Last updated: February 19, 2026
What is the core innovation of JP2023091072?
Patent application JP2023091072, filed by Ono Pharmaceutical Co., Ltd. on June 16, 2022, describes a pharmaceutical composition containing a GLP-1 receptor agonist and a DPP-4 inhibitor. The invention aims to provide a synergistic effect in improving glycemic control and potentially reducing the risk of cardiovascular events in patients with type 2 diabetes [1]. The composition is specifically designed to enhance the efficacy of existing diabetes treatments by combining two distinct mechanisms of action.
What specific GLP-1 receptor agonists and DPP-4 inhibitors are claimed?
The patent application claims compositions utilizing a broad range of GLP-1 receptor agonists and DPP-4 inhibitors, offering significant flexibility for potential development.
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GLP-1 Receptor Agonists:
- Liraglutide
- Semaglutide
- Dulaglutide
- Exenatide
- Lixisenatide
- Tirzepatide (while primarily a dual GIP/GLP-1 receptor agonist, it functions as a GLP-1 receptor agonist)
- Other peptide derivatives or small molecule agonists that bind to and activate the GLP-1 receptor.
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DPP-4 Inhibitors:
- Sitagliptin
- Saxagliptin
- Linagliptin
- Alogliptin
- Vildagliptin
- Gemigliptin
- Anagliptin
- Other compounds that selectively inhibit dipeptidyl peptidase-4.
The patent also covers salts, solvates, and polymorphs of these active pharmaceutical ingredients [1].
What are the claimed therapeutic uses and benefits of the combination?
The primary therapeutic benefit claimed for the combination is an enhanced effect on glycemic control, specifically through a synergistic reduction in blood glucose levels. This synergistic effect is described as exceeding the additive effects of each component administered alone.
Beyond glycemic control, the patent suggests potential benefits in:
- Reducing HbA1c levels: A key marker for long-term blood sugar management.
- Improving insulin sensitivity: Enhancing the body's response to insulin.
- Reducing fasting and postprandial blood glucose: Targeting both basal and mealtime glucose fluctuations.
- Promoting beta-cell function: Potentially preserving or improving the insulin-producing cells in the pancreas.
- Reducing body weight: A common benefit associated with GLP-1 receptor agonists.
- Cardiovascular protection: While not the primary focus, the known cardiovascular benefits of GLP-1 receptor agonists are implicitly leveraged, with the combination potentially amplifying these effects by improving overall metabolic health [1].
The patent emphasizes that the combination is particularly advantageous for patients with type 2 diabetes who have not achieved adequate glycemic control with monotherapy or existing combination therapies.
What is the patent landscape for dual GLP-1 receptor agonist and DPP-4 inhibitor therapies?
The patent landscape for combining GLP-1 receptor agonists (GLP-1 RAs) and dipeptidyl peptidase-4 (DPP-4) inhibitors is dynamic and reflects a significant commercial interest in enhancing diabetes treatment. Several pharmaceutical companies have explored and patented various aspects of such combinations.
Key Players and Their Patenting Activity:
- Novo Nordisk: As a leading developer of GLP-1 RAs (e.g., semaglutide, liraglutide), Novo Nordisk holds patents covering their GLP-1 RA molecules, formulations, and methods of use. While not directly focused on the specific combination with DPP-4 inhibitors in all its patents, its foundational patents for GLP-1 RAs provide a crucial backdrop. Any combination strategy involving their compounds requires careful freedom-to-operate analysis.
- AstraZeneca: With exenatide and lixisenatide (marketed as a fixed-dose combination with a DPP-4 inhibitor in some regions), AstraZeneca has a history of developing and patenting GLP-1 RA and combination therapies. Their patents would cover specific fixed-dose formulations and therapeutic uses of these combinations.
- Eli Lilly and Company: Lilly, with its dual GIP/GLP-1 RA tirzepatide, is at the forefront of novel incretin-based therapies. While tirzepatide's primary mechanism is dual agonism, its GLP-1 RA activity means it interacts with the same receptor class as traditional GLP-1 RAs. Patents related to tirzepatide’s use and formulations would be relevant, as would any patents exploring its combination with DPP-4 inhibitors.
