Thrombin receptor antagonists

Details Thrombin receptor antagonists Thrombin receptor antagonists

C - Chemistry, Metallurgy

07

K

C07K 7/00 (2006.01) A61K 38/04 (2006.01) C07K 5/04 (2006.01) C07K 5/065 (2006.01) C07K 5/107 (2006.01) C07K 7/02 (2006.01) C07K 7/06 (2006.01) C12N 9/64 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2140543

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 formula (I) in which R1 and R3 are amide linkages, N-alkylamide linkages, or isosteric replacements of such linkages; R2 is either a neutral amino acid side chain or a hydrophobic radical; R4 is hydrophobic radical; R5 is CO, CH2 or SO; X is either of formula (II) in which R6 and R7 are H, alkyl, cycloalkylalkyl, alkoxyalkyl, alkylthioalkyl or arylalkyl, and R8 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.

Dérivés de peptides, servant d'antagonistes de récepteurs de la thrombine, qui possèdent une spécificité pour le récepteur de la thrombine cellulaire, sans interférer dans les activités catalytiques de la thrombine. Lesdits dérivés présentent généralement la formule (I) dans laquelle R1 et R3 sont des liaisons amides, des liaisons N-alkylamide ou des remplacements isostériques de telles liaisons; R2 est soit une chaîne latérale d'acide aminé neutre, soit un radical hydrophobe; R4 est un radical hydrophobe; R5 est CO, CH2 ou SO; X est soit de la formule (II) dans laquelle R6 et R7 sont H, alkyle, cycloalkylalkyle, alcoxyalkyle, alkylthioalkyle ou arylalkyle et R8 est un radical hydrophobe, soit un reste hydrophobe; Y est alcoxy, hydroxy, amino, alkylamino, dialkylamino dans lesquels tout groupe alkyle peut être substitué par une fraction basique; Z est un reste d'acide aminé ou de peptide; et m est zéro ou un.

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