Substituted pharmacologically acitve imidazole derivatives and their preparation and use.

摘要

The invention provides novel compounds of the formula:
<Chemistry id="chema01" num="0001"><Image id="ia01" he="29" wi="64" file="IMGA0001.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>or
<Chemistry id="chema02" num="0002"><Image id="ia02" he="27" wi="76" file="IMGA0002.TIF" imgContent="chem" imgFormat="TIFF" inline="no" /></Chemistry>wherein each of R<Sub>1</Sub>, R<Sub>2</Sub> and R<Sub>3</Sub>, which can be the same or different, is hydrogen, chloro, bromo, fluoro, methyl, ethyl, methoxy, amino, hydroxy or nitro; R<Sub>4</Sub> is hydrogen or alkyl of 1 to 7 carbon atoms; R<Sub>5</Sub> is hydrogen or a straight or branched alkyl group of 1 to 5 carbon atoms or a phenyl group; R<Sub>6</Sub> is hydrogen or an alkyl group of 1 to 7 carbon atoms or a substituted or unsubstituted benzyl group; and n is 0 or 1; provided that when R<Sub>2</Sub>, R<Sub>3</Sub>, R<Sub>4</Sub>, R<Sub>5</Sub> and R<Sub>6</Sub> are all hydrogen and R, is
<UnorderedLists id="ula01" listStyle="none"><ListItem>a) chloro, R, must be in the 3-position</ListItem><ListItem>b) methyl or methoxy, then R<Sub>1</Sub> must be in the 2- or 3- position</ListItem><ListItem>c) hydrogen, then n must be other than 1</ListItem></UnorderedLists>
and their non-toxic pharmaceutically acceptable acid addition salts. Processes for the preparation of these compounds are described, as are novel pharmaceutical compositions comprising the compounds or their salts. These compounds exhibit valuable pharmacological activity and are useful in the treatment of mammals, e.g. as diuretic agents. Furthermore, they have antithrombotic and anti-hypertensive effects.