9-[4-[4-(2,3-dihydro-1-oxo-1H-isoindol-2-yl)-1-piperidinyl]butyl]-N-propyl-9H-fluorene-9-carboxamide

• 分子结构分类: 有机化合物 - 苯类化合物 - 芴
• 英文名称: 9-[4-[4-(2,3-dihydro-1-oxo-1H-isoindol-2-yl)-1-piperidinyl]butyl]-N-propyl-9H-fluorene-9-carboxamide
• 英文别名: 9-[4-[4-(3-oxo-1H-isoindol-2-yl)piperidin-1-yl]butyl]-N-propylfluorene-9-carboxamide
• 化学式: C₃₄H₃₉N₃O₂
• 分子量: 521.703
• InChiKey: XPSLLBXVEDRXQQ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.6
• 重原子数：
  39
• 可旋转键数：
  9
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  52.6
• 氢给体数：
  1
• 氢受体数：
  3

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。
• 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。
• Substituted quinoline compounds
  申请人：Bertinato Peter

  公开号：US20050234099A1

  公开（公告）日：2005-10-20

  This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R 1 -R 7 , X 1 , m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.

  本发明涉及公式（I）中的MTP / Apo-B分泌抑制剂，其中R1-R7，X1，m和n如规范中所定义，以及包含该化合物的制药组合物，以及该化合物和组合物的使用方法。本发明的化合物在治疗肥胖和相关疾病，状况或障碍方面是有用的。
• Use of APO B secretion/MTP inhibitors
  申请人：Pfizer Products Inc.

  公开号：EP1099438A2

  公开（公告）日：2001-05-16

  The invention relates to methods and pharmaceutical compositions useful in reducing food intake in an animal, preferably a mammal including a human subject or a companion animal, using a microsomal triglyceride transfer protein apolipoprotein B (apo B) secretion/microsomal triglyceride transfer protein (MTP) inhibitor. The invention preferably relates to methods and pharmaceutical compositions useful in reducing food intake in an animal, preferably a mammal including a human subject or a companion animal, using an apo B secretion/MTP inhibitor, and an anti-obesity agent. The invention further relates to a kit comprising an amount of anapolipoprotein B secretion/microsomal triglyceride transfer protein inhibitor and a pharmaceutically acceptable carrier, vehicle or diluent in a first unit dosage form; an amount of an anti-obesity agent and a pharmaceutically acceptable carrier, vehicle or diluent in a second unit dosage form; and a container.

  本发明涉及使用微粒体甘油三酯转移蛋白载脂蛋白B(apo B)分泌/微粒体甘油三酯转移蛋白(MTP)抑制剂减少动物（最好是哺乳动物，包括人或伴侣动物）食物摄入量的方法和药物组合物。本发明优选涉及使用载脂蛋白B分泌/甘油三酯转移蛋白抑制剂和抗肥胖剂减少动物（优选哺乳动物，包括人类或伴侣动物）食物摄入量的方法和药物组合物。本发明还涉及一种试剂盒，包括一定量的载脂蛋白 B 分泌/微粒体甘油三酯转移蛋白抑制剂和药学上可接受的载体、载体或稀释剂（第一单位剂型）；一定量的抗肥胖剂和药学上可接受的载体、载体或稀释剂（第二单位剂型）；以及一个容器。