摘要:
The invention relates to a substituted-pyrimidone derivative represented by formula (I) or a salt thereof: wherein:
X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom; Y represents a bond, a carbonyl group, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the rings being optionally substituted; R2 represents a phenyl group or a naphthalene ring; the phenyl group and the naphthalene ring being optionally substituted; R3 represents a hydrogen atom or a C 1-6 alkyl group; R4 represents a C 1-2 perhalogenated alkyl group or a C 1-3 halogenated alkyl group; R5 represents a hydrogen atom; a C 1-6 alkyl group or a halogen atom; n represents 0 to 3; and p+q=0-3.
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:
The invention relates to a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I) or a salt thereof: wherein:
R1 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R2 represents a hydrogen atom, a C 1-6 alkyl group optionally substituted by 1 to 4 substituents selected from a halogen atom, a hydroxyl group or a C 1-4 alkoxy group; a C 1-2 perhalogenated alkyl group, a benzyl group, a phenethyl group, a benzyloxycarbonyl group, a C 1-4 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 or an imidazole ring; the benzyl group, the benzyloxycarbonyl group, the benzenesulfonyl group, the benzoyl group and the rings being optionally substituted by 1 to 4 substituents selected from a C 1-6 alkyl group, a benzene 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; R3 represents a 2, 3 or 4-pyridine ring optionally substituted by a C 1-4 alkyl group, C 1-4 alkoxy group or a halogen atom; R4 represents a C 1-4 alkyl group optionally substituted by a hydroxyl group, a C 1-4 alkoxy group or a halogen atom and n represents 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 disease.
摘要:
The invention relates to substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein:
X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom; Y represents a bond, a carbonyl group, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the rings being optionally substituted; R2 represents a phenyl group or a naphthalene ring; the phenyl group and the naphthalene ring being optionally substituted; R3 represents a hydrogen atom or a C 1-6 alkyl group; R4 represents a phenyl group, a pyridinyl group or a naphthalene ring, the groups and the ring being optionally substituted; R5 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; n represents 0 to 3; and p+q=0-3.
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:
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 C 1-2 alkyl group and a hydrogen atom; Y represents a bond, a ethenylene group, a ethynylene group, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a nitrogen atom being optionally; or a methylene group optionally substituted; R1 represents a pyrimidine group optionally substituted; R2 may represent a C 1-6 alkyl group optionally substituted by a C 6,10 aryloxy or a C 6,10 arylamino group ; a C 3-6 cycloalkyl group, a C 1-4 alkylthio group, a C 1-4 alkoxy group, a C 1-2 perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a phenyl ring, an indanyl ring, a 5,6,7,8-tetrahydronaphthyl ring, a naphthyl ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring ; R3 and R4 represents each independently a hydrogen atom, C 1-6 alkyl group, a hydroxy group, a C 1-4 alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C 1-6 alkyl 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.
摘要:
The invention relates to a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I) or a salt thereof: wherein:
R1 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R2 represents a hydrogen atom, a C 1-6 alkyl group optionally substituted by 1 to 4 substituents selected from a halogen atom, a hydroxyl group or a C 1-4 alkoxy group; a C 1-2 perhalogenated alkyl group, a benzyl group, a phenethyl group, a benzyloxycarbonyl group, a C 1-4 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 or an imidazole ring; the benzyl group, the phenethyl group, the benzyloxycarbonyl group, the benzenesulfonyl group, the benzoyl group and the rings being optionally substituted by 1 to 4 substituents selected from a C 1-6 alkyl group, a benzene 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; R3 represents a 2, 4 or 5-pyrimidine ring optionally substituted by a C 1-4 alkyl group, C 1-4 alkoxy group or a halogen atom; R4 represents a C 1-4 alkyl group optionally substituted by a hydroxyl group, a C 1-4 alkoxy group or a halogen atom and n represents 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 disease.
摘要:
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 C 1-2 alkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group, an oxygen atom, a sulphur atom, a sulfonyl group, a sulfoxide group, a carbonyl group, a hydroxyiminomethylene group, a dioxolan group, a nitrogen atom being optionally substituted; or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring optionally substituted; R2 may represent a C 1-6 alkyl group optionally; a C 3-6 cycloalkyl group, a C 1-4 alkylthio group, a C 1-4 alkoxy group, a C 1-2 perhalogenated alkyl group, a C 1-3 halogenated alkyl group, a phenylthio group, a benzyl group, a phenyl ring, a 5,6,7,8-tetrahydronaphthyl ring, a naphthyl ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring ; R3 and R4 represents, each independently, a hydrogen atom, a C 1-6 alkyl group, a hydroxy group, a C 1-4 alkoxy group or a halogen atom; R5 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; with the proviso that when R3 and R4 represent each a hydrogen atom then R5 is not a hydrogen 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.
摘要:
A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof:
wherein: Y represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom; Z represents a bond, an oxygen atom, a nitrogen atom substituted by a hydrogen atom or a C 1-3 alkyl group, a sulphur atom, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom or a C 1-6 alkyl group; R5 represents a hydrogen atom, a C 1-6 alkoxy carbonyl group or a C 1-6 alkyl group optionally substituted; R6 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R7 represents a hydrogen atom or a C 1-6 alkyl group; n represents 0 to 3; m represents 0 to 1; o represents 0 to 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 disease.
摘要翻译:由式(I)表示的嘧啶酮衍生物或其盐或其溶剂合物或其水合物:其中:Y表示两个氢原子,硫原子,氧原子或C 1-2烷基和氢原子 ; Z表示键,氧原子,被氢原子或C 1-3烷基取代的氮原子,硫原子,任选取代的亚甲基; R1表示2,3或4-吡啶环或2,4或5-嘧啶环,该环任选被取代; R2代表苯环或萘环; 所述环任选被取代; R 3表示氢原子,C 1-6烷基或卤素原子; R 4表示氢原子或C 1-6烷基; R5表示氢原子,C 1-6烷氧基羰基或任选取代的C 1-6烷基; R6表示氢原子,C 1-6烷基或卤素原子; R 7表示氢原子或C 1-6烷基; n表示0〜3; m表示0〜1; o表示0至2.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GSK3 2异常活动引起的神经变性疾病,例如阿尔茨海默病 。
摘要:
The invention relates to 3-ketoester of formula (IV)
wherein R1 represents a 2, 3 or 4-pyridine ring optionally substituted by a C 3-6 cycloalkyl group, a C 1-4 alkyl group, a C 1-4 alkoxy group, a benzyl group or a halogen atom, R5 is an halogen atom and R is an alkyl.
摘要翻译:本发明涉及式(IV)的3-酮酯,其中R 1表示任选被C 3-6环烷基取代的2,3或4-吡啶环,C 1-4烷基, C 1-4烷氧基,苄基或卤素原子,R 5为卤素原子,R为烷基。
摘要:
The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein:
X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a C 1-2 alkyl group and a hydrogen atom; Y represents a bond, a carbonyl group, a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring or a 2, 4 or 5-pyrimidine ring, the ring being optionally substituted; R2 represents a benzene ring or a naphthalene ring; the rings being optionally substituted; R3 represents a hydrogen atom, a C 1-6 alkyl group or a halogen atom; R4 represents a hydrogen atom, a C 1-4 alkoxy carbonyl group, a C 1-6 alkyl group optionally substituted; o and m represent 1 to 2; n represents 0 to 3; p represents 0 to 2; and q represents 0 to 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 disease.