6,7,8,9-SUBSTITUTED 1-PHENYL-1,5-DIHYDRO-PYRIDO(3,2-B)INDOL-2-ONES USEFUL AS ANTI-INFECTIVE PHARMACEUTICAL AGENTS

6,7,8,9-SUBSTITUTED 1-PHENYL-1,5-DIHYDRO-PYRIDO(3,2-B)INDOL-2-ONES USEFUL AS ANTI-INFECTIVE PHARMACEUTICAL AGENTS

This invention concerns the compounds the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein X is NR2, O, S, SO, SO2; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methani...

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Hauptverfasser: RABOISSON, PIERRE JEAN-MARIE, BERNARD, PEETERS, ANNICK ANN, WIGERINCK, PIET, TOM, BERT, PAUL, SURLERAUX, DOMINIQUE, LOUIS, NESTOR, GHISLAIN, KESTELEYN, BART, RUDOLF, ROMANIE, VENDEVILLE, SANDRINE, MARIE, HELENE, KINDERMANS, NATALIE, MARIA, FRANCISCA
Format: Patent
Sprache:eng ; fre ; ger
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Zusammenfassung:This invention concerns the compounds the N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein X is NR2, O, S, SO, SO2; R1 is hydrogen, cyano, halo, substituted carbonyl, methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, Het1 or Het2; n is 1, 2 or 3; R2 is hydrogen, aryl substituted with a radical -COOR4; or R2 is substituted C1-10alkyl, C2-10alkenyl or C3-7cycloalkyl; or R2 is a radical of formula: -CpH2p-CH(OR14)-CqH2q-R15 (b-3); -CH2-CH2-(O-CH2-CH2)m-OR14 (b-4); -CH2-CH2-(O-CH2-CH2)m-NR5aR5b(b-5) -a1=a2-a3=a4- is -CH-CH-CH-CH-; -N-CH-CH-CH-; -CH-N-CH-CH-; -CH-CH-N-CH-; -CH-CH-CH-N- (c-5); wherein one of the hydrogen atoms in (c-1)-(c-5) is replaced by particular radicals; R3 is nitro, cyano, amino, halo, hydroxy, C1-4alkyloxy, hydroxycarbonyl, substituted carbonyl, methanimidamidyl, mono- or di(C1-4alkyl)methanimidamidyl, N-hydroxy-methanimidamidyl or Het1.