5-aminoquinolone carboxylic acid derivative and antibacterial agent
containing the same as active ingredient
    19.
    发明授权
    5-aminoquinolone carboxylic acid derivative and antibacterial agent containing the same as active ingredient 失效
    5-氨基喹诺酮羧酸衍生物和含有活性成分的抗菌剂

    公开(公告)号:US5430028A

    公开(公告)日:1995-07-04

    申请号:US185898

    申请日:1994-01-26

    摘要: A 5-aminoquinolone carboxylic acid derivative represented by the following general formula (1): ##STR1## wherein R.sup.1 means a hydrogen atom, an amino group, a linear or branched alkyl group having 1-5 carbon atoms and an alkylamino group containing a linear or branched alkyl group having 1-5 carbon atoms, R.sup.2 denotes a hydrogen atom or a linear or branched alkyl group having 1-5 carbon atoms, X stands for a halogen atom, Y means CH.sub.2, NH, CHR.sup.3 NR.sup.3, (R.sup.3 denoting a linear or branched alkyl group having 1-5 carbon atoms) or an oxygen atom, and Z stands for an oxygen atom or 2 hydrogen atoms, or a salt thereof, and an antibacterial agent containing such a derivative or salt as an active ingredient.The derivative or salt thereof exhibits strong anti-bacterial activities against Grampositive bacteria including tolerant bacteria, and is satisfactorily absorbed in a living body.

    摘要翻译: PCT No.PCT / JP93 / 00694 Sec。 371日期1994年1月26日 102(e)日期1994年1月26日PCT提交1993年5月25日PCT公布。 出版物WO93 / 24460 PCT 日期:1993年12月9日,下列通式(1)表示的5-氨基喹诺酮羧酸衍生物:其中R 1表示氢原子,氨基,直链或支链烷基, 5个碳原子和含有1-5个碳原子的直链或支链烷基的烷基氨基,R2表示氢原子或具有1-5个碳原子的直链或支链烷基,X表示卤素原子,Y表示CH2 ,NH,CHR 3 NR 3,(R3表示具有1-5个碳原子的直链或支链烷基)或氧原子,Z表示氧原子或2个氢原子,或其盐,以及含有这些的抗菌剂 衍生物或盐作为活性成分。 其衍生物或盐对包括耐受性细菌的细菌性细菌表现出强的抗菌活性,并且令人满意地吸收在生物体内。

    Imidazole derivative
    20.
    发明授权
    Imidazole derivative 失效
    咪唑衍生物

    公开(公告)号:US5164513A

    公开(公告)日:1992-11-17

    申请号:US747632

    申请日:1991-08-20

    IPC分类号: C07D521/00

    摘要: Novel imidazole derivatives and their acid adducts are disclosed. The imidazole derivatives are represented by formula: ##STR1## wherein R.sub.1 represents an alkyl group, R.sub.2 represents a hydrogen atom, an alkyl group which may have a substituent, or an aralkyl group which may have a substituent, provided that R.sub.1 and R.sub.2 are not both methyl groups at the same time. They have strong antimicrobial activity, especially against those fungi belonging to the genera Candida, Trichophyton, Microsporum, and Epidermorphyton, as well as against Gram-positive bacteria, and thus is useful as a antimicrobial agent.

    摘要翻译: 公开了新的咪唑衍生物及其酸加成物。 咪唑衍生物由下式表示:其中R1表示烷基,R2表示氢原子,可以具有取代基的烷基或可具有取代基的芳烷基,条件是R1和 R2不同时同时为甲基。 它们具有很强的抗微生物活性,特别是针对属于假丝酵母属,毛癣菌属,微孢子虫属和表皮假单胞菌属的真菌,以及抗革兰氏阳性菌,因此可用作抗微生物剂。