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QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS
专利权人:
JANSSEN PHARMACEUTICA N.V.
发明人:
GUILLEMONT, JEROME EMILE GEORGES,古乔治,古喬治,PASQUIER, ELISABETH THERESE JEANNE,佩斯尔,佩斯爾,LANCOIS, DAVID FRANCIS ALAIN,蓝亚伦,藍亞倫,ANDRIES, KOENRAAD JOZEF LODEWIJK MARCEL,安德斯,安德斯,KOUL, ANIL,郭安尔,郭安爾,BACKX, LEO J
申请号:
TW095128224
公开号:
TWI422374B
申请日:
2006.08.02
申请国别(地区):
TW
年份:
2014
代理人:
摘要:
Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of formula (I)a pharmaceutically acceptable acid or base addition salt, a quaternary amine, a stereochemically isomeric form, a tautomeric form or aN-oxide form thereof, wherein R1is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl p is 1 to 3 s is 0 to 4 R2is hydrogen halo alkyl hydroxy mercapto optionally substituted alkyloxy alkyloxyalkyloxy alkylthio mono or di(alkyl)amino wherein alkyl may optionally be substituted Ar Het or a radical of formula R3is alkyl, Ar, Ar-alkyl, Het or Het-alkyl q is 0 to 4 R4and R5each independently are hydrogen, alkyl or benzyl or R4and R5may be taken together including the N to which they are attached R6is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl or two vicinal R6radicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl r is 1 to 5 R7is hydrogen, alkyl, Ar or Het R8is hydrogen, alkyl, hydroxyl, aminocarbonyl, mono-or di(alkyl)aminocarbonyl, Ar, Het, alkyl substituted with one or two Het, alkyl substituted with one or two Ar, Het-C(=O)- or Ar-C(=O)- provided that when the R3bearing radical is placed in position 3 of the quinoline moiety R7is placed in position 4 and R2is placed in position 2 and represents hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula, then s is 1 to 4.本發明係關於一種化合物用於製造藥劑供治療細菌感染之用途,條件是該細菌感染不是分枝桿菌感染,該化合物是式(I)化合物其藥學上可接受的酸或鹼加成鹽、四級胺、立體化學異構物形式、互變異構物形式或N-氧化物形式,其中R1是氫、鹵基、鹵烷基、氰基、羥基、Ar、Het、烷基、烷氧基、烷硫基、烷氧基烷基、烷硫基烷基、Ar-烷基或二(Ar)烷基;p是1至3;s是0至4;R2是氫、鹵基、烷基、羥基、巰基、視需要經取代之烷氧基、烷氧基烷氧基、烷硫基、單或二(烷基)胺基其中烷基可視需要經取代、Ar、Het或式之基;R3是烷基、Ar、Ar-烷基、Het或Het-烷基;q是0至4;R4及R5
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