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    • 9. 发明申请
    • PYRIDOBENZOXAZINE DERIVATIVES
    • 吡咯烷酮衍生物
    • WO1998013370A1
    • 1998-04-02
    • PCT/JP1997003440
    • 1997-09-26
    • DAIICHI PHARMACEUTICAL CO., LTD.TAKEMURA, MakotoTAKAHASHI, HisashiKAWAKAMI, Katsuhiro
    • DAIICHI PHARMACEUTICAL CO., LTD.
    • C07D498/06
    • C07D498/06
    • Derivatives having potent antibacterial activities on gram-negative and gram-positive bacteria and, at the same time, favorable dynamics in vivo and a high safety; and excellent drugs. Compounds represented by general formula (I) and salts thereof, hydrates thereof, and antibacterial agents containing the same as the active ingredient. In said formula, R represents hydrogen or C1-6 alkyl optionally having substituent(s) selected from the group consisting of hydroxy, halogeno, C1-6 alkylthio and C1-6 alkoxy; R represents hydrogen or amino optionally having one or two substituents selected from the group consisting of formyl, C1-6 alkyl and C2-6 acyl; and R represents hydrogen, phenyl, acetoxymethyl, pivaloyloxymethyl, etoxycarbonyl, cholin, dimethylaminoethyl, 5-indanyl, phthalidinyl, 5-alkyl-2-oxo-1,3-dioxol-4-ylmethyl, 3-acetoxy-2-oxobutyl, C1-6 alkyl, C2-7 alkoxymethyl, or phenylalkyl composed of C1-6 alkylene and phenyl.
    • 衍生物对革兰阴性和革兰氏阳性细菌具有强力的抗菌活性,同时体内有利的动力学和高安全性; 和优良的药物。 由通式(I)表示的化合物及其盐,其水合物和含有该活性成分的抗菌剂。 在所述式中,R 1表示氢或任选具有选自羟基,卤代C 1-6烷硫基和C 1-6烷氧基的取代基的C 1-6烷基; R 2表示氢或任选具有一个或两个选自甲酰基,C 1-6烷基和C 2-6酰基的取代基的氨基; 并且R 3表示氢,苯基,乙酰氧基甲基,新戊酰氧基甲基,丁氧基羰基,胆碱,二甲基氨基乙基,5-二氢化茚基,邻苯二基苯基,5-烷基-2-氧代-1,3-二氧杂环戊烯-4-基甲基,3-乙酰氧基-2- 氧代丁基,C 1-6烷基,C 2-7烷氧基甲基或由C 1-6亚烷基和苯基组成的苯基烷基。