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    퀴놀린계 유도체와 그의 제조방법
    12.
    发明授权
    퀴놀린계 유도체와 그의 제조방법 失效
    喹啉衍生物及其制备方法

    公开(公告)号：KR1019970005298B1

    公开(公告)日：1997-04-15

    申请号：KR1019930009768

    申请日：1993-06-01

    Applicant: 한국화학연구원

    Inventor： 김완주 ,  이태석 ,  남근수 ,  김봉진 ,  박명환 ,  하재두 ,  공재양

    IPC: C07D471/04 ,  C07D401/04

    Abstract: Novel quinoline derivatives(I) exhibiting superior antimicrobial activity and pharmaceutically acceptable salts thereof are prepared. The carboxyl group of the quinoline compound is activated by carboxylic acid-active reagent and reacted with compound having activated methylene group and alkali or alkali earth metals to give the title compound. In formula I, R1 is C1-3 lower alkyl, halogen-substituted lower alkyl, phenyl or halogen-substituted phenyl; R2 is H, lower alkyl or amino; R3 is halogen or (substituted) heterocyclic compound; X is N or C-R4(where, R4 is H, halogen, lower alkyl, or lower alkoxy); Y and Z are H, ester, cyano, nitro, acyl, (substituted) amido, lower alkylsulfoxy, or lower alkylsulfone group.

    Abstract translation: 制备具有优异抗菌活性的新喹啉衍生物（I）及其药学上可接受的盐。 喹啉化合物的羧基被羧酸活性试剂活化，与具有活性亚甲基的化合物和碱金属或碱土金属反应，得到标题化合物。 在式I中，R 1是C 1-3低级烷基，卤素取代的低级烷基，苯基或卤素取代的苯基; R2是H，低级烷基或氨基; R3是卤素或（取代的）杂环化合物; X是N或C-R4（其中R4是H，卤素，低级烷基或低级烷氧基）; Y和Z是H，酯，氰基，硝基，酰基，（取代的）酰氨基，低级烷基亚磺酰基或低级烷基砜基。

    항균작용을 갖는 퀴놀린계 화합물과 그의 제조방법
    20.
    发明授权
    항균작용을 갖는 퀴놀린계 화합물과 그의 제조방법 失效
    抗微生物喹啉化合物及其制备方法

    公开(公告)号：KR1019910009333B1

    公开(公告)日：1991-11-11

    申请号：KR1019890015203

    申请日：1989-10-23

    Applicant: 한국화학연구원

    Inventor： 김완주 ,  박명환 ,  오종훈 ,  정명희 ,  김봉진

    IPC: C07D498/04 ,  C07D498/06

    CPC classification number: C07D519/00

    Abstract: Quinolone derivs. of formula (I) and, when R1 is H, their acid addn. salts and hydrates are new. Z = halo or NH2; R1 = H or a cation. R2 = H, lower alkyl or formyl; m = 1-3; n = 1 or 2. Also claimed is the prepn. of (I) which comprises e.g. condensing corresp. quinolone deriv. with a leaving gp. in the 10-position with a diazabicycloamine. (I) may be orally or parenterally administered at a dose of 0.1-1.5 (0.2-0.8) g/kay to a 60 kg adult. Cpds. (I) are used for the treatment of bacterial infections. (I) have a better and wider range of activity against Gram positive and Gram negative bacteria than existing quinolone antibacterial agents, esp. norfloxacin, ciprofloxacin and ofloxacin. (I) also have a good antibacterial activity against methicillin resistant bacteria.

    Abstract translation: 喹诺酮衍生物。 的式（I）化合物，当R 1为H时，其酸加成。 盐和水合物是新的。 Z =卤素或NH 2; R1 = H或阳离子。 R2 = H，低级烷基或甲酰基; m = 1-3; n = 1或2.还要求是prepn。 的（I），其包含例如 冷凝对应 喹诺酮衍生物 离开gp。 在10位与二氮杂双环胺。 （I）可以以0.1-1.5（0.2-0.8）g / kay的剂量口服或非肠道给药至60kg成人。 CPDS。 （I）用于治疗细菌感染。 （I）比现有的喹诺酮抗菌剂具有更好和更广泛的抗革兰氏阳性和革兰氏阴性菌的活性，特别是。 诺氟沙星，环丙沙星和氧氟沙星。 （I）对耐甲氧西林细菌也具有良好的抗菌活性。

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