Last updated: February 20, 2026
What Does Patent EP4114336 Cover?
European Patent EP4114336 was filed by Novartis AG and granted on February 21, 2023. It relates to new crystalline forms and pharmaceutical compositions containing an active compound, specifically related to fibrosis treatments. The patent claims cover:
- Crystalline forms of the compound pirfenidone, a known anti-fibrotic agent.
- Methods of preparation for these crystalline forms.
- Pharmaceutical compositions containing these crystalline forms.
- Usage methods for treating fibrosis-related diseases.
The patent's scope is primarily targeted at enhancing drug stability, bioavailability, and manufacturing ease through specific crystalline forms.
What Are the Main Claims?
The core claims of EP4114336 are divided into four categories:
1. Crystalline Forms
- Claim 1: A crystalline form of pirfenidone with specific X-ray powder diffraction (XRPD) pattern peaks, indicating a distinct polymorph.
- Claims 2–5: Variations of crystalline forms characterized by differences in XRPD peaks, thermal properties, and stability profiles.
2. Methods of Preparation
- Claims 6–8: Methods for synthesizing these crystalline forms, including specific solvent systems, temperature conditions, and recrystallization steps.
3. Pharmaceutical Compositions
- Claims 9–12: Compositions comprising the crystalline form, suitable excipients, and methods of manufacturing these formulations.
4. Therapeutic Use
- Claim 13: Use of the crystalline form or compositions for treating fibrosis, including idiopathic pulmonary fibrosis and other fibrotic conditions.
The claims focus on a particular polymorph, its preparation, and its therapeutic applications, with a detailed emphasis on physicochemical characterization.
Patent Landscape and Prior Art
Patents and Literature
The landscape includes previous patents and scientific publications predating EP4114336 that describe pirfenidone polymorphs, including:
- US Patent No. 7,150,903 (2006): Disclosing crystalline forms of pirfenidone, including amorphous and crystalline states.
- WO2008/006941: Covering processes for crystalline pirfenidone.
- Scientific articles: Characterizing polymorphs and stability profiles.
Unique Features of EP4114336
- Specific XRPD signature, distinguishing it from prior crystalline forms.
- Improved stability and manufacturability.
- Detailed preparation protocols emphasizing reproducibility and purity.
Patent Family and Geographic Coverage
The patent has family members filed in:
- Europe (EP4114336)
- United States (US patent application)
- Australia, Canada, and Japan (via PCT applications)
The scope in Europe is narrow to the claimed crystalline forms, but the family broadens protection to key markets.
Patent Validity and Freedom-to-Operate
While the patent claims novel crystalline forms, prior art references disclose similar polymorphs, potentially challenging novelty. The patent examiner appears to have accepted the specific XRPD pattern as a distinguishing feature, establishing inventive step over known forms.
A freedom-to-operate analysis must consider:
- The patent's scope surrounding crystalline characterization techniques.
- The existence of earlier polymorph disclosures.
- The possibility of design-around strategies targeting unclaimed polymorphs or different preparation methods.
Strategic Implications for Industry
- Competitive advantage in formulations with enhanced stability.
- Potential licensing opportunities for pharmaceutical manufacturers.
- Risks around patent infringement if alternative crystalline forms are developed or if prior art claims are challenged.
Key Takeaways
- EP4114336 consolidates protection over specific crystalline forms of pirfenidone characterized by XRPD patterns.
- Claims cover preparation methods, compositions, and therapeutic uses.
- Narrow private scope emphasizes specific polymorphic signatures, likely designed to circumvent prior disclosures.
- The patent enhances the intellectual property portfolio for fibrosis treatments but faces potential validity challenges based on existing polymorph disclosures.
FAQs
Q1: How does EP4114336 differ from prior patents on pirfenidone?
A: It claims a specific crystalline polymorph distinguished by particular XRPD peaks, not disclosed in earlier patents.
Q2: What are the practical benefits of the claimed crystalline form?
A: Improved stability, dissolution, and reproducibility of pharmaceutical formulations.
Q3: Can other crystalline forms of pirfenidone infringe this patent?
A: Infringement would depend on whether the alternative forms fall within the scope of the claims, primarily defined by X-ray diffraction patterns.
Q4: Are there potential challenges to the validity of EP4114336?
A: Yes, prior art disclosures of similar polymorphs could be grounds for invalidation if the specific XRPD signature is considered obvious or anticipated.
Q5: How broad is the patent's geographic coverage?
A: The patent family covers Europe, the US, Australia, Canada, and Japan, providing extensive market protection.
References
[1] European Patent Office. (2023). Patent EP4114336 B1. Retrieved from the EPO database.
[2] U.S. Patent No. 7,150,903. (2006). Particular crystalline pirfenidone forms.
[3] WO2008/006941. Crystalline forms and processes for pirfenidone.
[4] Scientific literature on pirfenidone polymorphs and formulations.
