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    • 5. 发明授权
    • 1,8 benzonaphthyridine derivatives and antimicrobial compositions
    • 1,8苯并萘啶衍生物和抗微生物组合物
    • US5556861A
    • 1996-09-17
    • US472766
    • 1995-06-07
    • Eric BacqueMichel BarreauJean-Francois DesconcloisPhilippe GirardMichel KryvenkoMarc P. LavergneJean-Marc ParisGuy Picaut
    • Eric BacqueMichel BarreauJean-Francois DesconcloisPhilippe GirardMichel KryvenkoMarc P. LavergneJean-Marc ParisGuy Picaut
    • C07D471/04A61K31/435
    • C07D471/04
    • This invention relates to a novel 1,8 benzo[b]naphythyridine derivative of general formula (I), ##STR1## wherein R is H or a hydroxy, amino or alkylamino radical optionally substituted by amino or hydroxy, or R is dialkylamino of which the alkyl portions may form, with the nitrogen atom, a 5- or 6-membered heterocyclic ring which optionally contains a further heteroatom chosen from nitrogen, oxygen or sulphur, or R is C.sub.3-6 cycloalkylamino or an alkanylamino, N-alkyl N-alkanylamino or aminoalkylphenylamino radical; R.sub.1 and R.sub.2, which are the same or different, are in positions 2 and 3 and represent H, alkyl, C.sub.2-4 alkenyl, phenyl, or substituted phenyl, or R.sub.1 and R.sub.2 are in position 2 and represent alkyl; R.sub.3 is H or alkyl, fluoroalkyl, carboxyalkyl, C.sub.3-6 cycloalkyl, fluorophenyl, difluorophenyl, alkyloxy or alkylamino; and R.sub.4 is H or F, wherein the C.sub.1-4 alkanyl and alkyl radicals are linear or branched; stereoisomeric forms thereof or mixtures of these; and salts and hydrated forms thereof. These novel derivatives are useful as antimicrobials.
    • 本发明涉及通式(I)的新颖的1,8-苯并[b]萘啶衍生物,其中R是H或羟基,任选被氨基或羟基取代的氨基或烷基氨基,或R是 烷基部分可以与氮原子形成的二烷基氨基,其任选地含有选自氮,氧或硫的另外的杂原子的5-或6-元杂环,或R是C 3-6环烷基氨基或烷基氨基, 烷基N-烷基氨基或氨基烷基苯基氨基; R1和R2相同或不同,位于2和3位,代表H,烷基,C2-4烯基,苯基或取代苯基,或R1和R2位于2位,代表烷基; R3是H或烷基,氟代烷基,羧基烷基,C3-6环烷基,氟苯基,二氟苯基,烷氧基或烷基氨基; R4是H或F,其中C1-4烷基和烷基是直链或支链的; 其立体异构形式或它们的混合物; 及其盐和水合形式。 这些新型衍生物可用作抗微生物剂。