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US 5,843,900 AGranted
Bradykinin antagonists
AssigneeCortech, Inc.
InventorsJohn C. Cheronis, Albert Gyorkos, Lyle W. Spruce, Eric T. Whalley
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Abstract
The present invention relates to pharmaceutically effective heterodimers comprising a bradykinin antagonist component covalently linked to a mu-opioid agonist component.
Claims21
A heterodimer of the formula:
- (BKAn)(X)(Y)
- where BKAn is a bradykinin antagonist peptide selected from:
- DArg.sup.0 -Arg.sup.1 -Pro.sup.2 -Hyp.sup.3 -Gly.sup.4 -Iglb.sup.5 -Ser.sup.6 -DIglb.sup.7 -Oic.sup.8 -Arg.sup.9 ;
- DArg.sup.0 -Arg.sup.1 -Pro.sup.2 -Hyp.sup.3 -Gly.sup.4 -Thi.sup.5 -Ser.sup.6 -DIglb.sup.7 -Oic.sup.8 -Arg.sup.9 ;
- DArg.sup.0 -Arg.sup.1 -Pro.sup.2 -Hyp.sup.3 -Gly.sup.4 -Iglb.sup.5 -Ser.sup.6 -D-Tic.sup.7 -NChg.sup.8 -Arg.sup.9 ;
- or an analog thereof, said analog comprising an L-Arg or L-Lys in the 0-position or a D- or L-Lys in the 0-6 position of said peptide;
- Y is dihydromorphine or morphine;
- and
- X is a linker;
- where X is attached to said BKAn peptide via the 0, 1, 2, 3, 5 or 6 position amino acid residue of said peptide;
- wherein said heterodimer retains bradykinin antagonist activity.
8 more elements
A heterodimer of the formula:
- (BKAn)(X)(Y)
- where BKAn is a bradykinin antagonist peptide;
- Y is fentanyl;
- and
- X is a linker;
- where X is attached to said BKAn peptide via the 0, 1, 2, 3, 5 or 6 position amino acid residue of said peptide;
- wherein said heterodimer retains bradykinin antagonist activity.
4 more elements
Dependencies are inferred from the claim text.