Sanofi-aventis

Sanofi

Ahmed Abouabdellah

Christian Hoornaert

Antonio Almario Garcia

Philippe Yaiche

Julien Vache

Adrien Tak Li

Aude Fayol

Mourad Saady

Antoine Ravet

Alistair Lochead

Jacques Froissant

Gihad Dargazanli

Nathalie Chereze

Florence Medaisko

Jean Jeunesse

Michele Bas

Frederic Puech

Philippe Burnier

Tak Adrien Li

Luc Even

Corinne Veronique

Peter Hamley

Jochen Görlitzer

Regine Bartsch-Li

The invention relates to compounds corresponding to the general formula (I):  The invention also relates to a process for the preparation of the compounds of formula (I), to compositions comprising them and to their therapeutic application.

Alkyl-heterocycle carbamate derivatives, their preparation and their therapeutic application

The invention relates to the novel products of formula (I): in which: Ra represents H, Hal, aryl or heteroaryl, which is optionally substituted; Rb represents H, Rc, &#x2014;COORc-CO&#x2014;Rc or &#x2014;CO&#x2014;NRcRd; where Rc represents alkyl, cycloalkyl, heterocycloalkyl, aryl and heteroaryl, all optionally substituted; Rd represents H, alk or cycloalkyl; these products being in all the isomer forms and the salts, as medicaments, in particular as MET inhibitors.

Alkylthiazol carbamate derivatives, preparation thereof and therapeutic use thereof

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

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 compound corresponding to general formula (I): in which Rrepresents a phenyl or naphthalenyl group optionally substituted with one or more halogen atoms or hydroxyl, cyano, nitro, (C-C)alkyl, (C-C)alkoxy, trifluoromethyl, trifluoromethoxy, benzyloxy, (C-C)cycloalkyl-O&#x2014; or (C-C)cycloalkyl(C-C)alkoxy groups; Rrepresents either a group of general formula CHRCONHRin which Rrepresents a hydrogen atom or a methyl group and Rrepresents a hydrogen atom or a (C-C)alkyl, (C-C) cycloalkyl or (pyridin-4-yl)methyl group; or a 2,2,2-trifluoroethyl group; or an (imidazol-2-yl)methyl group; or a (benzimidazol-2-yl)methyl group; or a phenyl group optionally substituted with one or more halogen atoms or cyano, nitro, (C-C)alkyl, (C-C)alkoxy, trifluoromethyl or trifluoromethoxy groups; and n represents a number ranging from 1 to 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Also disclosed and claimed are the pharmaceutical compositions derived therefrom and their therapeutic use in treating a wide variety of diseases.

Derivatives of dioxan-2-alkyl carbamates, preparation thereof and application thereof in therapeutics

The invention relates to a compound having general formula (I): Wherein m, Rand Rare as defined herein. The invention also relates to the use of the compound in therapeutics. More specifically, the compounds of the invention are inhibitors of the FAAH enzyme, and therefore, can be used for the treatment of various disorders associated with FAAH enzyme, which include in a non-limiting manner, pain, eating disorders, neurological and psychiatric pathologies, among other disorders.

Derivatives of 1-piperazine- and 1-homopiperazine-carboxylates, preparation method thereof and use of same as inhibitors of the FAAH enzyme

Therapeutic uses of a compound corresponding to the general formula (I): in which A=N or CR; R=H, F, OH, CN, CF, C-alkyl, C-alkoxy; n=2 or 3 and m=2 when A=N; n=1, 2 or 3 and m=1 or 2 when A=CR; B=covalent bond or C-alkylene; R=optionally substituted heteroaryl; R=CHRCONHR; R=H or C-alkyl; R=H, C-alkyl, C-cycloalkyl, C-cycloalkyl-C-C-alkylene;in the form of a base, an acid-addition salt, a hydrate or a solvate.

Therapeutic uses of derivatives of piperidinyl- and piperazinyl-alkyl carbamates

The invention relates to a compound of formula (I): Wherein m, n, X, Y, R, R, Rand Rare as defined herein. The invention also relates to the use of same in therapeutics.

Aryloxyalkylcarbamate-type derivatives, preparation method thereof and use of same in therapeutics

The present invention comprises alkylpiperazine- and alkylhomopiperazine carboxylates and their derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of disease and other pathological conditions are not generated and the incidence of the disease is greatly reduced.

Derivatives of alkylpiperazine- and alkylhomopiperazine-carboxylates, preparation method thereof and use of same as fatty acid amido hydrolase enzyme inhibitors

The present invention comprises peridinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase (FAAH) enzyme inhibitors. These derivatives exert various pharmacological activities by interacting, inter alia, with cannabinoid and vanilloid receptors. By inhibiting the metabolic activity of the FAAH enzyme, compounds often responsible for the onset of a large variety of diseases and other pathological conditions are not generated and the incidence of the disease is greatly reduced.

Piperidinylalkylcarbamate derivatives, methods for their preparation and the therapeutic use thereof as fatty acid amido hydrolase enzyme inhibitors

A compound corresponding to general formula (I): in which Rrepresents a phenyl or naphthalenyl group optionally substituted with one or more halogen atoms or hydroxyl, cyano, nitro, (C-C)alkyl, (C-C)alkoxy, trifluoromethyl, trifluoromethoxy, benzyloxy, (C-C)cycloalkyl-O&#x2014; or (C-C)cycloalkyl(C-C)alkoxy groups; Rrepresents either a group of general formula CHRCONHRin which Rrepresents a hydrogen atom or a methyl group and Rrepresents a hydrogen atom or a (C-C)alkyl, (C-C)cycloalkyl or (pyridin-4-yl)methyl group; or a 2,2,2-trifluoroethyl group; or an (imidazol-2-yl)methyl group; or a (benzimidazol-2-yl)methyl group; or a phenyl group optionally substituted with one or more halogen atoms or cyano, nitro, (C-C)alkyl, (C-C)alkoxy, trifluoromethyl or trifluoromethoxy groups; and n represents a number ranging from 1 to 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate. Also disclosed and claimed are the pharmaceutical compositions derived therefrom and their therapeutic use in treating a wide variety of diseases.

The invention relates to a compound having general formula (I): Wherein n, A, R, R, and Rare as defined herein. The invention also relates to methods of preparation of compound of formula (I) as well as its use in therapeutics.

Growing community of inventors

Thiais, France

Ahmed Abouabdellah