Prior art

The US patent 9474780, titled "GIP and GLP-1 co-agonist compounds," relates to dual incretin peptide mimetic compounds that agonize receptors for both human glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide-1 (GLP-1), and are useful for treating type 2 diabetes mellitus (T2D). The patent specifically claims compounds with a defined peptide sequence and a chemical modification at Lysine 20 involving a linker and a fatty acid chain.

The most relevant prior art explicitly cited in the description of US9474780, which describes GIP analogs exhibiting both GIP and GLP-1 activity, are:

1. WO 2013/164483

   • Full Citation: WO 2013/164483 A1, "GIP-GLP-1 DUAL AGONIST COMPOUNDS AND METHODS"
   • Publication/Filing Date: Publication Date: November 7, 2013; International Filing Date: May 3, 2013.
   • Brief Description: This patent describes truncated GIP analogues with one or more substitutions compared to wild-type GIP, which may have altered, preferably increased, GLP-1 activity, and provides GIP-GLP-1 dual agonist compounds and associated methods. The US9474780 patent itself notes that this prior art describes "GIP analogs as exhibiting both GIP and GLP-1 activity."
   • Potential Anticipation (35 U.S.C. § 102): This reference potentially anticipates the broad concept of dual GIP-GLP-1 agonism for treating metabolic disorders (e.g., T2D), as claimed in US9474780. Specifically, it might anticipate the general utility claims such as:
     • Claim 1: The fundamental concept of a compound being a GIP and GLP-1 co-agonist. However, the specific structural features of Claim 1 (Aib at X1 and X2, K at position 20 with specific chemical modification, X3 as Phe or 1-Nal, and optional C-terminal amidation) are specific to US9474780 and not explicitly disclosed as a whole in WO 2013/164483.
     • Claims 13, 14, 17, 18: Methods of treating type 2 diabetes mellitus comprising administering an effective amount of a dual GIP/GLP-1 co-agonist, especially in combination with other anti-diabetic agents. The novelty in these claims for US9474780 would lie in the specific compound being administered.

2. WO 2014/192284

   • Full Citation: WO 2014/192284 A1, "PEPTIDE COMPOUND"
   • Publication/Filing Date: Publication Date: December 4, 2014; International Filing Date: May 27, 2014.
   • Brief Description: This patent provides a novel peptide compound having an activating action on GLP-1 receptors and GIP receptors and its use as a medicament. It describes a peptide containing a partial sequence represented by a specific formula. Similar to the above, US9474780 notes this reference describes "GIP analogs as exhibiting both GIP and GLP-1 activity."
   • Potential Anticipation (35 U.S.C. § 102): This reference also broadly anticipates the concept of a peptide with dual GLP-1 and GIP receptor agonism. Given its later publication date compared to WO 2013/164483, it reinforces the general inventive concept. However, its specific peptide sequences and modifications would need to be compared directly to the detailed structural claims of US9474780. It could potentially anticipate:
     • Claim 1: The broad idea of a peptide compound acting as a dual GIP-GLP-1 agonist. However, the detailed chemical structure of the compounds claimed in US9474780, particularly the specific Aib substitutions and the detailed fatty acid linker conjugation at K20, would likely differentiate US9474780 from WO 2014/192284, unless specific embodiments within WO 2014/192284 closely match these features.
     • Claims 13, 14, 17, 18: Methods of treating T2D using a dual agonist.

3. WO 2011/119657

   • Full Citation: WO 2011/119657 A1, "NOVEL PEPTIDES AND METHODS FOR THEIR PREPARATION AND USE"
   • Publication/Filing Date: Publication Date: September 29, 2011; International Filing Date: March 23, 2011.
   • Brief Description: This patent relates to peptides that exhibit activity for both GIP receptor (GIP-R) and GLP-1 receptor (GLP-1-R) and are selective over the glucagon receptor (Gluc-R). Specifically, it provides GIP analogs with amino acid substitutions to modulate activity for both GIP-R and GLP-1-R and maintain selectivity over Gluc-R. US9474780 explicitly states this reference describes "GIP analogs as exhibiting both GIP and GLP-1 activity."
   • Potential Anticipation (35 U.S.C. § 102): This is the earliest of the cited WO patents and establishes the concept of GIP analogs with dual GIP-R and GLP-1-R activity, and importantly, selectivity over the glucagon receptor. This broader concept of dual agonism with selectivity is a key aspect of the background of US9474780. It potentially anticipates:
     • Claim 1: The general concept of a dual GIP-GLP-1 agonist peptide.
     • Claims 13, 14, 17, 18: Methods of treating T2D using such dual agonists.

It's crucial to note that while these prior art documents describe the concept of GIP and GLP-1 co-agonism, US9474780 claims very specific structural modifications to achieve improved properties such as balanced co-agonist activity, selectivity against glucagon and GLP-2 receptors, low immunogenicity, and pharmacokinetic characteristics supporting once-weekly dosing. The differentiation of US9474780 lies in the precise sequence modifications (e.g., Aib at positions 2 and 13) and the specific chemical conjugation at Lysine 20 involving a linker with two ethoxy-ethoxy-acetyl units, one or two gamma-glutamic acid units, and a fatty acid chain with a specific length (b=10 to 20 carbon atoms). These specific structural elements, as defined in claims 1-11 of US9474780, are what the patent asserts as novel and non-obvious over the broader prior art.