항균 작용을 갖는 2,5-디히드로-1H-피롤로[3.4.C]피리딘 유도체와 그의 제조방법
    46.
    发明授权
    항균 작용을 갖는 2,5-디히드로-1H-피롤로[3.4.C]피리딘 유도체와 그의 제조방법 失效
    2,5-DIHYDRO-1H-吡咯烷酮| 3,4,C - 吡啶衍生物及其制备方法

    公开(公告)号:KR1019920008165B1

    公开(公告)日:1992-09-24

    申请号:KR1019900011885

    申请日:1990-08-02

    Abstract: Quinolne derivs. of formula (I) and their pharmaceutically acceptable salts are prepd.by condensing a pyridine deriv. of formula (II) and a quinoline carboxylic acid deriv. of formula (III) in the presence (or absence) of a solvent, at room temp. - 200 deg.C for 2-16 hrs. In the formulas, Z1, Z2 nd Z3 each = H, C1-3 alkyl, halogen, cyano, amino, hydroxy, C1-3 alkylamine or alkoxy; R1= ethyl or cyclopropyl; R2 and R3=H,F,Br or Cl; X=N, methyne or fluoromethyne, The cpds. (I) are useful as an antibacterial agent.

    Abstract translation: 喹啉衍生物 式(I)化合物及其药学上可接受的盐是通过将吡啶衍生物缩合制备的。 的式(II)和喹啉羧酸衍生物。 在存在(或不存在)溶剂的情况下,在室温下进行。 - 200℃2-16小时。 在式中,Z 1,Z 2,Z 3各自为H,C 1-3烷基,卤素,氰基,氨基,羟基,C 1-3烷基胺或烷氧基; R1 =乙基或环丙基; R2和R3 = H,F,Br或Cl; X = N,甲炔或氟甲炔,cpds。 (I)可用作抗菌剂。

    항균작용을 갖는 벤즈옥사진 카르복실산 유도체와 그의 제조방법
    49.
    发明授权
    항균작용을 갖는 벤즈옥사진 카르복실산 유도체와 그의 제조방법 失效
    苯并吖啶甲酸衍生物及其制备方法

    公开(公告)号:KR1019910009334B1

    公开(公告)日:1991-11-11

    申请号:KR1019890016019

    申请日:1989-11-06

    Abstract: Benzoxazine carboxylic acid derivs. of formula (I) are new. In (I), R1-R5 each = H or lower alkyl; R6 and R7 each = H or C1-3 linear or cyclic lower alkyl, or substd. lower alkyl; the methyl gp. in the 3-position may be (S)-form or racemic form. Also claimed is the prepn. of (I) which comprises condensing a corresp. benzoxazine carboxylic acid deriv. of formula (II) with a 2,5- dihydropyrrole deriv. of formula (III) in the presence or absence of a solvent. Cpds. (I) have a good antibacterial activity and broad spectrum antibacterial action against Gram positive and Gram negative bacteria.

    Abstract translation: 苯并恶嗪羧酸衍生物。 式(I)的化合物是新的。 在(I)中,R 1 -R 5各自为H或低级烷基; R6和R7各自为H或C1-3直链或环状低级烷基,或被取代。 低级烷基 甲基gp。 在3位可以是(S)形式或外消旋形式。 还声称是prepn。 (I),其包括冷凝对应物。 苯并恶嗪羧酸衍生物。 式(II)与2,5-二氢吡咯衍生物反应。 在式(III)的存在或不存在下进行。 CPDS。 (I)对革兰氏阳性和革兰氏阴性菌具有良好的抗菌活性和广谱抗菌作用。

    항균작용을 갖는 퀴놀린계 화합물과 그의 제조방법
    50.
    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

    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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