroxy-2-(4-(phenyloxy)phenyl)-1-((3-((1,1,2,2-tetrafluoroethyl)oxy)phenyl)methyl)ethyl)-6,7-dihydro-5H-benzo[a]cycloheptene-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: N-((1RS,2SR)-2-hydroxy-2-(4-(phenyloxy)phenyl)-1-((3-((1,1,2,2-tetrafluoroethyl)oxy)phenyl)methyl)ethyl)-6,7-dihydro-5H-benzo[a]cycloheptene-1-carboxamide
• 英文别名: N-[1-hydroxy-1-(4-phenoxyphenyl)-3-[3-(1,1,2,2-tetrafluoroethoxy)phenyl]propan-2-yl]-8,9-dihydro-7H-benzo[7]annulene-4-carboxamide
• 化学式: C₃₅H₃₁F₄NO₄
• 分子量: 605.6
• InChiKey: SEOPLSZCSRBPCA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8.8
• 重原子数：
  44
• 可旋转键数：
  11
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.23
• 拓扑面积：
  67.8
• 氢给体数：
  2
• 氢受体数：
  8

反应信息

• 作为产物：
  描述：

  (1RS,2SR)-2-amino-1-(4-(phenyloxy)phenyl)-3-(3-((1,1,2,2-tetrafluoroethyl)oxy)phenyl)-1-propanol 、 6,7-dihydro-5H-benzo[a]cycloheptene-1-carboxylic acid 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 、 1-羟基苯并三唑 在 乙酸乙酯 、 盐酸 、 sodium hydroxide 、 Brine 、 magnesium sulfate 、 ethyl acetate n-hexane 作用下， 以 乙腈 、 水 为溶剂， 反应 16.0h， 以gave the title compound (285 mg, 68%)的产率得到N-((1RS,2SR)-2-hydroxy-2-(4-(phenyloxy)phenyl)-1-((3-((1,1,2,2-tetrafluoroethyl)oxy)phenyl)methyl)ethyl)-6,7-dihydro-5H-benzo[a]cycloheptene-1-carboxamide
  参考文献：
  名称：

  Aminoethanol derivatives

  摘要：

  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。

  公开号：

  US20040127574A1

文献信息

• 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。
• Method of inhibiting remnant lipoprotein production
  申请人：Japan Tobacco, Inc.

  公开号：EP2316447A1

  公开（公告）日：2011-05-04

  The present invention aims at provision of a method for inhibiting remnant lipoprotein production and a remnant lipoprotein production inhibitor, which includes administering a compound having a CETP inhibitory activity to an administration subject. The remnant lipoprotein production inhibitor of the present invention contains a compound having a CETP inhibitory activity as an active ingredient.

  本发明旨在提供一种抑制残余脂蛋白生成的方法和一种残余脂蛋白生成抑制剂，其中包括向给药对象施用一种具有CETP抑制活性的化合物。本发明的残余脂蛋白生成抑制剂含有一种具有 CETP 抑制活性的化合物作为活性成分。
• Method of Inhibiting remnant lipoprotein production
  申请人：Japan Tobacco, Inc.

  公开号：EP2319509A1

  公开（公告）日：2011-05-11

  The present invention aims at provision of a method for inhibiting remnant lipoprotein production and a remnant lipoprotein production inhibitor, which includes administering a compound having a CETP inhibitory activity to an administration subject. The remnant lipoprotein production inhibitor of the present invention contains a compound having a CETP inhibitory activity as an active ingredient.

  本发明旨在提供一种抑制残余脂蛋白生成的方法和一种残余脂蛋白生成抑制剂，其中包括向给药对象施用一种具有CETP抑制活性的化合物。本发明的残余脂蛋白生成抑制剂含有一种具有 CETP 抑制活性的化合物作为活性成分。
• Method for inhibiting lipid absorption and lipid absorption inhibitor
  申请人：Yonemori Fumihiko

  公开号：US20060270705A1

  公开（公告）日：2006-11-30

  The present invention relates to a method of inhibiting lipid absorption through the small intestine, which comprises administering a compound having a CETP inhibitory activity to an administration subject, and an inhibitor of lipid absorption through the small intestine characterized in that it comprises a compound having a CETP inhibitory activity as an active ingredient. The lipid absorption inhibitor of the present invention can prevent and/or treat diseases such as for example hyperlipidemia, arteriosclerosis, coronary artery diseases, obesity, diabetes, hypertension and metabolic syndrome by inhibiting lipid absorption through the small intestine.
• METHOD OF INHIBITING REMNANT LIPOPROTEIN PRODUCTION
  申请人：Okamoto Hiroshi

  公开号：US20110189210A1

  公开（公告）日：2011-08-04

  The present invention aims at provision of a method for inhibiting remnant lipoprotein production and a remnant lipoprotein production inhibitor, which includes administering a compound having a CETP inhibitory activity to an administration subject. The remnant lipoprotein production inhibitor of the present invention contains a compound having a CETP inhibitory activity as an active ingredient.