2-methyl-4-(N-ethyl-N-n-butyl)amino-8-(2,4,6-trimethylphenyl)-quinoline

• 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: 2-methyl-4-(N-ethyl-N-n-butyl)amino-8-(2,4,6-trimethylphenyl)-quinoline
• 英文别名: 4-(butyl-ethyl-amino)-2-methyl-8-(2,4,6-trimethyl-phenyl)-quinoline；Butyl-ethyl-[2-methyl-8-(2,4,6-trimethyl-phenyl)-quinolin-4-yl]-amine；N-butyl-N-ethyl-2-methyl-8-(2,4,6-trimethylphenyl)quinolin-4-amine
• 化学式: C₂₅H₃₂N₂
• 分子量: 360.542
• InChiKey: YLBFOSKJJOYRAY-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  7.1
• 重原子数：
  27
• 可旋转键数：
  6
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  16.1
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  2,4,6-三甲基苯硼酸 在 四(三苯基膦)钯 、 sodium carbonate 、 对甲苯磺酸 、 三氯氧磷 作用下， 以 二苯醚 、 苯 为溶剂， 生成 2-methyl-4-(N-ethyl-N-n-butyl)amino-8-(2,4,6-trimethylphenyl)-quinoline
  参考文献：
  名称：

  Synthesis and SAR of 8-Arylquinolines as potent corticotropin-Releasing factor1 (CRF1) receptor antagonists

  摘要：

  A series of 4-substituted 8-aryl-2-methylquinolines 4 was designed and synthesized as highly potent antagonists for the human CRF1 receptor. This series of compounds displayed parallel SAR to other bicyclic systems such as pyrazolo[l,5-a]pyrimidines, with several compounds possessing low nanomolar binding affinity. In addition to the high potency, the basicity of this 4-aminoquinoline core may offer CRF1 antagonists with lower lipophilicity. (C) 2003 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(03)00684-x

文献信息

• Quinoline and quinazoline derivatives having corticotropin releasing factor (CRF) antagonist activity
  申请人：Duphar International Research B.V.

  公开号：US06350750B1

  公开（公告）日：2002-02-26

  The present invention relates to novel compounds, to a method for the preparation of these novel compounds, to pharmaceutical compositions containing one or more of these compounds as an active component and to methods of using these in the treatment of stress-related disorders.

  本发明涉及新化合物，涉及制备这些新化合物的方法，涉及含有这些化合物之一或多个作为活性成分的药物组合物，以及使用这些化合物治疗与压力相关的疾病的方法。
• Substituted6,6-hetero-bicyclicderivatives
  申请人：——

  公开号：US20030114671A1

  公开（公告）日：2003-06-19

  This invention relates to compounds of the formula 1 wherein A, B, D, E, K, G, R 3 and R 5 are defined as in the specification, and to the pharmaceutically acceptable salts of such compounds.

  该发明涉及公式1中的化合物，其中A、B、D、E、K、G、R3和R5如规范中定义的那样，以及这些化合物的药用盐。
• Use of CRF antagonists and related compositions for treating depression and modifying the circadian rhytm
  申请人：Pfizer Products Inc.

  公开号：EP1082960A2

  公开（公告）日：2001-03-14

  A corticotropin releasing factor (CRF) antagonist is administered to treat a condition selected from the group consisting of: c)disorders that can be treated by altering circadian rhythm; and d)depression, further wherein a second compound for treating depression is administered, the second compound for treating depression having an onset of action that is delayed with respect to that of the CRF antagonist.

  一种促肾上腺皮质激素释放因子（CRF）拮抗剂用于治疗选自以下组别的疾病： c)可通过改变昼夜节律来治疗的疾病；以及 d)抑郁症，其中还施用了治疗抑郁症的第二种化合物，治疗抑郁症的第二种化合物的起效时间比CRF拮抗剂的起效时间延迟。
• Use of corticotropin releasing factor antagonists for treating syndrome X
  申请人：Pfizer Products Inc.

  公开号：EP1097709A2

  公开（公告）日：2001-05-09

  The present invention relates to compositions and methods of achieving a thereapeutic effect including, the treatment or prevention of syndrome X in an animal, preferably a mammal including a human subject or a companion animal, using a corticotropin releasing factor (CRF) antagonist alone or together with a glucocorticoid receptor antagonist.

  本发明涉及单独使用促肾上腺皮质激素释放因子（CRF）拮抗剂或与糖皮质激素受体拮抗剂一起使用以达到治疗或预防动物（最好是哺乳动物，包括人类或伴侣动物）X综合征的效果的组合物和方法。
• Combinations of corticotropin releasing factor antagonists and growth hormone secretagogues
  申请人：Pfizer Products Inc.

  公开号：EP1149583A2

  公开（公告）日：2001-10-31

  This invention is directed to pharmaceutical compositions comprising corticotropin releasing factor antagonist and growth hormone or growth hormone secretagogues, prodrugs thereof, or pharmaceutically acceptable salts of said compounds or said prodrugs. The invention is also directed to the use of such compositions in the treatment or prevention of osteoporosis and heart-related diseases (including congestive heart failure) in mammals, particularly humans.

  本发明涉及包含促肾上腺皮质激素释放因子拮抗剂和生长激素或生长激素促泌剂、其原药或所述化合物或所述原药的药学上可接受的盐的药物组合物。本发明还用于治疗或预防哺乳动物，特别是人类的骨质疏松症和心脏相关疾病（包括充血性心力衰竭）。