ANDRIES, KOENRAAD JOZEF LODEWIJK MARCEL,安瑞斯,安瑞斯,KOUL, ANIL,郭安尼,郭安尼
申请号：
TW094143290
公开号：
TWI404535B
申请日:
2005.12.08
申请国别(地区):
TW
年份:
2013
代理人:
摘要：
Use of a compound of formula (Ia) or (Ib) for the manufacture of a medicament for the treatment of latent tuberculosis, wherein the compound of formula (Ia) or (Ib) isa pharmaceutically acceptable salt, a quaternary amine, a N-oxide, a tautomeric form or a stereochemically isomeric form thereof wherein R1is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkylp is 1, 2, 3 or 4R2is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formulaR3is alkyl, Ar, Ar-alkyl, Het or Het-alkylq is zero, 1, 2, 3 or 4R4and R5each ihdependently are hydrogen, alkyl or benzylor R4and R5may be 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 a bivalent radical -CH=CH-CH=CH-r is 1, 2, 3, 4 or 5R7is hydrogen, alkyl, Ar or HetR8is hydrogen or alkylR9is oxoor R8and R9together form the radical=N-CH=CH-.本發明係關於式(Ia)或(Ib)之化合物製造藥劑用於治療潛伏期結核病之用途,其中式(Ia)或(Ib)之化合物是其藥學上可接受的鹽、其四級胺、其N-氧化物、其互變異構物形式或其立體化學異構物形式,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、巰基、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;q是0、1、2、3或4;R4及R5各獨立地是氫、烷基或苄基;或R4及R5可以一起包括和其連結之N;R6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R6基可以一起形成二價基-CH=CH-CH=CH-;r是1、2、3、4或5;R7是氫、烷基、Ar或Het;R8是氫或烷基;R9是酮基;或R8及R9一起形成=N-CH=CH-基。
