Elisabeth Thérèse Jeanne Pasquier,Jérôme Emile Georges Guillemont
申请号：
BRPI0507076
公开号：
BRPI0507076B1
申请日:
2005.01.21
申请国别(地区):
BR
年份:
2019
代理人:
摘要：
substituted quinolines and their use as mycobacterial inhibitors. The present invention relates to novel substituted quinoline derivatives according to formula (Ia) or formula (Ib) as well as salts, quaternary amines, stereochemically isomeric forms, tautomeric forms and n-oxide forms thereof. derivatives wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, air, het, alkyl, alkyloxy, alkylite, alkyloxyalkyl, alkylthioalkyl, aralkyl or di (ar) alkyl； p is 1, 2, 3 or 4； R 2 is hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di (alkyl) amino or a radical of formula； R3 is alkyl, air, aralkyl, het or hetalkyl； R4 is hydrogen, alkyl or benzyl； R5 is hydrogen, halo, haloalkyl, hydroxy, air, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, aralkyl or di (ar) alkyl； or two vicinal radicals R5 may be joined together to form together with the phenyl ring to which a naphthyl is attached； r is 1,2,3,4 or 5； R6 is hydrogen, alkyl, ar or het； R7 is hydrogen or alkyl； R 8 is oxo； or r ^ 7 ^ and r ^ 8 ^ taken together form the radical -ch <；154>； ch-n <；154>；； z is ch ~ 2 ~ or c (<；154>； o). The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such as m. tuberculosis, m.bovis, m. avium, m. smegmatis and m. Marinum. Also claimed are a pharmaceutical composition containing a compound of the present invention, 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.quinolinas substituídas e seu uso como inibidores micobacterianos. a presente invenção refere-se a novos derivados de quinolina substituida de acordo com a fórmula geral (la) ou com a fómula geral (lb) bem como a sais, amina quaternárias, formas estereoquimicamente isoméricas, formas tautoméricas e formas de n-óxido desses derivados, onde r^ 1^ é hidrogênio, halo, halo
