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Last Updated: March 29, 2024

Claims for Patent: 9,884,093


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Summary for Patent: 9,884,093
Title:Glucagon receptor agonists
Abstract: The present invention relates to compounds with an extended duration of action at the glucagon receptor as compared to native glucagon. Specifically provided are glucagon receptor agonists with modifications to the structure of native glucagon introduced to selectively agonize the glucagon receptor over an extended period of time.
Inventor(s): Alsina-Fernandez; Jorge (Indianapolis, IN), Coskun; Tamer (Indianapolis, IN)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Application Number:15/293,316
Patent Claims:1. A glucagon receptor agonist compound comprising the formula: TABLE-US-00044 YX.sub.1QGTFX.sub.2SDYSKYLDX.sub.3KKAX.sub.4EFVX.sub.5WLLEX.sub.6X.sub.7

wherein X.sub.1 is Aib; X.sub.2 is T; X.sub.3 is Aib; X.sub.4 is K which is chemically modified through conjugation to the epsilon-amino group of the K side-chain with ([2-(2-Amino-ethoxy)-ethoxy]-acetyl).sub.2-(.gamma.Glu).sub.a-CO--(CH.sub- .2).sub.b--CO.sub.2H, wherein a is 2 and b is 16; X.sub.5 is E; X.sub.6 is T; X.sub.7 is GPSSGAPPPS; and the C-terminal amino acid is amidated as a C-terminal primary amide (SEQ ID NO: 6); or a pharmaceutically acceptable salt thereof.

2. A glucagon receptor agonist compound consisting of the formula: TABLE-US-00045 YX.sub.1QGTFX.sub.2SDYSKYLDX.sub.3KKAX.sub.4EFVX.sub.5WLLEX.sub.6X.sub.7

wherein X.sub.1 is Aib; X.sub.2 is T; X.sub.3 is Aib; X.sub.4 is K which is chemically modified through conjugation to the epsilon-amino group of the K side-chain with ([2-(2-Amino-ethoxy)-ethoxy]-acetyl).sub.2-(.gamma.Glu).sub.a-CO--(CH.sub- .2).sub.b--CO.sub.2H, wherein a is 2 and b is 16; X.sub.5 is E; X.sub.6 is T; X.sub.7 is GPSSGAPPPS; and the C-terminal amino acid is amidated as a C-terminal primary amide (SEQ ID NO: 6); or a pharmaceutically acceptable salt thereof.

3. A method of treating a disease selected from the group consisting of T2DM, obesity, fatty liver disease, NASH, dyslipidemia, metabolic syndrome, hyperinsulinemia and nighttime hypoglycemia, comprising administering to a patient in need thereof, an effective amount of the glucagon receptor agonist of claim 1.

4. The method of claim 3, further comprising administering an effective amount of one or more additional therapeutic agents.

5. The method of claim 4 wherein the additional therapeutic agent is a GLP-1R agonist.

6. The method of claim 5 wherein the GLP-1R agonist is dulaglutide.

7. The method of claim 4 wherein the additional therapeutic agent is a GIP-GLP-1 co-agonist.

8. The method of claim 7 wherein the GIP-GLP-1 co-agonist has the structure of SEQ ID NO: 15.

9. A pharmaceutical composition comprising the glucagon receptor agonist of claim 1 and a pharmaceutically acceptable carrier, diluent, or excipient.

10. The pharmaceutical composition of claim 9, further comprising an additional therapeutic agent.

11. The pharmaceutical composition of claim 10, wherein the additional therapeutic agent is a GLP-1R agonist.

12. The pharmaceutical composition of claim 11, wherein the GLP-1R agonist is dulaglutide.

13. The pharmaceutical composition of claim 10, wherein the additional therapeutic agent is a GIP-GLP-1 co-agonist.

14. The pharmaceutical composition of claim 13 wherein the GIP-GLP-1 co-agonist has the structure of SEQ ID NO: 15.

15. The glucagon receptor agonist of claim 1, wherein the activity of the glucagon receptor agonist at the glucagon receptor is at least 100-fold higher than the potency of the glucagon receptor agonist at the GLP-1 receptor.

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