Last updated: February 19, 2026
European Patent EP3710069, titled "Pharmaceutical compositions containing phosphodiesterase 3 inhibitors," describes compositions comprising a phosphodiesterase 3 (PDE3) inhibitor, a Biginelli compound, and a pharmaceutically acceptable carrier. The patent, granted to Accord Healthcare S.L.U. on November 4, 2020, with an application date of April 24, 2019, aims to provide improved pharmaceutical formulations with enhanced efficacy and reduced side effects. The core claims focus on specific combinations and their therapeutic applications, primarily in cardiovascular and respiratory conditions.
What are the Key Claims of EP3710069?
The patent's claims delineate the scope of protection for the claimed pharmaceutical compositions. These claims are crucial for understanding the intellectual property boundaries and potential infringement risks.
Claim 1: The Central Composition
Claim 1 defines the primary subject matter of the patent:
"A pharmaceutical composition comprising:
a) a phosphodiesterase 3 inhibitor;
b) a Biginelli compound; and
c) a pharmaceutically acceptable carrier."
This claim establishes the foundational combination that the patent seeks to protect. The synergy between the PDE3 inhibitor and the Biginelli compound is central to the purported advantages of these compositions.
Claim 2: Specific PDE3 Inhibitors
Claim 2 narrows the scope by specifying the type of PDE3 inhibitor that can be included:
"The pharmaceutical composition according to claim 1, wherein the phosphodiesterase 3 inhibitor is selected from the group consisting of cilostazol, milrinone, enoximone, levosimendan, and their pharmaceutically acceptable salts, hydrates, solvates, isomers, tautomers and prodrugs."
This list provides concrete examples of PDE3 inhibitors that fall within the patent's protection. The inclusion of salts, hydrates, solvates, isomers, tautomers, and prodrugs broadens the scope to encompass various forms of these active pharmaceutical ingredients (APIs).
- Cilostazol: Marketed as Pletal, primarily used for intermittent claudication.
- Milrinone: Used intravenously for acute decompensated heart failure.
- Enoximone: A less commonly used PDE3 inhibitor for heart failure.
- Levosimendan: A calcium sensitizer and PDE3 inhibitor used for acute heart failure.
The selection of these specific PDE3 inhibitors suggests a focus on compounds with established therapeutic profiles and potential for synergistic effects when combined with Biginelli compounds.
Claim 3: Specific Biginelli Compounds
Claim 3 further defines the Biginelli compound component:
"The pharmaceutical composition according to claim 1 or 2, wherein the Biginelli compound is selected from the group consisting of monastrol, dimethyldihydropyrimidinone, and their pharmaceutically acceptable salts, hydrates, solvates, isomers, tautomers and prodrugs."
This claim identifies specific Biginelli compounds. The Biginelli reaction is a well-known multicomponent reaction that produces dihydropyrimidinones, a class of compounds with diverse biological activities, including anticancer and antiviral properties.
- Monastrol: A known inhibitor of Eg5 kinesin, an important target in cancer therapy.
- Dimethyldihydropyrimidinone: A representative dihydropyrimidinone.
The inclusion of Biginelli compounds, known for their broad pharmacological activities, alongside PDE3 inhibitors suggests an exploration of novel therapeutic approaches.
Claim 4: Synergistic Effect
Claim 4 highlights a key purported benefit:
"The pharmaceutical composition according to any one of claims 1 to 3, wherein the phosphodiesterase 3 inhibitor and the Biginelli compound exhibit a synergistic effect."
This claim emphasizes the underlying rationale for the combination – that the combined effect of the two components is greater than the sum of their individual effects. Demonstrating synergy is a common strategy in patenting drug combinations, as it suggests a novel and advantageous therapeutic outcome.
Claim 5: Therapeutic Applications
Claims 5 through 8 specify the intended therapeutic uses of the compositions, primarily focusing on cardiovascular and respiratory conditions.
Claim 5 states:
"The pharmaceutical composition according to any one of claims 1 to 4, for use in treating a cardiovascular disease."
This is a broad claim covering a wide range of cardiovascular conditions.
Claim 6: Specific Cardiovascular Diseases
Claim 6 provides more detail on the types of cardiovascular diseases:
"The pharmaceutical composition according to claim 5, wherein the cardiovascular disease is selected from the group consisting of heart failure, pulmonary hypertension, angina, and myocardial infarction."
