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Co-agonists of the GLP-1 and amylin receptors

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  • Publication Date:
    August 06, 2024
  • معلومة اضافية
    • 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
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      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