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NOVEL INHIBITORS OF THE ENZYME ACTIVATED FACTOR XII (FXIIA)
专利权人:
发明人:
申请号:
EP16722090.4
公开号:
EP3288962A1
申请日:
2016.04.27
申请国别(地区):
EP
年份:
2018
代理人:
摘要:
The present invention relates to a bicyclic inhibitor of the coagulation enzyme activated factor XII (FXIIa) comprising or consisting of the peptide) (X1)(X2)(X3)n(X4)RL(X5)(X6)m(X7)(X9)l(X10)(X11)(X12)(X13)(X14)k(X15)(X16), wherein (X1) is present or absent and, if present, is an amino acid (X2) is an amino acid with a side chain (X3) is an amino acid and n is between 0 and 3, preferably 0 or 1 and most preferably 0 (X4) is an aliphatic L-amino acid or a cyclic L-amino acid, preferably L, P or an aromatic L-amino acid, and most preferably an aromatic L-amino acid (X5) is an amino acid (X6) is an amino acid and m is between 0 and 3, preferably 0 or 1 and most preferably 0 (X7) is an amino acid with a side chain (X9) is an amino acid and l is between 0 and 3, preferably 0 or 1 and most preferably 0 (X10) is an amino acid (X11) is an amino acid, preferably Q (X12) is a hydrophobic L-amino acid, preferably an aliphatic L-amino acid, and is most preferably L (X13) is an amino acid (X14) is an amino acid and k is between 0 and 3, preferably 0 or 1 and most preferably 0, (X15) is an amino acid with a side chain and (X16) is present or absent and, if present, is an amino acid and wherein the side chains of (X2), (X7) and (X15) are connected via a connecting molecule, said connecting molecule having at least three functional groups, each functional group forming a covalent bond with one of the side chains of (X2), (X7) and (X15).
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