Synthelabo

Sanofi-aventis

Mitsubishi Pharma Corporation

Sanofi

Patrick Andre Lardenois

Jonathan Reid Frost

Alistair Lochead

Henry Najer

Alain Nedelec

Thierry Gallet

Mourad Saady

Philippe Yaiche

Franck Slowinski

Gabor I Koletar

Claude C Morel

Regis Dupont

Yannick Evanno

Antonio Almario Garcia

Don Pierre Giudicelli

Odile LeClerc

Alexander E Wick

Pascal George

Samir Jegham

Mireille Sevrin

Christian Hoornaert

Ahmed Abouabdellah

Frederic Galli

Séverine Marguerie

David Machnik

Gihad Dargazanli

Frank Marguet

Nathalie Rakotoarisoa

Danielle De Peretti

Icilio A Cavero

André Malanda

Jean Bertin

Corinne Rousselle

Yves Robert Pascal

Bogdan Iliesco-Branceni

Alfred Saarmets

Anne Olivier

Jean Pierre Lefevre

Jean P Thenot

Maria C Renones

Jonathan B Frost

The present invention discloses and claims compounds of general formula in which X, R, P, Q, R and W are as described herein. The compounds of the invention are useful in a variety of therapeutic applications.

1,4-diazabicyclo[3.2.2]nonanecarboxamide derivatives, preparation and therapeutic use thereof

Compounds of formula (I): wherein R, R, R, R, R, and X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.

Polysubstituted 2-aryl-6-phenylimidazo[1,2-A]pyridine derivatives, and preparation and therapeutic use thereof

Compounds of formula (I): wherein R, R, R, R, Rand X are as defined in the disclosure, or an acid addition salt thereof, and the therapeutic use and process of synthesis thereof.

[object Object]

The present invention is related to a compound of formula (I) wherein R, R, Rand Rare as defined herein, or an addition salt of an acid thereof, the pharmaceutical composition and preparation thereof, and the therapeutic use thereof in the treatment or the prevention of diseases involving Nurr-1 nuclear receptors, also known as NR4A2, NOT, TINUR, RNR-1 and HZF3.

2-aryl-6-phenylimidazo[1,2-a]pyridine derivatives, preparation thereof and therapeutic use thereof

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.

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 present invention discloses and claims compounds of general formula in which X represents a nitrogen atom or a group of formula C&#x2014;R, P represents a group of formula C&#x2014;R, Q represents a group of formula C&#x2014;R, R represents a group of formula C&#x2014;R, W represents a group of formula C&#x2014;R, or one of the symbols P, Q, R and W represents a nitrogen atom, Rrepresents a hydrogen atom or an alkyl group, Rrepresents a hydrogen atom or an alkyl group, R, R, Rand Reach represent a hydrogen or halogen atom, or an alkyl, alkoxy, nitro, amino, trifluoromethyl, cyano or amino group or other functional groups. The compounds of the invention are useful in a variety of therapeutic applications.

1,4-Diazabicyclo[3.2.2]nonanecarboxamide derivatives, preparation and therapeutic use thereof

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

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

5-Naphthalen-1-yl-1,3-dioxane derivatives, preparation and therapeutical

The present invention provides a piperidine derivative of formula (I) ##STR1## in which R represents a straight- or branched-chain (C.sub.1 -C.sub.19)alkyl group, a straight- or branched-chain (C.sub.2 -C.sub.19)alkenyl group, a (C.sub.3 -C.sub.6)cycloalkyl group, a cycloalkylmethyl group in which the cycloalkyl moiety has from three to six carbon atoms, a phenyl group which is optionally substituted by a halogen atom or a phenyl methyl group which is optionally substituted by a halogen atom, or an addition salt thereof, in the form of an optically pure enantiomer or of a mixture of enantiomers, a process for making them and their therapeutic application.

Alpha-(4-chlorophenyl)-4-[(4-fluorphenyl)-methyl]piperidine-1-ethanol

A compound which is an ethanol or ethanone derivative of general formula (I) ##STR1## in which X represents CO or CHOH, or is an addition salt thereof with an acid, and, when X represents CHOH, is in the form of a pure enantiomer or a mixture of enantiomers, can be used for the treatment and prevention of cerebral disorders.

1-(3,4-dihydro-2-oxo-1H-quinolin-6-yl)-2-[4-(2-phenylethyl)piperidin-1-yl]e

A compound, in the form of a pure optical isomer or a mixture thereof, of formula (I): ##STR1## in which: Z represents a group of formula --CH.sub.2 --, --C(CH.sub.3).sub.2 --, --CH.dbd.CH--, --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --NH-- or --N(CH.sub.3)CH.sub.2 --, in which the nitrogen is bonded to the carbonyl group;

Derivatives of (1-hydroxy-2-piperidylalkyl-indol-2-ones, 2-quinolinones,

Pyridine derivatives of the general formula (I) ##STR1## in which X is --O-- or --NH--, R.sub.1 is a phenyl group optionally substituted by one or two halogen atoms or a methyl, ethyl, trifluoromethyl, methoxy or phenyl group or, when R.sub.2 is not a benzyl group, an amino group, or is a naphthyl or benzodioxanyl group, and R.sub.2 is hydrogen or a benzyl group, or when X is --O--, R.sub.2 can also be a methyl or ethyl group, and their pharmaceutically acceptable acid addition salts are useful as antianoxics.

Anti-anoxic furo- or pyrrolo-pyridine compounds and pharmaceutical

Growing community of inventors

Gentilly, France

Patrick Andre Lardenois