Bifunctional inhibitors of thrombin and platelet activation

C - Chemistry – Metallurgy – 12 – N

Patent

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Details

C12N 15/62 (2006.01) A61K 38/48 (2006.01) A61K 38/58 (2006.01) C07K 14/245 (2006.01) C07K 14/46 (2006.01) C07K 14/815 (2006.01) C07K 19/00 (2006.01) C12N 1/21 (2006.01) C12N 15/15 (2006.01) C12N 15/31 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2096545

2096545 9210575 PCTABS00013 The present invention relates to novel, bifunctional inhibitors of both platelet activation and thrombin. These bifunctional inhibitors are characterized by two domains - a glycoprotein IIb/IIIa inhibitory domain and a thrombin inhibitory domain. The invention also relates to DNA sequences which encode the bifunctional inhibitors of this invention, recombinant DNA molecules which contain these DNA sequences and host transformed with these DNA molecules. The invention further relates to the recombinant expression of the bifunctional inhibitors of this invention by transformed hosts as well as to methods for purifying such recombinant bifunctional inhibitors. This invention also provides compositions and methods employing the novel bifunctional inhibitors alone or together with a fibrinolytic agent. Such compositions may be useful in patients for treating thrombotic disease, increasing reocclusion time, decreasing reperfusion time, simultaneously inhibiting thrombin- and platelet-mediated functions and inhibiting malignant cell growth.

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