N-[4-(azetidin-1-yl)-4-oxobutyl]-5-chloro-1-[(Z)-1-[(5-chloro-1,3-thiazol-2-yl)amino]prop-1-enyl]spiro[2H-indole-3,3'-pyrrolidine]-1'-carboxamide

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 英文名称: N-[4-(azetidin-1-yl)-4-oxobutyl]-5-chloro-1-[(Z)-1-[(5-chloro-1,3-thiazol-2-yl)amino]prop-1-enyl]spiro[2H-indole-3,3'-pyrrolidine]-1'-carboxamide
• 化学式: C₂₅H₃₀Cl₂N₆O₂S
• 分子量: 549.5
• InChiKey: YVJAPNXHHMZSGY-SEJLVSSPSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.7
• 重原子数：
  36
• 可旋转键数：
  7
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.48
• 拓扑面积：
  109
• 氢给体数：
  2
• 氢受体数：
  6

文献信息

• NOVEL SPIROINDOLINE COMPOUND, AND MEDICINAL AGENT COMPRISING SAME
  申请人：Kowa Company, Ltd.

  公开号：EP2781521A1

  公开（公告）日：2014-09-24

  The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic β-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.]

  本发明提供了一种通式(1)如下所示的新型化合物，它在肝脏和胰腺β细胞中具有葡萄糖激酶激活作用，可作为预防和/或治疗由高血糖引起的疾病，如糖尿病的药物。 由通式（1）代表的螺吲哚啉化合物，或其盐，或该化合物或其盐的溶液： [其中环 A 代表含氮的 5-10 位杂芳基； R1和R2相同或不同，各自代表氢原子、卤素原子、卤代 C1-6烷基、C6-10芳基、氰基、任选具有取代基的C1-6烷基、任选具有取代基的C2-6烯基等；R3代表氢原子、任选具有取代基的C1-6烷基等；R4代表氢原子、卤素原子、任选具有取代基的C1-6烷基等]。