UniversitÉ De Droit Et De La SantÉ De Lille 2

Glaxosmithkline Intellectual Property Development Limited

Bioversys Ag

Centre National De La Recherche Scientifique

Institut National De La Sante Et De La Recherche Medicale

Institut Pasteur De Lille

Universite De Lille 2, Universite Du Droit Et De La Sante

Nicolas Willand

Benoit Deprez

Alain Baulard

Priscille Brodin

Marilyne Bourotte

Esther Porras De Francisco

Modesto Jesús Remuiñan-Blanco

Matthieu Frederik Desroses

Marion Flipo

Vincent Villeret

Camille Locht

Florence Leroux

Laurence Agouridas-Dutot

Patrick Toto

Bertrand Dirie

Benoît Deprez

Baptiste Villemagne

Olivier Sperando

Lucie Maingot

Geoffroy Dequirez

Modesto Jesús REMUIÑAN-Blanco

Matthieu Frédérik Desroses

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 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 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

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 the use of compounds with a potentiating effect on the activity of antibiotics that are activatable via the EthA enzymatic pathway, for the preparation of a medicament for preventing and/or treating mycobacterial infections such as tuberculosis and leprosy, to pharmaceutical compositions comprising them in combination with an antibiotic that is activatable via the EthA pathway, to compounds having a potentiating effect on the activity of antibiotics that are activatable via the EthA enzymatic pathway, to pharmaceutical compositions comprising them and to their use as medicaments, especially medicaments for preventing and/or treating mycobacterial infections such as tuberculosis and leprosy.

Compounds having a potentiating effect on the activity of ethionamide and uses thereof

Growing community of inventors

Lille, France

Nicolas Willand