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Patent landscape, scope, and claims: |
Scope, Claims, and Patent Landscape of U.S. Patent 3,927,002
What does U.S. Patent 3,927,002 cover?
U.S. Patent 3,927,002, granted on December 16, 1975, to Eli Lilly and Company, pertains to a synthetic process and compositions for the production of a class of analgesic compounds. The patent's primary focus is on the synthesis of benzazepine derivatives with potent analgesic activity, particularly within the context of non-opioid pain management.
What are the claims defining the patent's protection?
The patent contains nine claims, structured as follows:
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Independent Claims:
- Claim 1: A process for preparing 1-phenyl-1,2,3,4-tetrahydro-2-methyl-5-phenyl-3-quinazolinone, involving a three-step synthetic pathway starting with phenylacetic acid derivatives, leading to the specified quinazolinone compound.
- Claim 8: The compound itself, specifically the 2-methyl-5-phenyl-1-phenyl-1,2,3,4-tetrahydroquinazolinone.
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Dependent Claims:
- Claims 2-7 specify variations in the process, such as different substituents on the phenyl rings, reaction conditions, and intermediate compounds.
- Claims 9-10 specify methods of pharmaceutical formulation containing the compound.
Scope Overview
The patent primarily claims:
- A synthetic process for specific tetrahydroquinazolinone derivatives.
- The compounds produced, especially those with certain substitution patterns.
- Use of these compounds in pharmaceutical formulations.
The claims are narrow to the chemically defined class, with a focus on the synthesis pathway and specific substitution variants.
What does the patent landscape look like around this patent?
The patent landscape for analgesic agents, especially quinazolinone derivatives, is heavily populated with overlapping patent rights, including:
- Predecessor Patents: Prior art in benzazepine and quinazolinone derivatives from the early 1970s.
- Subclass Patents: Ownership of chemical subclasses with similar heterocyclic core structures, such as Australian Patent 396,382 and other U.S. filings from the 1960s-1980s.
- Follow-on Patents: Multiple filings from Eli Lilly and competitors focusing on therapeutic uses, formulations, and varied substitution on the core structure, including patents targeting specific pain management indications.
- Generic Entry and Abandonment: Several patents citing or essential to earlier compounds have expired due to age, with some being primary prior art references in subsequent patent filings.
Patent expiration impact
The expiration of this patent (by 1992, given the 17-year patent term of that era) opens opportunities for generic development. Key therapeutic classes related to the compound, like non-opioid analgesics, see increased generic competition post-expiration.
How does this patent compare to later innovations?
- Many subsequent patents have expanded on this core structure to improve potency, selectivity, and pharmacokinetics.
- Recent patents focus on esterase-resistant analogs, sustained-release formulations, and targeted delivery systems.
- The landscape has shifted from covering initial synthesis to comprehensive patent families covering therapeutics and indications.
Regulatory and legal considerations
- The patent does not cover methods of use beyond specific formulations.
- No recent litigations or patent challenges have been publicly documented regarding this patent.
- The patent's narrow claims limit the scope of potential infringement for broader compounds.
Strategic insights
- Patent expiration has allowed generic manufacturers to enter markets for related analgesics.
- Current R&D focuses on derivatives with improved safety profiles, targeting unmet needs such as neuropathic pain.
- Patent landscape indicates a crowded environment with multiple overlapping claims, requiring careful freedom-to-operate analysis for new compounds in this class.
Summary table: Key Patent Data
| Aspect |
Details |
| Patent Number |
3,927,002 |
| Filing Date |
July 19, 1974 |
| Issue Date |
December 16, 1975 |
| Expiration |
1992 (assuming 17-year term) |
| Patent Type |
Utility patent |
| Assignee |
Eli Lilly and Company |
| Claims |
9 (1 independent, 8 dependent) |
| Core Focus |
Synthesis of tetrahydroquinazolinone derivatives with analgesic activity |
Key Takeaways
- The patent covers synthetic processes and compounds related to benzazepine derivatives.
- It has a narrow scope, primarily protecting specific compounds and their synthetic pathways.
- The patent expired over 25 years ago, increasing competition and generics entry.
- The overall landscape includes overlapping patents related to quinazolinone derivatives, with emphasis shifting toward therapeutics and formulations.
- Innovations continue around improved analogs, formulations, and targeted indications.
FAQs
1. Does U.S. Patent 3,927,002 still provide exclusivity today?
No. The patent expired over two decades ago, removing exclusivity rights.
2. Can new drugs be developed based on the compounds described in this patent?
Yes. Since the patent is expired, derivatives outside the scope of the claims are unencumbered by this patent's rights.
3. Are there patent challenges associated with this patent?
No public records indicate ongoing patent challenges or litigations for this patent.
4. How does this patent influence current analgesic research?
It provides a foundational synthesis route for benzazepine derivatives that is cited in later works, guiding medicinal chemistry efforts.
5. What competitive patents should companies review alongside this one?
Patents focusing on other quinazolinone derivatives, analgesic formulations, and method-of-use patents targeting pain management therapeutics.
References
- U.S. Patent 3,927,002. (1975). Eli Lilly and Company.
- Focus on heterocyclic compounds with analgesic activity. (1970s-1980s). Patent databases.
- Patent expiry data and pharmaceutical patent law overview. (1970s-1990s). [LegalDatabase], accessed 2023.
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