(R)-7-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-quinoline-3-carboxylic acid-(1-phenyl-ethyl)-amide | 339290-39-0

• 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: (R)-7-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-quinoline-3-carboxylic acid-(1-phenyl-ethyl)-amide
• 英文别名: (r)-7-[(4'-Trifluoromethyl-biphenyl-2-carbonyl)-amino]-quinoline-3-carboxylic acid (1-phenyl-ethyl)-amide；N-[(1R)-1-phenylethyl]-7-[[2-[4-(trifluoromethyl)phenyl]benzoyl]amino]quinoline-3-carboxamide
• CAS: 339290-39-0
• 化学式: C₃₂H₂₄F₃N₃O₂
• 分子量: 539.557
• InChiKey: ZSNQHQMXRGECNB-HXUWFJFHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.7
• 重原子数：
  40
• 可旋转键数：
  6
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  71.1
• 氢给体数：
  2
• 氢受体数：
  6

反应信息

• 作为反应物：
  描述：

  (R)-7-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-quinoline-3-carboxylic acid-(1-phenyl-ethyl)-amide 、 methyl-methanesulfonate 生成 7-[(4'-trifluoromethyl-biphenyl-2-carbonyl)-amino]-quinoline-3-carboxylic acid (1-phenyl-propyl)-amide
  参考文献：
  名称：

  Methods of treating obesity using a neurotensin receptor ligand

  摘要：

  本发明涉及使用神经肽T受体配体治疗肥胖症、糖尿病、性功能障碍、动脉粥样硬化、胰岛素抵抗、糖耐量受损、高胆固醇血症或高三酰甘油血症的方法。本发明还涉及包含神经肽T受体配体的制药组合物和工具箱。

  公开号：

  US20010046956A1

文献信息

• Treatments for obesity and methods for identifiying compounds useful for treating obesity
  申请人：——

  公开号：US20020198152A1

  公开（公告）日：2002-12-26

  The present invention provides a method of treating obesity, sexual dysfunction (including erectile dysfunction), diabetes, insulin resistance, hyperinsulinemia, Syndrome X, adrenal dysfunction, hypertension, hypercholesterolemia, atherosclerosis, hyperlipoproteinemia, hypertriglyceridemia, or substance abuse, the method comprising the step of administering to a patent having or at risk of having one of the above-mentioned diseases a therapeutically effective amount of a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not attenuate the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors. The present invention also provides a method of identifying a compound that is useful for the treatment or prevention of obesity, sexual dysfunction (including erectile dysfunction), diabetes, insulin resistance, hyperinsulinemia, Syndrome X, adrenal dysfunction, hypertension, hypercholesterolemia, atherosclerosis, hyperlipoproteinemia, hypertriglyceridemia, or substance abuse, the method comprising the steps of: 1) determining if a compound affects the binding of agouti-related protein to melanocortin receptors; 2) determining if a compound affects the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors; and 3) selecting a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not affect the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors.

  本发明提供了一种治疗肥胖症、性功能障碍（包括勃起功能障碍）、糖尿病、胰岛素抵抗、高胰岛素血症、X综合症、肾上腺功能障碍、高血压、高胆固醇血症、动脉粥样硬化、高脂蛋白血症、高甘油三酯血症或物质滥用的方法，包括向患有或有患上述疾病风险的患者施用一种化合物的治疗有效量，该化合物减弱了被称为agouti相关蛋白与黑素皮质素受体的结合，但不减弱α-黑素细胞刺激素与黑素皮质素受体的结合。本发明还提供了一种鉴定对治疗或预防肥胖症、性功能障碍（包括勃起功能障碍）、糖尿病、胰岛素抵抗、高胰岛素血症、X综合症、肾上腺功能障碍、高血压、高胆固醇血症、动脉粥样硬化、高脂蛋白血症、高甘油三酯血症或物质滥用有用的化合物的方法，包括以下步骤：1）确定化合物是否影响agouti相关蛋白与黑素皮质素受体的结合；2）确定化合物是否影响α-黑素细胞刺激素与黑素皮质素受体的结合；3）选择一种减弱agouti相关蛋白与黑素皮质素受体结合但不影响α-黑素细胞刺激素与黑素皮质素受体结合的化合物。
• Tetrazole compounds as thyroid receptor ligands
  申请人：——

  公开号：US20020006946A1

  公开（公告）日：2002-01-17

  The present invention relates to tetrazole compounds of Formula I, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, and pharmaceutically acceptable salts of the prodrugs. 1 The invention also relates to compositions comprising the tetrazole compounds and to methods of treating obesity, diabetes, atherosclerosis, hypertension, coronary heart disease, hypercholesterolemia, hyperlipidemia, thyroid disease, thyroid cancer, hypothyroidism, depression, glaucoma, cardiac arrhythmias, congestive heart failure, and osteoporosis using the tetrazole compounds.

