Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-08-30
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...
514399, 514400, 5483151, 5483171, 5483225, 5483431, 5483435, 5483461, A61K 31415, C07D23302, C07D23340, C07D23338
Patent
active
058114459
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/FR95/00228, filed Feb. 27, 1995.
The present invention relates to a new use of imidazole derivatives for the treatment of illnesses involving the AT.sub.1 and AT.sub.2 receptors of angiotensin, some of these products, their preparation, their use as medicaments and the pharmaceutical compositions containing them.
Angiotensin II is known to be a circulatory hormone which can also act as a neuropeptide at the level of the central nervous system as indicated in particular in the European Patent Applications EP 0,465,368 and EP 0,503,162, or also International Patent Application WO 91/14367.
It has recently been shown that in fact two sub-types of angiotensin II receptors exist: the AT.sub.1 receptor and the AT.sub.2 receptor.
Research was initially centered on showing AT.sub.1 receptor antagonists as substances with anti-hypertensive activity.
It has just been shown that the products of formula (I) of the present invention have an affinity not only for the AT.sub.1 receptor but also for the AT.sub.2 receptor.
The products of formula (I) of the present invention can thus quite particularly be the subject of a new use for the treatment of illnesses resulting from an abnormal stimulation of the AT.sub.1 and AT.sub.2 receptors of angiotensin II.
Therefore a subject of the present invention is the new use, for the preparation of pharmaceutical compositions intended for the treatment of illnesses resulting from an abnormal stimulation of the AT.sub.1 and AT.sub.2 receptors of angiotensin II, of products of formula (I): ##STR2## in which
R.sub.1 represents a linear or branched alkyl, alkylthio and alkoxy radical containing at most 6 carbon atoms, an aryl, arylthio or aryloxy radical, an arylalkyl radical in which the alkyl radical is linear or branched and contains at most 6 carbon atoms,
R.sub.2 represents:
a) the --S--R, --O--R and ##STR3## radicals in which R represents a linear or branched alkyl or alkenyl radical containing at most 8 carbon atoms, a cycloalkyl radical containing at most 6 carbon atoms or an aryl radical, the alkyl, alkenyl, cycloalkyl and aryl radicals being optionally substituted by one or more radicals chosen from halogen atoms, the hydroxyl radical, linear or branched alkoxy and alkylthio radicals containing at most 6 carbon atoms and a phenyl radical itself optionally substituted by one or more radicals chosen from halogen atoms, the hydroxyl radical and linear or branched alkoxy radicals containing at most 6 carbon atoms,
b) a halogen atom,
c) a ##STR4## radical in which Z represents a hydroxyl, alkoxy or free, salified or esterified carboxy radical,
R.sub.3 is chosen from
a free, salified or esterified carboxy radical,
an acyl radical, optionally substituted by a phenyl, thienyl or tetrazolyl radical,
a halogen atom,
a linear or branched alkyl, alkenyl or alkylthio radical containing at most 8 carbon atoms, the following radicals: ##STR5## radicals in which:
either R.sub.6 and R.sub.7 or R.sub.8 and R.sub.9, identical or different, are chosen from: alkylsulphonyl and arylsulphonyl radicals, the radicals being optionally substituted by one or more identical or different radicals chosen from halogen atoms, the hydroxyl radical, alkoxy radicals containing at most 6 carbon atoms or the free, salified or esterified carboxy radical, alkyl and alkenyl radicals contain at most 6 carbon atoms, these aryl, arylalkyl and arylalkenyl radicals being optionally substituted by one or more radicals chosen from halogen atoms, hydroxyl and nitro radicals, alkyl, alkenyl, haloalkyl, alkoxy and acyl radicals containing at most 6 carbon atoms, the amino radical optionally substituted by one or two identical or different alkyl radicals containing at most 6 carbon atoms and free, salified or esterified carboxy radicals,
or on the one hand R.sub.6 and R.sub.7 and on the other hand R.sub.8 and R.sub.9 form respectively with the nitrogen atom to which they are linked a heterocyclic radical, chosen from the following radicals: imidazolyl, pyrrolyl, pyrrolinyl, pyrrolidinyl, piperidi
REFERENCES:
patent: 5527919 (1996-06-01), Bhatnagar et al.
1-Pharmacology vol. 120, 1994 p. 21 Bioorganic & Medical Chemistry Letters. vol. 4, No. 1 pp. 69-74 1994.
Corbier Alain
Deprez Pierre
Fortin Michel
Guillaume Jacques
Higel Floyd D.
Roussel Uclaf
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