2-(2,3-dihydro-1H-inden-2-ylamino)-4-pyridin-4-yl-1H-pyrimidin-6-one

• 分子结构分类: 有机化合物 - 苯类化合物 - 茚满类
• 英文名称: 2-(2,3-dihydro-1H-inden-2-ylamino)-4-pyridin-4-yl-1H-pyrimidin-6-one
• 化学式: C₁₈H₁₆N₄O
• 分子量: 304.3
• InChiKey: FUUKYZHDJNNCEW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.7
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  66.4
• 氢给体数：
  2
• 氢受体数：
  2

文献信息

• 2-[Indanylamino]pyrimidone and 2-[tetrahydronaphthalenylamino]pyrimidone derivatives
  申请人：SANOFI-SYNTHELABO

  公开号：EP1136486A1

  公开（公告）日：2001-09-26

  The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof: wherein R1 represents a hydrogen atom or a C1-6 alkyl group; R2 represents a hydrogen atom or 1 to 3 substituents selected from a C 1-6 alkyl group, halogen atom, a C1-2 perhalogenated alkyl group, a C1-3 halogenated alkyl group, a hydroxyl group, a C1-6 alkoxy group, methylenedioxy group, a nitro, a cyano, an amino, a C1-6 monoalkylamino group, C2-10 dialkylamino group ; C1-6 alkylcarbonylamino group, C6,10 arylcarbonylamino group; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom and n represents 0 or 1, when n represents 0 then m is 2 or 3, and when n represents 1 then m is 1 or 2. 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 such as Alzheimer's disease, Parkinson's disease, frontoparietal dementia, corticobasal degeneration, Pick's disease, cerebrovascular accidents and brain and spinal trauma and peripheral neuropathies.

  该发明涉及一种由式（I）表示的嘧啶酮衍生物或其盐： 其中，R1代表氢原子或C1-6烷基；R2代表氢原子或1至3个取代基，所述取代基选自C1-6烷基、卤原子、C1-2全卤代烷基、C1-3卤代烷基、羟基、C1-6烷氧基、亚甲二氧基基团、硝基、氰基、氨基、C1-6单烷基氨基、C2-10双烷基氨基、C1-6烷基羰基氨基、C6,10芳基羰基氨基；R3代表2、3或4-吡啶基，该基团可选择地被C1-4烷基、C1-4烷氧基或卤原子取代，n代表0或1，当n代表0时，m为2或3，当n代表1时，m为1或2。该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，例如阿尔茨海默病、帕金森病、额颞型痴呆、皮质基底节变性、皮克氏病、脑血管意外和脑脊髓损伤及周围神经病变。