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US 6,747,127 B1Granted
Substituted heterocyclic acyl-tripeptides useful as thrombin receptor modulators
AssigneeOrtho-McNeil Pharmaceutical, Inc.
InventorsDavid F. McComsey, Bruce E. Maryanoff, Michael J. Hawkins
Life of this patent
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Abstract
The invention is directed to substituted heterocyclic acyl-tripeptides useful as thrombin receptor modulators, their use in wound healing and preventing platelet aggregation. Pharmaceutical compositions comprising the substituted heterocyclic acyl-tripeptides of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
Claims9
A compound represented by the general formula (I):
- wherein A1 is an amino acid residue selected from the group consisting of cyclohexylalanine, Leu, Ile, Arg, Lys, Phe, substituted Phe, Tyr and Trp;
- A2 is an amino acid residue selected from the group consisting of Lys, Orn, Arg, and homo Arg;
- A3 is an amino acid residue selected from the group consisting of Phe, substituted Phe, homo Phe, Tyr, Trp, phenylglycine, 2-thienylalanine, 3-thienylalanine, cyclohexylalanine, Leu, Ile, Asn, Gin, Arg, homo Arg, Orn and Lys;
- X is selected from the group consisting of CO, CS, and SO2;
- Y is selected from the group consisting of aryl, substituted aryl, heterocycloalkyl, substituted heterocycloalkyl, heteroaryl, substituted heteroaryl, heteroarylethylenyl, substituted heteroarylethylenyl, arylacrylamidoheteroaryl, substituted arylacrylamidoheteroaryl, heteroarylacrylamidoheteroaryl and substituted heteroarylacrylamidoheteroaryl, provided that Y is not pyrrolidinyl, phenyl or 2-aminophenyl;
- Z is selected from the group consisting of NH2, NH-alkyl, NH-aralkyl, and Arg-NH2;
- and
- wherein all amino acids are of the L configuration;
- and any pharmaceutically acceptable salt thereof.
6 more elements
Dependencies are inferred from the claim text.