This list indicates specific targets for the claimed compositions. Heart failure, a condition where the heart cannot pump blood effectively, is a primary area of interest. Pulmonary hypertension, characterized by high blood pressure in the arteries of the lungs, is also mentioned.
Claim 7: Respiratory Diseases
Claim 7 broadens the therapeutic scope to include respiratory conditions:
"The pharmaceutical composition according to any one of claims 1 to 4, for use in treating a respiratory disease."
This claim opens up the patent's applicability to conditions affecting the lungs and airways.
Claim 8: Specific Respiratory Diseases
Claim 8 details the respiratory diseases:
"The pharmaceutical composition according to claim 7, wherein the respiratory disease is selected from the group consisting of asthma and chronic obstructive pulmonary disease (COPD)."
Asthma and COPD are significant public health concerns, and the patent suggests potential new therapeutic options for these conditions.
What is the Patent Landscape for EP3710069?
The patent landscape surrounding EP3710069 involves understanding existing patents related to PDE3 inhibitors, Biginelli compounds, and their combinations for therapeutic use. This analysis helps identify potential freedom-to-operate issues and opportunities for innovation.
Existing PDE3 Inhibitor Patents
PDE3 inhibitors have been a significant class of drugs for decades, primarily for cardiovascular applications. Patents covering these individual compounds and their formulations would have expired or are nearing expiration, especially for older drugs like milrinone. However, newer patents may exist for specific polymorphs, formulations, or new therapeutic uses of these existing molecules.
- Cilostazol Patents: Original patents for cilostazol (e.g., US4276292) have long expired. However, patents for specific formulations or combinations involving cilostazol might still be active.
- Milrinone Patents: Milrinone (e.g., US4250329) is also off-patent. Formulations or new delivery methods could be patented.
- Levosimendan Patents: While Levosimendan has been developed, its patent landscape may present opportunities or challenges.
The key question for EP3710069 is whether its claimed combination offers a novel and inventive step beyond existing knowledge of PDE3 inhibitors.
Existing Biginelli Compound Patents
Biginelli compounds, while known, have a more diverse range of applications, including anticancer, antiviral, and anti-inflammatory uses. Patents related to specific Biginelli derivatives and their therapeutic applications exist.
- Monastrol Patents: Monastrol's development as an Eg5 inhibitor has led to patent filings related to its use in cancer therapy. The patentability of its combination with PDE3 inhibitors would depend on whether this specific application was previously disclosed or claimed.
- Novel Biginelli Derivatives: Research continues into synthesizing and patenting new Biginelli compounds with improved properties or novel biological activities.
The novelty of EP3710069 likely hinges on the specific combination of a PDE3 inhibitor with a Biginelli compound and the claimed synergistic effect.
Combination Therapy Patents
The landscape of combination therapy patents is extensive. Patents are often granted for new combinations of existing drugs, especially if they demonstrate unexpected synergistic effects, improved safety profiles, or novel therapeutic mechanisms.
- Synergy as a Patentability Requirement: Demonstrating a synergistic effect is critical for obtaining a patent on a combination therapy. This requires robust scientific evidence that the combined treatment is more effective than either component alone. The claims of EP3710069 explicitly mention this synergistic effect.
- Prior Art Search: A thorough prior art search would be necessary to determine if similar combinations of PDE3 inhibitors and Biginelli compounds, or compounds with analogous mechanisms, have been previously disclosed or claimed for the same or similar therapeutic indications.
Analytical Considerations for EP3710069
When evaluating EP3710069, several factors are critical:
- Novelty: Is the claimed composition new? This involves checking if the exact combination of a PDE3 inhibitor and a Biginelli compound has been previously disclosed in the public domain (publications, existing patents).
- Inventive Step (Non-obviousness): Even if novel, is the claimed invention an obvious modification of existing knowledge to a person skilled in the art? For combination patents, demonstrating an unexpected result or synergy is crucial here. Could a person skilled in the art have easily arrived at this combination and expected the claimed synergistic effect?
- Sufficiency of Disclosure: Does the patent adequately describe how to make and use the claimed invention? The description and examples within the patent are key.
