ANDRIES, KOENRAAD JOZEF LODEWIJK MARCEL,安马瑟,安馬瑟,KOUL, ANIL,郭安尔,郭安爾,LANCOIS, DAVID FRANCIS ALAIN,蓝亚恩,藍亞恩,MOTTE, MAGALI MADELEINE SIMONE,莫赛门,莫賽門,GUILLEMONT, JEROME EMILE GEORGES,古乔治,古喬治
申请号：
TW095123049
公开号：
TWI413520B
申请日:
2006.06.27
申请国别(地区):
TW
年份:
2013
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 (Ia) or (Ib)aN-oxide, a tautomeric form or a stereochemically isomeric form thereof wherein A-is a counter ion R1is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl p is 1 to 4 R2is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino orwherein Y is CH2, O, S, NH or N-alkyl 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 -CH=CH-CH=CH- r is 1 to 5 R7is hydrogen, alkyl, Ar or Het R8is hydrogen or alkyl R9is oxo or R8and R9taken together form -CH=CH-N= R10is alkyl, alkylcarbonyl, Ar, Ar-alkyl, Ar-carbonyl, Het1-alkyl or Het1-carbonyl.本發明係有關一種以化合物製造用於治療細菌感染之醫藥上之用途,但其限制條件為該細菌感染不為分枝桿菌(Mycobacteria)感染,該化合物為式(Ia)或(Ib)化合物其N-氧化物、互變異構型或立體化學異構型,其中A-為抗衡離子;R1為氫、鹵基、鹵烷基、氰基、羥基、Ar、Het、烷基、烷基氧、烷基硫、烷基氧烷基、烷基硫烷基、Ar-烷基或二(Ar)烷基;p為1至4;R2為氫、羥基、氫硫基、烷基氧、烷基氧烷基氧、烷基硫、單-或二(烷基)胺基或其中Y為CH2、O、S、NH或N-烷基;R3為烷基、Ar、Ar-烷基、Het或Het-烷基;q為0至4;R4與R5分別獨立為氫、烷基或苯甲基;或R4與R5可與其所附接之氮共同形成;R6為氫、鹵基、鹵烷基、羥基、Ar、烷基、烷基氧、烷基硫、烷基氧烷基、烷基硫烷基、Ar-烷基或二(Ar)烷基;或兩個相鄰R6基團可共同形成-CH=CH-CH=CH-;r為1至5;R7為氫、烷基、Ar或Het;R8為氫或烷基;R9為氧代基;或R8與R9共同形成-CH=CH-N=;R10為烷基、烷基羰基、Ar、Ar-烷基、Ar-羰基、Het1-烷基或Het1-羰基。
