Thrombin inhibitors based on the amino acid sequence of hirudin

Details Thrombin inhibitors based on the amino acid sequence of hirudin Thrombin inhibitors based on the amino acid sequence of hirudin

C - Chemistry, Metallurgy

12

P

C12P 7/62 (2006.01) A61K 38/58 (2006.01) C07C 69/593 (2006.01) C07C 311/64 (2006.01) C07K 7/02 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) C07K 14/815 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2085465

A thrombin inhibitor comprising a first bulky hydrophobic portion interacting with the catalytic sits of thrombin responsi- ble for proteolysis and a second portion at least maintaining the hydrophobic and acidic character of amino acids 55 to 60 of na- tive hirudin at the C-terminal non-catalytic region of N-acetyl-hirudin45-65. Between the first and second portions is a divalent linker moiety having a chain length of at least 10 carbon atomes. Preferably, the bulky hydrophobic portion comprises at least one amino acid of D-configuration. The compounds are useful in the treatment of thrombotic disorders.

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