申请人:Laboratoire Roger Bellon
公开号:US05556861A1
公开(公告)日:1996-09-17
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.
这项发明涉及一种新型1,8-
苯并[b]
萘啉衍
生物,其通式为(I),其中R为H或一个羟基、
氨基或烷基
氨基基团,该基团可选择通过
氨基或羟基进行取代,或R为二烷基
氨基,其中烷基部分可以与
氮原子形成一个含有
氮、
氧或
硫的5-或6-成员杂环环,或R为C.sub.3-6
环烷基
氨基或烷基
氨基,N-烷基N-烷基烷
氨基或
氨基烷基
苯氨基基团;R.sub.1和R.sub.2在2和3位置,代表H、烷基、C.sub.2-4
烯基、
苯基或取代
苯基,或R.sub.1和R.sub.2在2位置,代表烷基;R.sub.3为H或烷基、
氟烷基、羧基烷基、C.sub.3-6
环烷基、
氟苯基、二
氟苯基、烷
氧基或烷基
氨基;R.sub.4为H或F,其中C.sub.1-4烷基和烷基基团为直链或支链;其立体异构体形式或这些形式的混合物;以及其盐和
水合形式。这些新型衍
生物可用作抗微
生物药物。