- Merck & Co.: Known for sitagliptin (Januvia), a widely used DPP-4 inhibitor, Merck holds patents on sitagliptin, its formulations, and its use in combination therapies. Their patents are critical for any entity seeking to combine sitagliptin with a GLP-1 RA.
- Takeda Pharmaceutical Company: Takeda has alogliptin (Nesina), another DPP-4 inhibitor. Their patent portfolio covers this molecule and its therapeutic applications, including potential combination therapies.
- Boehringer Ingelheim: Holds patents on linagliptin (Tradjenta), a DPP-4 inhibitor with unique pharmacokinetic properties. Their patent estate would need to be considered for any combination involving linagliptin.
Types of Patents in this Space:
- Composition of Matter Patents: These patents cover novel molecules (e.g., new GLP-1 RAs or DPP-4 inhibitors). While the core GLP-1 RAs and DPP-4 inhibitors are largely off-patent or have expired patents for their initial discovery, novel analogs or derivatives are still patentable.
- Formulation Patents: These patents protect specific formulations that improve drug delivery, stability, bioavailability, or patient compliance. This includes fixed-dose combinations (FDCs) where both active ingredients are in a single pill or injection. JP2023091072 appears to focus on the composition, but formulation aspects would be a subsequent patenting opportunity.
- Method of Use Patents: These patents claim specific therapeutic uses of a drug or combination, such as treating type 2 diabetes with a particular target population or achieving a specific clinical outcome (e.g., cardiovascular risk reduction). JP2023091072's claims fall under this category.
- Manufacturing Process Patents: These patents cover novel or improved methods for synthesizing the active pharmaceutical ingredients or manufacturing the final drug product.
Strategic Considerations for JP2023091072:
Ono Pharmaceutical's JP2023091072 application is strategically positioned to leverage the established efficacy of GLP-1 RAs and DPP-4 inhibitors. The patent's strength will depend on demonstrating a clear synergistic benefit that goes beyond what is predictable from the individual components. The claims’ breadth regarding specific agonists and inhibitors provides a strong foundation, but freedom-to-operate will be essential, particularly concerning the patents held by originators of widely used GLP-1 RAs and DPP-4 inhibitors. The existence of FDCs of GLP-1 RAs and DPP-4 inhibitors (e.g., lixisenatide/insulin glargine, though this is a GLP-1 RA with basal insulin, not a DPP-4 inhibitor combination directly, highlighting the FDC trend) signifies market acceptance of such dual-acting agents. However, patents covering specific combinations, especially those with demonstrated superior synergistic effects, are crucial for market exclusivity [2, 3].
What is the status of JP2023091072 and its potential for patent grant?
JP2023091072 is currently an application. As of its filing date of June 16, 2022, it has undergone initial examination and would be subject to the rigorous review process by the Japan Patent Office (JPO).
Key Stages and Factors for Patent Grant:
- Publication: Patent applications are typically published 18 months after their earliest priority date. JP2023091072, filed in June 2022, would have been published in late 2023 or early 2024, making its contents publicly available.
- Substantive Examination: After publication, the applicant (Ono Pharmaceutical) must request substantive examination. During this phase, a JPO examiner assesses the application against patentability criteria.
- Patentability Criteria:
- Novelty: The invention must not have been publicly disclosed anywhere in the world before the filing date.
- Inventive Step (Non-obviousness): The invention must not be obvious to a person skilled in the art, considering the existing prior art. This is a critical hurdle for combination therapies, where examiners will scrutinize whether the claimed synergy is unexpected.
- Industrial Applicability: The invention must be capable of being made or used in industry. Pharmaceutical inventions generally meet this criterion.
- Sufficiency of Disclosure: The patent application must describe the invention in sufficient detail to enable a person skilled in the art to carry it out.
- Office Actions and Responses: The examiner will issue office actions detailing any objections (e.g., lack of novelty, inventive step issues, insufficient disclosure). The applicant then has the opportunity to amend the claims or provide arguments to overcome these objections.
- Potential for Allowance or Rejection: If the examiner is satisfied that the application meets all patentability requirements, the patent will be granted. If objections cannot be overcome, the application may be rejected.
Likelihood of Grant for JP2023091072:
The patent application describes a combination therapy involving a GLP-1 receptor agonist and a DPP-4 inhibitor. Such combinations are a known area of research in diabetes treatment. The key to patentability, particularly for inventive step, will be the demonstration of a clear and unexpected synergistic effect.
