C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 14/815 (2006.01) A61K 38/58 (2006.01) C08L 25/06 (2006.01) C08L 23/08 (2006.01) C08L 25/08 (2006.01)
Patent
CA 2305380
The present invention relates to a new thrombin inhibitor of formula (I) comprising an S subsite blocking segment (AS), an S' subsite blocking segment (Z), and a fibrinogen recognition exosite blocking segment (P). AS is linked to Z, which is linked to P according to the formula (1): AS-Z-P . The S' subsite blocking segment thus, besides binding to the thrombin S' subsites, connects the S subsite blocking segment and the fibrinogen recognition exosite blocking segment. This binding of Z segment together with the bindings of the AS and P segments, contributes to improve the affinity of the inhibitors significantly.
La présente invention concerne un nouvel inhibiteur de la thrombine qui correspond à la formule (I) et est constitué d'un segment de blocage (AS) du site secondaire S, d'un segment de blocage (Z) du site secondaire S' et d'un segment de blocage (P) de l'exosite de reconnaissance du fibrinogène. AS est lié à Z qui est, à son tour, lié à P conformément à la formule (1): AS-Z-P De cette manière, le segment de blocage du site secondaire S' se lie non seulement aux sites secondaires S' de la thrombine mais relie également le segment de blocage du site secondaire S au segment de blocage de l'exosite de reconnaissance du fibrinogène. Cette liaison du segment Z, combinée aux liaisons des segments AS et P, contribue à améliorer de façon appréciable l'affinité des inhibiteurs.
Konishi Yasuo
Slon Jacek
National Research Council Of Canada
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
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