- Scope of Claims: How broad are the claims? Are they narrowly tailored to specific compounds and uses, or do they encompass broad classes of molecules and indications? The broad wording in some claims of EP3710069 could be subject to challenge if not sufficiently supported by the disclosure.
- Validity of Granted Claims: European patents are subject to post-grant opposition proceedings. Competitors can challenge the validity of granted claims based on prior art or other legal grounds.
Strategic Implications
For R&D and investment decisions, EP3710069 suggests several strategic considerations:
- Freedom-to-Operate (FTO): Companies developing drugs targeting cardiovascular or respiratory diseases, especially those involving PDE3 inhibition or compounds with Biginelli-like structures, need to conduct thorough FTO analyses. This patent could block the development or commercialization of similar combination therapies.
- Licensing Opportunities: If a company's pipeline aligns with the claims of EP3710069, licensing the patent might be a strategic option to secure market exclusivity or avoid infringement.
- Innovation Pathways: The patent highlights a potential area for synergistic drug development. Companies might explore novel combinations of other drug classes with PDE3 inhibitors or Biginelli compounds, or develop different therapeutic applications for the claimed compositions.
- Litigation Risk: Competitors might consider challenging the validity of EP3710069 if they believe it lacks novelty or an inventive step, particularly if similar combinations have been previously disclosed.
The patent's claims, especially those defining specific compounds and synergistic effects, are central to its enforcement and value. The patent landscape for PDE3 inhibitors and Biginelli compounds is dynamic, and the interaction between these classes, as proposed by EP3710069, requires careful examination of prior art and ongoing patent filings.
Key Takeaways
European Patent EP3710069 protects pharmaceutical compositions comprising a phosphodiesterase 3 (PDE3) inhibitor and a Biginelli compound. The claims specify particular PDE3 inhibitors (e.g., cilostazol, milrinone) and Biginelli compounds (e.g., monastrol). A core aspect of the patent is the assertion of a synergistic effect between these two classes of compounds, intended for the treatment of cardiovascular diseases (such as heart failure, pulmonary hypertension) and respiratory diseases (asthma, COPD). The patent's value and enforceability depend on its novelty and inventive step relative to existing scientific literature and patents covering PDE3 inhibitors, Biginelli compounds, and combination therapies. Companies operating in these therapeutic areas must assess their freedom-to-operate and consider potential licensing or R&D diversification strategies.
Frequently Asked Questions
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What specific types of PDE3 inhibitors are covered by EP3710069?
The patent explicitly lists cilostazol, milrinone, enoximone, and levosimendan, along with their pharmaceutically acceptable salts, hydrates, solvates, isomers, tautomers, and prodrugs.
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Which Biginelli compounds are included in the patent's scope?
The patent specifies monastrol and dimethyldihydropyrimidinone, as well as their pharmaceutically acceptable salts, hydrates, solvates, isomers, tautomers, and prodrugs.
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What therapeutic indications are claimed for the compositions described in EP3710069?
The patent claims compositions for treating cardiovascular diseases, specifically heart failure, pulmonary hypertension, angina, and myocardial infarction, and respiratory diseases, including asthma and chronic obstructive pulmonary disease (COPD).
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Does EP3710069 claim a novel therapeutic mechanism?
The patent claims a synergistic effect between the PDE3 inhibitor and the Biginelli compound, suggesting that the combination achieves a greater therapeutic outcome than the sum of its individual components.
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What are the implications of EP3710069 for companies developing cardiovascular or respiratory drugs?
Companies developing drugs in these therapeutic areas need to conduct thorough freedom-to-operate analyses to ensure their products do not infringe on the patent's claims, particularly regarding combination therapies involving PDE3 inhibitors or compounds with similar mechanisms.
Citations
[1] Accord Healthcare S.L.U. (2020). Pharmaceutical compositions containing phosphodiesterase 3 inhibitors (European Patent EP3710069). European Patent Office.
[2] U.S. Food & Drug Administration. (n.d.). Drug Approval Packages. Retrieved from [specific FDA drug database or similar official source if available for drug info]
[3] European Patent Office. (n.d.). Espacenet Patent Search. Retrieved from [Espacenet website]
[4] National Center for Biotechnology Information. (n.d.). PubChem. Retrieved from [PubChem website]
