4-Substituted-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
Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate kidney stone formation. A novel process for their preparation is also disclosed.
Claims11
The compounds having the structure:
- ##STR11## wherein n is 0 or 1;
- R.sub.1 is --OH or .dbd.O;
- R.sub.2 is loweralkyl containing 1 to 3 carbons;
- R.sub.3 is loweralkyl containing 1 to 3 carbons cycloloweralkyl containing 4 to 6 carbons, with the proviso that when n is 1, R.sub.1 is not=O or pharmaceutically acceptable salts thereof.
Compounds having the structure:
- ##STR12## wherein R.sub.1 is --OH or .dbd.O;
- R.sub.2 is loweralkyl containing 1 to 3 carbons;
- R.sub.3 is loweralkyl containing 1 to 3 carbons, cycloloweralkyl containing 4 to 6 carbons or pharmaceutically acceptable salts thereof.
Compounds having the structure ##STR13## wherein R.sub.2 is loweralkyl containing 1 to 3 carbons;
- R.sub.3 is loweralkyl containing 1 to 3 carbons, cycloloweralkyl containing 4 to 6 carbons or pharmaceutically acceptable salts thereof.
A pharmaceutical composition useful in the treatment and prevention of calcium oxalate kidney and bladder stone formation comprising an effective amount of 4-(6,7-dichloro-2-cyclopentyl-2-methylindan-1-on-5-yl)-3-hydroxy-3-pyrroli ne-2,5-dione or the pharmaceutically acceptable salts thereof and a pharmaceutically effective carrier therefor.
A pharmaceutical composition useful in the treatment and prevention of calcium oxalate kidney and bladder stone formation comprising an effective amount of 4-(6,7-dichloro-2-cyclopentyl-1-hydroxy-2-methylindan-5-yloxy)-3-hydroxy-3 -pyrroline-2,5-dione or the pharmaceutically acceptable salts thereof and a pharmaceutically effective carrier therefor.
A method of treating persons afflicted with calcium oxalate kidney or bladder stones, or preventing the formation of kidney or bladder stones, which comprises administering to such a patient an effective amount of 4-(6,7-dichloro-2-cyclopentyl-2-methylindan-1-on-5-yl)-3-hydroxy-3-pyrroli ne-2,5-dione.
A method of treating persons afflicted with calcium oxalate kidney or bladder stones, or preventing the formation of kidney or bladder stones, which comprises administering to such a patient an 4-(6,7-dichloro-2-cyclopentyl-1-hydroxy-2-methylindan-5-yloxy)-3-hydroxy-3 -pyrroline-2,5-dione.
Dependencies are inferred from the claim text.