Daniel F. J. Vernier,Frank Christopher Odds,IMRE CHRISTIAN FRANCIS CSOKA,Jozef Franz Elizabetha Van Gestel,Jérôme Emile Georges Guillemont,KOENRAAD JOZEF LODEWIJK MARCEL ANDRIES,Laurence Françoise Ber
申请号：
BRPI0312927
公开号：
BRPI0312927B1
申请日:
2003.07.18
申请国别(地区):
BR
年份:
2018
代理人:
摘要：
"Quinoline derivatives and their use as mycobacterial inhibitors". The present invention relates to novel substituted quinoline derivatives according to generic formula (ia) or generic formula (ib), pharmaceutically acceptable acid or base addition salts thereof, stereochemically isomeric forms thereof, tautomeric forms thereof and its n-oxide forms. 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 wherein, independently of each other, r ^ 1 ^ is bromo, p = 1, r ^ 2 ^ is alkyloxy, r ^ 3 ^ is optionally substituted naphthyl or phenyl, q = 1, r ^ R 4 and R 5 are each independently hydrogen, methyl or ethyl, R 6 is hydrogen, R is 0 or 1 and R 7 is hydrogen. A composition comprising a pharmaceutically acceptable carrier and, as an 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 the preparation of compounds is also claimed. claimed."derivados de quinolina e seu uso como inibidores micobacteriais". a presente invenção refere-se a novos derivados de quinolina substituídos de acordo com a fórmula genérica (ia) ou a fórmula genérica (ib), seus sais de adição ácido ou básica farmaceuticamente aceitáveis, suas formas estereoquimicamente isoméricas, as suas formas tautoméricas e as suas formas n-óxido. os compostos reivindicados são úteis para o tratamento de doenças micobacteriais, particularmente aquelas doenças causadas por micobactérias patogênicas como mycobacterium tuberculosis, m. bovis, m. avium e m. marinum. em particular, compostos são reivindicados, nos quais, independentemente uns dos outros, r^ 1^ é bromo, p = 1, r^ 2^ é alquilóxi, r^ 3^ é naftila ou fenila opcionalmente substituída, q = 1, r^
