Heteroaryl substituted 2-pyridinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyridinyl-2,3-dihydroimidazo[1,2-a]pyrimidin-5(1H)one derivatives
申请人:SANOFI-SYNTHELABO
公开号:EP1340758A1
公开(公告)日:2003-09-03
The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein:
X represents two hydrogen atoms, a sulphur atom, an oxygen atom or a C1-2 alkyl group and a hydrogen atom;
Y represents a bond, an ethenylene group, an ethynylene group or a methylene group optionally substituted;
R1 represents a 2, 3 or 4-pyridine ring optionally substituted;
R2 represents a heterocyclic bicyclic rings, having 1-4 heteroatoms selected from an oxygen atom, a sulfur atom and a nitrogen atom and having 5-9 carbon atoms, of formula
R3 represents a hydrogen atom, a C1-6 alkyl group, a hydroxy group, a C1-4 alkoxy group or a halogen atom;
R4 represents a hydrogen atom, a C1-6 alkyl group, a C1-4 alkoxy group or a halogen atom;
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 or GSK3β and cdk5/p25, such as Alzheimer disease.
本发明涉及一种由公式(I)表示的嘧啶酮衍生物或其盐,其中:X代表两个氢原子,一个硫原子,一个氧原子或一个C1-2烷基基团和一个氢原子;Y代表键,乙烯基团,乙炔基团或者一个可选取代的亚甲基基团;R1代表一个可选取代的2,3或4-吡啶环;R2代表一个杂环双环环,具有1-4个从氧原子、硫原子和氮原子中选取的杂原子和5-9个碳原子,其化学式为;R3代表一个氢原子,一个C1-6烷基基团,一个羟基,一个C1-4烷氧基或者一个卤素原子;R4代表一个氢原子,一个C1-6烷基基团,一个C1-4烷氧基或者一个卤素原子。本发明还涉及一种药物,其中包括所述衍生物或其盐作为活性成分,可用于预防和/或治疗由GSK3β或GSK3β和cdk5/p25的异常活性引起的神经退行性疾病,例如阿尔茨海默病。