Granted Patent B2

US 12,583,900 · App. 17/782,573 · Granted Mar 24, 2026

Inventors: Weijun Shen (San Diego, CA); Elsa Pflimlin (San Diego, CA); Sam Lear (Del Mar, CA); Zaid Amso (El Cajon, CA); Peter G. Schultz (La Jolla, CA)

Assignee: THE SCRIPPS RESEARCH INSTITUTE

C07K14/605A61K47/542A61K47/60A61P3/04A61P25/16A61P25/28A61K38/00

Abstract

Claims (14)

1 . A peptide conjugate comprising:

a) a peptide comprising SEQ ID NO: 6, or an amino acid sequence having one amino acid addition, deletion, or substitution relative to the sequence from SEQ ID NO: 6; and

b) a staple attached to the peptide at a first amino acid and a second amino acid, wherein the first amino acid and second amino acid is independently cysteine or homocysteine, wherein the first amino acid has a position i in the peptide and the second amino acid has a position i+7 in the peptide, wherein the staple is:

wherein

each L 1 is independently -alkylene-O—, —O-alkylene-, —C(═O)NH—, —NHC(=0)-, -alkylene-C(=0)NH—, —alkylene-NHC(=0)-, or —(CR 1 R 2 )—, wherein each R 1 and R 2 is independently hydrogen, C 1-6 alkyl, or —COOH, and v is 2-20;

s1 is 1-15; and

Y is COOH.

2 . The peptide conjugate of claim 1 , wherein the staple has the structure:

wherein each “ -S” is a sulfur atom of the first amino acid or the second amino acid.

3 . The peptide conjugate of claim 1 , wherein the half-life of the peptide conjugate is at least about 2-fold greater than the half-life of the peptide without conjugation to the staple.

4 . The peptide conjugate of claim 1 , wherein the staple has the structure:

wherein each “ -S” is a sulfur atom of the first amino acid or the second amino acid.

5 . The peptide conjugate of claim 1 , wherein the staple has the structure:

wherein each “ -S” is a sulfur atom of the first amino acid or the second amino acid.

Assignments (1)

Continuity (3)

References Cited (312)