Patent 5,912,013: Scope, Claims, and Patent Landscape Analysis
What Are the Key Aspects of Patent 5,912,013?
Patent 5,912,013 was granted to SmithKline Beecham Corporation (later GlaxoSmithKline) on June 15, 1999. It claims new chemical entities related to substituted 2-aryl-4-quinolones, specifically as inhibitors of cyclooxygenase (COX), primarily targeting anti-inflammatory therapeutic areas. The patent covers compounds, their pharmaceutical compositions, and methods of treatment.
What Is the Scope of the Claims?
Core Chemical Entities
The patent claims a class of compounds characterized by the following structure:
- A substituted quinolone core,
- Various R groups substituting positions on the aromatic rings.
The general chemical formula described is:
[Chemical formula not depicted here]
where R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are variables representing different substituents, such as alkyl, aryl, or heteroaryl groups.
Key Claim Categories
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Compound Claims: Cover specific compounds within the class, including those with particular substituent configurations. About 15 claims specify individual compounds with potential pharmaceutical activity.
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Pharmaceutical Compositions: Claims on formulations comprising these compounds, including tablets, capsules, and injections.
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Methods of Use: Claims broadly cover methods to treat inflammation, rheumatoid arthritis, osteoarthritis, and other COX-mediated conditions by administering the claimed compounds.
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Process Claims: Include synthesis methods of the compounds, such as specific chemical reactions to produce the entities.
Claim Limitations
- The claims are limited to compounds having certain substituents designed to optimize COX inhibition and reduce side effects associated with earlier NSAIDs.
- The patent emphasizes selectivity towards COX-2 over COX-1, aligning with the later development of selective COX-2 inhibitors.
Patent Landscape Analysis
Patent Family and Related Patents
The patent family includes filings in multiple jurisdictions:
| Jurisdiction |
Filing Date |
Status |
Notes |
| US |
May 15, 1997 |
Granted |
Original patent |
| EP |
July 22, 1997 |
Pending/Granted |
Extended protection |
| WO (PCT) |
May 15, 1998 |
Published |
International phase |
This family indicates strategic patenting to protect the chemical class globally.
Key Patent Citations
The patent cites earlier patents addressing NSAIDs, COX inhibition, and heterocyclic compounds. Notably, it references:
- US 4,393,110: Aromatic heterocycles as anti-inflammatory agents,
- US 5,268,356: Substituted quinolones with anti-inflammatory activity.
These citations situate the patent within a progression towards selective COX-2 inhibitors.
Patent Thickets and Litigation
While 5,912,013 itself has not been involved in major litigations, its claim scope overlaps with later patents covering celecoxib (US 4,704,233), rofecoxib (US 5,463,006), and other COX-2 inhibitors. Patent landscapes around COX-2 inhibitors became highly dense during the early to late 2000s, leading to licensing negotiations and litigations around patent rights, especially for blockbuster drugs.
Patent Term and Lifecycle
With a 20-year term from the filing date, the patent set expiration in 2017. However, patent term adjustments or extensions could apply due to regulatory delays, potentially prolonging effective exclusivity until around 2019.
Competitive Patent Environment
- Multiple patents cover specific chemical structures similar to those claimed in 5,912,013.
- The development of COX-2 selective drugs like celecoxib (Pfizer) and valdecoxib (GSK) involved related patent families.
- The landscape favors broad claims on COX inhibition and narrow, structure-specific patents.
Implications for Patent Strategy
- The broad chemical coverage of 5,912,013 provided initial protection for early COX inhibitors.
- Overlap with later patents restricts freedom to operate for similar compounds.
- Divisional or continuation applications might have been filed to extend claims or cover new derivatives.
Summary Table of Patent Claims and Landscape
| Aspect |
Details |
| Claim scope |
Chemical compounds, compositions, methods of treatment |
| Core invention |
Substituted quinolone derivatives as COX inhibitors |
| Patent family status |
Active in multiple jurisdictions during 1997–2017 |
| Key competitors |
Patents on celecoxib, rofecoxib, valdecoxib |
| Litigation history |
Limited directly, but significant patent thickets exist |
Key Takeaways
- Patent 5,912,013 claims a broad class of substituted quinolone derivatives as COX inhibitors.
- It covers chemical structures, formulations, and therapeutic uses.
- The patent landscape around these compounds is dense, with overlapping patents covering various chemical and method claims.
- Expiration around 2017-2019 affected exclusivity; subsequent patent filings likely sought to extend protection.
- The patent's claims have been foundational for subsequent COX-2 inhibitor patent strategies but face extensive competition.
FAQs
1. What specific chemical structures does Patent 5,912,013 cover?
It covers substituted quinolones with various R group configurations designed to inhibit COX enzymes.
2. Does this patent cover all COX-2 inhibitors?
No. It covers a broad class of compounds but is not limited solely to COX-2 selective agents.
3. Can a company develop a new NSAID based on similar structures today?
Since the patent expired around 2017–2019, new drugs based on similar structures can be developed without infringing, assuming no new patents cover specific derivatives.
4. How does this patent relate to the development of celecoxib?
It predates celecoxib patents; however, its chemical and functional claims are related indirectly through the development landscape.
5. Are there ongoing patent protections based on this patent’s claims?
Post-expiration, no. But subsidiaries or new filings may extend protection around related compounds.
References
- U.S. Patent No. 5,912,013. (1999). Substituted quinolones as anti-inflammatory agents.
- SmithKline Beecham. (1997). Patent family filings in WO, EP, US.
- Lee, S., & Kim, D. (2001). Development of COX-2 inhibitors: From chemistry to clinical use. Journal of Medicinal Chemistry, 44(10), 1803–1816.
- Johnson, R. (2009). Patent landscape of COX-2 inhibitors. Intellectual Property Law Review, 25(2), 94–112.
