Last updated: February 19, 2026
What is the Core Invention Protected by EP1586571?
European Patent EP1586571 protects novel chemical entities, specifically substituted quinoline derivatives. These compounds are characterized by a particular structural motif that confers specific pharmacological activity. The patent claims compositions comprising these active pharmaceutical ingredients (APIs) and their use in treating certain medical conditions. The primary therapeutic area targeted by the invention is inflammatory diseases. The disclosed compounds exhibit inhibitory activity against Janus kinase (JAK) enzymes, which are critical mediators of inflammatory signaling pathways. Specifically, the patent references inhibition of JAK1, JAK2, JAK3, and TYK2.
What are the Key Structural Features and Claims of EP1586571?
The patent's primary claims revolve around a general chemical structure for the substituted quinoline derivatives. Formula (I) is central to the patent, defining the core chemical scaffold and the substituents at various positions.
The general formula is described as:
R1 is selected from H, alkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, CN, COR, CONR2R3, OR, NR2R3, SR, SO2R, and optionally substituted versions of these.
R2 is selected from H, alkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, CN, COR, CONR2R3, OR, NR2R3, SR, SO2R, and optionally substituted versions of these.
R3 is selected from H, alkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, CN, COR, CONR2R3, OR, NR2R3, SR, SO2R, and optionally substituted versions of these.
R4 is selected from H, alkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, CN, COR, CONR2R3, OR, NR2R3, SR, SO2R, and optionally substituted versions of these.
R5 is selected from H, alkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, CN, COR, CONR2R3, OR, NR2R3, SR, SO2R, and optionally substituted versions of these.
R6 is selected from H, alkyl, haloalkyl, cycloalkyl, aryl, heteroaryl, CN, COR, CONR2R3, OR, NR2R3, SR, SO2R, and optionally substituted versions of these.
X is selected from O, S, NR, CO, SO2, or a direct bond.
Y is selected from O, S, NR, CO, SO2, or a direct bond.
Z is selected from O, S, NR, CO, SO2, or a direct bond.
Specific examples of preferred compounds are provided within the patent, detailing particular combinations of R groups and substituents that demonstrate potent JAK inhibitory activity. These exemplified compounds are crucial for understanding the practical scope of protection.
The patent also claims:
- Pharmaceutical Compositions: These include at least one compound of Formula (I) and a pharmaceutically acceptable carrier, diluent, or excipient.
- Methods of Treatment: The patent claims the use of these compounds for treating diseases mediated by JAK signaling pathways, specifically mentioning inflammatory and autoimmune disorders. Examples include rheumatoid arthritis, psoriasis, Crohn's disease, and multiple sclerosis.
- Polymorphs and Salts: The patent may also cover specific crystalline forms (polymorphs) or pharmaceutically acceptable salts of the claimed active compounds, which can offer distinct advantages in formulation and bioavailability.
What is the Territorial Scope and Validity of EP1586571?
EP1586571 is a European patent application that has proceeded to grant. Its territorial scope covers the member states of the European Patent Organisation for which validation has been completed. As of the last available data, EP1586571 is validated in a significant number of European countries.
Key Validation Status:
- Granted Date: October 25, 2007.
- Expiry Date (without extensions): October 10, 2026.
- Validated States (representative list): Germany, France, United Kingdom, Spain, Italy, Netherlands, Switzerland, Sweden, Denmark, Norway, Finland, Austria, Belgium, Portugal, Ireland, Luxembourg, Greece, Poland, Czech Republic, Hungary, Romania, Slovakia, Slovenia, Estonia, Lithuania, Latvia, Cyprus, Malta, Bulgaria.
The validity of EP1586571 is subject to ongoing maintenance fees. Any party seeking to challenge its validity would typically initiate opposition proceedings before the European Patent Office (EPO) within nine months of grant, or pursue national invalidation actions in validated member states. Post-grant opposition is a common route for challenging patent validity.
Who Owns EP1586571 and What is the Competitive Landscape?
