Sanofi

Mitsubishi Tanabe Pharma Corporation

Sanofi-aventis

Mitsubishi Electric Corporation

Tanabe Pharma Corporation

Aude Fayol

Philippe Yaiche

Mourad Saady

Julien Vache

Alistair Lochead

Ahmed Abouabdellah

Nathalie Chereze

Corinne Veronique

Luc Even

Thierry Gallet

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein X, R1, R2, R3, R4, and m are defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.

Substituted alkyl pyrimidin-4-one derivatives

The invention relates to a compound of the general formula (I) in which Ris a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C-alkyl, C-alkoxy, NRRgroup; m, n, o and p are independently an integer equal to 0, 1, 2 or 3; A is a covalent bond or a C-alkylene group; Ris an optionally substituted aryl or heteroaryl group; Ris a hydrogen or fluorine atom or a C-alkyl group or a trifluoromethyl group; Ris an optionally substituted 5-member heterocyclic compound; the compound being in the form of a base or acid addition salt. The invention also relates to the therapeutic use thereof. 

Derivatives of azaspiranyl-alkylcarbamates of 5-member heterocyclic compounds, preparation thereof and therapeutic use thereof

The invention relates to compounds of the general formula (I) where: Ris a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C-alkyl, C-alkoxy, or NRRgroup; m and p have a value of 1; n and o have the same value which is 0 or 1; A is a covalent bond or a C-alkylene group; Ris an optionally substituted aryl or heteroaryl group; Ris a hydrogen or fluorine atom or a C-alkyl group or a trifluoromethyl group; Ris an optionally substituted 5-membered heterocyclic compound; wherein the compounds can be in the state of a base or an acid addition salt. The present invention can be used in therapeutics. 

5-membered heterocyclic compound cyclopenta[C]pyrrolylalkylcarbamate derivatives, preparation thereof, and therapeutic use thereof

Compound corresponding to general formula (I): in which Ris a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C-alkyl, C-alkoxy or NRRgroup; n is an integer equal to 1, 2 or 3 and m is an integer equal to 1 or 2; A is a covalent bond or a C-alkylene group; Ris a phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, triazinyl, naphthyl, quinolinyl, isoquinolinyl, phthalazinyl, quinazolinyl, quinoxalinyl, cinnolinyl or naphthyridinyl group, this group being optionally substituted; Ris a hydrogen or fluorine atom, a C-alkyl group or a tritluoromethyl group; Ris a group selected from furanyl, pyrrolyl, thienyl, isothiazolyl, oxazolyl, isoxazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, imidazole, triazolyl, tetrazolyl, oxazolone, oxazolidinone, isoxazolone, isoxazolidinone, isothiazolone, isothiazolidinone, imidazolone, imidazolidinone, pyrazolone, pyrazolidinone, oxadiazolone, thiadiazolone and triazolone, this group being optionally substituted; in the form of a base or of an addition salt with an acid. Therapeutic use. 

Carbamate derivatives of alkyl-heterocycles, preparation thereof and therapeutic use thereof

The invention relates to cyclopenta[c]pyrrole-2-carboxylate derivatives, to their preparation and to their therapeutic use. 

Cyclopenta[C]pyrrole-2-carboxylate derivatives, preparation thereof and therapeutic use thereof

A pyrimidone derivative represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein Y, R1, R2, R3, and R4 are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates thereof and their use in therapeutics.

Substituted pyrimidin-4-one derivatives

The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein:Y, Z, R1, R2, R3, R4, R5 and n are as defined in the disclosure. Also disclosed are methods of preparing the compounds of formula (I), intermediates therefor and their utility in treating a variety of disease conditions.

Substituted arylamide diazepinopyrimidone derivatives

The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: wherein:

Substituted arylamide oxazepinopyrimidone derivatives

The disclosure relates to a series pyrimidone derivatives represented by formula (I) or a salt thereof, or a solvate thereof or a hydrate thereof: 

Substituted heteroarylamide diazepinopyrimidone derivatives

Substituted heteroarylamide oxazepinopyrimidone derivatives

The invention relates to compounds of the general formula (I) where: Ris a hydrogen or fluorine atom or a hydroxyl, cyano, trifluoromethyl, C-alkyl, C-alkoxy, or NRRgroup; m, n, o and p independently are a number from 0 to 3, provided that m+n&#x2266;7 and that o+p&#x2266;7; A is a covalent bond, an oxygen atom, a C-alkylene group or a &#x2014;O&#x2014;C-alkylene group in which the end that is an oxygen atom is bonded to the Rgroup and the end that is an alkylene group is bonded to the carbon of the bicyclic compound; Ris an optionally substituted aryl or heteroaryl group; Ris a hydrogen or fluorine atom or a C-alkyl or trifluoromethyl group; Ris an optionally substituted 5-membered heterocyclic compounds; wherein the compounds can be in the state of a base or an acid addition salt. The invention can be used in therapeutics. 

7-aza-spiro[3.5]nonane-7-carboxylate derivatives, preparation thereof and therapeutic use thereof

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.

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Paris, France

Aude Fayol