1-[[4-(Carboxymethylsulfonylamino)phenyl]methyl]-5-[2-[(2-hydroxy-3-phenoxypropyl)amino]propyl]indole-2-carboxylic acid

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吲哚及其衍生物
• 英文名称: 1-[[4-(Carboxymethylsulfonylamino)phenyl]methyl]-5-[2-[(2-hydroxy-3-phenoxypropyl)amino]propyl]indole-2-carboxylic acid
• 化学式: C₃₀H₃₃N₃O₈S
• 分子量: 595.7
• InChiKey: RZTVYCMFTPMJRT-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  42
• 可旋转键数：
  15
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  176
• 氢给体数：
  5
• 氢受体数：
  10

文献信息

• B-3-adrenergic agonists as antidiabetic and antiobesity agents
  申请人：PFIZER INC.

  公开号：EP0822185A1

  公开（公告）日：1998-02-04

  The present invention relates to certain compounds of the formula (I) the racemic-enantiomeric mixtures and optical isomers of said compounds, prodrugs thereof and the pharmaceutically acceptable salts, depicted below, which are β-adrenergic receptor agonists and accordingly have utility as, inter alia, hypoglycemic and antiobesity agents. The invention also relates to methods of use for the compounds and to compositions containing them. The compounds of the present invention also possess utility for increasing lean meat deposition and/or improving the lean meat to fat ratio in animals, e.g., ungulate animals, companion animals, especially dogs, and poultry. The compounds of formula (I) have the following structure wherein R1, R2, R3, R4 and R5 are as defined in the specification.

  本发明涉及以下结构的某些化合物（I）的拉氏-对映混合物和光学异构体，以及这些化合物的前药和药用盐，如下所示，它们是β-肾上腺素受体激动剂，因此在降糖和抗肥胖剂等方面具有用途。该发明还涉及这些化合物的使用方法和含有它们的组合物。本发明的化合物还具有增加瘦肉沉积和/或改善动物（例如有蹄动物、伴侣动物，尤其是狗，和家禽）中的瘦肉与脂肪比例的用途。式（I）的化合物具有以下结构，其中R1、R2、R3、R4和R5如规范中所定义。
• US5859044A
  申请人：——

  公开号：US5859044A

  公开（公告）日：1999-01-12