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US 2022/0177538 A1Published application
Co-agonists at glp-1 and gip receptors suitable for oral delivery
OwnerPatrick J. Knerr, Brian Finan +2inventors
InventorsPatrick J. Knerr, Brian Finan, Richard Dimarchi, Lars Linderoth
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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.
Claims16
A compound comprising a peptide and a substituent;
- wherein the amino acid sequence of the peptide is
- (SEQ ID NO.:
- 47)
- YX2EGTX6TSDYSX12X13LEX16QAAX20X21FX23
- X24WLLX28GX30X31X32X33X34X35X36X37X38X39
- with an optional amide modification of the C-terminus, wherein
- X2 is Aib or A
- X6 is F or V
- X12 is I or Y
- X13 is Y, A, L, or I
- X16 is K or E
- X20 is Q, R, E, or H
- X21 is A or E
- X23 is I or V
- X24 is E, Q, or N
- X28 is A or R
- X30 is G or absent
- X31 is P or absent
- X32 is E, S or absent
- X33 is S, K or absent
- X34 is G or absent
- X35 is A or absent
- X36 is P or absent
- X37 is P or absent
- X38 is P or absent
- X39 is S or absent;
- and wherein the substituent is attached to the peptide via Lysine (K) at position 16 or 33;
- or a pharmaceutically acceptable salt hereof.
25 more elements
A peptide having the amino acid sequence
- (SEQ ID NO.:
- 47)
- YX2EGTX6TSDYSX12X13LEX16QAAX20X21FX23X24
- WLLX28GX30X31X32X33X34X35X36X37X38X39
- with an optional amide modification of the C-terminus;
- wherein
- X2 is Aib or A
- X6 is F or V
- X12 is I or Y
- X13 is Y, A, L, or I
- X16 is K or E
- X20 is Q, R, E, or H
- X21 is A or E
- X23 is I or V
- X24 is E, Q, or N
- X28 is A or R
- X30 is G or absent
- X31 is P or absent
- X32 is E, S or absent
- X33 is S, K or absent
- X34 is G or absent
- X35 is A or absent
- X36 is P or absent
- X37 is P or absent
- X38 is P or absent
- X39 is S or absent.
23 more elements
Dependencies are inferred from the claim text.