| abstract |
The invention relates to N-substituted hetero-cyclic derivatives. These derivatives have the formula (see fig.I) in which: R1 and R2 are similar or different and are each independently hydrogen or a group selected from a C1-C6 alkyl, a C1-C4 alkoxy, an amino, an aminomethyl, a carboxyl, an alkoxycarbonyl in which the alkoxy is C1-C4, a cyano, a tetrazolyl, a methyltetrazolyl, a methylsulfonylamino, a trifluoromethylsulfonylamino, a trifluoromethylsulfonylaminomethyl, an N-cyano-acetamide, an N-hydroxyacetamide, an N-4-carboxy-1,3-thiazol-2-yl)acetamide, a ureido, a 2-cyano-guanidinocarbonyl, a 2-cyanoguanidinomethyl, an imidazol-1-ylcarbonyl and a 3-cyano-2-methylisothio-ureidomethyl, with the proviso that at least one of the substituents R1 or R2 is other than hydrogen; R3 is a hydrogen, a C1-C6 alkyl which is unsubstituted or substituted by one or more halogen atoms, a C2-C6 alkenyl, a C3-C7 cycloalkyl, a phenyl, a phenylalkyl in which the alkyl is C1-C3, or a phenylalkenyl in which the alkenyl is C2-C3, said phenyl groups being unsubstituted or monosubstituted or polysubstituted by a halogen atom, a C1-C4 alkyl, a C1-C4 halogenoalkyl, a C1-C4 polyhalogenoalkyl, a hydroxyl or a C1-C4 alkoxy; R4 and R5 are each independently a C1-C6 alkyl, a phenyl or a phenylalkyl in which the alkyl is C1-C3, said alkyl, phenyl and phenylalkyl groups being unsubstituted or substituted by one or more halogen atoms or by a group selected from a C1-C4 perfluoroalkyl, a hydroxyl and a C1-C4 alkoxy; or R4 and R5 together form a group of the formula =CR7R8, in which R7 is hydrogen, a C1-C4 alkyl or a phenyl and R8 is a C1-C4 alkyl or a phenyl; or else R4 and R5 together are either a group of the formula (CH2)n or a group of the formula (CH2)pY (CH2)q, in which Y is either an oxygen-atom, or a sulfur atom, or a carbon atom substituted by a C1-C4 alkyl group, a phenyl or a phenylalkyl in which the alkyl is C1-C3, or a group N-R6, in which R6 is a hydrogen, a C1-C4 alkyl, a phenylalkyl in which the alkyl is C1-C3, a C1-C4 alkylcarbonyl, a C1-C4 halogenoalkylcarbonyl, a C1-C4 polyhalogenoalkylcarbonyl, a benzoyl, an alpha-aminoacyl or an N-protecting group, or R4 and R5, together with the carbon atom to which they are bonded, form an indane or an adamantane; - p + q = m; - n is an integer between 2 and 11; - m is an integer between 2 and 5; - X is an oxygen atom or sulfur atom; and - z and t are zero or one is zero and the other is one; and its salts (sic). |