Patent US4542158A successfully refreshed from Google Patents.
US4542158A
Expired / Lapsed
US
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Prodrug esters of diflunisal and related compounds
Assignee: Merck and Co Inc
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Filing: 1982-10-25
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Granted: 1985-09-17
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Expires: 2002-10-25
Abstract
Abstract 1-(Alkoxy or aroxy)carbonyloxyalkyl esters of diflunisal and related compounds are stable in aqueous medium and non-irritant to mucous membranes of mouth, throat, and stomach. Accordingly, they are useful Prodrugs of the analgesic and anti-inflammatory drug, diflunisal.
Inventors
- 👤 Conrad P. Dorn
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 11:42
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/21; A61K31/265; C; C07; C07C; C07C69/00; C07C69/96
Claims Analysis
Total Claims: 9
Claim 1
Independent Claim
60 words
A compound of structural formula (I): ##STR11## wherein: R is (a) C 1-6 alkyl; or (b) C 3-6 cycloalkyl; R 1 is (a) hydrogen; (b) C 1-6 alkyl; or (c) C 3-6 cycloalkyl; R 2 is (a) hydrogen; (b) C 1-6 alkanoyl; (c) C 1-6 alkoxycarbonyl; R 3 is (a) hydrogen; or (b) C 1-6 alkyl; and X is halo.
Claim 2
Dependent Claim
60 words
A compound of structural formula (I): ##STR11## wherein: R is (a) C 1-6 alkyl; or (b) C 3-6 cycloalkyl; R 1 is (a) hydrogen; (b) C 1-6 alkyl; or (c) C 3-6 cycloalkyl; R 2 is (a) hydrogen; (b) C 1-6 alkanoyl; (c) C 1-6 alkoxycarbonyl; R 3 is (a) hydrogen; or (b) C 1-6 alkyl; and X is halo.
Claim 3
Dependent Claim
26 words
The compound of claim 1 having the structural formula: ##STR12## wherein R is (a) C 1-6 alkyl; and R 1 is hydrogen or C 1-6 alkyl.
Claim 4
Dependent Claim
10 words
The compound of claim 1 having the structural formula: ##STR13##
Claim 5
Dependent Claim
81 words
A pharmaceutical composition for treating and/or controlling inflammation, pain or fever in a mammal comprising a pharmaceutical carrier and an effective amount of a compound of formula: ##STR14## wherein: R is (a) C 1-6 alkyl; or (b) C 3-6 cycloalkyl; R 1 is (a) hydrogen; (b) C 1-6 alkyl; or (c) C 3-6 cylcoalkyl; R 2 is (a) hydrogen; (b) C 1-6 alkanoyl; (c) C 1-6 alkoxycarbonyl; R 3 is (a) hydrogen; or (b) C 1-6 alkyl; and X is halo.
Claim 6
Dependent Claim
81 words
A pharmaceutical composition for treating and/or controlling inflammation, pain or fever in a mammal comprising a pharmaceutical carrier and an effective amount of a compound of formula: ##STR14## wherein: R is (a) C 1-6 alkyl; or (b) C 3-6 cycloalkyl; R 1 is (a) hydrogen; (b) C 1-6 alkyl; or (c) C 3-6 cylcoalkyl; R 2 is (a) hydrogen; (b) C 1-6 alkanoyl; (c) C 1-6 alkoxycarbonyl; R 3 is (a) hydrogen; or (b) C 1-6 alkyl; and X is halo.
Claim 7
Independent Claim
83 words
A method of treating and/or controlling inflammation, pain and fever comprising the administration of a mammal in need of such treatment an effective amount of a compound of formula: ##STR15## wherein: R is (a) C 1-6 alkyl; or (b) C 3-6 cycloalkyl; R 1 is (a) hydrogen; (b) C 1-6 alkyl; or (c) C 3-6 cycloalkyl; R 2 is (a) hydrogen; (b) C 1-6 alkanoyl; (c) C 1-6 alkoxycarbonyl; R 3 is (a) hydrogen; or (b) C 1-6 alkyl; and X is halo.
Claim 8
Independent Claim
83 words
A method of treating and/or controlling inflammation, pain and fever comprising the administration of a mammal in need of such treatment an effective amount of a compound of formula: ##STR15## wherein: R is (a) C 1-6 alkyl; or (b) C 3-6 cycloalkyl; R 1 is (a) hydrogen; (b) C 1-6 alkyl; or (c) C 3-6 cycloalkyl; R 2 is (a) hydrogen; (b) C 1-6 alkanoyl; (c) C 1-6 alkoxycarbonyl; R 3 is (a) hydrogen; or (b) C 1-6 alkyl; and X is halo.
Claim 9
Dependent Claim
28 words
The method of claim 5 wherein the compound is of structural formula: ##STR16## wherein R is C 1-6 alkyl; and R 1 is hydrogen or C 1-6 alkyl.
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) | 1988-09-16 | 1989-03-18 | 1989-09-17 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-09-16 | 1993-03-18 | 1993-09-17 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-09-16 | 1997-03-18 | 1997-09-17 | $7700.00 | Window Closed / Lapsed |