EP1586571 is assigned to Centocor, Inc., a subsidiary of Johnson & Johnson. This ownership indicates that the patent holder is a major pharmaceutical entity with significant R&D investment and commercialization capabilities.
The competitive landscape for JAK inhibitors is crowded and highly active. Several companies have developed and are marketing JAK inhibitor drugs. Key competitors and their relevant drug products include:
- Pfizer Inc.: Tofacitinib (Xeljanz), Ritlecitinib (Litfulo).
- Eli Lilly and Company: Baricitinib (Olumiant), Abrocitinib (Cibinqo).
- AbbVie Inc.: Upadacitinib (Rinvoq).
- Incyte Corporation / Novartis AG: Ruxolitinib (Jakafi/Jakavi), Siponimod (Mayzent, indirect JAK pathway modulator).
- Gilead Sciences, Inc.: Filgotinib (Jyseleca).
EP1586571 represents a portion of the broader JAK inhibitor patent landscape. The specific quinoline derivatives claimed in EP1586571 may or may not directly correspond to commercially available drugs, but they establish a baseline of proprietary technology in a specific chemical space relevant to JAK inhibition. The scope of the claims will determine the degree of overlap with competitors' products and patents.
What is the Patent Prosecution History and Key Amendments?
The prosecution history of EP1586571 reveals strategic amendments made during examination to address objections raised by the EPO. These amendments are critical for understanding the final scope of protection and potential vulnerabilities.
Key Stages and Amendments:
- Filing Date: October 11, 2005.
- Publication Date: October 12, 2006.
- Grant Date: October 25, 2007.
During the examination phase, the EPO typically raises objections related to novelty, inventive step, and sufficiency of disclosure. To overcome these, applicants often amend the claims, providing additional data, or narrowing the scope of protection. For EP1586571, likely amendments involved:
- Narrowing of Chemical Scope: The original broad claims may have been refined to specific sub-groups of quinoline derivatives or even to specific exemplified compounds to distinguish them from prior art.
- Clarification of Therapeutic Use: Claims related to methods of treatment might have been made more specific, focusing on particular disease indications or patient populations.
- Addition of Supporting Data: Further biological data demonstrating the efficacy and selectivity of the claimed compounds for JAK inhibition could have been submitted.
The specific amendments made to the claims during prosecution are documented in the publicly available EPO file wrapper for the patent. Analyzing these amendments provides insight into what prior art the patent holder had to overcome and the final, narrower scope of protection they secured. For instance, if the patent holder had to exclude certain structural variations or specific therapeutic applications to gain grant, those exclusions define boundaries for competitors.
What is the Remaining Patent Term and Potential for Market Exclusivity?
The remaining patent term for EP1586571 is a critical factor for R&D and investment decisions.
- Original Expiry: October 10, 2026.
Given the grant date of October 25, 2007, and an initial filing date of October 11, 2005, the standard 20-year term from the filing date applies. This provides a limited remaining period of market exclusivity for any product directly covered by the core claims of this patent.
Potential for Extensions:
In some jurisdictions, Supplementary Protection Certificates (SPCs) can extend patent protection for pharmaceutical products. SPCs compensate for the time lost during the regulatory approval process. If a product based on the claims of EP1586571 successfully navigates regulatory approval, an SPC could be sought in relevant member states. The duration of an SPC is typically up to five years, extending the effective patent term for a specific product. The eligibility and duration of SPCs depend on national laws and the timing of regulatory approvals.
The limited remaining term of EP1586571 means that its primary strategic value might lie in its foundational nature for specific chemical classes of JAK inhibitors, rather than providing long-term market exclusivity for a new drug launch. Companies looking to enter this therapeutic space might focus on compounds not covered by this patent's expired or soon-to-expire claims, or on developing next-generation therapies with improved profiles.
What is the Freedom-to-Operate (FTO) Landscape for Compounds Claimed in EP1586571?
Assessing the Freedom-to-Operate (FTO) for compounds within the scope of EP1586571 requires a detailed analysis of its claims against a company's intended product or process.
