ANDRIES, KOENRAAD JOZEF LODEWIJK MARCEL,安戴斯,KOUL, ANIL,高安尼,GUILLEMONT, JEROME EMILE GEORGES,古雷蒙,LANCOIS, DAVID FRANCIS ALAIN,蓝寇斯,藍寇斯,MOTTE, MAGALI MADELEINE SIMONE,莫特,DORANGE, ISMET,窦瑞吉
申请号：
TW095123127
公开号：
TWI387457B
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)a pharmaceutically acceptable acid or base addition salt thereof, a stereochemically isomeric form thereof, a tautomeric form thereof 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, 2, 3 or 4；R2is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di (alkyl) amino or a radical of formula；R3is alkyl, Ar, Ar－alkyl, Het or Het－alkyl；q is 1, 2 or 3；R4and R5are hydrogen, alkyl or benzyl；or R4and R5together and including the N to which they are attached may form a ring；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 a bivalent radical of formula －CH＝CH－CH＝CH－；r is 1, 2, 3, 4 or 5；R7is hydrogen, alkyl, Ar or Het；R8is hydrogen or alkyl；R9is oxo；or R8and R9together form the radical－CH＝CH－N＝.一化合物用於製造治療細菌感染之醫藥品的用途，前提是該細菌感染非為分枝桿菌感染，該化合物為式(Ia)或(Ib)化合物其藥學上可接受的酸式或鹼式加成鹽、其立體化學異構形式、其互變異構形式或其N－氧化物形式，其中R1為氫、鹵基、鹵烷基、氰基、羥基、Ar、Het、烷基、烷基氧基、烷基硫基、烷基氧基烷基、烷基硫基烷基、Ar－烷基或二(Ar)烷基；p為1、2、3或4；R2為氫、羥基、巰基、烷基氧基、烷基氧基烷基氧基、烷基硫基、單或二(烷基)胺基或具式之基；R3為烷基、Ar、Ar－烷基、Het或Het－烷基；q為1、2或3；R4與R5為氫、烷基或苄基；或R4與R5一起並包括其所鍵接的N可形成一環；R6為氫、鹵基、鹵烷基、羥基、Ar、烷基、烷基氧基、烷基硫基、烷基氧基烷基、烷基硫基烷基、Ar－烷基或二(Ar)烷基；或兩鄰位R6基可一起形成具式－CH＝CH－CH＝CH－之二價基；r為1、2、3、4或5；R7為氫、烷基、Ar或Het；R8為氫或烷基；R9為氧代基；或R8與R9一起形成－CH＝CH－N＝基。
