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1. 发明公开

EP3192802A1 STABILIZED PEPTIDE DERIVATIVES 审中-公开
标题翻译：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。

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