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US 2026/0193290 A1Published application
Convergent peptide synthesis methods
AssigneeAmgen Inc.
InventorsJames Murray, Matthew G. Beaver, Raymond Sarksian, Abhishek Kothari, Ogonna Nwajiobi, James Falsey
Life of this patent
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Abstract
Convergent pathways for the preparation of a peptide by solid phase peptide synthesis or liquid phase peptide synthesis, as well as peptide fragments suitable for use in such pathways, are provided. The convergent pathways may be utilized for the synthesis of agonists of the glucagon-like peptide 1 receptor (GLP-1R) such as the peptide component of maridebart cafraglutide.
Claims50
A method of preparing Peptide A or a variant thereof, comprising:
- (A) coupling a protected variant of Fragment 5 with a protected variant of Fragment 6 to form a protected variant of Peptide B;
- and/or
- (B) coupling a protected variant of Fragment 1 with a protected variant of Fragment 2B to form a protected variant of Peptide D;
- and/or
- (C) coupling a protected variant of Peptide B with a protected variant of Peptide D to form a protected variant of Peptide A,
- wherein Peptide A has the amino acid sequence of SEQ ID NO:
- 7, Peptide B has the amino acid sequence of SEQ ID NO:
- 9, Peptide D has the amino acid sequence of SEQ ID NO:
- 15, Fragment 1 has the amino acid sequence of SEQ ID NO:
- 1, Fragment 2B has the amino acid sequence of SEQ ID NO:
- 16, Fragment 5 has the amino acid sequence of SEQ ID NO:
- 5, and Fragment 6 has the amino acid sequence of SEQ ID NO:
- 6.
10 more elements
A molecule selected from:
- (SEQ ID NO:
- 166)
- Boc-His(Trt)-Aib-Glu(OtBu)-Gly-Thr(tBu)-Phe-
- Thr(tBu)-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-
- Ser(Psi(Me,Me)Pro)-OH;
- (SEQ ID NO:
- 30)
- H-Tyr(tBu)-Leu-Glu(OtBu)-Glu(OtBu)-Gln(Trt)-
- Ala-Ala-Lys(Boc)-Glu(OtBu)-Phe-Ile-OH;
- (SEQ ID NO:
- 169)
- Boc-His(Trt)-Aib-Glu(OtBu)-Gly-Thr(tBu)-Phe-
- Thr(tBu)-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-Ser(tBu)-
- Ser(Psi(Me,Me)Pro)-Tyr(tBu)-Leu-Glu(OtBu)-
- Glu(OtBu)-Gln(Trt)-Ala-Ala-Lys(Boc)-Glu(OtBu)-
- Phe-Ile-OH;
- (SEQ ID NO:
- 59)
- Trt-Ala-Trp(Boc)-Leu-Val-Lys(Boc)-Gly-Gly-Gly-OH;
- (SEQ ID NO:
- 130)
- H-Gly-Gly-Gly-Gly-Ser(Psi(Me,Me)Pro)-Gly-Gly-
- Gly-Gly-Ser(Psi(Me,Me)Pro)-Gly-Gly-Gly-Gly-
- Ser(Psi(Me,Me)Pro)-Lys(ivDde)-NH2;
- (SEQ ID NO:
- 170)
- Trt-Ala-Trp(Boc)-Leu-Val-Lys(Boc)-Gly-Gly-Gly-
- Gly-Gly-Gly-Gly-Ser(Psi(Me,Me)Pro)-Gly-Gly-
- Gly-Gly-Ser(Psi(Me,Me)Pro)-Gly-Gly-Gly-Gly-
- Ser(Psi(Me,Me)Pro)-Lys(ivDde)-NH2;
- (SEQ ID NO:
- 147)
- H-Ala-Trp(Boc)-Leu-Val-Lys(Boc)-Gly-Gly-Gly-
- Gly-Gly-Gly-Gly-Ser(Psi(Me,Me)Pro)-Gly-Gly-
- Gly-Gly-Ser(Psi(Me,Me)Pro)-Gly-Gly-Gly-Gly-
- Ser(Psi(Me,Me)Pro)-Lys(ivDde)-NH2;
- and
- (SEQ ID NO:
- 171)
- Boc-His(Trt)-Aib-Glu(OtBu)-Gly-Thr(tBu)-Phe-
- Thr(tBu)-Ser(tBu)-Asp(OtBu)-Tyr(tBu)-
- Ser(tBu)-Ser(Psi(Me,Me)Pro)-Tyr(tBu)-Leu-
- Glu(OtBu)-Glu(OtBu)-Gln(Trt)-Ala-Ala-
- Lys(Boc)-Glu(OtBu)-Phe-Ile-Ala-Trp(Boc)-
- Leu-Val-Lys(Boc)-Gly-Gly-Gly-Gly-Gly-Gly-
- Gly-Ser(Psi(Me,Me)Pro)-Gly-Gly-Gly-Gly-
- Ser(Psi(Me,Me)Pro)-Gly-Gly-Gly-Gly-
- Ser(Psi(Me,Me)Pro)-Lys(ivDde)-NH2,
- or a salt thereof.
46 more elements
Dependencies are inferred from the claim text.