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US 6,610,852 B2Granted
Post-Amadori inhibitors of advanced glycation reactions
AssigneeKansas University Medical Center
InventorsRaja Khalifah, Aaron Ashley Booth
Life of this patent
Estimating the term…
Abstract
The present invention provides novel compounds, pharmaceutical compositions, methods, and kits for inhibiting the conversion of Amadori compounds to post Amadori advanced glycation endproducts, and for treating and preventing chronic tissue damage and diabetic complication.
Claims5
A compound of the formula
- wherein R1, R1′, R5, and R5′ are independently selected from the group consisting of (CH2)nX wherein n is between 0 and 6 and X is H, OH, SH, COOH or NH2;
- and mono-, di-, or tri-halogenated C1-6 alkyl, C 1-6 alkoxy, or C 1-6 alkenyl;
- with the proviso that at least one R1, R1′, R5, and R5′ is selected from the group consisting of OH, SH, and NH2;
- wherein R2, R2′, R4 and R4′ are independently selected from the group consisting of (CH2)nZ, wherein n has the meaning given above and Z is H, OH, SH, COOH, or NH2;
- and mono-, di-, or tri-halogenated C1-6 alkyl, C 1-6 alkoxy, or C 1-6 alkenyl;
- wherein R3 and R3′ are independently selected from the group consisting of H and mono-, di-, or tri-halogenated C1-6 alkyl, or are absent;
- wherein R6 and R6′ are (CH2)x, wherein x is between 1 and 6;
- wherein R7 is selected from NH and HOP═O;
- or wherein R6, R6′, and R7 combine to form an aryl group, heteroaryl group, or
- or a pharmaceutically acceptable salt thereof;
- wherein the compound is not dipyridoxylamine;
- and
- wherein if R7 is NH, R6 and R6′ are CH2, and one of R5 or R5′ is OH, then the other of R5 and R5′ is selected from the group consisting of (CH2)nX wherein n is between 0 and 1 and X is H, OH, SH, COOH or NH2;
- and mono-, di-, or tri-halogenated C 1-6 alkoxy, or C 1-6 alkenyl.
11 more elements
Dependencies are inferred from the claim text.