Anticoagulant peptidyl-arginine aldehyde derivatives

Details Anticoagulant peptidyl-arginine aldehyde derivatives Anticoagulant peptidyl-arginine aldehyde derivatives

C - Chemistry, Metallurgy

07

K

C07K 5/083 (2006.01) A61K 38/06 (2006.01) C07K 5/065 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2256391

The invention relates to new peptidyl-arginine aldehyde derivatives of general formula (1): Q-D-Xaa-Pro-Arg-H, wherein Q represents an acyl group of formula Q'-O-CO-, where Q' represents an alkyl group with 1-3 carbon atoms, D-Xaa represents 3-cyclobutyl-D-alanyl- or 3-cyclo-pentyl-D-alanyl- group, Pro stands for L-prolyl- group, and Arg stands for L-arginyl- group, and acid-addition salts thereof formed with an organic or inorganic acid and pharmaceutical compositions containing the same. The compounds of formula (I) have valuable therapeutic, particularly anticoagulant, properties together with inhibiting platelet functions and thrombosis development.

L'invention concerne des nouveaux dérivés de peptidyl-arginine aldéhyde de formule générale (I) Q-D-Xaa-pro-Arg-H, et leurs sels d'addition d'acide formés avec un acide organique ou inorganique. Dans ladite formule (I), Q représente un groupe acyle de formule Q'-O-CO-, où Q' représente un groupe alkyle à 1 à 3 atomes de carbone, D-Xaa représente un groupe 3-cyclobutyl-D-alanyl- ou 3-cyclo-pentyl-D-alanyl-, Pro représente un groupe L-propyl-, et Arg un groupe L-arginyl-. Elle porte aussi sur des compositions pharmaceutiques les contenant. Les composés de formule (I) présentent des propriétés thérapeutiques précieuses, en particulier anticoagulantes, inhibent les fonctions des plaquettes et le développement de la thrombose.

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