Christian HEINIS,Simon MIDDENDORP,Jonas Alfred Karl WILBS,Vanessa BAERISWYL
申请号：
MX2017013892
公开号：
MX2017013892A
申请日:
2016.04.27
申请国别(地区):
MX
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)(X5)(X6)m(X7)(X9)l(X10)(X11)(X< sup>12)(X13)(X14)k(X 15)(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 presente invención se refiere a un inhibidor bicíclico del factor XII activado por la enzima de coagulación (FXIIa) que comprende o que consiste del péptido (X1) (X2) (X3)n(X4)RL(X5) (X6)m(X7) (X9)l(X10) (X11) (X12) (X13) (X14)k(X15) (X16), en donde (X1) está presente o ausente y, si está presente, es un aminoácido (X2) es un aminoácido con una cadena lateral (X3) es un aminoácido y n está entre 0 y 3, preferiblemente 0 o 1 y lo más preferiblemente 0 (X4) es un aminoácido L alifático o un aminoácido L cíclico, preferiblemente L,