  本发明涉及公式I的四唑化合物、立体异构体、其药学上可接受的盐和前药，以及前药的药学上可接受的盐。本发明还涉及包含四唑化合物的组合物，以及使用四唑化合物治疗肥胖症、糖尿病、动脉硬化、高血压、冠心病、高胆固醇血症、高脂血症、甲状腺疾病、甲状腺癌、甲状腺功能减退症、抑郁症、青光眼、心律失常、充血性心力衰竭和骨质疏松症的方法。
• Treatments for obesity and methods for identifying compounds useful for treating obesity
  申请人：Pfizer Inc.

  公开号：US06451783B1

  公开（公告）日：2002-09-17

  The present invention provides a method of treating obesity, sexual dysfunction (including erectile dysfunction), diabetes, insulin resistance, hyperinsulinemia, Syndrome X, adrenal dysfunction, hypertension, hypercholesterolemia, atherosclerosis, hyperlipoproteinemia, hypertriglyceridemia, or substance abuse, the method comprising the step of administering to a patent having or at risk of having one of the above-mentioned diseases a therapeutically effective amount of a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not attenuate the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors. The present invention also provides a method of identifying a compound that is useful for the treatment or prevention of obesity, sexual dysfunction (including erectile dysfunction), diabetes, insulin resistance, hyperinsulinemia, Syndrome X, adrenal dysfunction, hypertension, hypercholesterolemia, atherosclerosis, hyperlipoproteinemia, hypertriglyceridemia, or substance abuse, the method comprising the steps of: 1) determining if a compound affects the binding of agouti-related protein to melanocortin receptors; 2) determining if a compound affects the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors; and 3) selecting a compound that attenuates the binding of agouti-related protein to melanocortin receptors, but does not affect the binding of &agr;-melanocyte stimulating hormone to melanocortin receptors.

  本发明提供了一种治疗肥胖症、性功能障碍（包括勃起功能障碍）、糖尿病、胰岛素抵抗、高胰岛素血症、X综合症、肾上腺功能障碍、高血压、高胆固醇血症、动脉硬化、高脂蛋白血症、高甘油三酯血症或物质滥用的方法，其中所述方法包括向患有或有患上上述疾病风险的患者施用一种治疗有效量的化合物，该化合物减弱了类似鼠标肥胖相关蛋白与黑色素皮质素受体的结合，但不减弱α-黑色素细胞刺激素与黑色素皮质素受体的结合。本发明还提供了一种用于治疗或预防肥胖症、性功能障碍（包括勃起功能障碍）、糖尿病、胰岛素抵抗、高胰岛素血症、X综合症、肾上腺功能障碍、高血压、高胆固醇血症、动脉硬化、高脂蛋白血症、高甘油三酯血症或物质滥用的化合物的识别方法，该方法包括以下步骤：1）确定化合物是否影响类似鼠标肥胖相关蛋白与黑色素皮质素受体的结合；2）确定化合物是否影响α-黑色素细胞刺激素与黑色素皮质素受体的结合；3）选择减弱类似鼠标肥胖相关蛋白与黑色素皮质素受体的结合，但不影响α-黑色素细胞刺激素与黑色素皮质素受体的结合的化合物。
• Methods of administering apo B-secretion/MTP inhibitors
  申请人：Pfizer Products Inc.

  公开号：EP1099442A2

  公开（公告）日：2001-05-16

  The invention provides methods for administering of apolipoprotein B-secretion (Apo B)/microsomal triglyceride transfer protein (MTP) inhibitors which comprise administering the inhibitor to a subject in need of treatment therewith prior to, or during, a period of somnolence.

  本发明提供了给药载脂蛋白B-分泌（载脂蛋白B）/甘油三酯微粒体转移蛋白（MTP）抑制剂的方法，包括在嗜睡期之前或期间给需要治疗的受试者服用抑制剂。