Sanofi-Aventis

Mitsubishi Pharma Corporation

Sanofi

Mitsubishi Tanabe Pharma Corporation

Franck Slowinski

Alistair Lochead

Mourad Saady

Philippe Yaiche

Frank Halley

Patrick Andre Lardenois

Alain Nedelec

Thierry Gallet

Julien Vache

Odile LeClerc

Corinne Terrier

Eric Nicolai

Victor Certal

Youssef El Ahmad

Séverine Marguerie

Nathalie Chereze

Pascal George

Patrick Mougenot

Frédéric Petit

Anne-Marie Periers

Omar Ben Ayad

Odile Leclerc

Marc Bianciotto

Patrick Bernardelli

Alice Da Rocha

Béatrice De Bruin

Mourad Saadi

The invention relates to compounds of the general formula (I): wherein R, m, n and o are as defined herein. The invention also relates to a method for preparing the same and to the application in therapy.

Azabicycloalkane derivatives, preparation thereof and use thereof in therapy

The invention relates to compounds of the general formula (I): Wherein R, m, n and o are as defined herein. The invention also relates to a method for preparing the same and to the application in therapy.

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein Y, Z, R1, R2, R3, R4, R5, R6, R7, n, m, and o are as described herein. 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.

Substituted bicyclic pyrimidone derivatives

The invention relates to use of substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as defined herein. 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 disease caused by abnormal activity of GSK3&#x3b2;, such as Pick's disease among various other diseases as claimed herein.

Use of 8-substituted-6,7,8,9-tetrahydropyrimido[1,2-a] pyrimidin-4-one derivatives

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.

[object Object]

The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein: X, Y, R1, R2, R3, R4, o, m, n, p and q are as defined herein. 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.

The invention relates to therapeutic uses of a dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, m, n, p and q are as described herein. 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;, such as Alzheimer disease.

Substituted 8'-pyridinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a] pyrimidin-6-one and 8&#x2032;-pyrimidinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a] pyrimidin-6-one derivatives

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 therapeutic uses of a 2-(diaza-bicyclo-alkyl)-pyrimidone derivative represented by formula (I): Wherein R1, R2, R3, R4 and n are as defined herein. Specifically, the compounds of formula (I) are used for preventive and/or therapeutic treatment of a neurodegenerative disease caused by abnormal activity of GSK3&#x3b2;, such as Alzheimer's disease. The invention relates also to intermediates for the preparation of compound of formula (I).

Use of substituted 2-(diaza-bicyclo-alkyl)-pyrimidone derivatives for the treatment of neurodegenerative diseases

The invention relates to use of a substituted-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as described 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 disease caused by abnormal activity of GSK3&#x3b2;, such as Pick's disease.

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 dihydrospiro-[cycloalkyl]-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, m, n, p and q are as described herein. 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.

Substituted 8'-pyridinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a]pyrimidin-6-one and 8&#x2032;-pyrimidinyl-dihydrospiro-[cycloalkyl]-pyrimido[1,2-a]pyrimidin-6-one derivatives

The invention relates to a dihydrospiro-[cycloalkylamine]-pyrimidone derivative represented by formula (I) or a salt thereof:  wherein X, Y, R1, R2, R3, R4, o, m, n, p and q are as defined herein. 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.

The invention relates to substituted-pyrimidone derivatives represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as defined herein. 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's disease.

8-Substituted-6,7,8,9-tetrahydropyrimido [1,2-a] pyrimidin-4-one derivatives.

The invention relates to a substituted-pyrimidone derivative represented by formula (I) or a salt thereof: wherein X, Y, R1, R2, R3, R4, R5, n, p and q are as described herein. 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.

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Thieux, France

Franck Slowinski