US4500540A
Expired / Lapsed
US
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Thromboxane synthase inhibitors as insulin lowering agents and antionbesity agents
Assignee: Hoffmann La Roche Inc
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Filing: 1982-06-11
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Granted: 1985-02-19
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Expires: 2002-06-11
Abstract
Abstract The present disclosure relates to the use of thromboxane synthase inhibitors as antiobesity agents and insulin lowering agents. Such compounds fall into a variety of classes among which are 1-substituted imidazoles, 4-substituted imidazoles, 3-substituted pyridines, 3-substituted indoles, 4-substituted pyrimidines, 5-substituted tetrazoles, pyrazolidines, quinazolines, and substituted xanthene carboxylic acids.
Inventors
- 👤 James G. Hamilton
- 👤 Ann C. Sullivan
- 👤 Lawrence D. Tobias
- 👤 Joseph Triscari
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-29 09:50
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/40; A61K31/38; A61K31/41; A61K31/415; A61K31/435; A61K31/44; A61K31/495; A61K31/505
Claims Analysis
Total Claims: 35
Claim 1
Independent Claim
115 words
A method for reducing body weight in obese mammals which comprises orally administering, to the mammal to be treated, an amount effective for reducing body weight of a thromboxane synthase inhibitor of the formula: ##STR6## wherein R is H, NO 2 , or --C 2 -C 4 alkenyl; R 1 is H, C 1 -C 11 alkyl, acetyl, propionyl, butyryl, phenyl, phenyl substituted by one or two substituents independently selected from the group consisting of C 1 -C 3 alkoxy, C 1 -C 4 alkyl, Cl, F, Br, NO 2 , acetyl, propionyl, butyryl or hydroxy, phenylalkyl, or 3-indolo optionally substituted at the two position by C 1 -C 4 straight or branched chain alkyl.
Claim 2
Independent Claim
115 words
A method for reducing body weight in obese mammals which comprises orally administering, to the mammal to be treated, an amount effective for reducing body weight of a thromboxane synthase inhibitor of the formula: ##STR6## wherein R is H, NO 2 , or --C 2 -C 4 alkenyl; R 1 is H, C 1 -C 11 alkyl, acetyl, propionyl, butyryl, phenyl, phenyl substituted by one or two substituents independently selected from the group consisting of C 1 -C 3 alkoxy, C 1 -C 4 alkyl, Cl, F, Br, NO 2 , acetyl, propionyl, butyryl or hydroxy, phenylalkyl, or 3-indolo optionally substituted at the two position by C 1 -C 4 straight or branched chain alkyl.
Claim 3
Dependent Claim
22 words
The method of claim 1 wherein R is H, R 1 is C 1 -C 9 alkyl or para substituted phenyl hydroxy.
Claim 4
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 4-(1H-imidazol-1-yl)phenol.
Claim 5
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 3-(1H-imidazol-1-ylmethyl)-1H-indole.
Claim 6
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-[2-(1-methylethyl)phenyl]-1H-imidazole.
Claim 7
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-[4-(1H-imidazol-1-yl)phenyl]ethanone.
Claim 8
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 3-(1H-imidazol-1-yl)phenol.
Claim 9
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-[4-(1-methylethoxy)phenyl]-1H-imidazole.
Claim 10
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-(4-ethoxyphenyl)-1H-imidazole.
Claim 11
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-nonyl-1H-imidazole.
Claim 12
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-butyl-1H-imidazole.
Claim 13
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-(triphenylmethyl)-1H-imidazole.
Claim 14
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-(phenylmethyl)-1H-imidazole.
Claim 15
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-(beta-D-glucopyranosyl)-1H-imidazole.
Claim 16
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-[(2-chlorophenyl)diphenylmethyl]-1H-imidazole.
Claim 17
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-(4-methoxyphenyl)-1H-imidazole.
Claim 18
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1,1'-carbonothioylbis-1H-imidazole.
Claim 19
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-[2,4-dinitrophenyl]1H-imidazole.
Claim 20
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-(4-nitrophenyl)-1H-imidazole.
Claim 21
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1H-imidazole.
Claim 22
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-[2-(2,4-dichlorophenyl)-2-[(2,4-dichlorophenyl)methoxy]ethyl]-1H-imidazole.
Claim 23
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-acetyl-1H-imidazole.
Claim 24
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-ethyl-1H-imidazole.
Claim 25
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-[[(5-nitro-2-furanyl)methylene]amino]-2,4-imidazolidinedione.
Claim 26
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1-methyl-1H-imidazole.
Claim 27
Dependent Claim
15 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 3-(1H-imidazol-4-yl)-2-propenoic acid methyl ester.
Claim 28
Dependent Claim
12 words
The method of claim 1 wherein said thromboxane synthase inhibitor is 1H-4-nitroimidazole.
Claim 29
Dependent Claim
22 words
The method of claim 1 wherein said thromboxane synthase inhibitor is administered in dosages ranging from 0.1-200 mg per kg per day.
Claim 30
Dependent Claim
22 words
The method of claim 1 wherein said thromboxane synthase inhibitor is administered in dosages ranging from 0.1-50 mg per kg per day.
Claim 31
Dependent Claim
22 words
The method of claim 1 wherein said thromboxane synthase inhibitor is administered in dosages ranging from 0-10 mg per kg per day.
Claim 32
Dependent Claim
105 words
An oral composition for reducing body weight in obese mammals which comprises a pharmaceutically-acceptable carrier material and an amount effective for reducing body weight of a compound of the formula: ##STR7## wherein R is H, NO 2 , or C 2 -C 4 alkenyl; R 1 is H, acetyl, propionyl, butyryl, phenyl, phenyl substituted by one or two substituents independently selected from the group consisting of C 1 -C 3 alkoxy, C 1 -C 4 alkyl, Cl, F, Br, NO 2 , acetyl, propionyl, butyryl, or hydroxy, or 3-indolo optionally substituted at the two position by C 1 -C 4 straight or branched chain alkyl.
Claim 33
Dependent Claim
105 words
An oral composition for reducing body weight in obese mammals which comprises a pharmaceutically-acceptable carrier material and an amount effective for reducing body weight of a compound of the formula: ##STR7## wherein R is H, NO 2 , or C 2 -C 4 alkenyl; R 1 is H, acetyl, propionyl, butyryl, phenyl, phenyl substituted by one or two substituents independently selected from the group consisting of C 1 -C 3 alkoxy, C 1 -C 4 alkyl, Cl, F, Br, NO 2 , acetyl, propionyl, butyryl, or hydroxy, or 3-indolo optionally substituted at the two position by C 1 -C 4 straight or branched chain alkyl.
Claim 34
Dependent Claim
15 words
A composition in accordance with claim 31, wherein the compound of formula I is 1-[4-(1H-imidazol-1-yl)phenyl]ethanone.
Claim 35
Dependent Claim
15 words
A composition in accordance with claim 31, wherein the compound of formula I is 3-(1H-imidazol-1-ylmethyl)-1H-indole.
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USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1988-02-19 | 1988-08-20 | 1989-02-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1992-02-19 | 1992-08-20 | 1993-02-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1996-02-19 | 1996-08-20 | 1997-02-19 | $7700.00 | Window Closed / Lapsed |