2-[2-(2,4-Dichlorophenyl)ethylamino]-3-methyl-6-pyridin-4-ylpyrimidin-4-one

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: 2-[2-(2,4-Dichlorophenyl)ethylamino]-3-methyl-6-pyridin-4-ylpyrimidin-4-one
• 化学式: C₁₈H₁₆Cl₂N₄O
• 分子量: 375.2
• InChiKey: YGWJRXNEIGCXHK-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  25
• 可旋转键数：
  5
• 环数：
  3.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  57.6
• 氢给体数：
  1
• 氢受体数：
  3

文献信息

• 2-amino-3-(alkyl)-pyrimidone derivatives
  申请人：Almario Carcia Antonio

  公开号：US20050130998A1

  公开（公告）日：2005-06-16

  A pyrimidone derivative represented by formula (I) or a salt thereof: Wherein: R1 represents a hydrogen atom or a C 1-6 alkyl group which may be substituted by a C 6,10 aryl group; R2 represents a C 1-10 alkyl group which may be substituted, a C 2-6 alkenyl group which may be substituted, a C 3-6 alkynyl group which may be substituted, a C 3-6 cycloalkyl group which may be substituted, or a C 6-10 ARYL group which may be substituted; or R1 and R2 form together a C 2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula —(CH 2 ) 2 —X—(CH 2 ) 2 — or —(CH 2 ) 2 —X—(CH 2 ) 3 — where X represents a oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C 1-4 alkyl group, C 1-4 alkoxy group or halogen atom; and R4 represents a C 1-10 alkyl group optionally substituted by a hydroxyl group, amino, C 1-6 monoalkylamino group, C 2-12 dialkylamino group or C 6,10 aryl group which may be substituted. And 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.

  一种由公式（I）表示的吡啶酮衍生物或其盐： 其中： R1代表氢原子或C1-6烷基，该烷基可以被C6,10芳基置换； R2代表C1-10烷基，该烷基可以被置换，C2-6烯基，该烯基可以被置换，C3-6炔基，该炔基可以被置换，C3-6环烷基，该环烷基可以被置换，或C6-10芳基，该芳基可以被置换； 或者R1和R2一起形成可被置换的C2-6烷基； 或者R1和R2一起形成公式—（CH2）2—X—（CH2）2—或—（CH2）2—X—（CH2）3—的链，其中X代表可以被置换的氧原子，硫原子或氮原子； R3代表可选地被C1-4烷基，C1-4烷氧基或卤素原子置换的2、3或4-吡啶基； R4代表可选地被羟基，氨基，C1-6单烷基氨基，C2-12二烷基氨基或C6,10芳基置换的C1-10烷基。 以及一种药物，其中该衍生物或其盐作为活性成分，用于预防和/或治疗由GSK3β异常活动引起的神经退行性疾病，例如阿尔茨海默病。
• 2-AMINO-3-(ALKYL)-PYRIMIDONE DERIVATIVES AS GSK3.BETA. INHIBITORS
  申请人：SANOFI-SYNTHELABO

  公开号：EP1276738A1

  公开（公告）日：2003-01-22
• US6844335B2
  申请人：——

  公开号：US6844335B2

  公开（公告）日：2005-01-18
• US7378413B2
  申请人：——

  公开号：US7378413B2

  公开（公告）日：2008-05-27
• [EN] 2-AMINO-3-(ALKYL)-PYRIMIDONE DERIVATIVES AS GSK3.BETA. INHIBITORS<br/>[FR] DERIVES DU 2-AMINO-3-(ALKYL)-PYRIMIDONE, INHIBITEURS DU GSK3 DOLLAR G(B)
  申请人：SANOFI SYNTHELABO

  公开号：WO2001070729A1

  公开（公告）日：2001-09-27

  A pyrimidone derivative represented by formula (I) or a salt thereof, wherein: R1 represents a hydrogen atom or a C1-6 alkyl group which may be substituted by a C6,10 aryl group; R2 represents a C1-10 alkyl group which may be substituted, a C2-6 alkenyl group which may be substituted, a C3-6 alkynyl group which may be substituted, a C3-6 cycloalkyl group which may be substituted, or a C6-10 ARYL group which may be substituted; or R1 and R2 form together a C2-6 alkylene group which may be substituted; or R1 and R2 form together a chain of formula -(CH2)2-X-(CH2)2- or -(CH2)2 -X-(CH2)3- where X represents an oxygen atom, a sulfur atom, or a nitrogen atom which may be substituted; R3 represents a 2, 3 or 4-pyridyl group optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or halogen atom; and R4 represents a C1-10 alkyl group optionally substituted by a hydroxyl group, amino, C1-6 monoalkylamino group, C2-12 dialkylamino group or C?6,10? aryl group which may be substituted. And 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.