Inhibitors of thrombin

Details Inhibitors of thrombin Inhibitors of thrombin

C - Chemistry, Metallurgy

07

K

C07K 7/00 (2006.01) A61K 38/04 (2006.01) A61L 33/00 (2006.01) C07K 5/00 (2006.01) C07K 5/107 (2006.01) C07K 14/815 (2006.01) A61K 38/00 (2006.01) A61K 49/02 (1990.01)

Patent

CA 2079778

This invention relates to novel biologically active molecules which bind to and inhibit thrombin. These molecules comprise a catalytic site directed moiety (CSDM) of formula (I), wherein X is hydrogen or is characterized by a backbone chain consisting of from 1 to 100 at ~~~ R1 is selected from the group consisting of unsubstituted, mono-substituted, di-substituted and tri- substituted satura~~~ing structures; R2 is a bond or is characterized by a backbone chain consisting of from 1 to 5 atoms; R3 is a bond or is characterized by a backbone chain consisting of from 1 to 3 atoms; R4 is any amino acid; R5 is any L-ami- no acid which comprises a guanidinium- or amino-containing side chain group; R6 is a non-amide bond; and Y is charac- terized by a backbone chain consisting of from 1 to 9 atoms; or the formula (II), wherein R1 is selected from the group con- sisting of unsubstituted, mono-substituted, di-substituted and tri-substituted ring structures; R4' is any amino acid compris- ing a side chain group characterized by the capacity to accept a hydrogen bond at a pH of between about 5.5 and 9.5; and X, R2, R3, R5, R6 and Y are defined as above. Preferred thrombin inhibitors are further characterized by an anion binding exosite associating domain (ABEAM) and a linker portion of between 18.ANG. and 42.ANG. in length which connects the Y to the ABEAM. This invention also relates to compositions, combinations and methods which employ these molecules for therap- eutic, prophylactic and diagnostic purposes.

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