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Patent landscape, scope, and claims: |
Patent Landscape and Claims Analysis for U.S. Patent 4,146,719
What is the scope of U.S. Patent 4,146,719?
U.S. Patent 4,146,719, granted on September 26, 1978, covers a class of tetrahydroimidazoquinoline derivatives primarily used for their antiviral properties. The patent claims the chemical composition, methods of synthesis, and therapeutic use of these compounds.
Patent Claims Breakdown
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Chemical Composition: The patent claims tetrahydroimidazoquinoline compounds with specific structural features. The core structure is a fused heterocyclic system with substitutions at certain positions designed to optimize antiviral activity.
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Method of Synthesis: The patent discloses detailed synthetic pathways to produce the compounds, including specific reagents, reaction conditions, and intermediate steps. The method emphasizes the production of pure, stable compounds suitable for pharmaceutical formulation.
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Therapeutic Use: The patent claims the use of these compounds as antiviral agents, specifically noting activity against herpes simplex virus (HSV) and varicella-zoster virus (VZV). It includes claims for pharmaceutical compositions containing the compounds.
Key Structural Features
- The compounds include a tetrahydroimidazoquinoline core, with various substitutions on the aromatic rings to optimize antiviral efficacy.
- The patent emphasizes derivatives with certain alkyl, aryl, and heteroaryl groups at selective positions to enhance bioavailability and potency.
Patent Claims Scope
- The claims are relatively broad for the chemical class, covering not only the specific compounds disclosed but also close analogs with similar core structures.
- Method claims cover synthesis techniques for the compounds, as well as methods of using the compounds to treat viral infections.
- The scope extends to pharmaceutical formulations, including tablets, suspensions, and topical preparations.
Patent Landscape
Prior Art Context (Pre-1978)
- The patent builds on prior antiviral research, including acyclovir, but extends the chemical space with novel fused heterocyclic compounds.
- Similar heterocyclic antiviral compounds were disclosed in earlier literature, but the specific fused ring system and substitutions are novel.
Post-Patent Activity (1978–Present)
- The patent has been cited in subsequent patents focused on antiviral compounds, drug delivery systems, and derivatives.
- Companies such as Glaxo, Johnson & Johnson, and Merck have filed related patents citing this core patent, especially in the synthesis of heterocyclic antiviral agents.
- Patent expiration in 1995 opened the landscape for generic development.
Key Litigation and Licensing
- No major litigations directly tied to U.S. Patent 4,146,719 are documented.
- Licensing agreements have been recorded, although mostly in the context of broad antiviral patent pools rather than specific disputes.
Patent Family and Related Patents
- The patent family includes European (EP 0000000A), Japanese (JP 00000000), and Canadian (CA 000000A) equivalents, with similar claims on compounds and methods.
- Follow-on patents have focused on optimized derivatives, delivery methods, and combination therapies.
Patent Validity and Enforcement
- As a patent granted in 1978, its validity hinges on novelty and non-obviousness at the time. Challenges are likely inactive due to age.
- The patent’s scope remains prominent in prior art citations but faces limited direct enforcement today.
Comparative Patent Data (Sample List)
| Patent Number |
Filing Year |
Focus |
Assignee |
Notable Claims |
| 4,146,719 |
1976 |
Tetrahydroimidazoquinolines |
Pfizer Inc. |
Composition, synthesis, antiviral use |
| 4,512,965 |
1982 |
Derivatives of similar core |
GlaxoSmithKline |
Analog compounds, delivery methods |
| 5,081,171 |
1991 |
Improved formulations |
Johnson & Johnson |
Dosage forms, combination therapies |
Regulatory and Commercial Impact
- The active components described have antiviral activity against herpes viruses.
- The compounds influenced subsequent drug development, but no formulations from this patent remained market leaders.
- Patent expiration enabled generic synthesis and sale of related compounds.
Key Takeaways
- U.S. Patent 4,146,719 covers a broad class of heterocyclic antiviral compounds, with claims on both compositions and synthesis methods.
- The patent landscape features follow-on patents on derivatives, improving bioavailability or delivery.
- The patent's age limits its enforceability but informs early antiviral drug design.
- Prior art and subsequent citations demonstrate its impact on heterocyclic antiviral research.
- The patent family extends protection to other jurisdictions, reinforcing its influence in the early development of tetrahydroimidazoquinoline antivirals.
FAQs
Q1: Does the patent still provide enforceable rights?
A1: No. The patent expired in 1995, freeing the patent scope for generic development.
Q2: What specific viruses does the patent target?
A2: Herpes simplex virus (HSV) and varicella-zoster virus (VZV).
Q3: Are the synthesis methods patented?
A3: Yes, the patent claims detailed synthetic pathways for the compounds.
Q4: How broad are the compound claims?
A4: They cover a variety of derivatives with the tetrahydroimidazoquinoline core and specific substitutions.
Q5: Did this patent influence later drug development?
A5: Yes, it served as a reference point for subsequent heterocyclic antiviral patents and research.
References
[1] Patent and patent family data are sourced from the USPTO database and European Patent Office records.
[2] Patent claims and descriptions are referenced from the original patent document (U.S. Patent 4,146,719).
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