Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1997-01-31
1998-09-22
Higel, Floyd D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514396, 514398, 514399, 514400, 5483117, A61K 31415, C07D40506
Patent
active
058114440
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/FR95/01034 filed Aug. 1, 1995.
The present invention relates to the new use of derivatives of imidazole, new derivatives of imidazole, their preparation process, the new intermediates obtained, their use as medicaments and the pharmaceutical compositions containing them.
A subject of the present invention is the use for the preparation of pharmaceutical compositions intended for the treatment of illnesses resulting from an abnormal stimulation of the endothelin receptors, of the products of formula (I): ##STR2## in which: R.sub.1 represents a hydroxyl, alkyl, alkenyl, alkynyl, alkoxy, alkylthio radical, each of these radicals being linear or branched and containing at most 12 carbon atoms, a formyl radical or a cycloalkyl radical optionally interrupted by one or more heteroatoms and containing 3 to 7 carbon atoms, all these radicals being optionally substituted by one or more identical or different radicals chosen from halogen atoms, the following radicals: hydroxyl, free, salified, esterified or amidified carboxy, cyano, nitro, amino optionally substituted by one or two identical or different alkyl radicals containing at most 6 carbon atoms, cycloalkyl containing 3 to 7 carbon atoms, alkyl, alkenyl and alkoxy containing at most 6 carbon atoms, haloalkyl, alkylthio, haloalkylthio, haloalkoxy, phenoxy, phenylalkoxy, optionally substituted carbamoyl, acyl, acyloxy, optionally salified tetrazolyl and phenyl optionally substituted by one or more radicals chosen from halogen atoms, hydroxyl radicals, alkyl and alkoxy radicals containing at most 4 carbon atoms, trifluoromethyl, cyano, free, salified or esterified carboxy and tetrazolyl radicals, esterified or amidified carboxy or carboxy-carbonyl, nitro, cyano, and the --P(O)(OR).sub.2 radical in which R represents a hydrogen atom, an alkyl or phenyl radical, --X--R.sub.10 radical in which m1 represents an integer from 0 to 4, m2 represents an integer from 0 to 2 and --NR.sub.11 --CO--O--, --NR.sub.11 --CO--NR.sub.12 -- and --N=CR.sub.11 --NR.sub.12 -- radicals and R.sub.10 represents an alkyl, alkenyl or aryl radical, these radicals being optionally substituted by one or more identical or different radicals chosen from halogen atoms; the following radicals: hydroxyl; cycloalkyl containing 3 to 7 carbon atoms; alkyl, alkoxy, haloalkyl, alkylthio, haloalkylthio and haloalkoxy, linear or branched, containing at most 6 carbon atoms; phenoxy; phenylalkoxy; optionally substituted carbamoyl; acyl; acyloxy; free, salified or esterified carboxy; tetrazolyl; cyano; nitro; amino optionally substituted by one or two identical or different alkyl radicals containing at most 6 carbon atoms and aryl optionally substituted by one or more radicals chosen from halogen atoms, hydroxyl radicals, alkyl and alkoxy radicals containing at most 4 carbon atoms, trifluoromethyl, free, salified or esterified carboxy and tetrazolyl radicals, and R.sub.11 and R.sub.12, identical or different, are chosen from the hydrogen atom and the values defined for R.sub.10, or R.sub.4 represents the hydrogen atom; an alkyl, alkenyl, alkynyl and acyl radical, these radicals being linear or branched, containing at most 6 carbon atoms, and being optionally interrupted by one or more heteroatoms chosen from sulphur, oxygen or nitrogen atoms; an amino or carbamoyl radical optionally substituted by one or two identical or different alkyl or alkenyl radicals, containing at most 6 carbon atoms or the (CH.sub.2).sub.m1 --S(O).sub.m2 --XR.sub.10 radical as defined above; a cycloalkyl radical containing 3 to 6 carbon atoms or an aryl radical, the alkyl, alkenyl and aryl radicals of all the radicals which are represented by R.sub.4 being optionally substituted by one or more identical or different radicals chosen from: esterified or amidified carboxy radicals, alkenylthio, alkynylthio, acyl, acyloxy, acylthio, haloalkylthio, haloalkoxy, these radicals containing at most 6 carbon atoms, aryl, arylalkyl, arylalkenyl, arylthio, aryloxy and arylalkoxy in which the aryl radical is option
REFERENCES:
Chem. Abstracts. Oct. 14, 1995, vol. 103, No. 15, C. Paul Bianchi.
Baggaley et al. Journal of Med. Chemistry, 1975, vol. 18, No. 8, 4 pgs.
Stefonich et al., Il Farmaco Ed Sc., vol. 40, No. 6, pp. 429-441 (1985).
Heckmann Bertrand
Vevert Jean-Paul
Zhang Jidong
Higel Floyd D.
Roussel Uclaf
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