Benzofuran derivatives useful in treating diabetic complications

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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514463, 514469, 514470, 548309, 549433, 549466, 549468, 549470, 549471, A61K 3134, C07D30780, C07D30782

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active

046669310

ABSTRACT:
A benzofuran derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, a benzyl group, unsubstituted or substituted with a halogen atom or an alkyloxy group, or an alkyl group having 1 to 3 carbon atoms, R.sup.2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms, R.sup.3 is acetyl group, ethyl group, carboxyl group or 4-methyl-2,5-dioxoimidazolidine-4-yl group, R.sup.4 is hydrogen atom, hydroxyl group, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 9 carbon atoms, carboxymethoxy group, nitro group, acetoamino group, a benzylozy group unsubstituted or substituted with a halogen atom, nitro group or an alkyloxy group or a group having the formula: --OR.sup.6, wherein R.sup.6 is an alkenyl group having 2 to 4 carbon atoms or an alkyl group having 2 to 3 carbon atoms having a halogen atom, cyano group or oxo group, R.sup.5 is hydrogen atom or methylenedioxy group together with R.sup.4 group, n is 1 or 2, and the unsubstituted or substituted N-carboxymethylsulfamoyl group, R.sup.4 and R.sup.5 are attached at 3-position, 4-position, 5-position, 6-position or 7-position of the benzofuran ring, or a nontoxic salt thereof, process for preparing the same and a pharmaceutical composition containing the same.
The compounds of the present invention have powerful aldose reductase inhibiting activity, platelet aggregation inhibiting activity and arachidonic acid metabolism inhibiting activity and are useful for a remedy for treatment of diabetic complications.

REFERENCES:
patent: 2697719 (1954-12-01), Weisblat et al.
patent: 4540704 (1985-09-01), Ueda et al.
patent: 4544667 (1985-10-01), Shepard et al.
Aleksiev et al., Farmatsiya (Sofia) (1973), vol. 23(2), pp. 11-17, (Chemical Abstracts), vol. 79, 92556t, (1973).

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