Institut National De La Sante Et De La Recherche Medicale

Institut Pasteur De Lille

Université De Droit Et De La Santé De Lille 2

Glaxosmithkline Intellectual Property Development Limited

Bioversys Ag

Other

Université De Lille

Université De Lille 2 Droit Et Santé

Devgen Nv

Marc-Henry Pitty

Universite De Droit Et De Sante De Lille

Université Paris Descartes

Centre National De La Recherche Scientifique-Cnrs

Université De Droit Et Santé De Lille

Inserm

Benoit Deprez

Nicolas Willand

Alain Baulard

Denis Carniato

Priscille Brodin

Marilyne Bourotte

Cécile Bougeret

Esther Porras De Francisco

Karine Jaillardon

Olivier Busnel

Mathieu Gutmann

Modesto Jesús Remuiñan-Blanco

Florence Leroux

Fabrice Lejeune

Matthieu Frederik Desroses

Barbara Dubanchet

Terence Beghyn

Sara Sofia Gonzalez-Hilarion

Nathalie Hennuyer

Anne Muhr-Tailleux

Bart Staels

Marion Flipo

Sophie Lestavel

Julie Charton

Jean-Francois Briand

Thierry Bogaert

Philippe Verwaerde

Peter Van Endert

Vincent Villeret

Valentin Guillaume

Virgyl Camberlein

Cindy Anthonissen

Beatrice Bonnet

Damien Bosc

Charlotte Tabey Fleau

Rebecca Deprez Poulain

Pierre Sierocki

Ronan Gealageas

Jean-François Briand

Geoffroy Dequirez

Manuel Lassalle

Laurence Agouridas-Dutot

Lucie Maingot

Sylvain Picon

Karen Aknin

Rajaa Boulahjar

Olivier Sperando

Baptiste Villemagne

Dominique Thomas

Jouda Jakhlal

Cecile Bougeret

Modesto Jesús REMUIÑAN-Blanco

Matthieu Frédérik Desroses

The present disclosure relates to novel compounds of formula (I) which are useful as inhibitors of endoplasmic reticulum aminopeptidases (ERAP), in particular as inhibitors of ERAP2. The disclosure also relates to the therapeutic use of these compounds, in particular the use of these compounds in the treatment or prophylaxis of proliferative disorders, autoinflammatory disorders and autoimmune disorders.

ERAP inhibitors

The invention relates to compounds of Formula (I) and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by, such as tuberculosis.

Compounds

The invention relates to compounds of Formula (I) and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by, such as tuberculosis. 

The present invention is directed to novel compounds of formula (I), pharmaceutically acceptable salts or solvates thereof, and their use. 

Imidazol- or 1,2,4-triazol-derivatives and their use

The present invention relates to the compound of formula (I) for use in the treatment of a nonsense-mutation-mediated genetic disease.

Compound useful for the treatment of nonsense-mutation-mediated diseases and pharmaceutical composition comprising said compound

The present invention concerns a spiroisoxazoline compound of general formula (I): in which m and n are 0 or 1, R1 represents, inter alia, an optionally substituted alkyl chain, in particular substituted with fluorine or with a cyclic group, and R2 is chosen from phenyl and optionally substituted benzyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, and the heterocycles having 5 or 6 vertices comprising at least one atom chosen from S, N and O. The present invention also concerns the use of this compound as a drug, in particular in the treatment of bacterial and mycobacterial infections such as tuberculosis in combination with an antibiotic that is active against bacteria and/or mycobacteria, said compound potentiating the activity of said antibiotic.

Spiroisoxazoline compounds having an activity potentiating the activity of an antibiotic

The present invention concerns a compound of general formula (I): in which n=0 or 1, R1 represents an optionally substituted alkyl chain, in particular substituted alkyl chain, in particular substituted with fluorine, X is chosen from N and CH, and R2 is chosen from optionally substituted phenyl and benzyl, wherein the heterocycles having 6 vertices comprise one, two or three nitrogen atoms. The present invention also concerns the use of this compound as a medicament, in particular in the treatment of bacterial and mycobacterial infections such as tuberculosis in combination with an antibiotic that is active against bacteria and/or mycobacteria, said compound potentiating the activity of said antibiotic.

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The present invention is directed to novel compounds of Formula (I), pharmaceutically acceptable salts or solvates thereof, and their use. 

2-oxo-3,4-dihydropyridine-5-carboxylates and their use

The present invention concerns compounds of general formula (I): in which Y and Z are chosen from CH and N; T is chosen from CO or SO; n is 1 to 3; R1 represents a group chosen, for example, from C1-C3 alkyl chains unsubstituted or substituted by fluorine, the unsubstituted or substituted cyclic, cyano, azido, alkoxy and phenyl groups; and R is chosen from the azido, cyano, alkinyl and 2-benzothiazolyl groups and an optionally substituted aromatic heterocycle with five vertices; and the use thereof in the treatment of bacterial and mycobacterial infections such as, for example, tuberculosis, leprosy and atypical mycobacterial infections. The present invention also concerns pharmaceutical compositions comprising, as the active ingredient, at least one of the abovementioned compounds and optionally an antibiotic activatable via the EthA pathway.

Compounds for use in the treatment of mycobacterial infections

Piperazinyl derivatives of formula (I) and their use as a drug, particularly for the treatment of cancer, are disclosed. Also disclosed are pharmaceutical compositions comprising the piperazinyl derivatives, and methods for synthesizing the piperazinyl derivatives.

Piperazinyl derivatives for the treatment of cancer

The present invention relates to piperazinyl derivatives of formula (I) and the use thereof as a drug, particularly for the treatment of cancer, the pharmaceutical compositions containing said derivatives, and the method for synthesising same. 

The present invention relates to compounds of Formula (I) wherein R1 is chosen among the following radicals: and n=1 or 2 and m=1 or 2 with the proviso that m=2 when R1 is The present invention also relates to the use thereof as drugs, more particularly in the treatment of mycobacterial infections and more particularly in the treatment of tuberculosis. 

Fluoralkylcarbonyl-oxadiazoles

The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them. 

Compounds which can be used for the treatment of cancers

Growing community of inventors

Lille, France

Benoit Deprez