Triple GLP-1 / GIP / Glucagon Receptor Agonists

RU2025108435APending Publication Date: 2026-10-05OBSHCHESTVO S OGRANICHENNOJ OTVETABTVENNOSTJU GEROFARM
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Patent Information

Application Number
RU2025108435
Authority / Receiving Office
RU · RU
Patent Type
Applications
Current Assignee / Owner
Filing Date
2025-04-04
Publication Date
2026-10-05
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Claims

1. Triple GLP-1 / GIP / glucagon receptor agonist, general formula I L-R1-NH2(general formula I), where L is the amino acid sequence: X1-Aib-X3-GTFTSD-X 10 -X 11 -X 12 X 13 X 14 -X 15 X 16 X 17 -X 18 X 19 X 20 -X 21 -X 22 -X 23 -X 24 -X 25 -LX 27 -X 28 -X 29 -X 30 -X 31 (SEQ ID NO: 1), where X1 represents Y or H, X3 represents E, Q, D, M, Y, or L, X 10 represents Y, L, R or I, X 11 represents S, Y or A, X 12 X 13 X 14 is SYL, QLL, NYL, SEL, QYL, QHL, QML, SML, DLE, DAL, RTL, RAL, IAL or SGL, X 15 X 16 X 17 represents ESQ, EYR, LYQ, ELQ, EK* Q, EK * E, EK * A, DK * E, DK * H or EK * L, where K * is K-(AEEA-AEEA-γ-Glu-CO-(CH2)n-COOH), where n is an integer from 8 to 28, X 18 X 19 X 20 represents GAK * , NAK * , ASK * , AAK * , AAAib, RAL, AVQ, ATA, YLV, AID, AQA, IQA or TSA, where K * is K-(AEEA-AEEA-γ-Glu-CO-(CH2)n-COOH), where n is an integer from 8 to 28, X 21 X 22 X 23 is EFI, ERI, DFV, QFE, AYV, NFY, QFE, ALI, AFA or ASS, X 24 represents A, N, E, Q, D, S or G, X 25 represents N, T, W or Y, X 27 represents F, V, D, L, H, Y, M, R, A or L, X 28 represents N, E, S or D, X 29 represents R, G or D, X30 represents M, G or R, X 31 represents G, F or E, R1 is -SSGAPPPS, -ASGRPPPS, -WSGRPPPS, -HSGRPPPS, or absent; or a pharmaceutically acceptable salt thereof.

2. A triple agonist according to claim 1, wherein n is an integer from 10 to 18.

3. A pharmaceutical composition for the treatment and / or prevention of a metabolic disorder, comprising a triple GLP-1 / GIP / glucagon receptor agonist according to any one of claims 1 or 2 or a pharmaceutically acceptable salt thereof in a mixture with a carrier.

4. Use of a triple GLP-1 / GIP / glucagon receptor agonist according to any one of claims 1 or 2 or a pharmaceutically acceptable salt thereof for the treatment and / or prevention of a metabolic disorder.

5. The use of a triple GLP-1 / GIP / glucagon receptor agonist according to any one of claims 1 or 2, or a pharmaceutically acceptable salt thereof, for the treatment and / or prevention of diabetes or a diabetes-related disorder, or obesity or an obesity-related disorder.

6. Use of a triple GLP-1 / GIP / glucagon receptor agonist according to any one of claims 1 or 2 to lower blood glucose.

7. Use of a triple GLP-1 / GIP / glucagon receptor agonist according to any one of claims 1 or 2 for weight loss.