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    • 27. 发明申请
    • NOVEL QUINOLONE COMPOUNDS AND PROCESSES FOR PREPARATION THEREOF
    • 新型喹啉酮化合物及其制备方法
    • WO1992012155A1
    • 1992-07-23
    • PCT/KR1992000003
    • 1992-01-14
    • HANMI PHARMACEUTICAL CO., LTD.MOON, Soon, KuLEE, Gwan, SunRYOO, Eui, SangCHANG, Young, KilMOON, Young, HoKIM, Sang, TaeCHUN, Jong, PilKOH, Joon, HyungGIL, Young, Hwan
    • HANMI PHARMACEUTICAL CO., LTD.
    • C07D487/08
    • C07D487/04Y02P20/55
    • This invention relates to the novel quinolone compound of formula (I) having excellent antimicrobial activity both against gram positive and negative bacteria, its pharmaceutically acceptable salt, and the process for preparation thereof; wherein R is hydrogen or protective group, R is hydrogen, amino, alkylamino from one to four carbon atoms, hydroxy, alkoxy from one to four carbon atoms, mercapto, alkylthio from one to four carbon atoms, or halogen, R is alkyl from one to four carbon atoms, alkenyl from two to four carbon atoms, cycloalkyl from three to six carbon atoms, haloalkyl, hydroxyalkyl from two to four carbon atoms, methoxy, amino, alkylamino from one to two carbon atoms, dimethylamino, or optionally substituted phenyl with more than one of halogen atoms or alkyl from one to three carbon atoms, Z is an amine of formula (II), (wherein R is hydrogen or alkyl from one to four carbon atoms, R and R are, same or different, hydrogen or alkyl from one to two carbon atoms), X is N or C-R (wherein R is hydrogen, hydroxy, methyl, cyano, nitro, methoxy, halogen, or can form a bridge of formula (a), (b), (c) or (d) with R .
    • 本发明涉及对革兰氏阳性细菌和阴性细菌具有优异的抗微生物活性及其药学上可接受的盐的式(I)的新型喹诺酮化合物及其制备方法; 其中R 1为氢或保护基,R 2为氢,氨基,1至4个碳原子的烷基氨基,羟基,1至4个碳原子的烷氧基,1至4个碳原子的巯基,烷硫基,或卤素 R 3为1至4个碳原子的烷基,2至4个碳原子的烯基,3至6个碳原子的环烷基,2至4个碳原子的卤代烷基,羟基烷基,甲氧基,氨基,1至2个碳原子的烷基氨基 原子,二甲基氨基或具有多于一个卤素原子或1-3个碳原子的任选取代的苯基,Z是式(II)的胺,其中R 4是氢或1-4个碳原子的烷基 R 5和R 7相同或不同,氢或一至两个碳原子的烷基),X是N或CR 6(其中R 6是氢,羟基,甲基,氰基, 硝基,甲氧基,卤素,或可以与R 3形成式(a),(b),(c)或(d)的桥。