5-[2,2-dimethyl-6-(1-methyl-1H-pyrazol-3-ylcarbamoyl)-2,3-dihydro-benzofuran-4-yloxy]-3-fluoro-pyridine-2-carboxylic acid methylamide

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: 5-[2,2-dimethyl-6-(1-methyl-1H-pyrazol-3-ylcarbamoyl)-2,3-dihydro-benzofuran-4-yloxy]-3-fluoro-pyridine-2-carboxylic acid methylamide
• 英文别名: 5-[[2,2-dimethyl-6-[(1-methylpyrazol-3-yl)carbamoyl]-3H-1-benzofuran-4-yl]oxy]-3-fluoro-N-methylpyridine-2-carboxamide
• 化学式: C₂₂H₂₂FN₅O₄
• 分子量: 439.446
• InChiKey: PGTASNUKDCFAAX-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.2
• 重原子数：
  32
• 可旋转键数：
  5
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.27
• 拓扑面积：
  107
• 氢给体数：
  2
• 氢受体数：
  7

反应信息

• 作为产物：
  描述：

  甲胺 在 N,N-二甲基甲酰胺 草酰氯 、 三乙胺 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 2.5h， 以48%的产率得到5-[2,2-dimethyl-6-(1-methyl-1H-pyrazol-3-ylcarbamoyl)-2,3-dihydro-benzofuran-4-yloxy]-3-fluoro-pyridine-2-carboxylic acid methylamide
  参考文献：
  名称：

  WO2007/122482

  摘要：

  公开号：

文献信息

• FUSED PHENYL AMIDO HETEROCYCLIC COMPOUNDS
  申请人：Bai Hao

  公开号：US20080280875A1

  公开（公告）日：2008-11-13

  The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R 1 , R 1a , R 2 , R 3 , R 4 , L 2 , n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).

  本发明涉及以下式(I)的化合物：或其药用可接受的盐或溶剂，其中：环A为(4-12)成员杂环基；环B是从以下组中选择的融合苯环之一：环A、环B、环C、R1、R1a、R2、R3、R4、L2、n、t、w和z如规范中所定义。本发明还涉及包括式(I)的化合物的药物组合物以及治疗通过调节葡萄糖激酶介导的疾病的方法，该方法包括向哺乳动物施用有效量的式(I)的化合物。
• Fused Phenyl Amido Heterocyclic Compounds
  申请人：Bai Hao

  公开号：US20110039821A1

  公开（公告）日：2011-02-17

  The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R 1 , R 1a , R 2 , R 3 , R 4 , L 2 , n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).

  本发明涉及以下式子的化合物(I)或其药学上可接受的盐或溶剂： 其中，环A是(4-12)成员杂环基；环B是从以下组中选择的融合苯环：环A、环B、环C、R1、R1a、R2、R3、R4、L2、n、t、w和z在规范中定义。本发明还涉及包括式(I)化合物的药物组合物和通过调节葡萄糖激酶介导的疾病的治疗方法，该方法包括向哺乳动物施用式(I)化合物的有效量。
• Fused phenyl Amido heterocyclic compounds for the prevention and treatment of glucokinase-mediated diseases
  申请人：Pfizer Products Inc.

  公开号：EP2463283A1

  公开（公告）日：2012-06-13

  The present invention relates to a compound of formula (VIa): or a pharmaceutically acceptable s alt or solvate thereof, wherein Ring A is pyrazinyl and L1, R1, R1a, R4, L2, R2, R3, w and n are as defined herein. Such compounds are glucokinase agonists and useful in the treatment of diseases including diabetes and obesity.

  本发明涉及一种式 (VIa) 的化合物： 或其药学上可接受的 s alt 或溶液，其中环 A 是吡嗪基，L1、R1、R1a、R4、L2、R2、R3、w 和 n 如本文所定义。此类化合物是葡萄糖激酶激动剂，可用于治疗糖尿病和肥胖症等疾病。
• HETEROBICYCLIC AMIDES FOR THE PREVENTION AND TREATMENT OF GLUCOKINASE-MEDIATED DISEASES
  申请人：Pfizer Products Inc.

  公开号：EP2010520B1

  公开（公告）日：2012-09-12
• US7842713B2
  申请人：——

  公开号：US7842713B2

  公开（公告）日：2010-11-30