2-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-quinoline-6-carboxylic acid | 863492-37-9

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 喹啉及其衍生物
• 英文名称: 2-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-quinoline-6-carboxylic acid
• 英文别名: 2-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]quinoline-6-carboxylic acid
• CAS: 863492-37-9
• 化学式: C₂₄H₁₅F₃N₂O₃
• 分子量: 436.39
• InChiKey: OVONGKFMVDMZCZ-UHFFFAOYSA-N

物化性质

• 沸点：
  543.5±50.0 °C(predicted)
• 密度：
  1.421±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  32
• 可旋转键数：
  4
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.04
• 拓扑面积：
  79.3
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为反应物：
  描述：

  (S)-2-azido-1-phenyl-ethylamine hydrochloride 、 2-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-quinoline-6-carboxylic acid 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 、 三乙胺 、 碳酸氢钠 作用下， 以 二氯甲烷 、 水 为溶剂， 反应 16.0h， 生成 (S)-2-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-quinoline-6-carboxylic acid (2-azido-1-phenyl-ethyl)-amide
  参考文献：
  名称：

  [EN] SUBSTITUTED QUINOLINE COMPOUNDS
  [FR] COMPOSES DE QUINOLINE SUBSTITUES

  摘要：

  本发明涉及式(I)的MTP/Apo-B分泌抑制剂，其中R1-R7、X1、m和n的定义如说明书中所述，以及包含这些化合物的药物组合物，以及这些化合物和组合物的使用方法。本发明的化合物可用于治疗肥胖及其相关疾病、状况或失调。

  公开号：

  WO2005080373A1
• 作为产物：
  描述：

  2-氨基喹啉-6-甲酸苄酯 在 4-二甲氨基吡啶 、 lithium hydroxide monohydrate 、 盐酸-N-乙基-Nˊ-(3-二甲氨基丙基)碳二亚胺 作用下， 以 四氢呋喃 、 甲醇 、 二氯甲烷 、 水 为溶剂， 生成 2-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-quinoline-6-carboxylic acid
  参考文献：
  名称：

  Discovery of microsomal triglyceride transfer protein (MTP) inhibitors with potential for decreased active metabolite load compared to dirlotapide

  摘要：

  Analogues related to dirlotapide (1), a gut-selective inhibitor of microsomal triglyceride transfer protein (MTP) were prepared with the goal of further reducing the potential for unwanted liver MTP inhibition and associated side-effects. Compounds were designed to decrease active metabolite load: reducing MTP activity of likely human metabolites and increasing metabolite clearance to reduce exposure. Introduction of 4'-alkyl and 4'-alkoxy substituents afforded compounds exhibiting improved therapeutic index in rats with respect to liver triglyceride accumulation and enzyme elevation. Likely human metabolites of select compounds were prepared and characterized for their potential to inhibit MTP in vivo. Based on preclinical efficacy and safety data and its potential for producing short-lived, weakly active metabolites, compound 13 (PF-02575799) advanced into phase 1 clinical studies. (C) 2011 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2011.05.099

文献信息

• Dibenzyl Amine Compounds and Derivatives
  申请人：Chang George

  公开号：US20070213371A1

  公开（公告）日：2007-09-13

  Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

  二苯基胺化合物及其衍生物，含有这种化合物的药物组合物以及使用这种化合物提高某些血浆脂质水平，包括高密度脂蛋白胆固醇，并降低其他一些血浆脂质水平，如低密度脂蛋白胆固醇和甘油三酯，并据此治疗由高密度脂蛋白胆固醇水平低和/或低密度脂蛋白胆固醇和甘油三酯水平高加重的疾病，如动脉粥样硬化和心血管疾病在某些哺乳动物，包括人类。
• [EN] SUBSTITUTED HETEROARYL- AND PHENYLSULFAMOYL COMPOUNDS<br/>[FR] COMPOSES HETEROARYLE ET PHENYLSULFAMOYLE SUBSTITUES
  申请人：PFIZER PROD INC

  公开号：WO2005092845A1

  公开（公告）日：2005-10-06

  The present invention is directed at substituted heteroaryl- and phenylsulfamoyl compounds, pharmaceutical compositions containing such compounds and the use of such compounds as peroxisome proliferator activator receptor (PPAR) agonists. PPAR alpha activators, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases, in mammals, including humans. The compounds are also useful for the treatment of negative energy balance (NEB) and associated diseases in ruminants.

  本发明涉及取代杂环芳基和苯基磺酰胺化合物，含有这种化合物的药物组合物以及将这种化合物用作过氧化物酶增殖激活受体（PPAR）激动剂的用途。PPARα激活剂，含有这种化合物的药物组合物以及使用这种化合物提高特定血浆脂质水平，包括高密度脂蛋白胆固醇，并降低其他特定血浆脂质水平，如低密度脂蛋白胆固醇和甘油三酯，从而治疗由高密度脂蛋白胆固醇水平低和/或低密度脂蛋白胆固醇和甘油三酯水平高加重的疾病，如动脉粥样硬化和心血管疾病，在哺乳动物，包括人类中。这些化合物还可用于治疗反常能量平衡（NEB）和反常相关疾病的反刍动物。
• Tetrahydroisoquinoline LXR modulators
  申请人：Yang Wu

  公开号：US20070093523A1

  公开（公告）日：2007-04-26

  A compound of formula I wherein X, R 1 , R 2a , R 3a , R 3b , R 4a , R 4b , R 4c and R 5 are defined herein.

  其中X，R1，R2a，R3a，R3b，R4a，R4b，R4c和R5在此处定义。
• [EN] INDOLINE COMPOUNDS AND THEIR USE IN THE TREATMENT OF ARTERIOSCLEROSIS<br/>[FR] COMPOSES A BASE D'INDOLINE ET LEUR UTILISATION DANS LE TRAITEMENT DE L'ARTERIOSCLEROSE
  申请人：PFIZER PROD INC

  公开号：WO2006032987A1

  公开（公告）日：2006-03-30

  Indoline compounds, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.

  吲哚啉化合物，含有这种化合物的药物组合物，以及使用这种化合物来提高某些血浆脂质水平，包括高密度脂蛋白胆固醇，并降低其他一些血浆脂质水平，如低密度脂蛋白胆固醇和甘油三酯，并据此治疗由高密度脂蛋白胆固醇水平低和/或低密度脂蛋白胆固醇和甘油三酯水平高加重的疾病，如动脉粥样硬化和心血管疾病在某些哺乳动物中，包括人类。
• HETEROCYCLIC CETP INHIBITORS
  申请人：Salvati E. Mark

  公开号：US20070161685A1

  公开（公告）日：2007-07-12

  Compounds of formula Ia and Ib wherein A, B, C and R 1 are described herein.

  式Ia和Ib的化合物 其中A、B、C和R1 如本文所述。