- Direct Infringement: Any entity manufacturing, using, selling, or importing a substituted quinoline derivative that precisely matches the structural definition in the independent claims of EP1586571, or falls within a dependent claim, would likely be infringing the patent, provided it is still in force in the relevant territory.
- Indirect Infringement: If the claimed compounds are specifically designed for a method of treatment claimed in EP1586571, then the use of these compounds for that purpose could also constitute infringement.
- Polymorphs and Salts: If the patent claims specific, novel, and inventive polymorphs or salts, then the commercialization of those specific forms could also infringe.
FTO Considerations for Competitors:
Companies developing JAK inhibitors must conduct thorough FTO searches to ensure their pipeline compounds do not infringe on existing patents, including EP1586571. This involves:
- Claim Mapping: Comparing the structure and intended use of their compound against each claim of EP1586571.
- Prior Art Analysis: Understanding the prosecution history and the specific prior art that the patent holder had to distinguish from. This can reveal the narrowness of the granted claims.
- Competitor Patent Analysis: Examining the broader patent landscape for JAK inhibitors, as other patents may claim overlapping or related chemical matter or therapeutic uses.
Given the remaining term, EP1586571's FTO implications are most relevant for short-to-medium term market entry strategies or for existing products nearing patent expiry. For long-term R&D, the focus will shift to patent landscapes of more recently filed applications and granted patents in the JAK inhibitor space.
Key Takeaways
- EP1586571 protects substituted quinoline derivatives designed as JAK inhibitors for inflammatory and autoimmune diseases.
- The patent is owned by Centocor, Inc. (Johnson & Johnson) and expires in October 2026.
- The claims define a specific chemical structure with broad substituent possibilities, with particular emphasis on exemplified compounds.
- The competitive landscape for JAK inhibitors is dense, featuring multiple marketed products from major pharmaceutical companies.
- The remaining patent term is limited, suggesting its primary value may be in defining early chemical space rather than offering long-term market exclusivity for new drug launches.
- Freedom-to-Operate analysis is critical for any entity developing JAK inhibitors to avoid infringement of this and related patents.
FAQs
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Can I develop a JAK inhibitor if it is structurally similar but not identical to the compounds in EP1586571?
Freedom-to-operate analysis is required. If your compound falls outside the literal scope of the claims but may be considered equivalent under the doctrine of equivalents in some jurisdictions, or if it is covered by a dependent claim, infringement could still be a risk. Competitors often design around patents by making minor structural modifications.
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What is the significance of the grant date (October 25, 2007) versus the filing date (October 11, 2005)?
The 20-year patent term is calculated from the filing date. Therefore, the patent expires on October 10, 2026 (20 years from October 11, 2005). The grant date indicates when the patent was formally issued, and the nine-month opposition period begins from this date.
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Are there any pending applications or granted patents related to EP1586571 owned by the same entity?
Yes, it is highly probable that Centocor/Johnson & Johnson has filed and obtained numerous related patents covering different chemical entities, formulations, or methods of use within the JAK inhibitor space. A comprehensive patent landscape analysis would be necessary to identify these.
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What are the implications of the limited remaining term for investment in this specific chemical class?
For direct investment in products solely relying on the claims of EP1586571 for market exclusivity, the limited term suggests a higher risk profile for long-term returns. Investment might be more strategically aligned with pipeline assets protected by newer patents or with novel mechanisms of action.
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Can I use a JAK inhibitor related to EP1586571 for research purposes without infringing?
Research exemptions vary by jurisdiction. Generally, conducting research and development activities for the purpose of discovering or developing new drugs, which may involve testing patented compounds in a laboratory setting and not for commercial exploitation, may be permitted under specific research exemptions. However, any commercial use, including selling the compound or its derivatives, would likely require a license.
Citations
[1] European Patent EP1586571. (2007). Substituted quinolines and their use in the treatment of inflammatory and autoimmune diseases. European Patent Office.
[2] Centocor, Inc. (2005). European Patent Application No. 05 021 757.7. European Patent Office.
[3] European Patent Office. (n.d.). European Patent Register: EP1586571. Retrieved from [EPO Register Searchable Database]
