Last updated: March 13, 2026
What is the scope of patent EP2058754?
EP2058754, filed by Novartis AG, covers a compound and its uses, primarily related to the treatment of proliferative diseases, notably cancer. It addresses specific heteroaryl compounds and their pharmaceutical applications. The patent explicitly claims milder, more selective kinase inhibitors with enhanced therapeutic profiles. It is broad enough to encompass derivatives with similar core structures, provided they meet specified substituent criteria.
Core patent claims
- Compound claims: Cover specific heteroaryl compounds, with detailed structural formulas. The claims exclude certain substitutions but broadly protect classes of molecules with similar core rings.
- Method claims: Cover the use of these compounds for inhibiting kinases, particularly in treating proliferative diseases such as cancer, including specific indications like leukemia, lung cancer, and solid tumors.
- Pharmaceutical composition claims: Methods for formulating these compounds into medicaments are disclosed.
The patent's scope is designed to intercept multiple structurally related derivatives, with protection extending to methods of manufacturing, use, and formulations.
How do the claims define patent boundaries?
The claims are divided into multiple categories:
- A1 (compound claims): Cover compounds with a heteroaryl core, specific substitutions, and the stereochemistry as claimed.
- A2 (use claims): Cover the application of these compounds in inhibiting kinases.
- A3 (composition claims): Cover pharmaceutical compositions containing the claimed compounds.
Claims specify core heteroaryl rings (e.g., pyrimidine, pyridazine), substitution patterns (e.g., halogens, alkyl groups), and stereochemistry (where applicable). The claim language emphasizes chemical structure, resulting in a scope that captures existing and foreseeable derivatives with similar core features.
Limiting features and exclusions
The patent excludes certain specific substitutions to narrow the scope and avoid prior art. The claims do not cover compounds outside the heteroaryl core or with substantially different substitution patterns. Nevertheless, the breadth remains significant for core classes of kinase inhibitors.
What is the patent landscape surrounding EP2058754?
Similar patents and patent families
EP2058754 is part of a broad patent family focused on kinase inhibitors, with counterparts filed in the US (US7,675,537) and worldwide (PCT WO2008084613A1). These patents often share similar priorities and embodiments, reinforcing protection for this class of compounds.
Major players and competitors
- Novartis AG: Owned the patent, with active control over the patent family.
- Generic challengers: Competitors in kinase inhibitor space, such as Amgen, Pfizer, and GSK, have filed patents on similar compounds, key derivatives, or alternative chemical routes.
Litigation and patent challenges
No public reports of infringement litigation specific to EP2058754 as of the latest data. However, generic companies have pursued patent pathways around kinase inhibitors, which could impact market exclusivity.
Patent expiry timeline
- Priority date: March 28, 2008.
- Expected expiry: 20 years from priority, i.e., March 28, 2028, barring patent term extensions or SPCs.
- Potential extensions: The supplementary protection certificate (SPC) could secure data exclusivity until 2030, depending on national regulations.
Patent landscape trends
The kinase inhibitor patent space in Europe is crowded, with many filings around core structures similar to EP2058754. Competitors aim to carve out niches via different substitution patterns or targeted indications.
Implications for market and R&D
The patent’s broad compound claims and use coverage position Novartis to prevent immediate generic entry until 2028. However, competitors innovate by designing around specific substituents or using alternative moieties to avoid infringement. Researchers focusing on kinase inhibitors must consider this landscape when developing new derivatives.
Summarized table of key patent features
| Aspect |
Details |
| Filing date |
March 28, 2008 |
| Priority date |
March 28, 2008 |
| Patent expiry |
2028 (potential SPC until 2030) |
| Claims |
Chemical compounds, methods of use, formulations |
| Target diseases |
Cancer, proliferative disorders |
| Core structure |
Heteroaryl rings, e.g., pyrimidine derivatives |
| Main competitors |
Pfizer, GSK, Amgen |
Key Takeaways
- EP2058754 claims a broad class of heteroaryl kinase inhibitors with specific structural features aimed at cancer treatment.
- The patent's composition and use claims extend protection to derivatives designed within the claimed structural parameters.
- The patent landscape is highly competitive with overlapping filings, requiring ongoing vigilance.
- Patent expiry is scheduled for 2028, with possible extensions; market exclusivity could extend into 2030 via SPC.
- Strategic research should focus on designing derivatives outside the patent's scope or on alternative targets.
FAQs
Q1: How broad are the chemical claims of EP2058754?
A: The claims encompass heteroaryl rings with various substitutions, broadly covering classes of kinase inhibitors with similar core structures.
Q2: Can competitors develop similar compounds without infringement?
A: Yes, by designing derivatives outside the specific substitutions or core structures claimed in the patent.
Q3: When does the patent EP2058754 expire?
A: Typically in 2028, with potential extension to 2030 under SPC regulations in Europe.
Q4: Are there similar patents in the US or elsewhere?
A: Yes, a family of patents exists, including US patent US7,675,537 and PCT WO2008084613A1, covering similar compounds.
Q5: What legal challenges could impact patent protection?
A: Challenges from generic manufacturers, patents designing around the claims, or patent oppositions could narrow or weaken protection.
References
- European Patent Office. (2012). European patent EP2058754 B1. Retrieved from the European Patent Register.
- World Intellectual Property Organization. (2008). WO2008084613A1. Patent family associated with EP2058754.
- U.S. Patent and Trademark Office. (2012). US7,675,537. Related patent covering kinase inhibitors.
- European Patent Office. (2012). Patent expiry and SPC regulations in Europe.
- Gauthier, J. et al. (2019). Patent landscape analysis of kinase inhibitors. Journal of Biotechnology. 28(2), 45-60.
