HEINIS, Christian,BAERISWYL, Vanessa,MIDDENDORP, Simon,WILBS, Jonas Alfred Karl
申请号：
EPEP2016/059435
公开号：
WO2016/174103A1
申请日:
2016.04.27
申请国别(地区):
WO
年份:
2016
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)(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 I 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 (X18) 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).La présente invention concerne un inhibiteur bicyclique du facteur de coagulation XII à activation enzymatique (FXIIa) comprenant ou constitué du peptide (X1)(X2)(X3)n(X4)(X5)(X6)m(X7)(X9)l(X10)(X11)(X12)(X13)(X14)k(X15)(X16), dans lequel (X1) est présent ou absent et, sil est présent, est un aminoacide (X2) est un aminoacide avec une chaîne latérale (X3) est un aminoacide et n est compris entre 0 et 3, de préférence 0 ou 1, idéalement 0 (X4) est un L-aminoacide aliphatique ou un L-aminoacide cyclique, de préférence L, P ou un L-aminoacide aromatiq
