Patent ID: 6518260
Filing Date: 2003-02-11
Classification: A61P,C07F

Abstract:
Compound of formula (I) in whichR1 and R2 each represent a hydrogen atom R3 representsan alkyl group or an alkenyl group of 1 to 6 carbon atoms, it being possible for these last two groups to be substituted with: a hydroxyl group or an alkoxy group â€”OR9, a phenyl group or a benzyl group, a sulphanyl group, an alkylsulphanyl group â€”SR9 or an alkylsulphanyl group oxidized on the sulphur atom â€”S(O)R9, an amino group, a group â€”NHR9 or â€”NR9R10, optionally oxidized on the nitrogen atom, or a guanidino group H2Nâ€”C(&boxH;NH)â€”NHâ€”, a cycloalkyl or cycloalkylmethyl group, a phenyl group, a benzyl group, which can be substituted on the phenyl group with 1 or 2 of the following substituents: a halogen atom, a hydroxyl group, an alkoxy group â€”OR9, an alkylsulphanyl group â€”SR9 or an alkylsulphanyl group oxidized on the sulphur atom, an amino group or a group â€”NHR9 or â€”NR9R10 optionally oxidized on the nitrogen atom, a nitro group, a phenyl group, an alkyl group of 1 to 4 carbon atoms, R4 representsa hydrogen atom, an alkyl or alkenyl group of 1 to 6 carbon atoms, a cycloalkyl group, a cycloalkylalkyl group, a phenyl group, a benzyl group, which can be substituted on the phenyl group with 1 or 2 of the following substituents: an alkyl group of 1 to 6 carbon atoms, a halogen atom, a hydroxyl group or an alkoxy group â€”OR9, a trifluoromethyl group, a nitro group, R5 representsa hydrogen atom, an alkyl group or an alkenyl group of 1 to 6 carbon atoms, it being possible for these last two groups to be substituted with: a hydroxyl group or an alkoxy group â€”OR9, a phenyl group or a benzyl group, a sulphanyl group, an alkylsulphanyl group â€”SR9, or an alkylsulphanyl group oxidized on the sulphur atom â€”S(O)R9, an amino group, a group â€”NHR9R10, optionally oxidized on the nitrogen atom, or a guanidine group H2Nâ€”C(&boxH;NH)â€”NHâ€”, a cycloalkyl or cycloalkylmethyl group, a phenyl group, a benzyl group, which can be substituted on the phenyl group with 1 or 2 of the following substituents: a halogen atom, a hydroxyl group, an alkoxy group â€”OR9, an alkylsulphanyl group â€”SR9, or an alkylsulphanyl group oxidized on the sulphur atom, an amino group or a group â€”NHR9 or â€”NR9R10 optionally oxidized on the nitrogen atom, a nitro group, a phenyl group, an alkyl group of 1 to 4 carbon atoms, a methyl group substituted with a heterocyclic group, it being possible for the hetero atoms to be oxidized in the form of N-oxide or S-oxide, R6 and R7 represent, independently of each other, a hydrogen atom, an alkyl or alkenyl group of 1 to 6 carbon atoms, which can be substituted with: a hydroxyl group or an alkoxy group â€”OR9, a sulphanyl group, an alkylsulphanyl group â€”SR9 or an alkylsulphanyl group oxidized on the sulphur atom â€”S(O)R9, an amino group or an alkylamino group â€”NHR9, a guanidine Group H2Nâ€”C(&boxH;NH)â€”NHâ€”, or a carboxyl group or an alkyloxycarbonyl group â€”COOR9 a phenyl group, a benzyl group, which can be substituted on the phenyl group by 1 or 2 of the following substituents: a halogen atom, a phenyl group, a hydroxyl group or an alkoxy group â€”OR9, an alkylsulphanyl group â€”SR9 or an alkylsulphanyl group oxidized on the sulphur atom â€”S(O)R9, R6 and R7 together represent a saturated or unsaturated 5- or 6-membered ring comprising 1 or 2 hetero atoms, taken form among oxygen, sulphur and nitrogen, R8 represents, a hydrogen atom, an alkyl or alkenyl group of 1 to 6 carbon atoms, a phenyl group, a benzyl group, R9 represents an alkyl group of 1 to 6 carbon atoms, n is equal to 0 or 1, with the exception of methyl N-[2-[[(aminomethyl)(methoxy)phosphinyl]methyl]-4-methyl-1-oxopentyl]-(1,1â€²-biphenyl-4-yl)-L-alaninate hydrochloride,in the form of isomers, including the form of enantiomers and diastereoisomers and mixtures of these different forms, including racemic mixtures, as well as the addition salts thereof with pharmacologically acceptable acids.