Stapled and stitched polypeptides and uses thereof

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专利权人:

发明人:

VERDINE GREGORY L,HILINSKI GERARD

申请号：

IN9518/DELNP/2015

公开号：

IN2015DN09518A

申请日:

2015.10.12

申请国别(地区):

IN

年份:

2016

代理人:

摘要：

The present invention provides stapled polypeptides of the Formulae (I) and (VI): (I) (VI) and salts thereof wherein the groups ===== R , R , Rlc, R2a, R3a, R , R , R a, R , RA, Rz, Lia> Lib, L2, L3, X , v, w, p, m, s, n, t, and q are as defined herein. The present invention further provides methods of preparing the inventive stapled polypeptides from unstapled polypeptide precursors. The present invention further provides pharmaceutical compositions comprising a stapled polypeptide of Formula (I) or (VI), and methods of using the stapled peptides. The present invention also provides modifications of the staples post ring closing metathesis.

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