Tetrazole derivatives and aldose reductase inhibition therewith

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

1994-01-07

1996-06-18

Springer, David B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C07D25704, A61K 3141

Patent

active

RE0352810

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:
Sorensen et al, Acta Chem. Scand. 26:541-548, 1972.
Buckler et al, J. Med. Chem. 13:725-729, 1970.

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