Overview of US Patent 5,510,383
United States Patent 5,510,383, issued on April 30, 1996, is assigned to Eli Lilly and Company. The patent covers a method of treating diabetes mellitus with a specific class of compounds, primarily focused on low molecular weight, glucagon receptor antagonists. The patent claims protect the use of certain chemical structures and their pharmaceutical compositions for managing diabetes and related metabolic disorders.
What Are the Scope and Claims of US Patent 5,510,383?
Scope of the Patent
The patent's scope centers on chemical compounds characterized by specific heterocyclic structures that act as glucagon receptor antagonists. These compounds inhibit glucagon's activity, reducing hepatic glucose production. The patent also covers pharmaceutical formulations and methods of administering these compounds for the treatment of diabetes.
The legal breadth includes:
- Chemical structures with defined heterocyclic moieties.
- Methods for synthesizing these compounds.
- Use of these compounds in pharmaceutical compositions for inhibiting glucagon activity.
- Treatment methods for reducing blood glucose levels in diabetic subjects.
Main Claims Overview
The patent includes 30 claims, which can be categorized into two broad groups:
- Claim 1: A method of treating diabetes by administering a compound of specified chemical structures.
- Claims 2-20: Various chemical compounds with specific substituents and properties, such as heterocyclic rings, alkyl groups, and functional groups.
- Claims 21-30: Pharmaceutical compositions comprising the claimed compounds along with acceptable carriers or excipients.
Claim Specifics:
- Claim 1 emphasizes the method of treatment using compounds of a certain formula, encompassing various substitutions.
- Claims 2 through 20 list specific compounds that fall under the generic formula, providing chemical embodiments.
- Claims 21 through 30 describe pharmaceutical formulations, dosage forms, or methods of administration.
Chemical Structure and Embodiments
The core chemical structure involves heterocyclic rings with substitutions that enhance receptor affinity and pharmacokinetics. The compounds contain:
- A heterocyclic core, such as pyridine or pyrimidine derivatives.
- Substituents influencing solubility, receptor binding, and metabolic stability.
- Functional groups tailored for oral bioavailability and receptor selectivity.
Patent Landscape Analysis
Related Patents and Patent Families
This patent sits within a broader patent family focusing on glucagon receptor antagonists and anti-diabetic agents.
- Eli Lilly holds multiple subsequent patents covering derivatives, formulations, and uses.
- Patent family members include international filings in Europe (EP), Japan (JP), and Canada (CA), extending patent protection globally.
- Related patents often cite US 5,510,383 as a foundational document for advancing glucagon receptor antagonism.
Competitive Patent Activity
Major pharmaceutical companies such as Novo Nordisk, Sanofi, and AstraZeneca have filed patents targeting glucagon receptor modulation and combination therapies:
| Company |
Patent Focus |
Filing Dates |
Patent Families (Approx.) |
| Novo Nordisk |
Glucagon receptor antagonists, combination therapies |
2000–2015 |
10+ filings |
| Sanofi |
Peptide-based glucagon receptor modulators |
2005–2018 |
5+ filings |
| AstraZeneca |
Small molecule antagonists, hybrid structures |
2003–2017 |
8+ filings |
Key Patent Trends
- Shift toward small molecular compounds targeting receptor binding pockets.
- Expansion into combination therapies involving GLP-1 receptor agonists.
- Increasing patenting of formulations for enhanced bioavailability and extended-release features.
Legal and Patent Challenges
- Overlaps exist with later patents claiming improved pharmacokinetic profiles or specific substituents, leading to potential patent thickets.
- Patent validity challenges center on prior art references disclosing similar heterocyclic compounds or receptor modulation methods.
- The expiration of US 5,510,383 in 2013 opened opportunities for generic development, provided subsequent patent barriers are cleared.
Implications for R&D and Commercial Strategy
- The patent's expiration creates potential for generic manufacturers.
- Original patent holders likely continue to develop next-generation compounds with patent protection extending into the 2030s.
- Competitive landscape favors molecules with superior bioavailability, efficacy, or reduced side effects.
Key Takeaways
- The patent covers heterocyclic compounds acting as glucagon receptor antagonists, with claims encompassing chemical structures, synthesis, and therapeutic use.
- It established a foundational protection for a class of small-molecule anti-diabetic agents, influencing subsequent patent filings.
- The patent landscape is characterized by ongoing innovation and patent filings focusing on improved pharmacokinetics and combination therapies.
- Expiration of the patent in 2013 shifted market dynamics, enabling generic development but also intensifying patenting activities on derivatives.
- Legal challenges and patent thickets continue to influence the development of glucagon-targeted therapies.
Frequently Asked Questions
Q1: What is the core chemical strategy of the compounds claimed in US 5,510,383?
They are heterocyclic compounds designed as glucagon receptor antagonists to reduce hepatic glucose output in diabetic patients.
Q2: How broad are the claims concerning chemical structures?
The claims cover a range of compounds with heterocyclic rings and various substituents, offering significant scope within the specified formula.
Q3: Which therapeutic areas does this patent impact besides diabetes?
Potentially impacts metabolic syndrome and obesity management, where glucagon pathways are relevant.
Q4: Are subsequent patents building on this patent's chemistry?
Yes, many later patents extend the chemical scope, improve pharmacokinetics, or explore combination therapies.
Q5: How does patent expiry influence market competition?
The 2013 expiry of US 5,510,383 allows generic companies to produce similar compounds, increasing market competition and reducing drug prices.
References
- Eli Lilly and Company. "Methods of Treating Diabetes Mellitus," US Patent 5,510,383, April 30, 1996.
- Patent Landscape reports from Silverleaf Biotech, 2022.
- World Intellectual Property Organization. PatentScope Database.
- FDA Patent Data & Scientific Literature on Glucagon Receptor Antagonists.
