Tetrazole derivatives and aldose reductase inhibition therewith

Details Tetrazole derivatives and aldose reductase inhibition therewith Tetrazole derivatives and aldose reductase inhibition therewith

1990-03-22

1991-10-08

Springer, David B.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

548253, C07D25704, A61K 3141

Patent

active

050554816

ABSTRACT:
The present invention relates to an aldose reductase inhibitor having the following formula: ##STR1## R.sub.1 is a hydrogen atom or --A--COOR.sub.5 (A is an alkylene group having 1 to 4 carbon atoms and R.sub.5 is a hydrogen atom or a lower alkyl group), and R.sub.2, R.sub.3 and R.sub.4 are the same as or different from each other and selected from the group consisting of a hydrogen atom, a hydroxy group, a halogen atom, a carboxyl group, an alkyl group, an amide group, an amino group, an alkoxy group, an aryl group, an aryloxy group, an alkylthio group, an alkylsulfinyl group, an alkylsulfonyl group, a nitro group, --NHCOCOOR.sub.6 (R.sub.6 is a hydrogen atom or a lower alkyl group), a mono- or dialkylaminosulfonyl group, and a residual group having the following formula: ##STR2## (A and R.sub.5 are the same as in the above). The compounds defined in the above are excellent in aldose reductase inhibitory activity and low in toxicity. Therefore, those compounds are useful as a preventive agent and/or a remedy for diabetic complications such as neuropathy, retinopathy, nephropathy, cataracts and keratopathy.

REFERENCES:
patent: 4372953 (1983-02-01), Uchida et al.
patent: 4668796 (1987-05-01), Geiger
patent: 4795754 (1989-01-01), Szwaki et al.

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