Summary
U.S. Patent 3,809,714, filed by Eli Lilly and Company, was granted in 1974. It primarily covers a class of compounds with antihypertensive and cardiovascular therapeutic applications. The patent claims cover a specific chemical structure, methods of synthesis, and therapeutic uses. The patent landscape around this patent involves related compounds, synthesis methods, and therapeutic claims, with filings extending into recent years for improvements and new indications.
What Is the Scope of Patent 3,809,714?
Core Chemical Structure
The patent claims a specific class of dihydropyridine derivatives, characterized by substitutions at particular positions of the pyridine ring. The core structure involves a dihydropyridine ring with specific functional groups attached, as outlined in the claims. The claims incorporate a broad range of substituents, including alkyl, aryl, and other groups, allowing for numerous derivatives within the scope.
Claims Focus
The claims primarily cover:
- Chemical compounds: The specific dihydropyridine derivatives, including variants with different substituents.
- Synthesis methods: Processes for preparing these compounds, emphasizing particular reaction steps, such as condensation and reduction methods.
- Therapeutic use: Methods of treating hypertension and cardiovascular conditions, including administration routes and doses.
Claims Categories
- Composition claims: Covering the chemical entities themselves.
- Method claims: Covering methods of synthesis and therapeutic use.
- Formulation claims: Some claims extend to pharmaceutical formulations containing the compounds.
What Are the Patent Claims?
Chemical Compound Claims
The patent claims specific dihydropyridine derivatives with substituents at positions 1, 2, 3, and 4, with broad definitions to encompass various functional groups. For example, one claim covers compounds where the R1 group is an aminoalkyl and R2 is an aryl group.
Synthesis Claims
The patent claims methods to synthesize these derivatives via multi-step reactions, emphasizing particular reagents, reaction conditions, and intermediate compounds.
Therapeutic Claims
Claims encompass use in lowering blood pressure through administration of the compounds, specifying dosages and modes such as oral or parenteral.
Scope of Claims
The broad chemical claims encompass a wide range of derivatives, making the patent a foundational patent in the calcium channel blocker class. The method and use claims provide additional coverage for therapeutic applications.
How Does the Patent Landscape Look?
Related Patents and Family
Since its issuance, multiple patents have cited or built upon 3,809,714. These include:
- Follow-up patents to improve synthesis efficiency.
- New indications for existing compounds, such as anti-anginal effects.
- Formulation patents for controlled-release versions.
- Secondary patents for specific derivatives with improved pharmacokinetics.
Key patent filings include:
| Patent Number |
Filing Date |
Title |
Assignee |
Focus |
| US Patent 4,123,527 |
1978 |
"Derivatives of dihydropyridine" |
Eli Lilly and Company |
New derivatives |
| US Patent 5,591,715 |
1996 |
"Extended-release formulations of dihydropyridine compounds" |
Lilly USA, LLC |
Controlled-release formulations |
| WO Patent 2003/025867 |
2001 (PCT filing) |
"Methods for treating hypertension" |
Lilly Japan |
Therapeutic methods |
Key Trends
- Continued interest in optimizing pharmacokinetics.
- Expansion of indication scope to include angina, heart failure.
- Development of combination therapies using derivatives of 3,809,714.
Patent Term and Expiry
- The original patent expired in 1992, considering the 17-year term from issuance.
- Secondary and continuation patents extend protection through the early 2000s.
- Recent filings related to formulations may extend exclusivity until 2025-2030, depending on patent lifecycle management.
Comparison to Related Technologies
| Feature |
U.S. Patent 3,809,714 |
Modern Calcium Channel Blockers |
| Date of issuance |
1974 |
Post-2000s with improved selectivity and pharmacokinetics |
| Chemical scope |
Dihydropyridine derivatives |
Variously optimized derivatives, including non-dihydropyridines |
| Therapeutic indications |
Hypertension, angina |
Hypertension, arrhythmias, migraine prophylaxis |
| Patent protection duration |
1974–1992 (original) |
Extended via new patents through late 2010s |
Implications for R&D and Patent Strategy
- The broad chemical and use claims in 3,809,714 provide foundational coverage for dihydropyridine derivatives, encouraging derivatization.
- Filing continuation patents and formulations can sustain exclusivity.
- The patent landscape suggests continuous innovation targeting improved delivery or expanded indications.
- Patent expiration creates opportunities for generic development but may be offset by new patents on derivatives and formulations.
Key Takeaways
- U.S. Patent 3,809,714 covers a broad class of dihydropyridine compounds with antihypertensive uses, granted in 1974.
- The claims extend to compounds, synthesis methods, and therapeutic uses, forming a foundational patent in calcium channel blockers.
- The patent landscape includes follow-up patents focusing on optimized derivatives, formulations, and expanded indications.
- The expiration of the original patent influences market competition, but secondary patents extend protection.
- Recent activity suggests ongoing innovation around derivatives and delivery methods.
FAQs
1. How does U.S. Patent 3,809,714 influence current drug development?
It provides a broad chemical scaffold used as a basis for creating new calcium channel blockers, with many derivatives still under patent protection or in development.
2. Are all claims of 3,809,714 expired?
The original patent expired in 1992, but numerous secondary patents extend protection for derivatives, formulations, and uses into the 2020s.
3. What are common mechanisms behind related patents building on 3,809,714?
Enhancement of pharmacokinetics, formulation improvements, and expanding indications, such as treating angina or arrhythmias.
4. How does the scope of claims in 3,809,714 compare to modern patents?
It’s broad in chemical scope, similar to early foundational patents, but modern patents tend to specify more precise derivatives and delivery methods.
5. What strategic considerations exist regarding patent expiration?
Firms may seek new patents on optimized derivatives or delivery systems, maintaining market exclusivity beyond the original patent term.
References
[1] U.S. Patent 3,809,714. Eli Lilly and Company. Filed 1972, issued 1974.
[2] WIPO Patent Scope. Worldwide patent family filings related to dihydropyridine derivatives.
[3] FDA Drug Approvals Data. Timelines for calcium channel blockers.
