Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – 15 to 23 amino acid residues in defined sequence
Patent
1995-03-20
1999-02-02
Tsang, Cecilia J.
Chemistry: natural resins or derivatives; peptides or proteins;
Peptides of 3 to 100 amino acid residues
15 to 23 amino acid residues in defined sequence
530330, 530328, 514 13, 514 18, A61K 3804, C07K 500
Patent
active
058666818
ABSTRACT:
Peptide derivatives serving as thrombin receptor antagonists are disclosed, which bear specificity for the cellular thrombin receptor without interfering with the catalytic activities of thrombin. The derivatives generally have the formula ##STR1## in which R.sup.1 and R.sup.3 are amide linkages, N-alkylamide linkages, or isosteric replacements of such linkages; R.sup.2 is either a neutral amino acid side chain or a hydrophobic radical; R.sup.4 is hydrophobic radical; R.sup.5 is CO, CH.sub.2 or SO; X is either of the formula: ##STR2## in which R.sup.6 and R.sup.7 are H, alkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl or arylalkyl, and R.sup.8 is a hydrophobic radical, or a hydrophobic residue; Y is alkoxy, hydroxy, amino, alkylamino, dialkylamino, in which any of the alkyl groups may be substituted with a basic moiety; Z is an amino acid or peptide residue; and m is zero or one.
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Celsa Bennett
COR Therapeutics Inc.
Tsang Cecilia J.
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