Patent ID: 7070969
Filing Date: 2006-07-04
Classification: A61K,A61P,C07K

Abstract:
1. A substantially pure preparation of a plasmin inhibitor characterised in that it is a single stage competitive inhibitor of plasmin, wherein “substantially pure” means that at least 60% of the total material in the preparation is the plasmin inhibitor, and wherein the plasmin inhibitor comprises a polypeptide with at least 90% sequence identity to one selected from the group consisting of SEQ ID NO:2, SEQ ID NO:4, SEQ ID NO:6, SEQ ID NO:8, SEQ ID NO:10, SEQ ID NO:12, and the general formula: KDZPZŸCZLBBZBGXCZXXXBXFÃYXBZZZZCBZFBYGGCXBNANNFXTXEECE STCAA (I) (SEQ ID NO 67), wherein: X is any amino acid selected from the group consisting of Ala, Arg, Asn, Asp, Cys, Gln, Glu, Gly, His, Ile, Leu, Lys, Met, Phe, Pro, Ser, Thr, Trp, Tyr, Val, α-aminobutyric acid, L-N-methylalanine, α-amino-α-methylbutyrate, L-N-methylarginine, aminocyclopropane-carboxylate, L-N-methylasparagine, aminoisobutyric acid, L-N-methylaspartic acid, aminonorbornyl-carboxylate, L-N-methylcysteine, cyclohexylalanine, L-N-methylglutamine, cyclopentylalanine, L-N-methylglutamic acid, L-N-methylisoleucine, L-N-methylhistidine, D-alanine, L-N-methylleucine, D-arginine, L-N-methyllysine, D-aspartic acid, L-N-methylmethionine, D-cysteine, L-N-methylnorleucine, D-glutamate, L-N-methylnorvaline, D-glutamic acid, L-N-methylornithine, D-histidine, L-N-methylphenylalanine, D-isoleucine, L-N-methylproline, D-leucine, L-N-medlylserine, D-lysine, L-N-methylthreonine, D-methionine, L-N-methyltryptophan, D-ornithine, L-N-methyltyrosine, D-phenylalanine, L-N-methylvaline, D-proline, L-N-methylethylglycine, D-serine, L-N-methyl-t-butylglycine, D-threonine, L-norleucine, D-tryptophan, L-norvaline, D-tyrosine, α-methyl-aminoisobutyrate, D-valine, α-methyl-γ-aminobutyrate, D-α-methylalanine, α-methylcyclohexylalanine, D-α-methylarginine, α-methylcylcopentylalanine, D-α-methylasparagine, α-methyl-α-napthylalanine, D-α-methylaspartate, α-methylpenicillamine, D-α-methylcysteine, N-(4-aminobutyl)glycine, D-α-methylglutamine, N-(2-aminoethyl)glycine, D-α-methylhistidine, N-(3-aminopropyl)glycine, D-α-methylisoleucine, N-amino-α-methylbutyrate, D-α-methylleucine, α-napthylalanine, D-α-methyllysine, N-benzylglycine, D-α-methylmethionine, N-(2-carbamylediyl)glycine, D-α-methylornithiine, N-(carbamylmethyl)glycine, D-α-methylphenylalanine, N-(2-carboxyethyl)glycine, D-α-methylproline, N-(carboxymethyl)glycine, D-α-methylserine, N-cyclobutylglycine, D-α-methylthreonine, N-cycloheptylglycine, D-α-methyltryptophan, N-cyclohexylglycine, D-α-methyltyrosine, N-cyclodecylglycine, L-α-methylleucine, L-α-methyllysine, L-α-methylmethionine, L-α-methylnorleucine, L-α-methylnorvatine, L-α-methylornithine, L-α-methylphenylalanine, L-α-methylproline, L-α-methylserine, L-α-methylthreonine, L-α-methyltryptophan, L-α-methyltyrosine, L-α-methylvaline, L-N-methylhomophenylalanine, N-(N-(2,2-diphenylethyl carbamylmethyl)glycine, N-(N-(3,3-diphenylpropyl carbamylmethyl)glycine, and 1-carboxy-1-(2,2-diphenyl-ethyl amino)cyclopropane; Ÿ is a hydrophobic amino acid; Ã is an aromatic amino acid; Z is K, R, H, D, E, Q or N; and B is a neutral amino acid, or P, A, G, S, T, V or L.