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    • 6. 发明申请
    • QUINOLIZINONE TYPE COMPOUNDS
    • 喹诺酮类化合物
    • WO1995010519A1
    • 1995-04-20
    • PCT/US1994011166
    • 1994-09-30
    • ABBOTT LABORATORIES
    • ABBOTT LABORATORIESCHU, Daniel, T.LI, QunCOOPER, Curt, S.FUNG, Anthony, K., L.LEE, Cheuk, M.PLATTNER, Jacob, J.
    • C07D455/02
    • C07D471/04A61K38/00C07D213/61C07D213/68C07D455/02C07K5/06026
    • Antibacterical coumpounds having formula (I) and the pharmaceutically acceptable salts, esters and amides thereof, preferred examples of which include those coumpounds wherein R is cycloalkyl of from three to eight carbon atoms or substituted phenyl; R is selected from the group consisting of (a) halogen, (b) loweralkyl, (c) loweralkenyl, (d) cycloalkyl of from three to eight carbons, (e) cycloalkenyl of from four to eight carbons, (f) loweralkoxy, (g) aryloxy, (h) aryl(loweralkyl)oxy, (i) aryl(loweralkyl), (j) cycloalkyl(loweralkyl), (k) amino, (l) (loweralkyl)amino, (m) aryl(loweralkyl)amino, (n) hydroxy substituted (loweralkyl)amino, (o) phenyl, (p) substituted phenyl, (q) bicyclic nitrogen-containing heterocycle, (r) nitrogen-containingaromatic heterocycle, and (s) nitrogen-containing heterocycle having formula (Ia) where x is between zero and three; R is halogen; R is hydrogen, loweralkyl, a pharmaceutically acceptable cation, or a prodrug ester group; R is hydrogen, loweralkyl, halo(loweralkyl), or -NR R ; and R is loweralkyl, as wellas pharmaceutical compositions containing such compounds and the use of the same in the treatment of bacterial infections.
    • 具有式(I)的抗菌配方及其药学上可接受的盐,酯和酰胺,其优选实例包括其中R 1为3至8个碳原子的环烷基或取代的苯基的那些芳族基团; R 2选自(a)卤素,(b)低级烷基,(c)低级烯基,(d)3至8个碳的环烷基,(e)4至8个碳的环烯基,(f )低级烷氧基,(g)芳氧基,(h)芳基(低级烷基)氧基,(i)芳基(低级烷基),(j)环烷基(低级烷基),(k)氨基,(1)(低级烷基)氨基,(m) (低级烷基)氨基,(n)羟基取代的(低级烷基)氨基,(o)苯基,(p)取代的苯基,(q)双环含氮杂环,(r)含氮芳族杂环,和 具有式(Ia)的杂环,其中x在0和3之间; R 3是卤素; R 4是氢,低级烷基,药学上可接受的阳离子或前药酯基; R 5是氢,低级烷基,卤代(低级烷基)或-NR 13 R 14; R 6为低级烷基,以及含有这些化合物的药物组合物及其在治疗细菌感染中的用途。