4-(Substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase
AssigneeMerck & Co., Inc.
InventorsEdward J. Cragoe, Jr., Clarence S. Rooney, Haydn W. R. Williams
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Abstract
4-(Substituted thiazolyl)-3-hydroxy-3-pyrroline-2,5-diones of the formula: ##STR1## are inhibitors of glycolic acid oxidase useful in treating or preventing calcium oxalate kidney or bladder stones.
Claims2
A pharmaceutical composition for treating persons afflicted with calcium oxalate renal lithiasis or preventing the formation of calcium oxalate kidney or bladder stones comprising a pharmaceutically acceptable carrier and an effective amount of a compound of the formula:
- ##STR34## wherein n is 0 to 2;
- m is 0 to 3;
- R.sub.1, R.sub.2 and R.sub.3 are indeptendently hydrogen, halogen, loweralkyl containing 1 to 6 carbons, trifluoromethyl, and loweralkoxy containing 1 to 6 carbons or pharmaceutically acceptable salts thereof, with the proviso that the substituents on the thiazolyl ring are not adjacent.
A method of treating persons afflicted with calcium oxalate renal lithiasis or preventing the formation of calcium oxalate kidney or bladder stones which comprises administration to such patients an effective amount of compounds having the structure:
- ##STR35## wherein n is 0 to 2;
- m is 0 to 3;
- R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, halogen, loweralkyl containing 1 to 6 carbons, trifluoromethyl, and loweralkoxy containing 1 to 6 carbons or pharmaceutically acceptable salts thereof, with the proviso that the substituents on the thiazolyl ring are not adjacent.
Dependencies are inferred from the claim text.