Quinoline derivatives and their use as mycobacterial inhibitors

Details Quinoline derivatives and their use as mycobacterial inhibitors Quinoline derivatives and their use as mycobacterial inhibitors

C - Chemistry, Metallurgy

07

D

C07D 215/22 (2006.01) A61K 31/47 (2006.01) A61P 31/06 (2006.01) C07D 215/227 (2006.01) C07D 215/36 (2006.01) C07D 215/48 (2006.01) C07D 221/00 (2006.01) C07D 235/00 (2006.01) C07D 401/06 (2006.01) C07D 401/12 (2006.01) C07D 405/04 (2006.01) C07D 405/06 (2006.01) C07D 409/04 (2006.01) C07D 409/06 (2006.01) C07D 471/04 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2493225

The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or the general Formula (Ib), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the tautomeric forms thereof and the N-oxide forms thereof. The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such as Mycobacterium tuberculosis, M. bovis, M. avium and M. marinum. In particular, compounds are claimed in which, independently from each other, R1 is bromo, p=1, R2 is alkyloxy, R3 is optionally substituted naphthyl or phenyl, q=1, R4 and R5 each independently are hydrogen, methyl or ethyl, R6 is hydrogen, r is equal to 0 or 1 and R7 is hydrogen. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of mycobacterial diseases and a process for preparing the claimed compounds.

L'invention concerne de nouveaux dérivés substitués de quinoléine représentés par la formule (Ia) ou la formule (Ib), leurs sels d'apport basique ou acide acceptables sur le plan pharmaceutique, leurs formes isomères sur le plan stéréochimique, leurs formes tautomères et leurs formes N-oxyde. Ces composés sont utiles pour traiter des maladies mycobactériennes, en particulier, les maladies provoquées par des mycobactéries pathogènes, telles que mycobacterium tuberculosis, M. bovis, M. avium et M. marinum. Dans ces composés, R?1¿ représente brome, p=1, R?2¿ représente alkyloxy, R?3¿ représente naphtyle ou phényle éventuellement substitués, q=1, R?4¿ et R?5¿ indépendamment chacun représentent hydrogène, méthyle ou éthyle, R?6¿ représente hydrogène, r est égal à 0 ou 1 et R?7¿ représente hydrogène. L'invention concerne également une composition comprenant un véhicule acceptable sur le plan pharmaceutique et, en tant qu'ingrédient actif, une quantité thérapeutique efficace de ces composés, la mise en application de ces composés ou de ces compositions afin de préparer un médicament servant à traiter des maladies mycobactériennes et un procédé servant à préparer ces composés.

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