Imidazole protectorant for the stomach and intestine

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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Details

514249, 544350, 546121, C07D47104, C07D48704, A61K 31435, A61K 31495

Patent

active

051128349

DESCRIPTION:

BRIEF SUMMARY
FIELD OF USE OF THE INVENTION

The invention relates to new diazoles, processes for their preparation, their use and drugs containing them. The compounds according to the invention are used in the pharmaceutical industry as intermediates and for the manufacture of drugs.


KNOWN TECHNICAL BACKGROUND

The published European Patent Applications 0033094, 0068378, 0165545 and 0204285 disclose imidazopyridines and imidazoisoquinolines which, on account of their antisecretory and cytoprotective action, are intended for use in the treatment of ulcer.


DESCRIPTION OF THE INVENTION

It has been found that the new imidazole compounds described in greater detail below have interesting pharmacological properties, as a result of which they differ in a surprising and particularly advantageous manner from the above-mentioned known compounds.
The invention relates to new imidazole compounds of the formula I ##STR2## wherein R1 denotes hydrogen (H) or halogen, cyano-1-4C-alkyl or 1-4C-alkoxycarbonyl, halo-1-4C-alkyl, cyano-1-4C-alkyl, amino-1-4C-alkyl, mono- or di-1-4C-alkylamino-1-4C-alkyl, nitroso, nitro, amino, mono- or di-1-4C-alkylamino or 1-4C-alkoxycarbonyl, trifluoromethyl, trifluoromethyl, 2-hydroxy-3-methyl-trimethylene (--CH.sub.2 --CH(OH)--CH(CH.sub.3)--), 2-hydroxy-trimethylene (--CH.sub.2 --CH(OH)--CH.sub.2 --), 1-hydroxy-tetramethylene (--CH(OH)--CH.sub.2 --CH.sub.2 --CH.sub.2 --), 2-hydroxy-tetramethylene (--CH.sub.2 CH(OH)--CH.sub.2 --CH.sub.2 --), 1-hydroxy-pentamethylene (--CH(OH)--CH.sub.2 --CH.sub.2 --CH.sub.2 --CH.sub.2 --) or 2-hydroxy-pentamethylene (--CH.sub.2 --CH(OH)--CH.sub.2 --CH.sub.2 --CH.sub.2 --) and salts.
For the purposes of the present invention, halogen is bromine and in particular chlorine and fluorine.
1-4C-alkyl represents straight-chain or branched alkyl radicals having 1 to 4 carbon atoms. The butyl, isobutyl, secbutyl, tert-butyl, propyl, isopropyl, ethyl radicals and in particular the methyl radical may be mentioned as examples.
1-4C-alkoxy radicals contain, in addition to the oxygen atom, one of the above-mentioned 1-4C-alkyl radicals. The methoxy radical is preferred.
1-4C-alkoxycarbonyl radicals contain, in addition to the carbonyloxy group, one of the above-mentioned 1-4C-alkyl radicals. The methoxycarbonyl and the ethoxycarbonyl radicals are preferred.
Hydroxy-1-4C-alkyl represents the above-mentioned 1-4C-alkyl radicals to which a hydroxyl radical is bonded. The hydroxymethyl radical is preferred.
Halo-1-4C-alkyl represents the above-mentioned 1-4C-alkyl radicals to which a halogen atom is bonded. The chloromethyl radical is preferred.
Cyano-1-4C-alkyl represents the above-mentioned 1-4C-alkyl radicals to which a cyano radical is bonded. The cyanomethyl radical is preferred.
Amino-1-4C-alkyl represents the above-mentioned 1-4C-alkyl radicals to which an amino group is bonded.
Mono- or di-1-4C-alkylamino represents amino groups which are substituted by one or two of the above-mentioned 1-4C-alkyl radicals. The methylamino, ethylamino, diisopropylamino and in particular the dimethylamino groups may be mentioned as examples.
Mono- or di-1-4C-alkylamino-1-4C-alkyl represents the above-mentioned 1-4C-alkyl radicals to which one of the above-mentioned mono- or di-1-4C-alkylamino groups is bonded. The dimethylaminomethyl and the dimethylaminoethyl radicals are preferred.
1-4C-alkylene represents straight-chain alkylene radicals having 1 to 4 carbon atoms. The ethylene radical (--CH.sub.2 --CH.sub.2 --) and the methylene radical (--CH.sub.2 --) may be mentioned as preferred alkylene radicals.
Preferred salts for compounds of the formula I are all acid addition salts. The pharmacologically tolerated salts of the inorganic and organic acids usually used in the pharmaceutical sector may be mentioned in particular. Pharmacologically non-tolerated salts, which, for example, may initially be obtained as products of the process in the preparation of the compounds according to the invention on an industrial scale are converted into pharmacologically tolerated salts by processes known to o

REFERENCES:
patent: 3849396 (1974-11-01), Birkenmeyer
patent: 3849576 (1974-11-01), Kalopissis
patent: 3852279 (1974-12-01), Krapcho
patent: 4324796 (1982-04-01), Eistetter
patent: 4387099 (1983-06-01), Smith
patent: 4387219 (1983-06-01), Yamamoto
patent: 4395414 (1983-07-01), Eistetter
patent: 4409226 (1983-10-01), Bristol et al.
patent: 4430339 (1984-02-01), Eistetter
patent: 4686230 (1987-08-01), Rainer
patent: 4725601 (1988-02-01), Ueda et al.
patent: 4758579 (1988-07-01), Kohl
patent: 4831041 (1989-05-01), Shiokawa et al.
patent: 4886819 (1989-12-01), Ashimori
patent: 4920129 (1990-04-01), Shiokawa et al.

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