摘要:
The invention relates to a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): wherein: R1 represents a hydrogen atom, a C1-6 alkyl group or a halogen atom; R2 represents a hydrogen atom, a C1-6 alkyl group optionally substituted by 1 to 4 substituents selected from a halogen atom, a hydroxyl group, a C1-4 alkoxy group; a C1-2 perhalogenated alkyl group, a benzyl group, a phenethyl group, a benzyloxycarbonyl group, a C1-4 alkoxy carbonyl group, a benzene ring, a naphthalene ring, a quinoline ring, a phthalazine ring, a 5,6,7,8-tetrahydronaphthalene ring, a pyridine ring, an indole ring, a pyrrole ring, a thiophene ring, a benzenesulfonyl group, a benzoyl group, a pyridazine ring, a furan ring and an imidazole ring; each of the benzyl group, the phenethyl group, the benzyloxycarbonyl group, the benzenesulfonyl group, the benzoyl group and the benzene, naphthalene, quinoline, phthalazine, 5,6,7,8-tetrehydronaphthalene, pyridine, indole, pyrrole and thiophene rings being optionally substituted by 1 to 4 substituents selected from a C1-6 alkyl group, a benzene ring, 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 group, a cyano group, an amino group, a C1-6 monoalkylamino group and a C2-10 dialkylamino group; R3 represents a 2, 4 or 5-pyrimidine ring or a 2, 3 or 4-pyridine ring, the rings being optionally substituted by a C1-4 alkyl group, C1-4 alkoxy group or a halogen atom; R4 represents a C1-4 alkyl group optionally substituted by a hydroxyl group, a C1-4 alkoxy group or a halogen atom and n represents 1 or 2; or a salt thereof, or a solvate thereof or a hydrate thereof. 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.
摘要:
The invention relates to a imidazo[1,2-a]pyrimidone derivative represented by formula (I) or a salt thereof: R1 wherein X represents a bond, an ethenylene group, an ethenylene group, a methylene group optionally substituted; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted; R1 represents a 2, 4 or 5-pyrimidinyl optionally substituted; R2 represents a C1-6 alkyl group, a C1-2 perhalogenated alkyl group,a C1-3 halogenated alkyl group, a benzyl group, a benzene ring, a naphthalene ring, 5,6,7,8-tetrahydronaphthalene ring, a pyridine 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; 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, such as Alzheimer disease.
摘要翻译:本发明涉及由式(I)表示的咪唑并[1,2-a]嘧啶酮衍生物或其盐:R 1其中X表示键,亚乙烯基,亚乙烯基, 任选取代的亚甲基; 羰基,氧原子,硫原子,磺酰基,亚砜基或任选取代的氮原子; R 1表示任选取代的2,4或5-嘧啶基; R 2表示C 1-6烷基,C 1-12全卤代烷基,C 1-3烷基, 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,呋喃环或呋喃环 咪唑环,苄基和环任选被取代; 本发明还涉及包含所述衍生物或其盐作为活性成分的药物,其用于预防和/或治疗由GSK3beta异常活动引起的神经变性疾病,例如阿尔茨海默氏症 疾病。
摘要:
Compound corresponding to the general formula (I) in which R2 represents a chlorine atom, a methyl group or a 3-thienyl group. Therapeutic application.