US2023272029A1PendingUtilityA1
Co-agonists at glp-1 and gip receptors suitable for oral delivery
Est. expiryJul 22, 2040(~14 yrs left)· nominal 20-yr term from priority
A61K 47/64C07K 14/605A61K 47/542A61K 38/26A61K 38/00C07K 14/001A61P 3/10A61P 3/04A61P 1/16
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Claims
Abstract
Peptide co-agonists of the human GLP-1 and GIP receptors suitable for oral delivery, including long-acting derivatives, and their medical use in treatment and/or prevention of obesity, diabetes, and/or liver diseases are described.
Claims
exact text as granted — not AI-modified1 . A compound comprising a peptide and a substituent; wherein the amino acid sequence of the peptide is
(SEQ ID NO.: 47)
YX 2 EGTX 6 TSDYSX 12 X 13 LEX 16 QAAX 20 X 21 FX 23 X 24 WLLX 28 GX 30
X 31 X 32 X 33 X 34 X 35 X 36 X 37 X 38 X 39
with an optional amide modification of the C-terminus[H]; wherein
X 2 is Aib or A,
X 6 is F or V,
X 12 is I or Y,
X 13 is Y, A, L or I,
X 16 is K or E,
X 20 is Q, R, E, or H,
X 21 is A or E,
X 23 is I or V,
X 24 is E, Q or N,
X 28 is A or R,
X 30 is G or absent,
X 31 is P or absent,
X 32 is E, or absent,
X 33 is S, Kc or absent,
X 34 is G or absent,
X 35 is A or absent,
X 36 is P or absent,
X 37 is P or absent,
X 38 is P or absent, and
X 39 is S or absent;
wherein the substituent is attached to the peptide via Lysine (K) at position 16 or 33;
and wherein the substituent comprises at least one of HOOC—(CH 2 ) n —CO—, wherein n is 14, 16 or 18;
or a pharmaceutically acceptable salt hereof.
2 . The compound according to claim 1 , wherein X 32 X 33 X 34 X 35 is selected from the group consisting of: SSGA, ESGA, and SKGA.
3 . The compound according to claim 1 , wherein the amino acid sequence of the peptide is
(SEQ ID NO.: 37)
YX 2 EGTX 6 TSDYSX 12 X 13 LEX 16 QAAX 20 X 21 FX 23 X 24 WLLX 28 GGPS
SGAPPPS;
wherein
X 2 is Aib or A,
X 6 is F or V,
X 12 is I or Y,
X 13 is Y, A, L or I,
X 16 is K or E,
X 20 is Q, R, E, or H,
X 21 is A or E,
X 23 is I or V,
X 24 is E, Q or N, and
X 28 is A or R.
4 . The compound according to claim 1 , wherein X 13 LEX 16 QAAX 20 X 21 FX 23 X 24 is selected from the group consisting of: LLEKQAAREFIN, LLEKQAAREFIE, LLEKQAAQEFIE and LLEEQAAREFIE.
5 . The compound according to claim 1 , wherein the amino acid sequence of the peptide is selected from the group consisting of SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 5, SEQ ID NO: 6, SEQ ID NO: 7, SEQ ID NO: 8, SEQ ID NO: 9, SEQ ID NO: 10, SEQ ID NO: 11, SEQ ID NO: 12, SEQ ID NO: 13, SEQ ID NO:
14, SEQ ID NO: 15, SEQ ID NO: 16, SEQ ID NO: 17, SEQ ID NO: 18, SEQ ID NO: 19, SEQ ID NO: 20, SEQ ID NO: 21, SEQ ID NO: 22, SEQ ID NO: 23, SEQ ID NO: 24, SEQ ID NO: 26, SEQ ID NO: 27, SEQ ID NO: 33, SEQ ID NO: 34, and SEQ ID NO: 35.
6 . The compound according to claim 5 wherein the peptide comprises the amide modification of the C-terminus.
