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QUINOLINE DERIVATIVES AS ANTIBACTERIAL AGENTS
专利权人:
JANSSEN PHARMACEUTICA N.V.
发明人:
ANDRIES, KOENRAAD JOZEF LODEWIJK MARCEL,安戴斯,安戴斯,KOUL, ANIL,高安尼,高安尼,GUILLEMONT, JEROME EMILE GEORGES,古雷蒙,古雷蒙,MOTTE, MAGALI MADELEINE SIMONE,莫特,莫特
申请号:
TW095123051
公开号:
TWI392494B
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)alkylp is 1 to 4R2is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino orwherein Y is CH2, O, S, NH orN-alkylR3is Ar or HetR4and R5each independently are hydrogen, alkyl or benzylor R4and R5are taken together including the N to which they are attachedR6is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkylor two vicinal R6radicals may be taken together to form -CH=CH-CH=CH-r is 1 to 5R7is hydrogen, alkyl, Ar or HetR8is hydrogen or alkylR9is oxoor R8and R9together form -CH=CH-N=Alk is a straight or branched saturated hydrocarbon radical having from 1 to 6 carbon atoms.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至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,其中Y為CH2、O、S、NH或N-烷基;R3為Ar或Het;R4與R5各分別為氫、烷基或苄基;或R4與R5一起並包括其所鍵接的N;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-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R9一起形成-CH=CH-N=;Alk為具有1至6個碳原子的直鏈或支鏈飽和烴基。
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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