Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1998-05-20
2000-07-11
Higel, Floyd D.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
514396, 514397, 514398, 514399, 514400, 5482191, 548320, 5483205, 5483211, C07D23376, C07D23372, C07D23378, C07D23502, C07D40512, A61K 314166, A61N 528, A61N 1710
Patent
active
060875097
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 PCT/FR96/01846 filed Nov. 21, 1996.
The present invention relates to new fluorinated or hydroxylated phenylimidazolidines, their preparation process, the new intermediates obtained, their use as medicaments, their new use and the pharmaceutical compositions containing them.
A subject of the present invention is the products of formula (I): ##STR2## in which: R.sub.1 and R.sub.2, identical or different, are chosen from cyano, nitro, trifluoromethyl radicals and halogen atoms, alkynyl radical containing at most 10 carbon atoms and optionally substituted by one or more radicals chosen from halogen atoms and cyano, hydroxyl, alkoxy, carboxy, acyl and acyloxy radicals, in which, if appropriate, the alkyl, alkoxy and acyl radicals are linear or branched, containing at most 10 carbon atoms, the carboxy radical is free, salified, esterified or amidified and the hydroxy radical is free, esterified, etherified or protected, alkyl radical containing at most 4 carbon atoms and optionally substituted by a halogen atom, or form with the carbon atom to which they are linked a cyclic radical constituted by 3 to 7 members and optionally containing one or more identical or different heteroatoms, chosen from oxygen, sulphur or nitrogen atoms, enantiomeric and diastereoisomeric isomer forms, as well as the addition salts with mineral and organic acids or with mineral and organic bases of said products of formula (I).
In the products of formula (I) and in what follows:
The fluorine, chlorine or bromine atoms are preferred. radicals: methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, isopentyl, hexyl, isohexyl and also heptyl, octyl, nonyl and decyl, as well as their linear or branched position isomers,
Alkyl radicals having at most 6 carbon atoms are preferred and in particular the methyl, ethyl, propyl, isopropyl, n-butyl, n-pentyl and n-hexyl radicals. 1-propenyl, butenyl, 1-butenyl, pentenyl or hexenyl radicals as well as their linear or branched position isomers.
Among the alkenyl radicals, the vinyl, allyl, n-butenyl or isobutenyl values are preferred. carbon atoms such as for example ethynyl, propargyl, butynyl, pentynyl or hexynyl.
Among the alkynyl radicals, those with 4 carbon atoms are preferred and in particular the propargyl radical. propoxy, isopropoxy, Linear, secondary or tertiary butoxy, pentoxy or hexoxy radicals as well as their linear or branched position isomers. containing one or more identical or different heteroatoms, chosen from oxygen, sulphur or nitrogen atoms, designates on the one hand a cycloalkyl radical which itself designates in particular the cyclobutyl, cyclopentyl and cyclohexyl radicals and on the other hand a carbocyclic radical interrupted by one or more heteroatoms chosen from oxygen, nitrogen or sulphur atoms such as quite particularly the saturated monocyclic heterocyclic radicals such as for example the following radicals: oxetannyl, oxolannyl, dioxanyl, dithiolane, thiooxolane, thiooxane, pyrrolidinyl, piperidyl, piperazinyl, morpholinyl, azetidine, oxetane and thietane. butyryl and benzoyl radicals, but also the valeryl, hexanoyl, acryloyl, crotonoyl and carbamoyl radicals. have the meaning indicated above and for example the acetoxy or propionyloxy radicals. naphthyl and the heterocyclic monocyclic aryl radicals with 5 or 6 members or constituted by condensed rings, containing one or more heteroatoms preferably chosen from oxygen, sulphur and nitrogen. Among the heterocyclic aryl radicals with 5 members the following radicals can be mentioned: furyl, thienyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, thiadiazolyl, pyrazolyl, isoxazolyl, tetrazolyl.
Among the heterocyclic aryl radicals with 6 members, the pyridyl, pyrimidinyl, pyridazinyl, pyrazinyl radicals can be mentioned.
Among the condensed aryl radicals, the indolyl, benzofuranyl, benzothienyl, quinolinyl radicals can be mentioned.
The phenyl, tetrazolyl and pyridyl radicals are preferred. of the alkyl radicals and the aryl radicals mentioned above.
The benzyl, phenyleth
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Claussner Andre
Goubet Francois
Teutsch Jean-George
Higel Floyd D.
Hoechst Marion Roussel
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