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    BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR MT1-MMP
    1.
    发明公开
    BICYCLIC PEPTIDE LIGANDS SPECIFIC FOR MT1-MMP 审中-公开
    MT1-MMP特异性的双环肽配体

    公开(公告)号：EP3215518A1

    公开(公告)日：2017-09-13

    申请号：EP15790220.6

    申请日：2015-10-29

    申请人： Bicycle Therapeutics Limited

    发明人： TEUFEL, Daniel Paul ,  STACE, Catherine Lucy ,  PAVAN, Silvia ,  WALKER, Edward ,  BALDASSARRE, Leonardo

    IPC分类号： C07K7/08 ,  A61K47/50

    CPC分类号： C07K7/08 ,  A61K47/64 ,  A61K51/0482 ,  A61K51/08

    摘要： The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are high affinity binders of membrane type 1 metalloprotease (MT1-MMP).The invention also describes drug conjugates comprising said peptides,conjugated to one or more effector and/or functional groups which have utility in imaging and targeted cancer therapy.

    摘要翻译： 本发明涉及与分子支架共价结合的多肽，使得两个或更多个肽环在支架的附着点之间对齐。 具体而言，本发明描述了作为膜1型金属蛋白酶（MT1-MMP）的高亲和力结合剂的肽。本发明还描述了包含所述肽的药物缀合物，其与一种或多种效应物和/或官能团缀合，所述效应物和/或官能团可用于成像和 靶向癌症治疗。

    STABILIZED PEPTIDE DERIVATIVES
    5.
    发明公开
    STABILIZED PEPTIDE DERIVATIVES 审中-公开
    稳定的多肽衍生物

    公开(公告)号：EP3192802A1

    公开(公告)日：2017-07-19

    申请号：EP17152060.4

    申请日：2017-01-18

    申请人： Bicycle Therapeutics Limited

    发明人： Teufel, Daniel ,  Baldassarre, Leonardo ,  Mudd, Gemma ,  Pavan, Silvia

    IPC分类号： C07K7/08 ,  C12N9/64

    CPC分类号： C07K7/08 ,  A61K47/54 ,  C12N9/6491

    摘要： A compound comprising at least one looped peptide structure attached via at least two sulfone linkages formed through cysteine residues of the peptide to a scaffold, wherein the looped peptide comprises an amino acid sequence of formula (I):

             -C i -X-U/O-X-X-G-C ii -E-D-F-Y-X-X-C iii - (SEQ ID NO: 1)     (I)

    or a modified derivative, or pharmaceutically acceptable salt, thereof;
    wherein:
    C i , C ii and C iii represent first, second and third cysteine residues, respectively;
    X represents any amino acid residue;
    U represents a polar, uncharged amino acid residue selected from N, C, Q, M, S and T; and
    O represents a non-polar aliphatic amino acid residue selected from G, A, I, L, P and V.
    Preferably, the compound is a bicyclic peptide having two peptide loops between three sulfone linkages to the scaffold.

    摘要翻译： 包含至少一个环状肽结构的化合物，所述环状肽结构经由通过所述肽的半胱氨酸残基形成的至少两个砜键连接至支架，其中所述环状肽包含式（I）的氨基酸序列：-Ci-XU / OXXG-Cii -EDFYXX-Ciii-（SEQ ID NO：1）（I）或其修饰衍生物或其药学上可接受的盐; 其中：C 1，C 11和C 11分别代表第一，第二和第三半胱氨酸残基; X代表任何氨基酸残基; U代表选自N，C，Q，M，S和T的极性不带电荷的氨基酸残基; O代表选自G，A，I，L，P和V的非极性脂肪族氨基酸残基。优选地，该化合物是在与支架的三个砜键之间具有两个肽环的双环肽。

    NOVEL POLYPEPTIDES
    6.
    发明公开
    NOVEL POLYPEPTIDES 有权
    中性粒细胞多肽

    公开(公告)号：EP3062823A2

    公开(公告)日：2016-09-07

    申请号：EP14796237.7

    申请日：2014-10-28

    申请人： Bicycle Therapeutics Limited

    发明人： TEUFEL, Daniel ,  STACE, Catherine ,  WALKER, Edward

    IPC分类号： A61K47/48 ,  C07K7/08

    CPC分类号： C07K7/64 ,  A61K38/00 ,  C07K7/08 ,  C07K17/00

    摘要： The present invention relates to polypeptides which are covalently bound to molecular scaffolds such that two or more peptide loops are subtended between attachment points to the scaffold. In particular, the invention describes peptides which are specific for the human and rat protease plasma kallikrein and are modified in one or two peptide loops to enhance potency and/or protease resistance.

    摘要翻译： 本发明涉及与分子支架共价结合的多肽，使得在与支架的附着点之间对接两个或更多个肽环。 特别地，本发明描述了对人和大鼠蛋白酶血浆激肽释放酶特异的肽，并且在一个或两个肽环中被修饰以提高效力和/或蛋白酶抗性。

    PEPTIDES DERIVATIVES
    8.
    发明公开
    PEPTIDES DERIVATIVES 审中-公开
    肽衍生物

    公开(公告)号：EP3192801A1

    公开(公告)日：2017-07-19

    申请号：EP17152057.0

    申请日：2017-01-18

    申请人： Bicycle Therapeutics Limited

    发明人： TEUFEL, Daniel ,  Baldassarre, Leonardo

    IPC分类号： C07K7/08 ,  C07K19/00 ,  G01N33/68

    CPC分类号： C07K7/08 ,  G01N33/6845 ,  G01N2500/04

    摘要： A compound comprising at least one looped peptide structure attached via at least two oxoether linkages to a scaffold. Preferably the looped peptide structure is attached to the scaffold via at least three oxoether linkages. Also provided is a method of making a compound comprising at least one looped peptide structure attached via at least two oxoether linkages to a scaffold, the method comprising: providing a peptide having at least two amino acid residues having at least one -OH group in a side chain thereof; optionally converting said -OH groups to leaving groups; providing a scaffold molecule having at least two reactive sites for forming oxoether linkages with the said at least two amino acid residues; and forming said oxoether linkages between the peptide and the scaffold molecule.

    摘要翻译： 包含至少一个环状肽结构的化合物，其通过至少两个氧醚键连接到支架上。 优选地，环状肽结构通过至少三个氧醚键连接到支架。 还提供了制备包含至少一个环状肽结构的化合物的方法，所述环状肽结构通过至少两个氧代醚键连接至支架，所述方法包括：提供具有至少两个氨基酸残基的肽，所述氨基酸残基在 侧链; 任选地将所述-OH基团转化为离去基团; 提供具有至少两个用于与所述至少两个氨基酸残基形成氧醚键的反应位点的支架分子; 并在肽和支架分子之间形成所述氧杂醚键。