[2R,4S] 4-[acetyl-(3,5-bis-trifluoromethyl-benzyl)-amino]-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid isopropyl ester | 261947-38-0

• 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: [2R,4S] 4-[acetyl-(3,5-bis-trifluoromethyl-benzyl)-amino]-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid isopropyl ester
• 英文别名: (2R,4S)-4-(Acetyl(3,5-bis(trifluoromethyl)benzyl)amino)-2-ethyl-6-trifluoromethyl-3,4-dihydro-2H-quinoline-1-carboxylic acid isopropyl ester；propan-2-yl (2R,4S)-4-[acetyl-[[3,5-bis(trifluoromethyl)phenyl]methyl]amino]-2-ethyl-6-(trifluoromethyl)-3,4-dihydro-2H-quinoline-1-carboxylate
• CAS: 261947-38-0
• 化学式: C₂₇H₂₇F₉N₂O₃
• 分子量: 598.509
• InChiKey: TUPKOWFPVAXQFP-OFNKIYASSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.1
• 重原子数：
  41
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  49.8
• 氢给体数：
  0
• 氢受体数：
  12

文献信息

• Novel triazine compounds useful as sorbitol dehydrogenase inhibitors
  申请人：——

  公开号：US20030004166A1

  公开（公告）日：2003-01-02

  This invention is directed to sorbitol dehydrogenase inhibitory compounds of formula I 1 wherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing these compounds which inhibit sorbitol dehydrogenase and to methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy, diabetic cardiomyopathy and foot ulcers, by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of the present invention with a second pharmaceutical agent, including an aldose reductase inhibitor, a sodium hydrogen ion exchange (NHE-1) inhibitor, a glycogen phosphorylase inhibitor (GPI), a selective serotonin reuptake inhibitor, a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, an angiotensin converting enzyme inhibitor, a thiazolidinedione antidiabetic agent, an angiotensin 11 receptor antagonist, a &ggr;-aminobutyric acid (GABA) agonist, a phosphodiesterase type 5 inhibitor, an adenosine agonist, and a CETP inhibitor and to methods of using these combination compositions.

  这项发明涉及到化合物的抑制山梨醇脱氢酶的公式I1，其中R1、R2和R3如规范中所定义。这项发明还涉及含有这些化合物的药物组合物，其抑制山梨醇脱氢酶，并通过向患有糖尿病且因此有发生这些并发症风险的哺乳动物施用这些化合物的方法来治疗或预防糖尿病并发症，特别是糖尿病神经病变、糖尿病肾病、糖尿病微血管病、糖尿病大血管病、糖尿病心肌病和足部溃疡。这项发明还涉及含有本发明公式I的化合物与第二药物剂的组合的药物组合物，包括醛糖还原酶抑制剂、钠氢离子交换（NHE-1）抑制剂、糖原磷酸化酶抑制剂（GPI）、选择性5-羟色胺再摄取抑制剂、3-羟基-3-甲基戊二酸辅酶A还原酶抑制剂、血管紧张素转换酶抑制剂、噻唑烷二酮抗糖尿病药物、血管紧张素II受体拮抗剂、γ-氨基丁酸（GABA）激动剂、磷酸二酯酶5抑制剂、腺苷激动剂和CETP抑制剂，以及使用这些组合组合物的方法。
• 4-Amino substituted-2-substituted-1,2,3,4-tetrahydroquinoline compounds
  申请人：Ruggeri B. Roger

  公开号：US20060063803A1

  公开（公告）日：2006-03-23

  4-Amino substituted-2-substituted-1,2,3,4-tetrahydroquinoline 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.

  含有4-氨基取代-2-取代-1,2,3,4-四氢喹啉化合物的药物组合物，以及含有这种化合物的药物组合物，并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，并相应地治疗由于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。
• 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。
• ORALLY DISINTEGRATING TABLET COMPOSITIONS OF TEMAZEPAM
  申请人：VENKATESH Gopi M.

  公开号：US20090169620A1

  公开（公告）日：2009-07-02

  The compositions of the present invention are orally disintegrating tablet compositions comprising a therapeutically effective amount of at least one drug such as temazepam, 0.5-3% of an ODT binder polymer, a sugar alcohol and/or saccharide, and a disintegrant.

  本发明的组合物是口服快速溶解片剂组合物，包括至少一种药物（例如temazepam）的治疗有效量，0.5-3％的ODT结合剂聚合物，糖醇和/或糖类，以及一种分散剂。