4-(1-Ethyl-propylamino)-6-methyl-2-(2,4,6-trimethyl-phenoxy)-nicotinic acid methyl ester | 190771-02-9

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 4-(1-Ethyl-propylamino)-6-methyl-2-(2,4,6-trimethyl-phenoxy)-nicotinic acid methyl ester
• 英文别名: 4-(1-Ethyl-propylamino)-6-methyl-2-(2,4,6-trimethyl-phenoxy)nicotinic acid methyl ester；methyl 6-methyl-4-(pentan-3-ylamino)-2-(2,4,6-trimethylphenoxy)pyridine-3-carboxylate
• CAS: 190771-02-9
• 化学式: C₂₂H₃₀N₂O₃
• 分子量: 370.492
• InChiKey: MYFIUHJIEHESCM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  6.5
• 重原子数：
  27
• 可旋转键数：
  8
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.45
• 拓扑面积：
  60.4
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  4-(1-Ethyl-propylamino)-6-methyl-2-(2,4,6-trimethyl-phenoxy)-nicotinic acid methyl ester 在 AlCl₃ sodium hydroxide 、 LiAlH4 作用下， 以 四氢呋喃 、 乙醚 、 水 为溶剂， 生成 2-(均三甲苯基氧基)-3,6-二甲基-N-(3-戊烷基)-4-吡啶胺
  参考文献：
  名称：

  Method of treating heart failure

  摘要：

  本发明涉及一种治疗心力衰竭的方法，包括向哺乳动物施用有效治疗量的4-(1-乙基-丙氧基)-3,6-二甲基-2-(2,4,6-三甲基苯氧基)-吡啶和(3,6-二甲基-2-(2,4,6-三甲基苯氧基)-吡啶-4-基)-(1-乙基丙基)-胺或其药用可接受的盐。本发明还涉及使用这两种药物与其他治疗充血性心力衰竭化合物的组合物来治疗充血性心力衰竭的方法。

  公开号：

  US06043260A1
• 作为产物：
  描述：

  4-chloro-6-methyl-2-(2,4,6-trimethyl-phenoxy)-nicotinic acid methyl ester 、 3-氨基戊烷 在 氯化铵 、 乙酸乙酯 作用下， 以 二甲基亚砜 为溶剂， 反应 15.0h， 以to give 445.6 mg of yellow solid的产率得到4-(1-Ethyl-propylamino)-6-methyl-2-(2,4,6-trimethyl-phenoxy)-nicotinic acid methyl ester
  参考文献：
  名称：

  Corticotropin releasing factor antagonists

  摘要：

  Corticotropin-releasing factor (CRF) 拮抗剂具有以下公式，其中虚线、A、B、Y、Z、G、R3、R4、R5、R6、R16 和 R17 的定义如申请书所述，并提供了其制备方法。这些化合物及其药学上可接受的盐在治疗包括中枢神经系统和与压力相关的疾病方面是有用的。

  公开号：

  US07125880B1

文献信息

• Corticotropin releasing factor antagonists
  申请人：——

  公开号：US20020016328A1

  公开（公告）日：2002-02-07

  Corticotropin-releasing factor (CRF) antagonists having the formulae 1 wherein the dashed lines, A, B, Y, Z, G, R 3 , R 4 , R 5 , R 6 , R 16 and R 17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.

  具有以下公式的促肾上腺皮质激素释放因子（CRF）拮抗剂，其中虚线、A、B、Y、Z、G、R3、R4、R5、R6、R16和R17如申请中所定义，并且制备它们的过程。这些化合物及其药用盐可用于治疗包括中枢神经系统和与压力相关的疾病。
• Method of treating heart failure
  申请人：Pfizer Inc

  公开号：US06043260A1

  公开（公告）日：2000-03-28

  This invention relates to method for treating a mammal which presents with heart failure comprising administering to a mammal a therapeutically effective amount of wherein 4-(1-ethyl-propoxy)-3,6-dimethyl-2-(2,4,6-trimethyl-phenoxy)-pyridine and (3,6-dimethyl-2-(2,4,6-trimethyl-phenoxy)-pyridin-4-yl)-(1-ethyl-propyl)-a mine or a pharmaceutically acceptable salt thereof. This invention is also directed to methods of using combinations of those two agents with other congestive heart failure treating compounds to treat congestive heart failure.

