Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-06-28
1997-04-29
Haley, Jacqueline
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514414, 514423, 546164, 546169, 548510, 548540, A61K 3140, C07D20716
Patent
active
056249390
DESCRIPTION:
BRIEF SUMMARY
This application is a National Stage application of PCT/FR94/00008, filed Jan. 3, 1994, and published on Jul. 21, 1994, as WO 94/15914.
The present invention relates to derivatives of formula: ##STR2## to their salts, to their preparation and to the medicaments containing them.
In the formula (I),
R represents a hydrogen atom or an alkyl, cycloalkyl or phenylalkyl radical or a phenyl radical optionally substituted by one or more substituents chosen from halogen atoms and alkyl and alkoxy radicals,
R.sub.1 represents an alkyl radical containing 1 to 12 carbon atoms in a straight or branched chain and optionally mono- or polyunsaturated, a cycloalkyl radical containing 3 to 12 carbon atoms and optionally mono- or polyunsaturated, a polycycloalkyl radical containing 6 to 12 carbon atoms and optionally mono- or polyunsaturated, a phenylalkyl radical in which the phenyl ring is optionally substituted (by one or more substituents chosen from alkyl or alkoxy radicals or halogen atoms), a diphenylalkyl radical, a cinnamyl radical, a pyridyl radical optionally substituted by one or more alkyl radicals, a furyl radical optionally substituted by one or more alkyl radicals, a thienyl radical optionally substituted by one or more alkyl radicals, a quinolyl radical optionally substituted by one or more alkyl radicals, a naphthyl radical optionally substituted by one or more alkyl radicals, an indolyl radical optionally substituted by one or more alkyl radicals or a phenyl radical optionally substituted by one or more 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,
R.sub.2 represents a --(CH.sub.2).sub.n --CO--R.sub.6, --(CH.sub.2).sub.m --O--CO--R".sub.6 or --(CH.sub.2).sub.m --NR.sub.9 R.sub.10 chain, an oxazolinyl radical optionally substituted by one or more alkyl radicals or a 3-alkyloxadiazolyl radical,
R.sub.3 represents a hydrogen atom or an alkyl or cycloalkyl radical or a phenylalkyl radical optionally substituted by one or more substituents chosen from halogen atoms and alkyl and alkoxy radicals,
R.sub.4 represents a hydrogen atom or an alkyl radical, R.sub.5 represents a phenyl radical (optionally substituted by one or more 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 more 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, --CO--COOX, --alk--SO.sub.3 H (in salt form), --CH.dbd.CH--alk', --C(.dbd.NOH)--COOX, --S--alk--COOX, --SO--alk--COOX, --SO.sub.2 --alk--COOX, --O--CH.sub.2 --alk'--COOX, --CX.dbd.N--O--alk--COOX, --alk--N(OH)--CO--alk, --alk--SO.sub.2 H, --SO.sub.2 --NH--CO--R.sub.11, --SO.sub.2 --NH--SO.sub.2 --R.sub.11, --CO--NH--CO--R.sub.11, --CO--NH--SO.sub.2 --R.sub.11, --B(OH).sub.2, --C(NH.sub.2).dbd.NOH, --SO.sub.2 --NH--R.sub.12, --CO--NH--R.sub.12, ##STR3## or 2,2-dimethyl-4,6-dioxo-1,3-dioxan-5-yl radicals,
R.sub.6 represents a hydroxyl, alkoxy, cycloalkyloxy, cycloalkylalkyloxy, phenyl or --NR.sub.9 R.sub.10 radical,
R".sub.6 represents an alkoxy, cycloalkyloxy, cycloalkylalkyloxy, phenyl or --NR.sub.9 R.sub.10 radical,
R.sub.7 represents a hydrogen atom or an alkyl radical, a phenylalkyl radical or a phenyl radical optionally substituted by one or more substituents chosen from halogen atoms and alkyl, alkoxy and alkylthio radicals,
R.sub.8 represents an alkyl radical, a phenylalkyl radical or a phenyl radical optionally substituted by one or mor
REFERENCES:
patent: 4596789 (1986-06-01), Dutta et al.
patent: 4691007 (1987-09-01), Dutta et al.
Tetrahedron Letters, vol. 34, No. 3, 1993, Oxford GB, pp. 381-384, V. Maggard et al., "A Convenient Synthesis of the Conformality . . . "
Tetrahedron Letters, vol. 34, No. 10, 1993, Oxford GB, pp. 1665-1668, J. E. Baldwin et al., "Synthesis of a Bicyclic Gamma-Lactam . . . "
Capet Marc
Dubroeucq Marie-Christine
Haley Jacqueline
Rhone-Poulenc Rorer S.A.
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