Method and composition for treating thrombosis

Details Method and composition for treating thrombosis Method and composition for treating thrombosis

C - Chemistry, Metallurgy

12

Q

C12Q 1/56 (2006.01) A61K 38/08 (2006.01) A61K 38/10 (2006.01) A61K 38/16 (2006.01) C07K 4/00 (2006.01) C07K 7/02 (2006.01) C07K 7/06 (2006.01) C07K 7/08 (2006.01) C07K 7/54 (2006.01) C07K 7/64 (2006.01) C07K 14/00 (2006.01) C07K 14/705 (2006.01) C07K 14/75 (2006.01) G01N 33/86 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2165332

The invention provides cyclic peptides which inhibit platelet aggregation without causing prolonged bleeding time. The invention provides RGD or KGD containing peptides which are cyclized and contain hydrophobic amino acids adjacent to the carboxy terminus of the RGD sequence. Peptides of this nature are also provided which contain in addition to the hydrophobic amino acid an adjacent positively charged amino acid. Such peptides have a high affinity for the receptor IIb/IIIa and a low affinity for the fibronectin and vitronectin receptors. Such peptides can be administered in a suitable physiologically acceptable carrier to therapeutically treat thrombosis.

L'invention concerne des peptides cycliques qui inhibent l'agrégation plaquettaire sans provoquer un temps de saignement prolongé. L'invention concerne des peptides contenant des séquences RGD ou KGD qui sont cyclisés et qui contiennent des acides aminés hydrophobes attenants à la terminaison carboxy de la séquence RGD. Les peptides de cette nature contiennent, en plus de l'acide aminé hydrophobe, un acide aminé avoisinant chargé positivement. Ces peptides ont une haute affinité pour le récepteur IIb/IIIa et une faible affinité pour les récepteurs de la fibronectine et la vitronectine. Ces peptides peuvent être administrés dans un excipient approprié physiologiquement acceptable pour traiter thérapeutiquement la thrombose.

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