US4791131A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Analgesic and antiinflammatory 1-acyl-2-oxindole-3-carboxamides
Assignee: Pfizer Inc
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Filing: 1987-12-31
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Granted: 1988-12-13
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Expires: 2007-12-31
Abstract
Abstract Certain new 2-oxindole-3-carboxamide compounds having an acyl substituent at the 1-position are inhibitors of the cyclooxygenase (CO) and lipoxygenase (LO) enzymes, and are useful as analgesic and anti-inflammatory agents in mammalian subjects. In particular, the compounds of the invention are useful for acute administration for ameliorating or eliminating pain in human subjects recovering from surgery or trauma, and also for chronic administration for alleviating the symptoms of chronic diseases, such as rheumatoid arthritis and osteoarthritis, in human subjects.
Inventors
- 👤 Saul B. Kadin
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-03 16:20
CPC Classifications
C; C07; C07D; C07D401/00; C07D401/02; C07D401/12; C07D209/00; C07D209/02; C07D209/04; C07D209/30; C07D209/42; C07D409/00; C07D409/02; C07D409/12; C07D417/00; C07D417/02; C07D417/12; C07D491/00; C07D491/02; C07D491/04
Claims Analysis
Total Claims: 10
Claim 1
Independent Claim
82 words
A 1-acyl-2-oxindole-3-carboxamide compound of the formula ##STR10## and the pharmaceutically-acceptable base salts thereof; wherein X and Y are each selected from the group consisting of hydrogen, fluoro, chloro, bormo, trifluoromethyl and alkyl having 1 to 4 carbons; R 1 is selected from the group consisting of heterocyclic, mono-methyl heterocyclic, furymethyl and thienylmethyl; wherein said heterocyclic is selected form the group consisting of pyridyl, thienyl, furyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl and isoxazolyl; and R 2 is alkyl having 1 to 6 carbons.
Claim 2
Dependent Claim
82 words
A 1-acyl-2-oxindole-3-carboxamide compound of the formula ##STR10## and the pharmaceutically-acceptable base salts thereof; wherein X and Y are each selected from the group consisting of hydrogen, fluoro, chloro, bormo, trifluoromethyl and alkyl having 1 to 4 carbons; R 1 is selected from the group consisting of heterocyclic, mono-methyl heterocyclic, furymethyl and thienylmethyl; wherein said heterocyclic is selected form the group consisting of pyridyl, thienyl, furyl, pyrrolyl, thiazolyl, oxazolyl, imidazolyl, isothiazolyl and isoxazolyl; and R 2 is alkyl having 1 to 6 carbons.
Claim 3
Dependent Claim
13 words
A compound according to claim 1, wherein R 1 is furylmethyl or thienylmethyl.
Claim 4
Dependent Claim
11 words
A compound according to claim 2, wherein R 2 is methyl.
Claim 5
Dependent Claim
16 words
A compound according to claim 1, wherein R 1 is said heterocyclic or said mono-methyl heterocyclic.
Claim 6
Dependent Claim
18 words
The compound according to claim 3, wherein X and Y are each hydrogen and R 1 is 2-thienylmethyl.
Claim 7
Dependent Claim
18 words
The compound according to claim 4, wherein X is 5-chloro, Y is hydrogen and R 1 is 2-pyridyl.
Claim 8
Dependent Claim
37 words
A pharmaceutical composition, which comprises a pharmaceutically-acceptable carrier and a 1-acyl-2-oxindole-3-carboxamide compound according to claim 1, and wherein the weight ratio of the pharmaceutically-acceptable carrier to the 1-acyl-2-oxindole-3-carboxamide compound is in the range from 1:4 to 4:1.
Claim 9
Dependent Claim
31 words
A method of eliciting an analgesic response in a mammalian subject, which comprises administering to said mammalian subject an analgesic response eliciting amount of a 1-acyl-2-oxindole-3-carboxamide compound according to claim 1.
Claim 10
Dependent Claim
31 words
A method of treating an inflammatory disease in a mammalian subject, which comprises administering to said mammalian subject an inflammatory disease treating amount of a 1-acyl-2-oxindole-3-carboxamide compound according to claim 1.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1991-12-13 | 1992-06-13 | 1992-12-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1995-12-13 | 1996-06-13 | 1996-12-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1999-12-13 | 2000-06-13 | 2000-12-13 | $7700.00 | Window Closed / Lapsed |