methyl 2-[5-[[3-[2-[[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]methoxy]-4,6-dimethylpyrimidin-5-yl]-2-methylphenyl]methylamino]spiro[1,3-dihydroindene-2,1'-cyclopropane]-1-yl]acetate | 1253117-53-1

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚和异茚
• 英文名称: methyl 2-[5-[[3-[2-[[(4R)-2,2-dimethyl-1,3-dioxolan-4-yl]methoxy]-4,6-dimethylpyrimidin-5-yl]-2-methylphenyl]methylamino]spiro[1,3-dihydroindene-2,1'-cyclopropane]-1-yl]acetate
• CAS: 1253117-53-1
• 化学式: C₃₄H₄₁N₃O₅
• 分子量: 571.717
• InChiKey: LWKPNFLOIODFGG-QZWVJJBASA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.9
• 重原子数：
  42
• 可旋转键数：
  10
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.5
• 拓扑面积：
  91.8
• 氢给体数：
  1
• 氢受体数：
  8

文献信息

• CARBOXYLIC ACID COMPOUND
  申请人：Negoro Kenji

  公开号：US20120035196A1

  公开（公告）日：2012-02-09

  [Problem] The present invention has an object to provide a compound having a GPR40 agonistic activity, which is useful as a pharmaceutical composition, an insulin secretion promoter, or an agent for preventing/treating diabetes. [Means for Solution] The present inventors have extensively studied a compound having a GPR40 agonistic activity, and as a result, they have found that the compound (I) of the present invention or a pharmaceutically acceptable salt thereof, in which a carboxylic acid is bonded to a bicyclic or tricyclic moiety through methylene, and further, a benzene ring substituted with a monocyclic 6-membered aromatic ring is bonded to a bicyclic or tricyclic moiety through —O-methylene or —NH-methylene, has an excellent GPR40 agonistic activity. They have also found that the compound has an excellent insulin secretion promoting action and strongly inhibits increase in the blood glucose after glucose loading, thereby completing the present invention.

  本发明的目的是提供一种具有GPR40激动活性的化合物，可用作药物组合物、胰岛素分泌促进剂或预防/治疗糖尿病的药物。本发明的发明人广泛研究了具有GPR40激动活性的化合物，结果发现，本发明的化合物(I)或其药学上可接受的盐具有卓越的GPR40激动活性，其中羧酸通过亚甲基与双环或三环部分结合，并且苯环通过—O-亚甲基或—NH-亚甲基与单环6-成员芳香环结合到双环或三环部分。他们还发现该化合物具有卓越的胰岛素分泌促进作用，并强烈抑制葡萄糖负荷后血糖的增加，从而完成了本发明。