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    • 3. 发明申请
    • Treatment of latent tuberculosis
    • 治疗潜伏性结核病
    • US20060142279A1
    • 2006-06-29
    • US11296992
    • 2005-12-08
    • Koenraad Marcel AndriesAnil Koul
    • Koenraad Marcel AndriesAnil Koul
    • A61K31/541A61K31/5377A61K31/496A61K31/4709
    • A61K31/47A61K31/4704
    • 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) is a pharmaceutically acceptable salt, a quaternary amine, a N-oxide, a tautomeric form or a stereochemically isomeric form thereof wherein R1 is 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; R2 is hydrogen, hydroxy, mercapto, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula ;R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; q is zero, 1, 2, 3 or 4; R4 and R5 each independently are hydrogen, alkyl or benzyl; or R4 and R5 may be taken together including the N to which they are attached; R6 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R6 radicals may be taken together to form a bivalent radical —CH═CH—CH═CH—; r is 1, 2, 3, 4 or 5; R7 is hydrogen, alkyl, Ar or Het; R8 is hydrogen or alkyl; R9 is oxo; or R8 and R9 together form the radical ═N—CH═CH—.
    • 式(Ia)或(Ib)化合物在制备用于治疗潜伏性结核病的药物中的用途,其中式(Ia)或(Ib)化合物是药学上可接受的盐,季胺,N 氧化物,互变异构形式或其立体化学异构体形式,其中R 1是氢,卤素,卤代烷基,氰基,羟基,Ar,Het,烷基,烷氧基,烷硫基,烷氧基烷基,烷硫基烷基, 或二(Ar)烷基; p为1,2,3或4; R 2是氢,羟基,巯基,烷氧基,烷氧基烷氧基,烷硫基,一或二(烷基)氨基或式的基团; R 3是烷基,Ar,Ar - 烷基,Het或Het-烷基; q为零,1,2,3或4; R 4和R 5各自独立地是氢,烷基或苄基; 或R 4和R 5可以一起包括它们所连接的N; R 6是氢,卤素,卤代烷基,羟基,Ar,烷基,烷氧基,烷硫基,烷氧基烷基,烷硫基烷基,芳烷基或二(Ar) 或两个邻位R 6个基团可以一起形成二价基团-CH-CH-CH-CH-; r为1,2,3,4或5; R 7是氢,烷​​基,Ar或Het; R 8是氢或烷基; R 9是氧代; 或R 8和R 9一起形成基团-N-CH-CH-。