C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
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).
Bettens Eva
Canard Maxime Francis Jean-Marie Ghislain
de Vroey Veronique Corine Paul
Hertogs Kurt
Jochmans Dirk Edward Desire
Gowling Lafleur Henderson Llp
Tibotec Pharmaceuticals Ltd.
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