[2R,4S] 4-[(3,5-bis-trifluoromethyl-benzyl)-methoxycarbonyl-amino]-2-methyl-3,4,6,8-tetrahydro-2H-furo[3,4-g]quinoline-1-carboxylic acid ethyl ester | 398521-99-8

• 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: [2R,4S] 4-[(3,5-bis-trifluoromethyl-benzyl)-methoxycarbonyl-amino]-2-methyl-3,4,6,8-tetrahydro-2H-furo[3,4-g]quinoline-1-carboxylic acid ethyl ester
• 英文别名: ethyl (2R,4S)-4-[[3,5-bis(trifluoromethyl)phenyl]methyl-methoxycarbonylamino]-2-methyl-3,4,6,8-tetrahydro-2H-furo[3,4-g]quinoline-1-carboxylate
• CAS: 398521-99-8
• 化学式: C₂₆H₂₆F₆N₂O₅
• 分子量: 560.493
• InChiKey: NJNVNQZBKCXDGK-SZNDQCEHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.8
• 重原子数：
  39
• 可旋转键数：
  6
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.46
• 拓扑面积：
  68.3
• 氢给体数：
  0
• 氢受体数：
  11

文献信息

• CETP inhibitors in combination with antihypertensive agents and uses thereof
  申请人：Pfizer Inc.

  公开号：US20040039018A1

  公开（公告）日：2004-02-26

  This invention relates to pharmaceutical combinations of a cholesteryl ester transfer protein (CETP) inhibitor or a pharmaceutically acceptable salt thereof; and an antihypertensive agent or a pharmaceutically acceptable salt thereof, optionally in combination with an HMG CoA reductase inhibitor or a pharmaceutically acceptable salt thereof, kits containing such combinations and methods of using such combinations to treat subjects suffering from atherosclerosis, peripheral vascular disease, dyslipidemia, hyperbetaliproteinemia, hypoalphalipoproteinemia, hypercholesterolemia, hypertriglyceridemia, familial-hypercholesterolemia, cardiovascular disorders, angina, ischemia, cardiac ischemia, stroke, myocardial infarction, reperfusion injury, angioplastic restenosis, hypertension, vascular complications of diabetes, obesity or endotoxemia in a mammal (including a human being either male or female).

  本发明涉及一种胆固醇酯转移蛋白（CETP）抑制剂或其药学上可接受的盐与降压药剂或其药学上可接受的盐的药物组合，可选地与HMG CoA还原酶抑制剂或其药学上可接受的盐的药物组合，包含这种组合的套件以及使用这种组合治疗患有动脉粥样硬化、外周血管疾病、血脂异常、高β脂蛋白血症、低α脂蛋白血症、高胆固醇血症、高三酰甘油血症、家族性高胆固醇血症、心血管疾病、心绞痛、缺血、心肌缺血、中风、心肌梗死、再灌注损伤、血管成形术再狭窄、高血压、糖尿病血管并发症、肥胖或内毒素血症的哺乳动物（包括男性或女性人类）的使用方法。
• Methods of treatment with CETP inhibitors and antihypertensive agents
  申请人：Pfizer Inc.

  公开号：US20040053842A1

  公开（公告）日：2004-03-18

  This invention relates to cholesterol ester transfer protein (CETP) inhibitors, pharmaceutical compositions containing such inhibitors, and the use of such inhibitors to treat certain disease/conditions optionally in combination with certain therapeutic agents e.g., antihypertensive agents.

  本发明涉及胆固醇酯转移蛋白（CETP）抑制剂，含有这种抑制剂的药物组合物，以及使用这种抑制剂治疗某些疾病/症状，可选择性地与某些治疗药物如降压药物结合使用。
• Compositions of choleseteryl ester transfer protein inhibitors and HMG-CoA reductase inhibitors
  申请人：Pfizer Inc

  公开号：US20040132771A1

  公开（公告）日：2004-07-08

  A composition comprises (1) a solid amorphous adsorbate comprising a cholesteryl ester transfer protein (CETP) inhibitor and a substrate; and (2) an HMG-CoA reductase inhibitor. The solid amorphous adsorbate provides concentration enhancement of the CETP inhibitor relative to a control composition consisting essentially of the unadsorbed CETP inhibitor alone, resulting in improved bioavailability.

  这篇文章包括(1)一个固态无定形吸附剂，其中包含一个胆固醇酯转移蛋白(CETP)抑制剂和一个底物;和(2)一个HMG-CoA还原酶抑制剂。固态无定形吸附剂相对于仅由未吸附的CETP抑制剂组成的对照组成分提供了CETP抑制剂的浓度增强，从而提高了生物利用度。
• Pharmaceutical compositions of adsorbates of amorphous drug
  申请人：——

  公开号：US20030054037A1

  公开（公告）日：2003-03-20

  Pharmaceutical compositions comprise a low-solubility drug adsorbed onto a high surface area substrate to form an adsorbate. The compositions in some embodiments include a concentration-enhancing polymer.

  药物组合物包括低溶解度药物吸附在高表面积基质上形成吸附剂。在某些实施例中，该组合物包括浓度增强聚合物。
• Annulated 4-carboxyamino-2-methyl-1,2,3,4-tetrahydroquinolines as CETP inhibitors
  申请人：Pfizer Products Inc.

  公开号：EP0992496A1

  公开（公告）日：2000-04-12

  Cholesteryl ester transfer protein inhibitors of formula I, pharmaceutical compositions containing such inhibitors and the use of such inhibitors 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. R1, R3-R8 are as in the application, wherein R5 and R6 or R6 or R7 and/or R7 and R8 together form at least 1 4-8 membered ring.

  式 I 的胆固醇酯转移蛋白抑制剂、含有此类抑制剂的药物组合物以及使用此类抑制剂提高某些血浆脂质水平（包括高密度脂蛋白-胆固醇）和降低某些其他血浆脂质水平（如低密度脂蛋白-胆固醇和甘油三酯）的方法、如低密度脂蛋白胆固醇和甘油三酯，并据此治疗因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而恶化的疾病，如包括人类在内的一些哺乳动物的动脉粥样硬化和心血管疾病。 R1、R3-R8如本申请中所述，其中R5和R6或R6或R7和/或R7和R8共同形成至少1个4-8员环。