ANDRIES, KOENRAAD JOZEF LODEWIJK MARCEL,安德斯,安德斯,KOUL, ANIL,郭安尔,郭安爾,GUILLEMONT, JEROME EMILE GEORGES,古乔治,古喬治,PASQUIER, ELISABETH THERESE JEANNE,佩斯尔,佩斯爾
申请号：
TW095128222
公开号：
TWI385168B
申请日:
2006.08.02
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)a pharmaceutically acceptable acid or base addition salt thereof, a quaternary amine thereof, a stereochemically isomeric form thereof, a tautomeric form thereof or a N-oxide form thereof, wherein R1is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkyylthioalkyl, Ar-akyl or di(Ar)alkyl p is 1, 2, 3 or 4 R2is hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula R3is alkyl, Ar, Ar-alkyl, Het or Het-alkyl R4is hydrogen, alkyl or benzyl R5is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl or two vicinal R5radicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl r is 1, 2, 3, 4 or 5 R6is hydrogen, alkyl, Ar or Het R7is hydrogen or alkyl R8is oxo or R7and R8together form the radical-CH=CH-N= Z is CH2or C(=O).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(Ia)或(Ib)化合物其藥學上可接受的酸或鹼加成鹽、其四級胺、其立體化學異構物形式、其互變異構物形式或其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、2、3或4;R2是氫、羥基、硫基、烷氧基、烷氧基烷氧基、烷硫基、單或二(烷基)胺基或式之基;R3是烷基、Ar、Ar-烷基、Het或Het-烷基;R4是氫、烷基或苄基;R5是氫、鹵基、鹵烷基、羥基、Ar、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;或兩個相鄰的R5基可以與和其連接之苯基環一起形成萘基;r是1、2、3、4或5;R6是氫、烷基、Ar或Het;R7是氫或烷基;R8是酮基;或R7與R8一起形成基團-CH=CH-N=;Z是CH2或C(=O)。
