US 12,139,520 B2
HAM15-52 analogues with improved amylin receptor (hAMY3R) potency
Jens Christian Frøslev Nielsen, Høsholm (DK); Kristoffer Tobias Gustav Rigbolt, Høsholm (DK); Esben Matzen Bech, Høsholm (DK); Morten Lundh, Høsholm (DK); Paola Magotti, Høsholm (DK); Borja Ballarín-González, Høsholm (DK); Søren Ljungberg Pedersen, Borup (DK); and Niels Vrang, Høsholm (DK)
Assigned to GUBRA A/S, Hørsholm (DK)
Appl. No. 18/024,879
Filed by GUBRA A/S, Høsholm (DK)
PCT Filed Sep. 23, 2021, PCT No. PCT/EP2021/076250
§ 371(c)(1), (2) Date Mar. 6, 2023,
PCT Pub. No. WO2022/063925, PCT Pub. Date Mar. 31, 2022.
Claims priority of application No. 20198117 (EP), filed on Sep. 24, 2020.
Prior Publication US 2024/0101634 A1, Mar. 28, 2024
Int. Cl. C07K 14/575 (2006.01)
CPC C07K 14/575 (2013.01) 10 Claims
 
1. An hAM15-52 analogue or a pharmaceutically acceptable salt thereof comprising 38 amino acids (X1-X38) with an hAMY3R-EC50≤250 μM and an hAM1R-EC50≥25 nM, wherein the amino acid in position X4 is selected as F, Y, W, T, M, I, A, or C; X37 is selected as G, Y, S, W, T, Q, P, M, I, H, F, E, A, R, C, or K; X38 is selected as Hyp, Y, W, T, Q, P, M, I, H, F, E, A, R, or K; X11 is R, W, or Cit and wherein at least one of the positions X4, X37 or X38 is not the amino acid present in hAM15-52 (SEQ ID NO: 1) in said position and further wherein the hAM15-52 analogue has at least 50% identity to hAM15-52 (SEQ ID NO: 1).