- Patent Number:
12054,528
- Appl. No:
18/084088
- Application Filed:
December 19, 2022
- نبذة مختصرة :
The invention relates to a compound comprising a GLP-1 receptor agonist and an amylin receptor agonist. The invention also relates to a pharmaceutical formulation, suitable for but not limited to oral administration, which comprises such a compound. The compound and pharmaceutical formulation comprising it may be used for the medical treatment of subjects with overweight, obesity and associated co-morbidities.
- Inventors:
Novo Nordisk A/S (Bagsvaerd, DK)
- Assignees:
Novo Nordisk A/S (Bagsvaerd, DK)
- Claim:
1. A Glucagon-Like Peptide-1 (GLP-1) receptor-amylin receptor co-agonist, selected from the group consisting of H-Aib-EGTFTSDVSSYLEEQAAREFIAWLVRGR-K([2-[2-[2-[[2-[2-[2-[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl])-GGGGEASELSTAALGRLSAELHELATLPRTETGSGSP-amide: [chemical expression included] H-Aib-EGTFTSDVS-K([2-[2-[2-[2-[2-[2-[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl])-YLEEQAAREFIAWLVRGRGGGGGEASELSTAALGRLSAELHELATLPRTETGSGSP-amide: [chemical expression included] and H-Aib-EGTFTSDVSSYLEEQAAREFIAWLVRGR-K([2-[2-[2-[2-[2-[2-[[(4S)-4-carboxy-4-(19-carboxynonadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl])-GGGGEASELSTAALGRLSAELHELATLPRTETGSGSP-amide: [chemical expression included]
- Claim:
2. The GLP-1 receptor-amylin receptor co-agonist according to claim 1 , which is H-Aib-EGTFTSDVSSYLEEQAAREFIAWLVRGR-K([2-[2-[2-[2-[2-[2-[[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl])-GGGGEASELSTAALGRLSAELHELATLPRTETGSGSP-amide: [chemical expression included]
- Claim:
3. A pharmaceutical formulation comprising a GLP-1 receptor-amylin receptor co-agonist according to claim 2 and a pharmaceutically acceptable excipient.
- Claim:
4. A method of treating a human subject suffering from overweight, comprising administering to said human subject the pharmaceutical formulation according to claim 3 .
- Claim:
5. The method of claim 4 , wherein said human subject has an initial body mass index (BMI) of 27 or more.
- Claim:
6. The method of claim 5 , wherein said human subject has at least one weight-related comorbidity selected from the group consisting of diabetes, hypertension, dyslipidaemia, high cholesterol and obstructive sleep apnoea.
- Claim:
7. The method of claim 5 , wherein said human subject has cardiovascular disease, non-steroidal steatohepatitis or cognitive impairment.
- Claim:
8. A method of treating a human subject suffering from obesity, comprising administering to said human subject the pharmaceutical formulation according to claim 3 .
- Claim:
9. The method of claim 8 , wherein said human subject has an initial body mass index (BMI) of 30 or more.
- Claim:
10. The method of claim 9 , wherein said human subject has at least one weight-related comorbidity selected from the group consisting of diabetes, hypertension, dyslipidemia, high cholesterol and obstructive sleep apnoea.
- Claim:
11. The method of claim 9 , wherein said human subject has cardiovascular disease, non-steroidal steatohepatitis or cognitive impairment.
- Claim:
12. The GLP-1 receptor-amylin receptor co-agonist according to claim 1 , which is H-Aib-EGTFTSDVS-K([2-[2-[2-[2-[2-[2-[[(4S)-4-carboxy-4-(17-carboxyheptadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl])-YLEEQAAREFIAWLVRGRGGGGGEASELSTAALGRLSAELHELATLPRTETGSGSP-amide: [chemical expression included]
- Claim:
13. A pharmaceutical formulation comprising a GLP-1 receptor-amylin receptor co-agonist according to claim 12 and a pharmaceutically acceptable excipient.
- Claim:
14. A GLP-1 receptor-amylin receptor co-agonist according to claim 1 , which is H-Aib-EGTFTSDVSSYLEEQAAREFIAWLVRGR-K([2-[2-[2-[2-[2-[2-[[(4S)-4-carboxy-4-(19-carboxynonadecanoylamino)butanoyl]amino]ethoxy]ethoxy]acetyl]amino]ethoxy]ethoxy]acetyl])-GGGGEASELSTAALGRLSAELHELATLPRTETGSGSP-amide: [chemical expression included]
- Claim:
15. A pharmaceutical formulation comprising a GLP-1 receptor-amylin receptor co-agonist according to claim 14 and a pharmaceutically acceptable excipient.
- Claim:
16. A pharmaceutical formulation comprising a GLP-1 receptor-amylin receptor co-agonist according to claim 1 and a pharmaceutically acceptable excipient.
- Claim:
17. A method of treating a human subject suffering from overweight, comprising administering to said human subject the pharmaceutical formulation according to claim 16 .
- Claim:
18. The method of claim 17 , wherein said human subject has an initial body mass index (BMI) of 27 or more.
- Claim:
19. The method of claim 18 , wherein said human subject has at least one weight-related comorbidity selected from the group consisting of diabetes, hypertension, dyslipidaemia, high cholesterol and obstructive sleep apnoea.
- Claim:
20. The method of claim 18 , wherein said human subject has cardiovascular disease, non-steroidal steatohepatitis or cognitive impairment.
- Claim:
21. A method of treating a human subject suffering from obesity, comprising administering to said human subject the pharmaceutical formulation according to claim 16 .
- Claim:
22. The method of claim 21 , wherein said human subject has an initial body mass index (BMI) of 30 or more.
- Claim:
23. The method of claim 22 , wherein said human subject has at least one weight-related comorbidity selected from the group consisting of diabetes, hypertension, dyslipidaemia, high cholesterol and obstructive sleep apnoea.
- Claim:
24. The method of claim 22 , wherein said human subject has cardiovascular disease, non-steroidal steatohepatitis or cognitive impairment.
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- Other References:
Bower et al., “Molecular Signature for Receptor Engagement in the Metabolic Peptide Hormone Amylin,” ACS Pharmacol. Transl. Sci., 2018, vol. 1, pp. 32-49. cited by applicant
Enebo et al., “Safety, tolerability, pharmacokinetics, and pharmacodynamics of concomitant administration of multiple doses of cagrilintide with semaglutide 2⋅4 mg for weight management: a randomised, controlled, phase 1b trial”, The Lancet, May 2021, vol. 397, No. 10286, pp. 1736-1748. cited by applicant
Finan et al., Emerging opportunities for the treatment of metabolic diseases: Glucagon-like peptide-1 based multi-agonists, “Molecular and Cellular Endocrinology., Dec. 2015, vol. 418, pp. 42-54”. cited by applicant
Roberts et al., “Molecular and functional characterization of amylin, a peptide associated with type 2 diabetes mellitus,” PNAS, Dec. 1989, vol. 86, pp. 9662-9666. cited by applicant
Sun et al., “Bifunctional PEGylated Exenatide-Amylinomimetic Hybrids to Treat Metabolic Disorders: An Example of Long-Acting Dual Hormonal Therapeutics,” Journal of Medicinal Chemistry, 2013, vol. 56, pp. 9328-9341. cited by applicant
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- Primary Examiner:
Chandra, Gyan
- Attorney, Agent or Firm:
Hu, Jianjie
- الرقم المعرف:
edspgr.12054528
Processing Request
No Comments.