4'-trifluoromethyl-biphenyl-2-carboxylic acid-[2-(2-acetylamino-ethyl)-1,2,3,4-tetrahydro-isoquinolin-6-yl]-amide

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 4'-trifluoromethyl-biphenyl-2-carboxylic acid-[2-(2-acetylamino-ethyl)-1,2,3,4-tetrahydro-isoquinolin-6-yl]-amide
• 英文别名: N-[2-[2-(Acetylamino)ethyl]-1,2,3,4-tetrahydro-6-isoquinolinyl]-4'-(trifluoromethyl)[1,1'-biphenyl]-2-carboxamide；N-[2-(2-acetamidoethyl)-3,4-dihydro-1H-isoquinolin-6-yl]-2-[4-(trifluoromethyl)phenyl]benzamide
• 化学式: C₂₇H₂₆F₃N₃O₂
• 分子量: 481.518
• InChiKey: DJLMIXIBPMWLNC-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.5
• 重原子数：
  35
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.26
• 拓扑面积：
  61.4
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• Triamide-substituted heterobicyclic compounds
  申请人：Pfizer Inc.

  公开号：US20030187053A1

  公开（公告）日：2003-10-02

  The invention relates to triamide MTP/ApoB inhibitors of the formula 1 1 wherein R 1 -R 8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.

  本发明涉及三酰胺MTP/ApoB抑制剂，其化学公式为1，其中R1-R8如说明书所述，以及包含这些化合物的药物组合物及其用途，以及制备这些化合物的方法。本发明的化合物可用于治疗肥胖和脂质紊乱。
• Microsomal triglyceride transfer protein inhibitor
  申请人：Pfizer Inc

  公开号：US20040132745A1

  公开（公告）日：2004-07-08

  The present invention provides inhibitors of microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion having Formula (I) which are useful for the treatment of obesity and related diseases, as well as prevention and treatment of atherosclerosis and its clinical sequelae, for lowering serum lipids, and in the prevention and treatment of related diseases. The invention further relates to pharmaceutical compositions comprising the compounds of the present invention and to methods of treating obesity, atherosclerosis, and related diseases and/or conditions with the compounds of the present invention, either alone or in combination with other medicaments, including lipid-lowering agents. 1

  本发明提供了具有公式(I)的微粒体甘油三酯转运蛋白（MTP）和/或载脂蛋白B（Apo B）分泌抑制剂，用于治疗肥胖及相关疾病，以及预防和治疗动脉粥样硬化和其临床后遗症，降低血清脂质，以及预防和治疗相关疾病。本发明还涉及包含本发明化合物的药物组合物，以及使用本发明化合物单独或与其他药物（包括降脂药）联合治疗肥胖、动脉粥样硬化和相关疾病/状况的方法。
• Combination of MTP inhibitors or apoB-secretion inhibitors with fibrates for use as pharmaceuticals
  申请人：Boehringer Ingelheim Pharma KG

  公开号：US20030162788A1

  公开（公告）日：2003-08-28

  The invention relates to the use of fibrates for lowering the liver toxicity of MTP inhibitors as well as pharmaceutical compositions containing an MTP inhibitor and a fibrate.

  本发明涉及使用纤维酸衍生物来降低MTP抑制剂对肝脏的毒性，以及包含MTP抑制剂和纤维酸衍生物的药物组合物。
• Microsomal Triglyceride transfer protein inhibitor
  申请人：Pfizer Inc

  公开号：US20040132779A1

  公开（公告）日：2004-07-08

  The present invention provides inhibitors of microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion having Formula (I) which are useful for the treatment of obesity and related diseases, as well as prevention and treatment of atherosclerosis and its clinical sequelae, for lowering serum lipids, and in the prevention and treatment of related diseases. The invention further relates to pharmaceutical compositions comprising the compounds of the present invention and to methods of treating obesity, atherosclerosis, and related diseases and/or conditions with the compounds of the present invention, either alone or in combination with other pharmaceutical agents, including lipid-lowering agents. 1

  本发明提供了具有式（I）的微粒体三酰甘油转移蛋白（MTP）和/或载脂蛋白B（Apo B）分泌抑制剂，用于治疗肥胖和相关疾病，以及预防和治疗动脉粥样硬化及其临床后遗症，降低血清脂质，以及预防和治疗相关疾病。该发明还涉及包含本发明化合物的药物组合物，以及使用本发明化合物单独或与其他药物剂（包括降脂药物）联合治疗肥胖、动脉粥样硬化和相关疾病和/或症状的方法。
• 4'-trifluoromethylbiphenyl-2-carboxylic acid-[2-(2-acetylaminoethyl)-1,2,3,4-tetrahydroisoquinolin-6-yl]amide hydrochloride as apo B-secretion/MTP inhibitors
  申请人：PFIZER INC.

  公开号：EP0887345A1

  公开（公告）日：1998-12-30

  A hydrochloride salt of an Apo B secretion/MTP inhibitor, methods of making the salt, methods of using the salt and pharmaceutical compositions containing the salt are disclosed.

  揭示了一种Apo B分泌/MTP抑制剂的盐盐，以及制备该盐的方法、使用该盐的方法和含有该盐的药物组合物。