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
1998-09-15
Richter, Johann
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514396, 514399, 5483351, 5483265, 5483401, 5483411, 5483425, 5483421, 5483435, 5483461, A61K 31415, C07D23358, C07D23360, C07D23384
Patent
active
058078789
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/FR95/00227 filed Feb. 27, 1995.
The present invention relates to new tetrasubstituted derivatives of imidazole, their preparation process, the new intermediates obtained, their use as medicaments and the pharmaceutical compositions containing them.
A subject of the invention is the 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, aryloxy, arylalkyl radical, in which the alkyl radical is linear or branched and contains at most 6 carbon atoms, ##STR3## 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 following radicals: hydroxyl, linear or branched alkoxy and alkylthio containing at most 6 carbon atoms and phenyl 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, ##STR4## radical in which Z represents a hydroxyl, alkoxy or free, salified or esterified carboxy radical.
R.sub.3 is chosen from ##STR5## radical in which X represents an oxygen, sulphur atom, an N--O--R.sub.6 radical in which R.sub.6 represents a hydrogen atom or a linear or branched alkyl radical containing at most 6 carbon atoms, optionally substituted by a free, salified or esterified carboxy radical, ##STR6## in which R.sub.7 and R.sub.8, identical or different, represent a hydrogen atom, a linear or branched alkyl radical containing at most 6 carbon atoms, or a phenyl radical, the alkyl and phenyl radicals being optionally substituted by one or more radicals chosen from halogen atoms, the following radicals: hydroxyl, cyano, nitro, alkyl, cycloalkyl and alkoxy, linear or branched containing at most 6 carbon atoms, or R.sub.7 and R.sub.8 form together with the nitrogen atom to which they are linked a radical chosen from the following radicals: pyrrolyl, pyrrolinyl, pyrrolidinyl, piperazinyl, alkylpiperazinyl, phenylpiperazinyl, piperidyl, morpholinyl and indolinyl, alkyl radical containing at most 8 carbon atoms, the alkyl radical being substituted when X represents an oxygen atom and optionally substituted when X does not represent an oxygen atom, the cycloalkyl and alkyl radicals being if appropriate substituted by one or more radicals chosen from the following radicals: linear or branched alkylthio containing at most 8 carbon atoms, acyl, free, salified or esterified carboxy, halogen atoms, aryl and arylthio, optionally substituted by one or more radicals chosen from halogen atoms, hydroxyl, cyano, nitro, cycloalkyl, alkyl and alkoxy, linear or branched containing at most 6 carbon atoms, ##STR7## radical in which R.sub.9 represents a hydroxyl, alkoxy, alkylthio radical, an amino radical optionally substituted by a hydroxyl radical or by one or two alkyl radicals, the alkoxy, alkylthio and alkyl radicals being linear or branched containing at most 8 carbon atoms and optionally substituted by one or more radicals chosen from cycloalkyl radicals containing at most 6 carbon atoms and aryl radicals, optionally substituted by a tetrazolyl, alkylsulphonyl, arylsulphonyl or acyl radical or by one or two identical or different radicals chosen from the following radicals: phenyl, phenylalkyl and alkyl, linear or branched containing at most 6 carbon atoms, alkylsulphonyl, arylsulphonyl, acyl, phenyl, phenylalkyl and alkyl being optionally substituted by one or more radicals chosen from halogen atoms, the following radicals: hydroxyl, cyano, nitro, cycloalkyl, alkyl and alkoxy, linear or branched containing at most 6 carbon atoms, the tetrazolyl radical being optionally substituted by a linear or branched alkyl radical containing at most 6 carbon atoms or a phenyl radical, these alkyl and phenyl radicals being themselves optional
REFERENCES:
patent: 5468764 (1995-11-01), Heitsch et al.
"Potent Imidazole Angiotensin II Antagonists: Acyl Sulfonamides and Acyl Sulfamides as Tetrazole Replacements," Naylor et al., Bioorganic & Medicinal Chemistry Letters, vol. 4, No. 1, pp. 69-74, 1994.
Corbier Alain
Deprez Pierre
Fortin Michel
Guillaume Jacques
Heckmann Bertrand
Oswecki Jane C.
Richter Johann
Uclaf Roussel
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