Naphthalenylmethyl cycloalkenone acetic acids and analogs thereof useful as aldose reductase inhibitors
AssigneeAmerican Home Products Corporation
InventorMichael S. Malamas
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Abstract
The compounds of this invention which have the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1 -C.sub.8 alkyl, halogen, C.sub.1 -C.sub.8 alkoxy, or trifluoromethyl; R.sup.3 is --OH or --NHCO.sub.2 CH.sub.3 ; X is --CH.sub.2 -- or --OCH.sub.2 --; n is 1 or 2; or a pharmaceutically acceptable salt thereof, are useful in treating or inhibiting the long-term complications of diabetes such as diabetic retinopathy, nephropathy and neuropathy through the inhibition of the enzyme aldose reductase. Aldose reductase inhibitors have been shown to prevent the biochemical, functional and morphological changes induced by hyperglycemia.
Claims3
A compound having the formula:
- ##STR4## wherein:
- R.sup.1, R.sup.2 are independently hydrogen, C.sub.1 -C.sub.8 alkyl, halogen, C.sub.1 -C.sub.8 alkoxy, or trifluoromethyl;
- R.sup.3 is --OH or --NHCO.sub.2 CH.sub.3 ;
- X is --CH.sub.2 -- or --OCH.sub.2 --;
- n is 1 or 2;
- or a pharmaceutically acceptable salt thereof.
A pharmaceutical composition for the treatment or prevention of diabetic complications in a diabetic mammal which comprises a pharmaceutical carrier and a therapeutically effective amount of a compound having the formula:
- ##STR5## wherein:
- R.sup.1, R.sup.2 are independently hydrogen, C.sub.1 -C.sub.8 alkyl, halogen, C.sub.1 -C.sub.8 alkoxy, or trifluoromethyl;
- R.sup.3 is --OH or --NHCO.sub.2 CH.sub.3 ;
- X is --CH.sub.2 -- or --OCH.sub.2 --;
- n is 1 or 2;
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.