US4432992A
Expired / Lapsed
US
⏱️ 0.0 years remaining
4-[5(and 4)-Substituted-2-thienyl]-3-hydroxy-3-pyrroline-2,5-dione inhibitors of glycolic acid oxidase
Assignee: Merck and Co Inc
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Filing: 1979-11-05
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Granted: 1984-02-21
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Expires: 1999-11-05
Abstract
Abstract Novel 4-[5(and 4)-substituted-2-thienyl]-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.
Inventors
- 👤 Edward J. Cragoe, Jr.
- 👤 Clarence S. Rooney
- 👤 Haydn W. R. Williams
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-25 14:09
CPC Classifications
C; C07; C07D; C07D409/00; C07D409/02; C07D409/04; C07D333/00; C07D333/02; C07D333/04; C07D333/06; C07D333/22; C07D333/24
Claims Analysis
Total Claims: 12
Claim 1
Independent Claim
31 words
The compounds of the formula: ##STR9## wherein n is 0 to 2; X and Y are independently hydrogen, halogen, loweralkyl containing 1 to 4 carbons, or a pharmaceutically acceptable salt thereof.
Claim 2
Dependent Claim
31 words
The compounds of the formula: ##STR9## wherein n is 0 to 2; X and Y are independently hydrogen, halogen, loweralkyl containing 1 to 4 carbons, or a pharmaceutically acceptable salt thereof.
Claim 3
Dependent Claim
34 words
The compounds of claim 1 of the formula: ##STR10## wherein n is 0 to 2; X and Y are independently hydrogen, halogen, loweralkyl containing 1 to 4 carbons, or a pharmaceutically acceptable salt thereof.
Claim 4
Dependent Claim
28 words
The compounds of claim 1 of the formula: ##STR11## wherein X and Y are independently hydrogen, halogen, loweralkyl containing 1 to 4 carbons, or a pharmaceutically acceptable salt.
Claim 5
Dependent Claim
11 words
The compounds of claim 3 wherein X and Y are halogen.
Claim 6
Dependent Claim
7 words
A compound of claim 3 designated: 4-[5-(4-chlorophenyl)-2-thienyl]-3-hydroxy-3-pyrroline-2,5-dione.
Claim 7
Dependent Claim
39 words
A pharmaceutical composition useful in the treatment and prevention of calcium oxalate kidney and bladder stone formation comprising an effective amount of a compound of claim 1 or the pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier thereof.
Claim 8
Dependent Claim
35 words
A pharmaceutical composition useful in the treatment and prevention of calcium oxalate kidney and bladder stone formation comprising an effective amount of 4-[5-(4-chlorophenyl)-2-thienyl]-3-hydroxy-3-pyrroline-2,5-dione, or the pharmaceutically acceptable salts thereof and a pharmaceutically effective carrier thereof.
Claim 9
Dependent Claim
35 words
A pharmaceutical composition useful in the treatment and prevention of calcium oxalate kidney and bladder stone formation comprising an effective amount of 4-[5-(4-chlorophenyl)-2-thienyl]-3-hydroxy-3-pyrroline-2,5-dione, or the pharmaceutically acceptable salts thereof and a pharmaceutically effective carrier thereof.
Claim 10
Dependent Claim
40 words
A method of treating persons afflicted with calcium oxalate kidney or bladder stones or preventing the formation of calcium oxalate kidney or bladder stones which comprises administering to such a patient an effective amount of a compound of claim 1.
Claim 11
Independent Claim
35 words
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-[5-(4-chlorophenyl)-2-thienyl]-3 -hydroxy-3-pyrroline-2,5-dione.
Claim 12
Independent Claim
35 words
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-[5-(4-chlorophenyl)-2-thienyl]-3 -hydroxy-3-pyrroline-2,5-dione.
References Cited (Backward Citations)
US3340263A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1987-02-20 | 1987-08-22 | 1988-02-21 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1991-02-20 | 1991-08-22 | 1992-02-21 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1995-02-20 | 1995-08-22 | 1996-02-21 | $7700.00 | Window Closed / Lapsed |