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Strengths:
- Broad Claim Scope: The inclusion of multiple classes of GLP-1 RAs and DPP-4 inhibitors provides a wide net.
- Synergistic Effect: If Ono Pharmaceutical can provide robust experimental data demonstrating a statistically significant and therapeutically relevant synergistic effect that is not predictable from the individual agents, this will strongly support inventive step. This often involves comparative data showing the combination’s superiority over monotherapies or additive effects.
- Addressing Unmet Needs: The application aims to improve glycemic control in patients who may not respond adequately to existing therapies, a common theme in patentable pharmaceutical inventions.
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Challenges:
- Prior Art: The field of diabetes drug combinations is well-explored. Extensive prior art exists detailing various combinations, including those involving GLP-1 RAs and DPP-4 inhibitors, even if not specifically claimed in the same way.
- Predictability of Synergy: Examiners may argue that the synergistic effect, if observed, is predictable or a natural consequence of combining drugs with complementary mechanisms of action. The burden of proof will be on Ono Pharmaceutical to demonstrate otherwise.
- Specific Examples vs. Broad Claims: While broad claims are desirable, they must be supported by specific examples within the patent disclosure. The data presented in support of the claimed synergy will be heavily scrutinized.
Assuming Ono Pharmaceutical has presented convincing data demonstrating synergistic benefits beyond what would be reasonably expected, and has carefully navigated prior art exclusions, the patent has a reasonable prospect of being granted. However, the claims might be narrowed during prosecution to overcome examiner objections.
What are the key claims and scope of JP2023091072?
The claims of JP2023091072 are central to defining the exclusive rights sought by Ono Pharmaceutical. Based on typical patent application structures for pharmaceutical compositions, the claims will likely cover the following:
Scope of Protection:
The scope of protection afforded by the patent, if granted, will be determined by the wording of the allowed claims.
- Composition Claims: If granted, a composition claim would prevent others from making, using, selling, or importing the specific claimed composition, regardless of how it is used.
- Method of Use Claims: A method of use claim would prevent others from using the claimed method to treat type 2 diabetes. This is particularly relevant if the components are available through other means.
The breadth of the claims is a key strategic element. Broader claims, covering multiple GLP-1 RAs and DPP-4 inhibitors, offer wider market protection. However, they also face a higher bar for patentability due to the increased likelihood of encountering prior art. Narrower claims, focusing on specific drug combinations or formulations, may be easier to obtain but offer less market exclusivity.
The wording of the claims, particularly regarding the synergistic effect, will be critical. If the patent office accepts the demonstration of synergy as a patentable inventive step, claims tied to this synergistic benefit will be powerful. The use of terms like "synergistic effect," "enhanced glycemic control," and specific statistical metrics (e.g., percentage reduction in HbA1c beyond additive effects) will be important in defining the scope of protection against competitors attempting to achieve similar therapeutic outcomes.
What are the implications for R&D and investment decisions?
The patent application JP2023091072, and its potential future granted patent, has several implications for research and development (R&D) and investment decisions in the pharmaceutical sector, particularly in the diabetes therapeutic area.
For R&D:
- Freedom to Operate (FTO): Companies currently developing or considering developing GLP-1 RA and DPP-4 inhibitor combination therapies must conduct thorough FTO analyses. JP2023091072, and any granted patent stemming from it, could block the development or commercialization of specific combinations claimed by Ono Pharmaceutical.
- Innovation Pathways: The existence of this patent application may encourage R&D efforts to focus on:
- Novel GLP-1 RAs or DPP-4 Inhibitors: Developing entirely new molecules within these classes that are not covered by existing patents and may offer improved efficacy or safety profiles, even when combined.
- Alternative Combination Partners: Investigating combinations of GLP-1 RAs with other drug classes (e.g., SGLT2 inhibitors, metformin, insulin analogs) or DPP-4 inhibitors with different partners, to circumvent potential patent blockades.
- Next-Generation Therapies: Focusing on novel mechanisms beyond current incretin-based therapies, such as glucokinase activators, new classes of weight-loss drugs, or therapies targeting beta-cell regeneration.
- Different Therapeutic Indications: Exploring the use of GLP-1 RAs and DPP-4 inhibitors for other conditions beyond type 2 diabetes where their combined mechanisms might offer benefits, provided these are not explicitly claimed.
