New benzo (f) (1,7) naphthyridine derivatives, are antibacterial agents effective against Gram-positive bacteria, useful as topical drugs, disinfectants or preservatives

摘要

1-Oxo-1,4-dihydrobenzo (f) (1,7) naphthyridine-2-carboxylic acid derivatives (I), substituted by one cyclic amino group and one or two halo groups, are new. Benzo-naphthyridine and aminoquinoline derivative intermediates (A) and (X) are also new. Benzo-naphthyridine derivatives of formula (I), their stereoisomers, stereoisomer mixtures, metal salts and addition salts with acids or nitrogen-containing bases, are new. R1-R3 = H, halo or -NR5R6, provided that one is -NR5R6 and at least one of the other two is halo; NR5R6 = 5-7 membered heterocycle, which optionally (a) has two C atoms linked to each other by a 1-2C bridge; (b) contains a second N, O or S heteroatom; and/or (c) is substituted by one or more of phenyl (itself optionally substituted by halo, alkyl, haloalkyl, alkoxy or benzyloxy), benzyl, alkyl, OH, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl or benzylaminoalkyl; R4 = alkyl, fluoroalkyl, carboxyalkyl, 3-6C cycloalkyl, fluorophenyl, difluorophenyl, alkoxy or alkylamino; where alkyl moieties have 1-4C. Independent claims are included for: (1) the preparation of (I); and (2) new benzo-naphthyridine and aminoquinoline derivative intermediates of formulae (A) and (X). R'1-R'3 = H or halo, provided that at least two are halo; R'4 = as R4 or protected alkylamino; R = H or R'; and R' = 1-4C alkyl.