Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1998-06-09
2000-11-07
Power, Fiona T.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514397, 548250, 548252, 548253, 5483117, C07D40506, C07D40514, A61K 31415
Patent
active
061437743
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT FR96/01749 filed Nov. 7, 1996.
The present invention relates to new derivatives of imidazole N-benzyldioxole, their preparation process, the new intermediates obtained, their use as medicaments, the pharmaceutical compositions containing them and the new use of such derivatives of imidazole.
A subject of the present invention is the products of formula (I): ##STR2## in which: R.sub.1 represents an alkyl radical, optionally substituted by one or more hydroxyl or alkoxy radicals, the alkyl and alkoxy radicals being linear or branched and containing at most 6 carbon atoms, or a saturated or unsaturated cyclic radical constituted by 3 to 7 members, and optionally containing one or more identical or different heteroatoms chosen from oxygen, sulphur and nitrogen atoms, acid function or an acid isosteric function and Y represents the phenyl radical substituted by a dioxol radical and optionally substituted by another substituent chosen from halogen atoms and alkoxy and alkyl radicals containing at most 4 carbon atoms, 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: 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, radicals: methoxy, ethoxy, propoxy, isopropoxy, linear, secondary or tertiary butoxy, pentoxy or hexoxy as well as their linear or branched position isomers, represent a fluorine, bromine or iodine atom, members and optionally containing one or more identical or different heteroatoms, chosen from oxygen, sulphur or nitrogen atoms designates on the one hand a cycloalkyl radical such as for example the cyclopropyl, cyclobutyl radicals and quite particularly the cyclopentyl and cyclohexyl radicals or a carbocyclic radical interrupted by one or more heteroatoms chosen from oxygen, nitrogen or sulphur atoms such as quite particularly the dioxolane, dioxane, dithiolane, thiooxolane or thiooxane radical, on the other hand the phenyl, thienyl, furyl, pyridyl or tetrazolyl radicals, salified or esterified carboxy radical, the free or salified tetrazolyl radical, or the following radicals: containing at most 6 carbon atoms or a phenyl, pyridyl, pyrimidinyl, piperazinyl, thienyl or tetrazolyl radical, the alkyl, alkenyl and phenyl radicals being optionally substituted by one or more radicals chosen from halogen atoms and hydroxy, alkoxy or phenyl radicals, all the phenyl radicals and the piperazinyl radical being optionally substituted by a linear or branched alkyl radical containing at most 4 carbon atoms.
The carboxy radical or radicals of the products of formula (I) can be salified or esterified by various groups known to a man skilled in the art amongst which there can be mentioned, for example: equivalent of sodium, potassium, lithium, calcium, magnesium or ammonium or organic bases such as, for example, methylamine, propylamine, trimethylamine, diethylamine, triethylamine, N,N-dimethylethanolamine, tris (hydroxymethyl) amino methane, ethanolamine, pyridine, picoline, dicyclohexylamine, morpholine, benzylamine, procaine, lysine, arginine, histidine, N-methylglucamine, carbonyl groups such as, for example, methoxycarbonyl, ethoxycarbonyl, tert-butoxycarbonyl or benzyloxycarbonyl, these alkyl radicals being able to be substituted by radicals chosen for example from halogen atoms, hydroxyl, alkoxy, acyl, acyloxy, alkylthio, amino or aryl radicals such as, for example, in the following groups: chloromethyl, hydroxypropyl, methoxymethyl, propionyloxymethyl, methylthiomethyl, dimethylaminoethyl, benzyl or phenethyl.
The addition salts with mineral or organic acids of the products of formula (I) can be, for example, the salts formed with the following acids: hydrochloric, hydrobromic, hydroiodic, nitric, sulphuric, phosphoric, propionic, acetic, formic, benzo
REFERENCES:
patent: 5811444 (1998-09-01), Heckmann et al.
patent: 5856509 (1999-01-01), Heckmann et al.
Heckmann Bertrand
Jouquey Simone
Vevert Jean-Paul
Zhang Jidong
Hoechst Marion Roussel
Power Fiona T.
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