	US 12,297,250 B2
	Modified GIP peptide analogues
Alexander Hovard Sparre-Ulrich, Copenhagen N (DK); Bjørn Behrens Sivertsen, Copenhagen S (DK); Ditte Riber, Brønshøj (DK); and Mette Marie Rosenkilde, Hellerup (DK)
Assigned to ANTAG THERAPEUTICS APS, Copenhagen N (DK)
Appl. No. 17/298,512
Filed by Antag Therapeutics ApS, Copenhagen N (DK)
PCT Filed Dec. 3, 2019, PCT No. PCT/EP2019/083506 § 371(c)(1), (2) Date May 28, 2021, PCT Pub. No. WO2020/115048, PCT Pub. Date Jun. 11, 2020.
Claims priority of application No. 18209896 (EP), filed on Dec. 3, 2018; and application No. 19176739 (EP), filed on May 27, 2019.
Prior Publication US 2022/0298218 A1, Sep. 22, 2022
Int. Cl. C07K 14/605 (2006.01); A61K 38/00 (2006.01); A61K 38/22 (2006.01); C07K 14/645 (2006.01)

CPC C07K 14/605 (2013.01) [A61K 38/22 (2013.01); C07K 14/645 (2013.01); A61K 38/00 (2013.01)]

17 Claims

1. A glucose-dependent insulinotropic peptide (GIP) analogue consisting of the amino acid sequence of SEQ ID NO: 81:

(SEQ ID NO: 81)
3 4 5 6 7 8 9 10 11 12 13 14 15 16 17
E - G - T - F - I - S - E - Y - S - I - Aib - L - E - K - I

18 19 20 21 22 23 24 25 26 27 28 29 30
K - Q - Q - E - F - V - E - W - L - L - A - Q - K - Z,

wherein said amino acid sequence is modified by attaching a fatty acid molecule at one or more amino acid residue, directly or via a linker, at any one of positions 3 to 29 of SEQ ID NO: 81,

wherein Z is a peptide of one or more amino acid residues of GIP(31-42) (GKKNDWKHNITQ; SEQ ID NO: 2) or wherein Z is a peptide of one or more amino acid residues of Exendin-4 (HGEGTFTSDLSKQMEEEAVRLFIEWLKNGGPSSGAPPPS; SEQ ID NO: 3),

wherein said amino acid sequence is optionally C-terminally amidated (—NH2) or C-terminally carboxylated (—COOH), and

wherein said GIP analogue is an antagonist of GIPR.