Patent ID: 6150387
Filing Date: 2000-11-21
Classification: A61K,A61P

Abstract:
A method of preventing or reducing self-administration, by a human or animal patient, of a drug or a substance capable of giving rise to pharmacomania or to overuse, said method comprising administering to the patient in need of such preventing or reducing an effective amount of a compound of formula I: ##STR2## in which R represents a methylene, ethylene, SO, SO.sub.2 or CHOH radical or a sulphur atom, R.sub.1 represents a pyridyl radical optionally substituted with one or more identical or different alkyl radicals, a furyl radical optionally substituted with one or more identical or different alkyl radicals, a thienyl radical optionally substituted with one or more identical or different alkyl radicals, a quinolyl radical optionally substituted with one or more identical or different alkyl radicals, a naphthyl radical optionally substituted with one or more identical or different alkyl radicals, an indolyl radical optionally substituted with one or more identical or different alkyl radicals, or a phenyl radical optionally substituted with one or more identical or different substituents chosen from halogen atoms and alkyl, alkoxy, hydroxyl, nitro, amino, monoalkylamino, dialkylamino, alkoxycarbonyl, --CO--NR.sub.7 R.sub.8, --NH--CO--CH.sub.3, trifluoromethyl and trifluoromethoxy radicals, andR.sub.5 represents a hydrogen atom,or R represents a methylene radical, R.sub.1 represents a hydrogen atom and R.sub.5 represents a phenyl radical,or R represents a CHR.sub.6 radical and R.sub.1 and R.sub.5 each represent a hydrogen atom;R.sub.2 represents an alkoxycarbonyl, cycloalkyloxycarbonyl, cycloalkylalkyloxycarbonyl or --CONR.sub.9 R.sub.10 radical or a phenyl radical optionally substituted with one or more identical or different substituents chosen from alkyl, alkoxy, and hydroxyl radicals;R.sub.3 represents a phenyl radical optionally substituted with one or more identical or different substituents chosen from halogen atoms and alkyl, alkoxy and alkylthio radicals, or R.sub.3 represents a naphthyl, indolyl or quinolyl radical or a phenylamino radical, the phenyl ring of said phenylamino radical being optionally substituted by one or more identical or different substituents chosen from halogen atoms and alkyl, alkoxy, alkylthio, trifluoromethyl, carboxyl, alkoxycarbonyl, hydroxyl, nitro, amino, acyl, cyano, sulphamoyl, carbamoyl, hydroxyiminoalkyl, alkoxyiminoalkyl, hydroxyaminocarbonyl, alkoxyaminocarbonyl, 5-tetrazolyl, 5-tetrazolylalkyl, trifluoromethylsulphonamido, alkylsulphinyl, mono- or polyhydroxyalkyl, sulpho, -alk-O--CO-alk, -alk-COOX, -alk-O-alk, -alk'-COOX, --O-alk-COOX, --CH.dbd.CH--COOX and --CO--COOX radicals, or R.sub.3 represents an -alk-SO.sub.3 H radical in salt form or a --CH.dbd.CH-alk', --C(.dbd.NOH)--COOX, --S-alk-COOX, --O--CH.sub.2 -alk'-COOX, --CX.dbd.N--O-alk-COOX, -alk-N(OH)--CO-alk, or 2,2-dimethyl-4,6-dioxo-1,3-dioxan-5-yl radical;R.sub.4 represents a hydrogen atom or an alkyl radical;R.sub.6 represents a phenyl radical;R.sub.7 represents a hydrogen atom or an alkyl or phenylalkyl radical or a phenyl radical optionally substituted with one or more identical or different substituents chosen from halogen atoms and alkyl, alkoxy, and alkylthio radicals;R.sub.8 represents an alkyl or phenylalkyl radical or a phenyl radical optionally substituted with one or more identical or different substituents which are halogen atoms, alkyl, alkoxy or alkylthio radicals,or R.sub.7 and R.sub.8, with the nitrogen atom to which they are attached, form a saturated or unsaturated, mono- or polycyclic heterocycle containing 4 to 9 carbon atoms and one or more identical or different hetero atoms chosen from oxygen and nitrogen, and optionally substituted with one or more identical or different alkyl radicals;R.sub.9 represents a hydrogen atom or an alkyl, cycloalkylalkyl, cycloalkyl or phenylalkyl radical or a phenyl radical optionally substituted with one or more identical or different substituents chosen from halogen atoms and alkyl, alkoxy and alkylthio radicals;R.sub.10 represents an alkyl, cycloalkylalkyl, cycloalkyl or phenylalkyl radical or a phenyl radical optionally substituted with one or more identical or different substituents chosen from halogen atoms and alkyl, alkoxy and alkylthio radicals,or R.sub.9 and R.sub.10, together with the nitrogen atom to which they are attached, form a saturated or unsaturated, mono- or polycyclic heterocycle containing 4 to 9 carbon atoms and one or more identical or different hetero atoms chosen from oxygen, nitrogen, and sulfur, and are optionally substituted with one or more identical or different alkyl radicals;X represents a hydrogen atom or an alkyl or phenylalkyl radical;alk represents an alkyl or alkylene radical;alk' represents a hydroxyalkyl, hydroxyalkylene, alkoxyalkyl or alkoxyalkylene radical;wherein the alkyl, alkylene and alkoxy radicals or portions of radicals contain 1 to 4 carbon atoms in an unbranched or branched chain;wherein the acyl radicals contain 2 to 4 carbon atoms;wherein the cycloalkyl radicals contain 3 to 6 carbon atoms; andwherein said drug or substance capable of giving rise to pharmacomania or to overuse is not alcohol;or a racemate or enantiomer of said compound of Formula I when said compound of Formula I contains one or more asymmetric centers;or a pharmaceutically acceptable salt of a compound of Formula I, or of a racemate or enantiomer thereof.