US5500439A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Aminopyrazoles
Assignee: Synvista Therapeutics Inc
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Filing: 1993-12-09
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Granted: 1996-03-19
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Expires: 2013-12-09
Abstract
Abstract The present invention relates to compounds, compositions and methods for inhibiting nonenzymatic cross-linking (protein aging). Accordingly, a composition is disclosed which comprises aminopyrazoles capable of inhibiting the formation of advanced glycosylation endproducts of target proteins by reacting with the carbonyl moiety of an early glycosylation product of such target proteins formed by their initial glycosylation. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
Inventors
- 👤 Peter C. Ulrich
- 👤 Dilip R. Wagle
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-31 23:30
CPC Classifications
A; A61; A61K; A61K31/00; A61K31/33; A61K31/395; A61K31/41; A61K31/415
Claims Analysis
Total Claims: 20
Claim 1
Independent Claim
89 words
A method for inhibiting the advanced glycosylation of a target protein comprising contacting the target protein with an effective amount of composition comprising a compound selected from the group consisting of compounds of the formula ##STR10## wherein R is hydrogen, a lower alkyl or hydroxy lower alkyl group; R 1 is hydrogen, hydroxy a lower alkoxy group, a lower alkyl group or an aryl group; R 2 is hydrogen or an amino group; and their biologically or pharmaceutically acceptable acid addition salts; and mixtures thereof, and a carrier therefor.
Claim 2
Independent Claim
89 words
A method for inhibiting the advanced glycosylation of a target protein comprising contacting the target protein with an effective amount of composition comprising a compound selected from the group consisting of compounds of the formula ##STR10## wherein R is hydrogen, a lower alkyl or hydroxy lower alkyl group; R 1 is hydrogen, hydroxy a lower alkoxy group, a lower alkyl group or an aryl group; R 2 is hydrogen or an amino group; and their biologically or pharmaceutically acceptable acid addition salts; and mixtures thereof, and a carrier therefor.
Claim 3
Dependent Claim
16 words
The method of claim 1 wherein said compound has the formula wherein R 2 is hydrogen.
Claim 4
Dependent Claim
16 words
The method of claim 2 wherein said compound is 3-amino-5-hydroxypyrazole or a biologically acceptable salt thereof.
Claim 5
Dependent Claim
18 words
The method of claim 1 wherein said compound has the formula wherein R 2 is an amino group.
Claim 6
Dependent Claim
19 words
The method of claim 4 wherein said compound is 3,4-diamino-5-hydroxypyrazole sulfate or another biologically acceptable acid addition salt thereof.
Claim 7
Dependent Claim
19 words
The method of claim 4 wherein said compound is 1-methyl-3-1hydroxy-4,5-diaminopyrazole sulfate or another biologically acceptable acid addition salt thereof.
Claim 8
Dependent Claim
18 words
The method of claim 4 wherein said compound is 1-(2-hydroxyethyl)-3-hydroxy-4,5-diaminopyrazole sulfate or another biologically acceptable acid addition salt.
Claim 9
Dependent Claim
19 words
The method of claim 4 wherein said compound is 1-(2-hydroxypropyl)-3-hydroxy-4,5-diaminopyrazole sulfate or another biologically acceptable acid addition salt thereof.
Claim 10
Dependent Claim
19 words
The method of claim 4 wherein said compound is 1-(2-hydroxy-2-methylpropyl)-3-hydroxy-4,5-diaminopyrazole sulfate or another biologically acceptable acid addition salt thereof.
Claim 11
Independent Claim
100 words
A method for treating an animal to inhibit the formation of advanced glycosylation endproducts of a target protein within said animal, said method comprising administering an effective amount of a pharmaceutical composition, said pharmaceutical composition comprising a compound selected from the group consisting of compounds of the formula ##STR11## wherein R is hydrogen, a lower alkyl or hydroxy lower alkyl group; R 1 is hydrogen, hydroxy a lower alkoxy group, a lower alkyl group or an aryl group; R 2 is hydrogen or an amino group; and their pharmaceutically acceptable acid addition salts and mixtures thereof, and a carrier therefor.
Claim 12
Independent Claim
100 words
A method for treating an animal to inhibit the formation of advanced glycosylation endproducts of a target protein within said animal, said method comprising administering an effective amount of a pharmaceutical composition, said pharmaceutical composition comprising a compound selected from the group consisting of compounds of the formula ##STR11## wherein R is hydrogen, a lower alkyl or hydroxy lower alkyl group; R 1 is hydrogen, hydroxy a lower alkoxy group, a lower alkyl group or an aryl group; R 2 is hydrogen or an amino group; and their pharmaceutically acceptable acid addition salts and mixtures thereof, and a carrier therefor.
Claim 13
Dependent Claim
16 words
The method of claim 10 wherein said compound has the formula wherein R 2 is hydrogen.
Claim 14
Dependent Claim
17 words
The method of claim 11 wherein said compound is 3-amino-5-hydroxypyrazole sulfate or another pharmaceutically acceptable salt thereof.
Claim 15
Dependent Claim
18 words
The method of claim 12 wherein said compound has the formula wherein R 2 is an amino group.
Claim 16
Dependent Claim
19 words
The method of claim 13 wherein said compound is 3,4-diamino-5-hydroxypyrazole sulfate or another pharmaceutically acceptable acid addition salt thereof.
Claim 17
Dependent Claim
19 words
The method of claim 13 wherein said compound is 1-methyl-3-hydroxy-4,5-diaminopyrazole sulfate or another pharmaceutically acceptable acid addition salt thereof.
Claim 18
Dependent Claim
18 words
The method of claim 13 wherein said compound is 1-(2-hydroxyethyl)-3-hydroxy-4,5-diaminopyrazole sulfate or another biologically acceptable acid addition salt.
Claim 19
Dependent Claim
19 words
The method of claim 4 wherein said compound is 1-(2-hydroxypropyl)-3-hydroxy-4,5-diaminopyrazole sulfate or another pharmaceutically acceptable acid addition salt thereof.
Claim 20
Dependent Claim
19 words
The method of claim 4 wherein said compound is 1-(2-hydroxy-2-methylpropyl)-3-hydroxy-4,5-diaminopyrazole sulfate or another pharmaceutically acceptable acid addition salt thereof.
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| 3.5 Years (Year 4) | 1999-03-19 | 1999-09-18 | 2000-03-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 2003-03-19 | 2003-09-18 | 2004-03-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 2007-03-19 | 2007-09-18 | 2008-03-19 | $7700.00 | Window Closed / Lapsed |