항균작용을 갖는 퀴놀린계 화합물과 그의 제조방법
    7.
    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。

    디아자비시클로아민 화합물과 그의 제조방법
    8.
    发明授权
    디아자비시클로아민 화합물과 그의 제조방법 失效
    二氮杂环胺化合物及其制备方法

    公开(公告)号:KR1019910009331B1

    公开(公告)日:1991-11-11

    申请号:KR1019890015204

    申请日:1989-10-23

    CPC classification number: C07D471/04 C07D487/04

    Abstract: Diazabicycloamine derivs. of formula (I) and their salts are new. In (I), m = 1-3; n = 1-2; and R1, R2 = H or lower alkyl. Also claimed is the preparation of (I) which comprises e.g. reacting tetrakis(halomethyl)ethylene (halo = Cl, Br or I) with NH3 to form (I) in which m and n = 1 and R1 and R2 = H. (I) is e.g. 3,7-diazabicyclo(3.3.0)oct-1(5)ene or 3,8-diazabicyclo(4.3.0)non-1(6)-ene. Cpd. (I) is used for mfg. new quinolone antibiotics (claimed), with high antibacterial activity against Gram negative and Gram positive bacteria and improved antibacterial activity against methicillin resistant Staphylococcus aureus compared to ofloxacin, norfloxacin and ciprofloxacin. The quinolone are used for treating urethritis. (I) is also used for the prepn. of cephalosporins. cpds.

    Abstract translation: 二氮杂双环胺衍生物。 的式(I)及其盐是新的。 在(I)中,m = 1-3; n = 1-2; 和R 1,R 2 = H或低级烷基。 还要求保护的是(I)的制备,其包括例如 使四(卤代甲基)乙烯(卤代= Cl,Br或I)与NH 3反应形成其中m和n = 1且R 1和R 2 = H的(I)。 3,3-二氮杂双环(3.3.0)辛-1(5)烯或3,8-二氮杂双环(4.3.0)非-1(6)烯。 CPD。 (I)用于制造。 与氧氟沙星,诺氟沙星和环丙沙星相比,新型喹诺酮类抗生素(要求保护)对革兰氏阴性和革兰氏阳性菌具有较高的抗菌活性,对耐甲氧西林金黄色葡萄球菌的抗菌活性更好。 喹诺酮用于治疗尿道炎。 (I)也用于制备。 的头孢菌素。 国家方案文件。

    항균작용을 갖는 퀴놀린계 화합물과 그의 제조방법
    9.
    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:KR1019910009330B1

    公开(公告)日:1991-11-11

    申请号:KR1019890015202

    申请日:1989-10-23

    CPC classification number: C07D471/04 C07D487/04

    Abstract: Quinolone derivs. of formula (I) and their acid addn. salts are new. In (I), X = C-H, C-F N; Z = H, halo or NH2; R1 = H or a cation; R2 = C1-4 (halo)hlkyl or hydroxyalkyl, or vinyl, C3-6 cycloalkyl or fluorophenyl; R3 = H, lower alkyl or formyl; m = 1- 3; n = 1 or 2. Also claimed is preparation of (I) which comprises e.g. condensing the corresponding quinolone derivative having a leaving gp. in the 7-position with a diazabicycloamine. (I) have improved and wider range of antibacterial activity against Gram positive and Gram negative bacteria than existing quinolone antibacterial agents, esp. norfloxacin, ciprofloxacin and ofloxacin. (I) have good antibacterial activity against methicillin resistant bacteria.

    Abstract translation: 喹诺酮衍生物。 的式(I)和它们的酸加成。 盐是新的。 在(I)中,X = C-H,C-F N; Z = H,卤素或NH 2; R1 = H或阳离子; R2 = C1-4(卤代)烷基或羟基烷基,或乙烯基,C3-6环烷基或氟苯基; R3 = H,低级烷基或甲酰基; m = 1- 3; n = 1或2.还要求保护的是(I)的制备。 冷凝具有离去gp的相应喹诺酮衍生物。 在7-位与二氮杂双环胺。 (I)比现有的喹诺酮类抗菌药物具有改善和更广泛的抗革兰氏阳性和革兰氏阴性菌的抗菌活性。 诺氟沙星,环丙沙星和氧氟沙星。 (I)对耐甲氧西林细菌具有良好的抗菌活性。

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