1-[2-(1H-indol-3-yl)ethyl]-7-pyridin-4-ylimidazo[1,2-a]pyrimidin-5-one

• 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-[2-(1H-indol-3-yl)ethyl]-7-pyridin-4-ylimidazo[1,2-a]pyrimidin-5-one
• 化学式: C₂₁H₁₇N₅O
• 分子量: 355.4
• InChiKey: GOHXVEZPCJNKEM-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.9
• 重原子数：
  27
• 可旋转键数：
  4
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.1
• 拓扑面积：
  64.6
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• 1-(Alkyl), 1-((heteroaryl)alkyl) and 1-((aryl)alkyl)-7-pyridin-4-ylimidazo(1,2a)pyrimidin-5(1H)-one derivatives
  申请人：SANOFI-SYNTHELABO

  公开号：EP1184384A1

  公开（公告）日：2002-03-06

  The invention relates to a imidazo[1,2-a]pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X represents a bond, a double bond, a triple bond, a methylene group optionally substituted by one or two groups selected from a C1-6 alkyl group, a hydroxy group and a C1-4 alcoxy group; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted by a C1-6 alkyl group; R1 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a benzyl group, a phenyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted by 1 to 3 substituents selected from a C1-6 alkyl group, a halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, a C1-4 alkoxy group, a nitro, a cyano, an amino, a C1-6 monoalkylamino group or a C2-10 dialkylamino group; and n represents 0 to 3. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3β.

  该发明涉及一种由式（I）表示的咪唑并[1,2-a]嘧啶酮衍生物或其盐：其中：X代表键，双键，三键，一个亚甲基基团，该基团可选择性地由C1-6烷基基团，羟基和C1-4醇氧基团中的一个或两个基团取代；一个羰基，氧原子，硫原子，磺酰基，亚砜基或氮原子，该基团可选择性地由C1-6烷基基团取代；R1代表一个2，3或4-吡啶基团，该基团可选择性地由C1-4烷基基团，C1-4烷氧基团或卤原子取代；R2代表一个C1-6烷基基团，一个C1-2全氟烷基基团，一个C1-3卤代烷基基团，一个苄基团，一个苯环，一个吡啶环，一个吲哚环，一个吡咯环，一个噻吩环，一个呋喃环或一个咪唑环，苄基团和环可选择性地由1至3个取代基团取代，所述取代基团选自C1-6烷基基团，卤原子，C1-2全氟烷基基团，C1-3卤代烷基基团，羟基，C1-4烷氧基团，硝基，氰基，氨基，C1-6单烷基氨基团或C2-10二烷基氨基团；n代表0至3。该发明还涉及一种药物，其包括作为预防和/或治疗由GSK3β异常活性引起的神经退行性疾病的活性成分的上述衍生物或其盐。
• 1-[alkyl],1-[(heteroaryl)alkyl] and 1-[aryl]alkyl]-7pyridinyl-imidazo[1,2-alpha]pyrimidin-5(1h)-one derivatives
  申请人：——

  公开号：US20040044010A1

  公开（公告）日：2004-03-04

  The invention relates to an imidazo[1,2-a]pyrimidone derivative represented by formula (1) or a salt thereof, wherein: X represents a bond, an ethenylene group, and ethenylene group, a methylene group optionally substituted by one or two groups selected from a C 1-6 alkyl group, a hydroxy group and a C 1-4 alkoxy group; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted by a C 1-6 alkyl group; R1 represents a 2,3 or 4-pyridyl group optionally substituted by a C 1-4 alkyl group, C 1-4 alkoxy group or a halogen atom; R2 represents a C 1-4 alkyl group, perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a benzyl group, a phenyl ring, a naphthyl ring, 5,6,7,8-tetrahydronaphthyl ring, a pyridyl ring, an indole ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring, the benzyl group and the rings being optionally substituted by 1 to 4 substituents selected from a C 1-4 alkyl group, a phenyl ring, a halogen atom, a C 1-2 perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a hydroxyl group, a C 1-4 alkoxy group, a nitro, a cyano, an amino, a C 1-6 monoalkylamino group or a C 2-10 dialkylamino group; and n represents 0 to 3. The invention relates also to a medicament comprising the said derivative or a salt thereof as an active ingredient which is used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3&bgr;, such as Alzheimer disease.

  本发明涉及一种由式（1）表示的咪唑并［1,2-a］嘧啶酮衍生物或其盐，其中：X代表键，乙烯基，乙烯基，取代1个或2个选自C1-6烷基，羟基和C1-4烷氧基的基团的亚甲基基团，羰基基团，氧原子，硫原子，磺酰基，亚磺酰基或氮原子，可选地取代C1-6烷基；R1代表取代为C1-4烷基，C1-4烷氧基或卤素原子的2,3或4-吡啶基团；R2代表C1-4烷基，全卤代烷基，C1-3卤代烷基，苄基，苯环，萘环，5,6,7,8-四氢萘环，吡啶环，吲哚环，吡咯环，噻吩环，呋喃环或咪唑环，苄基和环可选地取代1至4个取自C1-4烷基，苯环，卤素原子，C1-2全卤代烷基，C1-3卤代烷基，羟基，C1-4烷氧基，硝基，氰基，氨基，C1-6单烷基氨基或C2-10二烷基氨基的取代基；n代表0至3。本发明还涉及一种药物，包括所述衍生物或其盐作为活性成分，用于预防和/或治疗由GSK3β异常活性引起的神经退行性疾病，如阿尔茨海默病。
• 1-[Alkyl], 1-[(heteroaryl) alkyl] and 1-[(Aryl)alkyl]-7-pyridinyl-imidazo[1,2-a]pyrimidin-5(1H)-one derivatives
  申请人：Lochead Alistair

  公开号：US20060148825A1

  公开（公告）日：2006-07-06

  The invention relates to a method of treatment of a variety of neurodegenerative diseases such as Alzheimer disease using a imidazo[1,2-a]pyrimidone derivative represented by formula (I) or a salt thereof: Wherein X, R1, R2, and n are as defined herin.

  本发明涉及一种使用由式（I）代表的咪唑并[1,2-a]嘧啶酮衍生物或其盐治疗各种神经退行性疾病（如阿尔茨海默病）的方法： 其中 X、R1、R2 和 n 如其定义。
• 1-(ALKYL), 1-[(HETEROARYL)ALKYL] AND 1-[(ARYL)ALKYL]-7-PYRIDINYL-IMIDAZO(1,2-A)PYRIMIDIN-5(1H)-ONE DERIVATIVES
  申请人：SANOFI-SYNTHELABO

  公开号：EP1315730B1

  公开（公告）日：2004-06-30
• US7067521B2
  申请人：——

  公开号：US7067521B2

  公开（公告）日：2006-06-27