Amylin receptor agonists
Amylin receptor agonist compounds offer an oral treatment for overweight and obesity, effectively targeting related comorbidities through pharmaceutical compositions.
Patent Information
- Authority / Receiving Office
- HK · HK
- Patent Type
- Applications
- Current Assignee / Owner
- NOVO NORDISK AS
- Filing Date
- 2026-04-09
- Publication Date
- 2026-07-10
AI Technical Summary
Existing treatments for overweight and obesity lack effective pharmaceutical compositions that can be administered orally and address related comorbidities effectively.
Development of amylin receptor agonist compounds and pharmaceutical compositions for oral administration to treat overweight and obesity.
The amylin receptor agonist compounds provide a viable oral treatment option for overweight and obesity, potentially addressing related comorbidities.
Abstract
Description
Department: Chemistry Department Agent: Lin Yibin Date: 260408 Our Volume Number: HKP2520672 Related Document Number: WO 2024 / 133739 A1 Invention Title: Amylin Receptor Agonist Abstract: This invention relates to compounds comprising amylin receptor agonists. This invention also relates to pharmaceutical compositions suitable for, but not limited to, oral administration, comprising such compounds. These compounds and pharmaceutical compositions comprising them can be used for the medical treatment of subjects suffering from overweight, obesity, and related comorbidities.
Claims
CLAIMS1. An amylin receptor agonist comprising a peptide according to Formula I (SEQ ID NO: 36):AX2X3LX5TX7QTX10RLAEFLHHX19X20X21X22FGX25IX27X28X29TX31VGX34X35TX37, whereinX2 is S or G,X3 is N, H, S, Q, A or E,X5 is A or S,X7is A or L,X is Q or A,X19 is S or absent,X2o is S, or absent,X21 is D, E or absent,X22 is N, P or absent,X25 is A, K or P,X27 is L or P,X28 is S or P,X29 is S or P,X31 is D or E,X34 is S or P,X35 is N, D or E,X37is Y or P, wherein the peptide comprises a C-terminal amide, and with the proviso that at least two of the amino acids at positions 21 , 31 and 35 are an aspartic acid or a glutamic acid.
2. The amylin receptor agonist according to claim 1 comprising, a peptide according to Formula I (SEQ ID NO: 36), whereinX2is S or G,X3 is H, S, Q or E,Xs is S,X7is A,X is Q or A,X19 is S or absent, X20 is S or absent, X21 is D, E or absent, X22 is N, P or absent, X25 is A or P, X27 is L or P, X28 is S or P, X29 is S or P, X31 is D, X34 is S or P, X35 is N, D or E, X37 is P.
3. The amylin receptor agonist according to claim 1 or claim 2, comprising a peptide according to Formula I (SEQ ID NO: 36), wherein X2 is S or G, X3 is H, S, Q or E, Xs is S, X7is A, X is Q or A, X19 is absent, X2o is absent, X21 is absent, X22 is absent, X25 is A or P, X27 is L or P, X28 is S or P, X29 is S or P, X31 is D, X34 is S or P, X35 is N, D or E, X37 is P.
4. The amylin receptor agonist according to any one of the preceding claims, comprising a peptide according to Formula I (SEQ ID NO: 36), wherein X27X28X29 is selected from LPP or PSS.
5. An amylin receptor agonist comprising a peptide selected from the group consisting of SEQ ID NOs: 2-33, wherein the peptide comprises a C-terminal amide.
6. An amylin receptor agonist comprising a peptide selected from any one of the following:AGELSTAQTARLAEFLHHFGPILPPTDVGSETP (SEQ ID NO: 13), ASQLSTAQTARLAEFLHHSSDNFGPILPPTDVGSNTP (SEQ ID NO: 16), ASHLSTAQTARLAEFLHHSSDPFGAIPSSTDVGPDTP (SEQ ID NO: 19), wherein the peptide comprises a C-terminal amide.
7. The amylin receptor agonist according to any one of the preceding claims, further comprising a protraction moiety.
8. The amylin receptor agonist according to the preceding claim, wherein the protraction moiety represented by formula (A)-(B) is attached, via linker (A), to the alpha position of the alanine (Ala, A) at position 1 or to the epsilon position of the lysine (Lys, K) at position 25.
9. The amylin receptor agonist according to any one of claims 7 and 8, wherein the amino acid at position 25 is alanine (Ala, A) or Proline (Pro, P) when the protraction moiety is attached to the alanine (Ala, A) at position 1.
10. The amylin receptor agonist according the any one of claims 7 to 9, wherein the protractor (B) of the protraction moiety by formula (A)-(B) comprises a C14 diacid, C16 diacid, C18 diacid, or C20 diacid.
11. The amylin receptor agonist according the any one of claims 7 to 10, wherein the linker (A) of the protraction moiety comprises a moiety according to Chem. 8a:
12. An amylin receptor agonist selected from the group consisting of:Compound 3,Compound 5,Compound 7,Compound 10,Compound 12,Compound 14,Compound 15,Compound 20,Compound 24,Compound 25,Compound 27Compound 29,Compound 30,Compound 34,Compound 38,Compound 39,Compound 41 ,Compound 43; or a pharmaceutically acceptable salt, ester or amide thereof.
13. A pharmaceutical composition comprising the amylin receptor agonist and / or pharmaceutically acceptable salt, ester, or amide thereof, according to any one of the preceding embodiments, and one or more pharmaceutically acceptable excipients.
14. The amylin receptor agonist according to any one of claims 1 to 12 or the pharmaceutical composition according to claim 13 for use as a medicament.
15. The amylin receptor agonist according to any one of claims 1 to 12 or the pharmaceutical composition according to claim 13, for use in the treatment of subjects with: an initial body mass index (BMI) of 27 or more, such as 30 or more, optionally in the presence of at least one weight-related comorbidity; diabetes, optionally in the presence of at least one weight-related comorbidity; cardiovascular disease; non-alcoholic steatohepatitis and / or cognitive impairment, such as that caused by Alzheimer’s disease.