Thrombin inhibitors based on the amino acid sequence of hirudin

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 14/815 (2006.01) A61K 38/58 (2006.01) C07K 7/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2215702

A thrombin inhibitor comprising a first bulky hydrophobic portion interacting with the catalytic side of thrombin responsible for proteolysis and a second portion maintaining the hydrophobic and acidic character of amino acids 55 to 60 of native hirudin at the C-terminal non-catalytic region of N-acetyl- hirudin45-65. Between the first and second portions is a divalent linker moiety. The compound is useful in the treatment of thrombotic disorders.

La présente invention concerne un inhibiteur de thrombine comprenant une première partie hydrophobe volumineuse en interaction avec le site catalytique de la thrombine responsable de la protéolyse, et une deuxième partie qui maintient le caractère hydrophobe et acide des acides aminés 55 à 60 de l'hirudine naturelle dans la région non catalytique terminale de C de la N-acétyl-hirudine 45-65. Entre la première et la deuxième parties, il y a une portion de liaison bivalente. Ce composé convient particulièrement au traitement des perturbations thrombotiques.

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