N,N-bis(3-methylbutyl)-2-morpholin-4-yl-3-(3-pyrrolidin-1-ylprop-1-ynyl)imidazo[1,2-a]pyridine-6-carboxamide | 1219715-37-3

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 咪唑并吡啶类
• 英文名称: N,N-bis(3-methylbutyl)-2-morpholin-4-yl-3-(3-pyrrolidin-1-ylprop-1-ynyl)imidazo[1,2-a]pyridine-6-carboxamide
• CAS: 1219715-37-3
• 化学式: C₂₉H₄₃N₅O₂
• 分子量: 493.693
• InChiKey: NPCCJGIXUBCBKD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.4
• 重原子数：
  36
• 可旋转键数：
  10
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.66
• 拓扑面积：
  53.3
• 氢给体数：
  0
• 氢受体数：
  5

反应信息

• 作为产物：
  描述：

  吗啉 、 2-bromo-3-(3-pyrrolidin-1-yl-prop-1-ynyl)-imidazo[1,2-a]pyridine-6-carboxylic acid bis-(3-methyl-butyl)amide 在 tris-(dibenzylideneacetone)dipalladium(0) caesium carbonate 、 4,5-双二苯基膦-9,9-二甲基氧杂蒽 作用下， 以 1,4-二氧六环 为溶剂， 生成 N,N-bis(3-methylbutyl)-2-morpholin-4-yl-3-(3-pyrrolidin-1-ylprop-1-ynyl)imidazo[1,2-a]pyridine-6-carboxamide
  参考文献：
  名称：

  Substituted imidazopyridine, imidazopyrazine, imidazopyridazine and imidazopyrimidine derivatives as melanocortin-4 receptor antagonists

  摘要：

  本发明涉及根据式(I)的取代咪唑吡啶衍生物、咪唑吡嗪衍生物、咪唑吡嗪衍生物和咪唑嘧啶衍生物作为黑色素皮质激素-4受体（MC-4R）调节剂，特别是作为黑色素皮质激素-4受体拮抗剂。这些拮抗剂可用于治疗癌症恶病质、肌肉消耗、厌食症、呕吐、肌萎缩性侧索硬化（ALS）、焦虑和抑郁等疾病和疾病。

  公开号：

  EP2168965A1

文献信息

• [EN] SUBSTITUTED IMIDAZOPYRIDINE, IMIDAZOPYRAZINE, IMIDAZOPYRIDAZINE AND IMIDAZOPYRIMIDINE DERIVATIVES AS MELANOCORTIN-4 RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS D'IMIDAZOPYRIDINE SUBSTITUÉE, D'IMIDAZOPYRAZINE, D'IMIDAZOPYRIDAZINE ET D'IMIDAZOPYRIMIDINE UTILISÉS COMME ANTAGONISTES DU RÉCEPTEUR DE LA MÉLANOCORTINE-4
  申请人：SANTHERA PHARMACEUTICALS CH

  公开号：WO2010034500A1

  公开（公告）日：2010-04-01

  The present invention relates to substituted imidazopyridine derivatives, imidazopyrazine derivatives, imidazopyridazine derivatives and imidazopyrimidine derivatives according to formula (I) as melanocortin-4 receptor (MC-4R) modulators, in particular as melanocortin 4 receptor antagonists. The antagonists are useful for the treatment of disorders and diseases such as cachexia induced by e.g. cancer, chronic kidney disease (CKD) or chronic heart failure (CHF), muscle wasting, anorexia induced by e.g. chemotherapy or radiotherapy, anorexia nervosa, amyotrophic lateral sclerosis (ALS), pain, neuropathic pain, anxiety and depression, nausea and emesis.
• Substituted imidazopyridine, imidazopyrazine, imidazopyridazine and imidazopyrimidine derivatives as melanocortin-4 receptor antagonists
  申请人：Santhera Pharmaceuticals (Schweiz) AG

  公开号：EP2168965A1

  公开（公告）日：2010-03-31

  The present invention relates to substituted imidazopyridine derivatives, imidazopyrazine derivatives, imidazopyridazine derivatives and imidazopyrimidine derivatives according to formula (I) as melanocortin-4 receptor (MC-4R) modulators, in particular as melanocortin-4 receptor antagonists. The antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, emesis, amyotrophic lateral sclerosis (ALS), anxiety and depression.

  本发明涉及根据式(I)的取代咪唑吡啶衍生物、咪唑吡嗪衍生物、咪唑吡嗪衍生物和咪唑嘧啶衍生物作为黑色素皮质激素-4受体（MC-4R）调节剂，特别是作为黑色素皮质激素-4受体拮抗剂。这些拮抗剂可用于治疗癌症恶病质、肌肉消耗、厌食症、呕吐、肌萎缩性侧索硬化（ALS）、焦虑和抑郁等疾病和疾病。