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US3969518A
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Inhibiting xanthine oxidase with 3-haloalkyl substituted benzothiadiazine-1,1-dioxides
Assignee: Merck and Co Inc
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Filing: 1972-05-24
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Granted: 1976-07-13
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Expires: 1992-05-24
Abstract
Abstract Method for decreasing the concentration of uric acid in the blood and urine of a mammal by the administration of a 3-haloalkyl-1,2,4-benzothiadiazine-1,1-dioxide product or 3,4-dihydro derivative thereof. The products employed in this method of treatment are prepared by conventional methods employing the appropriate orthanilamide and haloalkanoic acid halide or carboxaldehyde. The products effect the lowering of the uric acid level by virtue of their xanthine oxidase inhibiting properties.
Inventors
- 👤 Frederick C. Novello
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-09 06:46
CPC Classifications
C; C07; C07D; C07D285/00; C07D285/15; C07D285/16; C07D285/18; C07D285/20; C07D285/22; C07D285/24; C07D285/26; C07D285/30
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
102 words
A method for inhibiting the action of xanthine oxidase in a mammal having an elevated blood uric acid level by orally administering to said mammal a dose sufficient to lower the blood uric acid level to normal for that species of a xanthine oxidase inhibitor selected from the group consisting of structure I and structure II: ##SPC2## or sodium or potassium salt thereof wherein R represents hydrogen, C 1-3 alkyl or allyl; R 1 represents hydrogen, C 1-3 alkyl or allyl; X represents halogen or trifluoromethyl; Y represents hydrogen, chloro or bromo; and R 2 represents mono- or polyhalo C 1-5 alkyl.
Claim 2
Independent Claim
102 words
A method for inhibiting the action of xanthine oxidase in a mammal having an elevated blood uric acid level by orally administering to said mammal a dose sufficient to lower the blood uric acid level to normal for that species of a xanthine oxidase inhibitor selected from the group consisting of structure I and structure II: ##SPC2## or sodium or potassium salt thereof wherein R represents hydrogen, C 1-3 alkyl or allyl; R 1 represents hydrogen, C 1-3 alkyl or allyl; X represents halogen or trifluoromethyl; Y represents hydrogen, chloro or bromo; and R 2 represents mono- or polyhalo C 1-5 alkyl.
Claim 3
Dependent Claim
14 words
The method of claim 1 wherein an active product having structure I is employed.
Claim 4
Dependent Claim
21 words
The method of claim 2 wherein in the product of structure I R and R 1 are each C 1-3 alkyl.
Claim 5
Dependent Claim
27 words
The method of claim 2 wherein the product of structure I R and R 1 each represent C 1-3 alkyl, X is chloro and Y is hydrogen.
Claim 6
Dependent Claim
32 words
The method of claim 2 wherein in the product of structure I R and R 1 each represent C 1-3 alkyl, X is chloro, Y is hydrogen and R 2 is chloromethyl.
Claim 7
Dependent Claim
11 words
The method of claim 2 wherein the active product is 3-chloromethyl-6-chloro-7-dimethylsulfamoyl-1,2,4-benzothiadiazine-1,1-dioxide.
Claim 8
Dependent Claim
19 words
The method of claim 2 wherein in the product of structure I X is trifluoromethyl and Y is hydrogen.
Claim 9
Dependent Claim
32 words
The method of claim 2 wherein in the product of structure I R and R 1 each represent C 1-3 alkyl, X is trifluoromethyl, Y is hydrogen and R 2 is chloromethyl.
Claim 10
Dependent Claim
11 words
The method of claim 2 wherein the active product is 3-chloromethyl-6-trifluoromethyl-7-dimethylsulfamoyl-1,2,4-benzothiadiazine-1,1-dioxide.
Claim 11
Dependent Claim
11 words
The method of claim 2 wherein the active product is 3-chloromethyl-6-trifluoromethyl-7-sulfamoyl-1,2,4-benzothiadiazine-1,1-dioxide.
Claim 12
Dependent Claim
14 words
The method of claim 1 wherein an active product having structure II is employed.
Claim 13
Dependent Claim
19 words
The method of claim 11 wherein in the product having structure II, X is chloro and Y is hydrogen.
Claim 14
Dependent Claim
28 words
The method of claim 11 wherein in the product having structure II, X is chloro, Y is hydrogen, R is C 1-3 alkyl and R 1 is hydrogen.
Claim 15
Dependent Claim
11 words
The method of claim 11 wherein the active product is 3-trichloromethyl-6-chloro-7-ethylsulfamoyl-3,4-dihydro-1,2,4-benzothiadiazine-1,1-dioxide.
Claim 16
Dependent Claim
19 words
The method of claim 11 wherein in the product of structure II, X is trifluoromethyl and Y is hydrogen.
Claim 17
Dependent Claim
11 words
The method of claim 11 wherein the active product is 3-chloromethyl-6-trifluoromethyl-7-sulfamoyl-3,4-dihydro-1,2,4-benzothiadiazine-1,1-dioxide.
Claim 18
Dependent Claim
24 words
The method of claim 1 wherein from about 100 to 800 milligrams per day of the xanthine oxidase inhibitor is administered in divided doses.
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) | 1979-07-13 | 1980-01-12 | 1980-07-13 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1983-07-13 | 1984-01-12 | 1984-07-13 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1987-07-13 | 1988-01-12 | 1988-07-13 | $7700.00 | Window Closed / Lapsed |