Sanofi-Aventis

Mitsubishi Pharma Corporation

Mitsubishi Pharma Corporation Tokyo

Séverine Marguerie

Alistair Lochead

Mourad Saady

Philippe Yaiche

Alain Nedelec

Thierry Gallet

Patrick Andre Lardenois

Franck Slowinski

Antonio Almario Garcia

Adrien Tak Li

The invention relates to use of a pyrimidone derivative represented by formula (I) or a salt thereof as therapeutic agents: Wherein m, n, p, X, Y, R1, R2, R3, R4 R5, are as defined herein. The invention specifically relates 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 GSK3&#x3b2; or GSK3&#x3b2; and cdk5/p25, such as Alzheimer disease.

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The invention relates to a method of treatment of a variety of neurodegenerative diseases such as Alzheimer disease using a imidazo[1,2-a]pyrimidone derivative represented by formula (I) or a salt thereof: Wherein X, R1, R2, and n are as defined herein.

1-[alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7-pyridinyl-imidazo[1,2-a]pyrimidin-5(1h)-one derivatives

The invention relates to therapeutic uses of a pyrimidone derivative represented by formula (I) or a salt thereof:  Wherein X, Y, R1, R2, m and n are as defined herein. Specifically, a medicament comprising the said derivative or a salt thereof as an active ingredient is used for preventive and/or therapeutic treatment of a neurodegenerative diseases caused by abnormal activity of GSK3&#x3b2; such as Alzheimer's disease.

The invention relates to an use of pyrimidone derivative represented by formula (I) or a salt thereof: wherein m, n, p, X, Y, R1, R2, R3, R4 and R5 are as defined herein for treating a variety of disease states. More specifically, the invention relates 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 GSK3&#x3b2; or GSK3&#x3b2; and cdk5/p25, such as Alzheimer's disease.

Use of 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 as therapeutic agents

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 Calkyl 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 nitrogen atom being optionally; or a methylene group optionally substituted; R1 represents a pyrimidine group optionally substituted; R2 may represent a Calkyl group optionally substituted by a Caryloxy or a Carylamino group; a Ccycloalkyl group, a Calkylthio group, a Calkoxy group, a Cperhalogenated alkyl group, a Chalogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene 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, Calkyl group, a hydroxy group, a Calkoxy group or a halogen atom; R5 represents a hydrogen atom, a Calkyl 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 GSK3&#x3b2;3 or GSK3&#x3b2;3 and cdk5/p25, such as Alzheimer disease.

Substituted 2-pyrimidinyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one and 7-pyrimidinyl-2,3-dihydroimidazo [1,2-a]pyrimidin-5(1H)one derivatives for neurodegenerative disorders

The invention relates to a pyrimidone derivative represented by formula (I) or a salt thereof wherein X represents two hydrogen atoms, a sulfur atom, an oxygen atom or a Calkyl group and a hydrogen atom; Y represents a bond, an ethenylene group, an ethynylene group an oxygen atom, a sulfur 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; or a methylene group optionally substituted; R1 represents a 2, 3 or 4-pyridine ring optionally substituted; R2 may represent a Calkyl group optionally; a Ccycloalkyl group, a Calkythio group, a Calkoxy group, a Cperhalogenated alkyl group, a Chalogenated alkyl group, a phenylthio group, a benzyl group, a benzene ring, an indan ring, a 5,6,7,8-tetrahydronaphthalene ring, a naphthalene ring, a pyridine ring, a pyrrole ring, a thiophene ring, a furan ring or an imidazole ring; R3 and R4 represent, each independently, a hydrogen atom, a Calkyl group, a hydroxy group, a Calkoxy group or a halogen atom; R5 represents a hydrogen atom, a Calkyl 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 GSK3&#x3b2; or GSK3&#x3b2;, and cdk5/p25, such as Alzheimer disease 

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

The invention relates to an imidazo[1,2-a]pyrimidone derivative represented by formula (1) or a salt thereof, wherein: X represents a bond, an ethenylene group, and ethenylene group, a methylene group optionally substituted by one or two groups selected from a Calkyl group, a hydroxy group and a Calkoxy group; a carbonyl group, an oxygen atom, a sulfur atom, a sulfonyl group, a sulfoxide group or a nitrogen atom being optionally substituted by a Calkyl group; R1 represents a 2,3 or 4-pyridyl group optionally substituted by a Calkyl group, Calkoxy group or a halogen atom; R2 represents a Calkyl group, a Cperhalogenated alkyl group, a Chalogenated alkyl group, a benzyl group, a phenyl ring, a naphthyl ring, 5,6,7,8-tetrahydronaphthyl ring, a pyridyl 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 by 1 to 4 substituents selected from a Calkyl group, a phenyl ring, a halogen atom, a Cperhalogenated alkyl group, a Chalogenated alkyl group, a hydroxyl group, a Calkoxy group, a nitro, a cyano, an amino, a Cmonoalkylamino group or a Cdialkylamino group; 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 GSK3&#x3b2;, such as Alzheimer disease.

1-[alkyl], 1-[(heteroaryl)alkyl] and 1-[(aryl)alkyl]-7pyridinyl-imidazo[1,2-alpha]pyrimidin-5(1H)-one derivatives

Imidazo[1,2-&#x3b1;]pyrimidinones and pyrimido[1,2-&#x3b1;]pyrimidinones useful for preventive and/or therapeutic treatment of neurodegenerative diseases, such as Alzheimer's disease, caused by abnormal GSK3&#x3b2; activity.

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Rennes, France

Séverine Marguerie