Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-11-26
1999-08-10
Jordan, Kimberly
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514317, 514323, 514324, 514326, 514422, 514424, 514429, 514811, A61K 31445, A61K 31425, A61K 3140
Patent
active
059359803
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to the use of derivatives of formula: ##STR2## their racemates and enantiomers, when they contain one or a number of asymmetric centres, and their salts in the treatment of chronic alcoholism or of conditions due to alcohol abuse and to the application of these derivatives in the preparation of medicaments intended for the treatment of chronic alcoholism or of conditions due to alcohol abuse.
In the formula (I),
either R represents a methylene, ethylene, SO, SO.sub.2, or CHOH radical or a sulphur atom, R.sub.1 represents a pyridyl radical which is optionally substituted by one or a number of alkyl radicals, a furyl radical which is optionally substituted by one or a number of alkyl radicals, a thienyl radical which is optionally substituted by one or a number of alkyl radicals, a quinolyl radical which is optionally substituted by one or a number of alkyl radicals, a naphthyl radical which is optionally substituted by one or a number of alkyl radicals, an indolyl radical which is optionally substituted by one or a number of alkyl radicals or a phenyl radical which is optionally substituted by one or a number of 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 or trifluoromethoxy radicals and R.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, --CONR.sub.9 R.sub.10 or phenyl radical which is optionally substituted by one or a number of substituents chosen from alkyl, alkoxy or hydroxyl radicals,
R.sub.3 represents a phenyl radical (optionally substituted by one or a number of substituents chosen from halogen atoms and alkyl, alkoxy and alkylthio radicals), a naphthyl radical, an indolyl radical, a quinolyl radical or a phenylamino radical in which the phenyl ring is optionally substituted by one or a number of substituents chosen from halogen atoms and alkyl, alkoxy, alkylthio, trifluoromethyl, carboxyl, alkoxycarbonyl, hydroxyl, nitro, amino, acyl, cyano, sulphamoyl, carbamoyl, hydroxyiminoalkyl, alkoxyiminoalkyl, hydroxyaminocarbonyl, alkoxyaminocarbonyl, tetrazol-5-yl, tetrazol-5-ylalkyl, trifluoromethylsulphonamido, alkylsulphinyl, mono- or polyhydroxyalkyl, sulpho, -alk-O--CO-alk, -alk-COOX, -alk-O-alk, -alk'-COOX, --O-alk-COOX, --CH=CH--COOX, --CO--COOX, -alk-SO.sub.3 H in the salt form, --CH=CH-alk', --C(=NOH)--COOX, --S-alk-COOX, --O--CH.sub.2 -alk'-COOX, --CX=N--O-alk-COOX, -alk-N(OH)--CO-alk or 2,2-dimethyl-4,6-dioxo-1,3-dioxan-5-yl radicals,
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, phenylalkyl or phenyl radical which is optionally substituted by one or a number of substituents chosen from halogen atoms and alkyl, alkoxy and alkylthio radicals,
R.sub.8 represents an alkyl, phenylalkyl or phenyl radical which is optionally substituted by one or a number of substituents chosen from halogen atoms and alkyl, alkoxy and alkylthio radicals, or else R.sub.7 and R.sub.8 form, with the nitrogen atom to which they are attached, a saturated or unsaturated, mono- or polycyclic heterocycle containing 4 to 9 carbon atoms and one or a number of heteroatoms (O, N) and which is optionally substituted by one or a number of alkyl radicals,
R.sub.9 represents a hydrogen atom or an alkyl, cycloalkylalkyl, cycloalkyl, phenylalkyl or phenyl radical which is optionally substituted by one or a number of substituents chosen from halogen atoms and alkyl, alkoxy and alkylthio radicals,
R.sub.10 represents an alkyl, cycloalkylalkyl, cycloalkyl, phenylalkyl or phenyl radical which is optionally substituted by one or a number of substituents chosen from halogen atoms and alkyl, alkoxy and al
REFERENCES:
patent: 5451582 (1995-09-01), Chambers et al.
Derwent Abstract of WO 9415915, (1994).
Derwent Abstract of WO 9301167, (1993).
Jordan Kimberly
Rhone-Poulenc Rorer S.A.
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