Patent ES-8307497-A1 (ES)
Title: Pharmaceutical compositions having normolipemic properties and containing compounds of the n-substituted benzenesulfonamide type.
IPC: A61K31/18
Filed: 1982-12-02
Abstract: 1. Claims (for the Contracting States : BE, CH, DE, GB, IT, LI, LU, NL, SE) Medicament possessing lipid-regulating properties, characterized by the fact that it contains, as active substance, if necessary in the state of a physiologically acceptable salt, and if necessary, in association with a pharmaceutical vehicle, a compound of the formula : see diagramm : EP0081425,P37,F1 in which : R1 , R2 represent each independently of one another : - a hydrogen atom - a linear or branched lower alkyl radical having from 1 to 4 carbon atoms - a cycloalkyl radical comprising from 3 to 6 carbon atoms - an aryl radical, unsubstituted or substituted by a nitro, amino, trifluoromethyl group or halogen atom or by a linear or branched lower alkyl residue having from 1 to 4 carbon atoms, by an alkoxy residue having from 1 to 4 carbon atoms, particularly methoxy, by an alkylsulfonyl group -SO2 R in which R is an alkyl residue having from 1 to 4 carbon atoms, by a sulfamyl group -SO2 NR'R" in which R' and R" represent, independently of one another, a hydrogen atom or an alkyl residue having from 1 to 4 carbon atoms R3 , R4 , R5 and R6 represent, independently of one another : - a hydrogen atom - a nitro group, an amino group, trifluoromethyl group or a halogen - a linear or branched lower alkyl residue having from 1 to 4 carbon atoms, an alkoxy residue having from 1 to 4 carbon atoms, an alkylsulfonyl group -SO2 R in which is an alkyl residue having from 1 to 4 carbon atoms, a sulfamyl group -SO2 NR'R" in which R' and R" represent, independently of one another, a hydrogen atom or an alkyl residue having from 1 to 4 carbon atoms provided that when one at least of the substituents R3 to R6 represents a NH2 group at the para position or a CH3 group at the para position, one at least of the other substituents of the aromatic nucleus is different from hydrogen R7 , R8 and R9 represent, independently of one another : - a hydrogen atom - an alkyl radical having 1 to 6 carbon atoms - a cycloalkyl radical comprising from 3 to 6 carbon atoms - an aralkyl radical, particularly phenylalkyl or naphthylalkyl, in which the alkyl radical has from 1 to 4 carbon atoms, unsubstituted or substituted by a nitro group, an amino group, a trifluoromethyl group, or halogen atom or by a linear or branched lower alkyl residue, by an alkoxy residue having from 1 to 4 carbon atoms, particularly methoxy, by an alkylsulfonyl group, -SO2 R2 in which R is an alkyl residue having from 1 to 4 carbon atoms, by a sulfamyl group -SO NR'R" in which R' and R" represent, independently of one another, a hydrogen atom or an alkyl residue having from 1 to 4 carbon atoms R10 represents : - a hydrogen atom - an acyl group comprising from 1 to 12 carbon atoms - n and m vary, independently of one another, from 0 to 10, preferably form 0 to 5, provided that the sum n + m does not exceed 12, preferably does not exceed 5. 1. Claims (for the Contracting State AT) Process for preparing a compound of formula : see diagramm : EP0081425,P39,F2 in which : R1 , R2 each represent independently of one another : - a hydrogen atom - a linear or branched lower alkyl radical having from 1 to 4 carbon atoms - a cycloalkyl radical comprising from 3 to 6 carbon atoms - an aryl radical, unsubstituted or substituted by a nitro group, an amino group, a trifluoromethyl group, a halogen atom or by a linear or branched lower alkyl residue having from 1 to 4 carbon atoms, by an alkoxy residue having from 1 to 4 carbon atoms, particularly methoxy, by an alkylsulfonyl group -SO2 R in which R is an alkyl residue having from 1 to 4 carbon atoms, by a sulfamoyl group -SO2 NR'R" in which R' and R" represent, independently of one another, a hydrogen atom or an alkyl residue having from 1 to 4 carbon atoms R3 , R4 , R5 and R6 represent, independently of one another : - a hydrogen atom - a nitro, amino, trifluoromethyl group or a halogen - a linear or branched lower alkyl residue having from 1 to 4 carbon atoms, an alkoxy residue having from 1 to 4 carbon atoms, an alkylsulfonyl -SO2 R group in which R is an alkyl residue having from 1 to 4 carbon atoms, a sulfamoyl -SO2 NR'R" group in which R' and R" represent, independently of one another, a hydrogen atom or an alkyl residue having from 1 to 4 carbon atoms provided that one at least of the substituents R3 to R6 is different from hydrogen and provided that when one at least of the substituents R3 to R6 represents a NH2 group at the para position or a CH3 group at the para position, one at least of the other substituents of the aromatic nucleus is different from hydrogen R7 , R8 and R9 represent, independently of one another : - a hydrogen atom - an alkyl radical having from 1 to 6 carbon atoms - a cycloalkyl radical comprising from 3 to 6 carbon atoms - an aralkyl radical, particularly phenylalkyl or naphthylalkyl, in which the alkyl radical has from 1 to 4 carbon atoms, unsubstituted or substituted by a nitro, amino, trifluoromethyl, or a halogen or by a linear or branched lower alkyl residue having from 1 to 4 carbon atoms, by an alkoxy residue having from 1 to 4 carbon atoms, particularly methoxy, by an alkylsulfonyl -SO2 R2 group in which R is an alkyl residue having from 1 to 4 carbon atoms, by a sulfamoyl -SO2 NR'R" group in which R' and R" represent, independently of one another, a hydrogen atom or an alkyl residue having from 1 to 4 carbon atoms R10 represents : - a hydrogen atom - an acyl group comprising from 1 to 12 carbon atoms n and m vary, independently of one another, from 0 to 10, preferably from 0 to 5, provided that the sum n + m does not exceed 12, preferably does not exceed 5 characterized by the fact a sulfohalogenide of formula : see diagramm : EP0081425,P40,F1 in which : X is a halogen group, particularly bromine of preferably chlorine A1 , A2 , A3 , A4 have any one of the meanings given for R3 , R4 , R5 and R6 , except NH2 is reacted on an amine of formula : see diagramm : EP0081425,P40,F2 in which : n and m have the above indicated meanings R1 , R2 , R7 , R8 , R9 and R10 have the above indicated meanings.