Substituted indolepyridinium as anti-infective compounds

C - Chemistry – Metallurgy – 07 – D

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C07D 471/04 (2006.01) A61K 31/437 (2006.01) A61P 31/18 (2006.01)

Patent

CA 2506316

The present invention concerns the compounds of formula (1) (R3)n P(I) N O R1 R2 their N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites, wherein n is 1, 2 or 3; R1 is H, CN, halo, aminoC(=O), C(=O)OH, C1-4-alkyloxyC(=O), C1-4alkylC(='O), mono- or di(C1- 4alkyl)aminoC(=O), arylaminoC(=O), N-(aryl)-N-(C1-4alkyl)aminoC(=O), methanimidamidyl, N-hydroxy-methanimidamidyl, mono- or di(C1- 4alkyl)methanimidamidyl, Het1 or Het2; R2 is H, C1-10alkyl, C2-10allkenyl, C3- 7cycloalkyl, wherein said C1-10alkyl,C2-10alkenyl and C3-7cycloalkyl may be optionally substituted; R3 is nitro, cyano, amino, halo, hydroxy,C1-4alkyloxy, hydroxyC(=O), aminoC(=O), C1-4alkyloxyC(=O), mono- or di(C1-4- alkyl)aminoC(=O), C1-4alkylC(=O), methanimidamidyl, mono- or di(C1- 4alkyl)methanimidamidyl, N-hydroxy methanimidamidyl or Het1; for use as a medicine. The invention further relates to a novel subgroup of the compounds of formula (I), and to compositions comprising compounds of formula (I).

La présente invention concerne les composés représentés par la formule (I) (1) (R¿3?)¿n ?P(I) N O R¿1 ?R¿2 ?les <i>N</i>-oxydes, sels, formes stéréo-isomères, mélanges racémiques, promédicaments, esters et métabolites de ceux-ci. Dans cette formule n est 1, 2 ou 3; R¿1? est H, CN, halo, aminoC(=O), C(=O)OH, C¿1-4-?alkyloxyC(=O), C¿1-4?alkylC(= O), mono- ou di(C¿1-4?alkyl)aminoC(=O), arylaminoC(=O), <i>N</i>-(aryl)-<i>N-</i>(C¿1-4?alkyl)aminoC(=O), méthanimidamidyle, <i>N</i>-hydroxy-méthanimidamidyle, mono- ou di(C¿1-4?alkyl)méthanimidamidyle, Het¿1? ou Het¿2?; R¿2? est H, C¿1-10?alkyle, C¿2-10?allkényle, C¿3-7?cycloalkyle, ces groupes C¿1-10?alkyle,C¿2-10?alkényle et C¿3-7?cycloalkyle pouvant éventuellement être substitués; R¿3? est nitro, cyano, amino, halo, hydroxy,C¿1-4?alkyloxy, hydroxyC(=O), aminoC(=O), C¿1-4?alkyloxyC(=O), mono- ou di(C¿1-4?-alkyl)aminoC(=O), C¿1-4?alkylC(=O), méthanimidamidyle, mono- ou di(C¿1-4?alkyl)méthanimidamidyle, <i>N</i>-hydroxy méthanimidamidyle ou Het¿1?; ces composés sont à usage médicinal. Cette invention concerne aussi un nouveau sous groupe de composés représentés par la formule (I) et des compositions comprenant les composés de la formule (I).

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