Laboratoire Roger Bellon

Aventis Pharma S.a.

Rhone-poulenc Sante

Guy Picaut

Philippe Girard

Michel Barreau

Jean-Francois Desconclois

Michel Antoine

Michel Tabart

Sylvie Wentzler

Michel Kryvenko

Jean-Fran&ccedil;ois Desconclois

Jean-Luc Malleron

Arielle Genevois-Borella

Jean-Marc Paris

Eric Bacque

Marc Pierre Lavergne

Marc P Lavergne

Benzo&lsqb;f&rsqb;naphthyridine derivatives, their preparation and compositions containing them

Benzo&lsqb;1,8&rsqb;naphthyridine derivatives, their preparation and pharmaceutical compositions which comprise them

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.

1,8 benzonaphthyridine derivatives and antimicrobial compositions

New benzo[b][1,8]naphthyridine derivatives of general formula (I), in which R.sub.1 is a hydrogen atom or a hydroxyl or alkyl radical, R.sub.2 is a hydrogen atom or an alkyl, fluoroalkyl, cycloalkyl (3 to 6 C), alkyloxy or alkylamino radical, R.sub.3 is a phenyl or phenylalkyl radical substituted with one or more halogen atoms or alkyl, cycloalkyl (3 to 6 C), alkyloxy, cyano, amino, alkylamino, dialkylamino, alkyloxyalkyl, hydroxyalkyl, hydroxyalkyloxy, methylenedioxy, aminoalkyl, alkylaminoalkyl or dialkylaminoalkyl radicals, or R.sub.3 is a heterocyclic radical, and R.sub.4 is a hydrogen atom or a fluorine atom, the alkyl radicals (1 to 4 C) being linear or branched, their salts, their preparation and compositions containing them. These new products are useful as antimicrobials, or in the treatment of AIDS. ##STR1##

Benzo[1,8]naphthyridine derivatives, their preparation and compositions

New benzo[b][1,8]naphthyridine derivatives of general formula (I) in which R.sub.1 is a hydrogen atom or an alkyl or hydroxyalkyl radical, R.sub.2 is a hydrogen atom or an alkyl, fluoroalkyl, cycloalkyl (3 to 6 C), alkoxy or alkylamino radical and R.sub.3 is alkyl, R.sub.4 and R.sub.5 are different and are hydrogen or alkyl, or R.sub.3 is H, alkyl or cycloalkyl and R.sub.4 and R.sub.5 are hydrogen, R.sub.6 is hydrogen or fluorine and n is equal to 1 or 2, their salts, their preparation and the compositions which contain them. These new products are used as antimicrobial agents ##STR1##

Benzo[1,8]naphthyridine derivatives, their preparation and the

New benzo[b][1,8]naphthyridine derivatives of general formula (I), in which R is a hydrogen atom or an alkyl, fluoroalkyl, cycloalkyl (3 to 6 C), alkoxy or alkylamino radical or an amine protective radical and either Hal is a fluorine, chlorine or bromine atom and R' is a hydrogen atom or Hal and R' are simultaneously fluorine atoms, their salts, their preparation and the compositions which contain them. These new products can be used as antimicrobial agents for topical application or as synthesis intermediates. ##STR1##

Benzo[1,8]naphthyridine derivatives as antimicrobials

New benzo[b][1,8]naphthyridine derivatives of general formula (I) in which R is a hydrogen atom or an alkyl, fluoroalkyl, cycloalkyl (3 to 6 C), alkoxy, alkylamino or protected alkylamino radical, Hal is F, Cl or Br if R' is hydrogen, or Hal and R' are F, and Alk is an alkyl radical, and their preparation. These new products can be used as intermediates for the preparation of biologically active products. ##STR1##

Benzo(1,8)naphthyridine derivatives as intermediates

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Villejuif, France

Guy Picaut