Sanofi-Aventis

Mitsubishi Pharma Corporation

Sanofi

Mitsubishi Tanabe Pharma Corporation

Sanofi-Synthelabo

Tanabe Pharma Corporation

Sanotl-Aventis

Thierry Gallet

Alistair Lochead

Mourad Saady

Philippe Yaiche

Alain Nedelec

Patrick Andre Lardenois

Franck Slowinski

Samir Jegham

Corinne Veronique

Séverine Marguerie

Antonio Almario Garcia

Adrien Tak Li

Nathalie Chereze

Odile LeClerc

Frederic Galli

Aude Fayol

Frédéric Galli

Fr&eacute;d&eacute;ric Galli

Axelle Samson

The present invention discloses a series of pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: Wherein X, Z, R1, R2, R3, R4, R5, R6, R7, n and m are as defined herein. Also disclosed herein are the methods of preparation of compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.

Heteroarylamide pyrimidone derivatives

Arylamide pyrimidone derivatives

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof are disclosed and claimed. Wherein m, n, o, Y, Z, R1, R2, R3, R4, R5 R6 and R7 are as described herein. Also disclosed are the salts of compounds of formula (I). 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 heteroaryl pyridopyrimidone 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 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

Compound corresponding to the general formula (I)in which R, R, R, Rand Reach represent a hydrogen or halogen atom or a nitro, amino, trifluoromethyl, trifluoroalkoxy, cyano, hydroxyl, (C&#x2013;C)alkyl or (C&#x2013;C)alkoxy group and Rrepresents a (C&#x2013;C)alkyl group. Therapeutic application.

4-(2 phenylthiazol-5-yl)-1, 4-diazabicyclo-[3.2.2]nonane derivatives, preparation and therapeutic use thereof

Compounds of general formulain which X represents an oxygen atom or a group of formula NZ in which Z represents a hydrogen atom or an alkyl group, n represents a number 0, 1 or 2, and R, R, R, Rand Reach represent a hydrogen or halogen atom or a trifluoromethyl, trifluoromethoxy, cyano, hydroxyl, alkyl, alkoxy, phenoxy or phenyl group optionally substituted with a halogen atom or a trifluoromethyl, cyano, hydroxyl, alkyl or alkoxy group, or alternatively Rand Rtogether form a group of formula &#x2014;OCHO&#x2014; or &#x2014;CHCHCHCH&#x2014;.Application in therapy.

1,4-diazabicyclo[3.2.2]nonane-4-carboxylates and carboxamide derivates, production and use thereof in therapeutics

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.

Growing community of inventors

Palaiseau, France

Thierry Gallet