7 . The compound according to claim 1 , wherein the substituent is selected from the group consisting of:
8 . The compound according to claim 1 , wherein the compound is selected from the group consisting of:
(Compound No. 1, SEQ ID NO: 1, Substituent: C),
(Compound No. 2, SEQ ID NO: 2, Substituent: C),
(Compound No. 3, SEQ ID NO: 2, Substituent: B),
(Compound No. 4, SEQ ID NO: 3, Substituent: B),
(Compound No. 5, SEQ ID NO: 3, Substituent: B),
(Compound No. 6, SEQ ID NO: 4, Substituent: B),
(Compound No. 7, SEQ ID NO: 4, Substituent: A),
No. 8, SEQ ID NO: 5, Substituent: B),
(Compound No. 9, SEQ ID NO: 6, Substituent: B),
(Compound No. 10, SEQ ID NO: 6, Substituent: A),
(Compound No. 11, SEQ ID NO: 5, Substituent: B),
(Compound No. 12, SEQ ID NO: 7, Substituent: B),
(Compound No. 13, SEQ ID NO: 8, Substituent: B),
(Compound No. 14, SEQ ID NO: 9, Substituent: B),
(Compound No. 15, SEQ ID NO: 10, Substituent: B),
(Compound No. 16, SEQ ID NO: 5, Substituent: C),
(Compound No. 17, SEQ ID NO: 11, Substituent: B),
(Compound No. 18, SEQ ID NO: 12, Substituent: B),
(Compound No. 19, SEQ ID NO: 13, Substituent: B),
(Compound No. 20, SEQ ID NO: 14, Substituent: B),
(Compound No. 21, SEQ ID NO: 15, Substituent: B),
(Compound No. 22, SEQ ID NO: 16, Substituent: B),
(Compound No. 23, SEQ ID NO: 17, Substituent: B),
(Compound No. 24, SEQ ID NO: 18, Substituent: B),
(Compound No. 26, SEQ ID NO: 20, Substituent: B),
(Compound No. 27, SEQ ID NO: 21, Substituent: B),
(Compound No. 28, SEQ ID NO: 22, Substituent: B),
(Compound No. 29, SEQ ID NO: 23, Substituent: B),
(Compound No. 30, SEQ ID NO: 24, Substituent: B),
(Compound No. 31, SEQ ID NO: 25, Substituent: B),
(Compound No. 32, SEQ ID NO: 25, Substituent: A),
(Compound No. 33, SEQ ID NO: 26, Substituent: B),
(Compound No. 34, SEQ ID NO: 27, Substituent: B),
(Compound No. 35, SEQ ID NO: 10, Substituent: A),
(Compound No. 36, SEQ ID NO: 27, Substituent: A),
(Compound No. 42, SEQ ID NO: 33, Substituent: B),
(Compound No. 43, SEQ ID NO: 34, Substituent: B),
(Compound No. 44, SEQ ID NO: 35, Substituent: B)
(Compound No. 45, SEQ ID NO: 34, Substituent: A),
(Compound No. 46, SEQ ID NO: 34, Substituent: E), and
(Compound No. 47, SEQ ID NO: 34, Substituent: E).
9 . (canceled)
10 . The compound according to claim 1 , wherein the compound is:
11 - 13 . (canceled)
14 . A peptide having the amino acid sequence
(SEQ ID NO.: 47)
YX 2 EGTX 6 TSDYSX 12 X 13 LEX 16 QAAX 20 X 21 FX 23 X 24 WLLX 28G X 30
X 31 X 32 X 33 X 34 X 35 X 36 X 37 X 38 X 39
with an optional amide modification of the C-terminus; wherein
X 2 is Aib or A,
X 6 is F or V,
X 12 is L, or Y,
X 13 is Y, A, L, or I,
X 16 is K or E,
X 20 is Q, R, E, or H,
X 21 is A or E,
X 23 is I or V,
X 24 is E, Q or N,
X 28 is A or R,
X 30 is G or absent,
X 31 is P or absent,
X 32 is E, S or absent,
X 33 is S, K or absent,
X 34 is G or absent,
X 35 is A or absent,
X 36 is P or absent,
X 37 is P or absent,
X 38 is P or absent, and
X 39 is S or absent.
15 . The peptide according to claim 14 where the amino acid sequence of the peptide is selected from the group consisting of SEQ ID NO: 1, SEQ ID NO: 2, SEQ ID NO: 3, SEQ ID NO: 4, SEQ ID NO: 5, SEQ ID NO: 6, SEQ ID NO: 7, SEQ ID NO: 8, SEQ ID NO: 9, SEQ ID NO: 10, SEQ ID NO: 11, SEQ ID NO: 12, SEQ ID NO: 13, SEQ ID NO: 14, SEQ ID NO: 15, SEQ ID NO: 16, SEQ ID NO: 17, SEQ ID NO: 18, SEQ ID NO: 19, SEQ ID NO: 20, SEQ ID NO: 21, SEQ ID NO: 22, SEQ ID NO: 23, SEQ ID NO: 24, SEQ ID NO: 26, SEQ ID NO: 27, SEQ ID NO: 33, SEQ ID NO: 34, and SEQ ID NO: 35.Join the waitlist — get patent alerts
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