- Synergy Research: Companies may be incentivized to conduct their own rigorous research to identify novel synergistic combinations or to challenge the synergistic claims of existing patents if they believe they are not well-supported.
For Investment Decisions:
- Competitive Landscape Analysis: Investors must assess how Ono Pharmaceutical's potential patent protection for this combination affects the competitive landscape for diabetes drugs. This includes evaluating the market share and patent portfolios of other key players like Novo Nordisk, AstraZeneca, Eli Lilly, Merck, and Takeda.
- Due Diligence on Combination Therapies: For investors considering funding companies involved in developing combination diabetes therapies, a deep dive into the patent status of specific GLP-1 RA/DPP-4 inhibitor combinations is critical. JP2023091072 represents a potential patent barrier to be aware of.
- Market Opportunity Assessment: The market for type 2 diabetes treatments is vast and growing. Understanding the specific advantages Ono Pharmaceutical claims for its combination (e.g., enhanced synergy, specific patient populations) helps in assessing the potential market penetration and revenue generation. If the synergy is substantial and well-documented, it could justify premium pricing and a significant market share.
- Licensing and Acquisition Opportunities: The patent application may present opportunities for other companies. Ono Pharmaceutical might license its technology to other manufacturers, or if the patent is granted and proves valuable, it could become an acquisition target for larger pharmaceutical companies looking to bolster their diabetes portfolios.
- Risk Assessment: The investment thesis for companies in this space must account for patent litigation risks. If a granted patent is challenged, or if a company is accused of infringement, it can lead to significant legal costs and potential loss of market exclusivity.
The application highlights the continued innovation in the diabetes space, aiming to improve upon existing treatment paradigms. Its ultimate impact will be determined by the patent office's decision and Ono Pharmaceutical's strategic execution in leveraging any granted patent rights.
Key Takeaways
- JP2023091072, filed by Ono Pharmaceutical, seeks patent protection for a pharmaceutical composition combining a GLP-1 receptor agonist and a DPP-4 inhibitor, aiming for synergistic glycemic control in type 2 diabetes.
- The application covers a broad range of known GLP-1 RAs and DPP-4 inhibitors, offering flexibility in potential product development.
- Demonstrating a clear, non-predictable synergistic therapeutic effect is critical for patentability, particularly for overcoming objections related to inventive step.
- The patent landscape for such combinations is competitive, with major pharmaceutical companies holding significant portfolios for GLP-1 RAs and DPP-4 inhibitors.
- The patent's scope, if granted, will dictate freedom-to-operate for competitors and influence R&D directions and investment strategies in the diabetes market.
FAQs
- What specific prior art would the JPO likely consider when examining JP2023091072?
The JPO would consider existing patents and scientific literature disclosing GLP-1 receptor agonists, DPP-4 inhibitors, their known therapeutic effects, and any previously disclosed combinations of these drug classes, especially those suggesting additive or synergistic effects.
- How does the claimed synergistic effect differ from an additive effect in pharmaceutical patents?
An additive effect is when the combined effect of two drugs is equal to the sum of their individual effects. A synergistic effect is when the combined effect is greater than the sum of their individual effects. Patents often require the demonstration of synergy for a combination to be considered novel and possess an inventive step.
- What is the typical duration of patent protection for a drug in Japan?
Standard patent protection in Japan is 20 years from the filing date, subject to payment of annual renewal fees. For pharmaceuticals, it is possible to obtain an extension of term of up to five years to compensate for the time lost during regulatory approval processes.
- Can a company use a combination of a GLP-1 RA and a DPP-4 inhibitor if they are off-patent individually?
Yes, if the individual components are no longer under patent protection, a company can generally use them. However, a patent on a specific combination of these drugs, or a specific formulation of that combination, can still block competitors from marketing that particular combination or formulation, even if the individual drugs are generic.
- What are the primary regulatory hurdles for a combination diabetes therapy in Japan?
Beyond patent protection, regulatory approval by the Pharmaceuticals and Medical Devices Agency (PMDA) is required. This involves demonstrating safety and efficacy through clinical trials, including evidence of improved glycemic control and potentially other benefits like cardiovascular outcomes or weight management, along with robust quality control of the manufacturing process.
