Antithrombosis agents
AssigneeCOR Therapeutics, Inc.
InventorDavid Wolf
Life of this patent
Estimating the term…
Abstract
Analogs of Factor Xa (Factor Xai) which are inactive as proteases in the prothrombinase reaction are useful in treatment of diseases characterized by thrombosis. These antithrombotic agents can be conveniently prepared using recombinant techniques.
Claims10
A two chain Factor Xai peptide modified from the native amino acid sequence of light chain positions 1-139 and heavy chain positions 1-254 of FIG. 1, wherein said Factor Xai is capable of competing with Factor Xa in the formation of prothrombinase complex and wherein said Factor Xai does not result in proteolytic activity when included in said complex, wherein the serin residue corresponding to that at position 185 of the heavy chain in FIG. 1 is replaced by a different amino acid and/or the aspartic acid residue at the position corresponding to that of position 88 of the heavy chain shown in FIG. 1 is replaced by an alternate amino acid.
A single-chain polypeptide which is convertible to Factor Xai by proteolysis;
- said Factor Xai being a modified form of the amino acid sequence of light chain positions 1-139 and heavy chain positions 1-254 of FIG. 1 wherein said Factor Xai is capable of competing with Factor Xa in the formation of a prothombinase complex and wherein said Factor Xai does not result in proteolytic activity when included in said complex, wherein the serine residue corresponding to that at position 185 of the heavy chain in FIG. 1 is replaced by an alternate amino acid and/or the aspartic acid residue at the position corresponding to that of position 88 of the heavy chain shown in FIG. 1 is replaced by an alternate amino acid.
Dependencies are inferred from the claim text.