  本发明涉及一种治疗心力衰竭的方法，包括向哺乳动物施用有效治疗量的4-(1-乙基-丙氧基)-3,6-二甲基-2-(2,4,6-三甲基苯氧基)-吡啶和(3,6-二甲基-2-(2,4,6-三甲基苯氧基)-吡啶-4-基)-(1-乙基丙基)-胺或其药用可接受的盐。本发明还涉及使用这两种药物与其他治疗充血性心力衰竭化合物的组合物来治疗充血性心力衰竭的方法。
• Use of 3,6-dimethyl-2-(2,4,6-trimethylphenoxy)-pyridines for treating heart failure
  申请人：Pfizer Products Inc.

  公开号：EP0951906A1

  公开（公告）日：1999-10-27

  This invention relates to treatments for a mammal which presents with heart failure comprising administering to a mammal a therapeutically effective amount of wherein 4-(1-ethyl-propoxy)-3,6-dimethyl-2-(2,4,6-trimethyl-phenoxy)-pyridine and (3,6-dimethyl-2-(2,4,6-trimethyl-phenoxy)-pyridin-4-yl)-(1-ethyl-propyl)-amine or a pharmaceutically acceptable salt thereof. This invention is also directed to combinations of those two agents with other congestive heart failure treating compounds to treat congestive heart failure.

  这项发明涉及治疗患有心力衰竭的哺乳动物，包括向哺乳动物施用治疗有效量的4-(1-乙基丙氧基)-3,6-二甲基-2-(2,4,6-三甲基苯氧基)-吡啶和(3,6-二甲基-2-(2,4,6-三甲基苯氧基)-吡啶-4-基)-(1-乙基丙基)-胺或其药用可接受的盐。该发明还涉及上述两种药物与其他治疗充血性心力衰竭的化合物的组合，用于治疗充血性心力衰竭。
• New uses for corticotropin releasing factor (CRF) antagonists
  申请人：PFIZER INC.

  公开号：EP0773023A1

  公开（公告）日：1997-05-14

  A method of treating, preventing or inhibiting a disorder selected from the group consisting of cardiovascular or heart related diseases such as stroke, hypertension, tachycardia, and congestive heart failure, osteoporosis, premature birth, psychosocial dwarfism, stress-induced fever, ulcer, diarrhea, post-operative ileus, and colonic hypersensitivity associated with psychopathological disturbance and stress, comprising administering to a mammal, including a human, in need of such treatment a therapeutically effective amount of a compound of the formula    or a pharmaceutically acceptable salt thereof, wherein A, B, D, E, Y, Z, R3, R4, and R5 are as defined herein.

  一种治疗、预防或抑制心血管或心脏相关疾病（如中风、高血压、心动过速和充血性心力衰竭）、骨质疏松症、早产、心理社交侏儒症、压力诱发发热、溃疡、腹泻、术后肠梗阻和与心理病理障碍和压力相关的结肠过敏反应的方法，包括向需要此类治疗的哺乳动物（包括人类）中，给予化合物的治疗有效量，该化合物的结构式如下：其中A、B、D、E、Y、Z、R3、R4和R5的定义如本文所述，或其药学上可接受的盐。
• New uses for corticotropin releasing factor antagonists
  申请人：——

  公开号：US20010000340A1

  公开（公告）日：2001-04-19

  A method of treating, preventing or inhibiting a disorder selected from the group consisting of cardiovascular or heart related diseases such as stroke, hypertension, tachycardia, and congestive heart failure, osteoporosis, premature birth, psychosocial dwarfism, stress-induced fever, ulcer, diarrhea, post-operative ileus, and colonic hypersensitivity associated with psychopathological disturbance and stress, comprising administering to a mammal, including a human, in need of such treatment a therapeutically effective amount of a compound of the formula 1 or pharmaceutically acceptable salt thereof, wherein A, B, D, E, Y, Z, R 3 , R 4 , and R 5 are as defined herein.

  一种治疗、预防或抑制选自心血管或心脏相关疾病（如中风、高血压、心动过速和充血性心力衰竭）、骨质疏松症、早产、心理社交侏儒症、应激性发热、溃疡、腹泻、术后肠梗阻和与心理病理障碍和应激有关的结肠过敏反应的方法，包括向需要该治疗的哺乳动物，包括人类，投与化合物1或其药学上可接受的盐的治疗有效量，其中A、B、D、E、Y、Z、R3、R4和R5如本文所定义。