Quinoline derivatives and their use as mycrobacterial inhibitors

• Main Authors: VERNIER DANIEL F. J, ODDS FRANK C, GUILLEMONT JEROME E. G, DECRANE LAURENCE F. B, VENET MARC G, POIGNET HERVE J. J, ANDILEITH K. J. L. M, GESTEL JOZEF F. E. VAN
• Format: Patent
• Language: Chinese; English
• Published: 26.10.2011
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

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, R is bromo, p=1, R is alkyloxy, R is optionally substituted naphthyl or phenyl, q=1, R and R each independently are hydrogen, methyl or ethyl, R is hydrogen, r is equal to 0 or 1and R 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