diethyl 5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-3H-1-benzofuran-2,2-dicarboxylate

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 香豆素
• 英文名称: diethyl 5-[2-[[2-(3-chlorophenyl)-2-hydroxyethyl]amino]propyl]-3H-1-benzofuran-2,2-dicarboxylate
• 化学式: C₂₅H₃₀ClNO₆
• 分子量: 476.0
• InChiKey: QIOUNMRNAWEYKW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.3
• 重原子数：
  33
• 可旋转键数：
  12
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.44
• 拓扑面积：
  94.1
• 氢给体数：
  2
• 氢受体数：
  7

文献信息

• Heterocyclic Beta-3 Adrenergenic Agonists
  申请人：PFIZER INC.

  公开号：EP0801060A1

  公开（公告）日：1997-10-15

  The present invention relates to certain compounds of the formula (I) the racemic-enantiomeric mixtures and optical isomers of said compounds and the pharmaceutically acceptable salts or prodrugs thereof, depicted below, which are β-adrenergic receptor agonists and accordingly have utility as, inter alia, hypoglycemic and antiobesity agents. More specifically, the compounds of the instant invention are selective agonists of β3-adrenergic receptor. The invention also relates to methods of use for the compounds and to pharmaceutical 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 and poultry. The compounds have the formula    wherein R1, R2, R3, R4, R5, Y and Z are as defined in the specification.

  本发明涉及某些式（I）化合物、所述化合物的外消旋-对映异构体混合物和光学异构体及其药学上可接受的盐或原药，如下所述，这些化合物是β-肾上腺素能受体激动剂，因此可用作降血糖药和抗肥胖药等。更具体地说，本发明的化合物是 β3-肾上腺素能受体的选择性激动剂。本发明还涉及化合物的使用方法和含有这些化合物的药物组合物。本发明的化合物还可用于增加瘦肉的沉积和/或改善动物（如蹄类动物、伴侣动物和家禽）的瘦肉脂肪比。本发明的化合物具有如下式子 其中 R1、R2、R3、R4、R5、Y 和 Z 如说明书中所定义。