Empower Clinic Services LLC v. Eli Lilly & Co

Prosecution History analysis

Examiner Search analysis

Invalidity Framework analysis

Petition

Petition Analysis

## 1. Case Identification
- Case Number: [IPR2025-01024](https://ai-lab.exparte.com/case/ptab/IPR2025-01024)
- Patent #: [9,474,780](https://ai-lab.exparte.com/patent/9474780)
- Filed: May 22, 2025
- Petitioner(s): [Empower Clinic Services, L.L.C.](https://ai-lab.exparte.com/party/empower-clinic-services-llc) (d/b/a Empower Pharmacy)
- Patent Owner(s): [Eli Lilly & Co.](https://ai-lab.exparte.com/party/eli-lilly-co)
- Challenged Claims: 1-7, 9-10, and 12-18

## 2. Patent Overview
- Title: GIP/GLP-1 Receptor Co-Agonist Compounds
- Brief Description: The [’780](https://ai-lab.exparte.com/patent/9474780) patent is directed to a genus of peptide compounds that function as dual agonists for the Glucose-dependent Insulinotropic Polypeptide (GIP) and Glucagon-like Peptide-1 (GLP-1) receptors. The claimed compounds are chemically modified with a conjugated moiety to improve their therapeutic properties.

## 3. Grounds for Unpatentability

#### Ground 1: Obviousness over Three Prior Art Publications - Claims 1-7, 9-10, and 12-18 are obvious over the ’657, ’483, and ’537 publications.
  - **Prior Art Relied Upon:** WO 2011/119657 A1 ([’657](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1007) publication), WO 2013/164483 A1 ([’483](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1008) publication), and WO 2006/097537 A2 ([’537](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1009) publication).
  - **Core Argument for this Ground:**
    - **Prior Art Mapping:** Petitioner argued that a person of ordinary skill in the art (POSA) would have arrived at the claimed invention through a series of predictable and well-motivated modifications to known compounds. The argument proceeds in three steps:
        1.  **Starting Point (’657 publication):** A POSA would have started with the promising GIP/GLP-1 dual agonist peptide disclosed in the [’657](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1007) publication (SEQ ID NO:1). This reference taught a lead compound with a desirable balance of GIP and GLP-1 activity, useful for treating diabetes and obesity. The [’657](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1007) publication also explicitly disclosed using either Phe or 1-Nal at position 22, which maps directly to the X3 limitation of challenged claim 1.
        2.  **C-Terminal Modification (’483 publication):** The [’483](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1008) publication taught improving GIP analogue peptides by replacing their C-terminal residues (from position 29 onward) with the well-known, stability-enhancing [exenatide](https://ai-lab.exparte.com/case/ptab/IPR2025-01024/doc/1054) C-terminal motif (GGPSSGAPPPS). Petitioner asserted a POSA would have been motivated to apply this teaching to the lead compound from the [’657](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1007) publication to improve its metabolic stability and reduce immunogenicity, as the [’657](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1007) peptide used a long, foreign C-terminal motif not found in natural ligands. This modification results in a peptide sequence falling within the scope of challenged claim 1.
        3.  **Half-Life Extension (’537 publication):** The [’537](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1009) publication taught achieving a protracted duration of action (once-weekly dosing) for GLP-1 agonists by conjugating a specific albumin-binding moiety—([2-(2-Amino-ethoxy)-ethoxy]-acetyl)2-(γGlu)-CO-(CH2)b-CO2H—to a lysine (Lys) residue. The [’483](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1008) publication also taught acylating dual agonists at Lys at position 20 to prolong their half-life. Petitioner contended that a POSA, having created the improved peptide from steps 1 and 2, would have been motivated to conjugate the specific, highly effective albumin-binding moiety from [’537](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1009) at the Lys20 position to achieve a desirable once-weekly dosing profile, a known goal in the field.
    - **Motivation to Combine (for §103 grounds):** The primary motivation was to improve a known, promising dual agonist peptide (’657) using established techniques to enhance its therapeutic properties. A POSA would combine [’657](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1007) and [’483](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1008) to replace a potentially immunogenic C-terminus with a proven, stabilizing motif. Subsequently, a POSA would incorporate the teaching of [’537](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1009) to apply a known, successful albumin-binding moiety to achieve the highly desirable goal of extended duration of action and once-weekly dosing, which had already been demonstrated for the GLP-1 agonist [semaglutide](https://ai-lab.exparte.com/case/ptab/IPR2025-01024/doc/1057).
    - **Expectation of Success (for §103 grounds):** Petitioner argued a POSA would have had a high expectation of success. The function of each component was well-understood: the [’657](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1007) peptide was a known dual agonist, the [exenatide](https://ai-lab.exparte.com/case/ptab/IPR2025-01024/doc/1054) C-terminus from [’483](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1008) was known to improve stability, and the albumin-binding moiety from [’537](https://ai-lab.exparte.com/docs/ptab/IPR2025-01024/1009) was known to dramatically extend half-life. The combination involved applying known solutions to known problems, with extensive prior art structure-activity relationship (SAR) data supporting the compatibility of the modifications.
    - **Key Aspects:** The argument hinges on the step-wise, logical assembly of known prior art elements, each chosen for its predictable contribution to the final compound's properties. The petitioner emphasized that the [’780](https://ai-lab.exparte.com/patent/9474780) patent’s claimed invention was not a breakthrough but rather the predictable outcome of routine optimization by a POSA using a finite number of known, suitable alternatives to improve a lead compound. The prior art also disclosed the specific variations recited in the dependent claims, such as using Phe at position 22 (claim 2), a fatty acid chain of 16 or 18 carbons (claims 5-6), and a single γGlu linker (claim 7).

## 7. Relief Requested
- Petitioner requested the institution of an inter partes review and the cancellation of claims 1-7, 9-10, and 12-18 of Patent [9,474,780](https://ai-lab.exparte.com/patent/9474780) as unpatentable.

Eli Lilly's GIP/GLP-1 dual agonist patent challenged: 3 prior art refs cited for obviousness against 16 claims for once-weekly obesity/diabetes drugs.