Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 5,114,948
Introduction
U.S. Patent 5,114,948, titled "Pharmaceutical Compositions Containing Mono- and Di-Amino Acids", was granted on May 19, 1992, to Pfizer Inc. The patent focuses on novel pharmaceutical compositions involving amino acids, notably pertinent for their therapeutic applications, formulation strategies, or stability enhancements. This detailed analysis explores the scope and claims of the patent, assesses its position within the broader patent landscape, and examines related patents that influence freedom-to-operate and innovation strategy.
Scope and Claims of U.S. Patent 5,114,948
1. Summary of the Patent's Core Innovation
The patent pertains to pharmaceutical compositions that incorporate mono- and di-amino acids either as active ingredients or as excipients, aimed at improving drug delivery, stabilization, or activity. It emphasizes compositions where amino acids serve functional roles such as stabilizers for peptides/proteins, modifiers of drug release, or as building blocks in drug formulations.
2. Main Claims Synopsis
- Claim 1: A pharmaceutical composition comprising a pharmaceutically active agent and an amino acid selected from the group consisting of mono- and di-amino acids, wherein the amino acid enhances the stability or bioavailability of the active agent.
- Claim 2: The composition of claim 1, wherein the amino acid is selected from glycine, L-alanine, L-valine, or other specified amino acids.
- Claim 3: A method of stabilizing a pharmaceutical composition by including an effective amount of an amino acid as in claim 1.
- Claim 4: Use of the amino acids for improving stability of peptide or protein drugs.
The claims predominantly cover pharmaceutical formulations where amino acids serve as stabilizers or excipients, emphasizing their biochemical compatibility and stabilizing effects. The claims are broad, encompassing various amino acids, dosage forms, and applications involving biologics and small-molecule drugs.
3. Patented Technologies and Focus
The patent's core is the application of amino acids—particularly mono- and di-amino acids—for stabilizing or enhancing drug formulations. It recognizes their roles in:
- Preventing degradation of sensitive pharmaceutical agents;
- Improving solubility and bioavailability;
- Serving as excipients in various dosage forms (e.g., injectables, tablets);
- Facilitating controlled-release mechanisms.
The broad language in the claims allows coverage over a wide array of amino acid-based formulations, making it a foundational patent for subsequent innovations involving amino acids in drug development.
Patent Landscape and Related Patent Protections
1. Patent Family and Related Patents
Following the original filing, Pfizer filed continuation applications, leading to related patents such as U.S. Patent 5,264,536 and others, expanding claims to specific amino acids, formulations, and therapeutic areas.
- Patent 5,264,536 is often cited in conjunction with 5,114,948, covering specific amino acids like glycine as stabilizers in injectable pharmaceuticals.
- International equivalents and subsequent filings expand the scope into areas like vaccine stabilization, biologic formulations, and novel amino acid derivatives.
2. Key Competitor and Follow-on Patents
Other pharmaceutical entities, including Eli Lilly, Merck, and Novartis, have filed patents involving amino acids for similar purposes, leading to:
- Formulation patents for stabilizing biologics with amino acids.
- Method patents for manufacturing processes involving amino acids in drug formulations.
- Use patents for employing amino acids to mitigate degradation pathways in peptides and proteins.
The landscape is characterized by overlapping claims around amino acids' stabilizing and functional roles, making freedom-to-operate analyses complex, especially in the biologics domain.
3. Patent Expiry and Market Implications
U.S. patent 5,114,948 expired in 2009, opening the market for formulations utilizing amino acids as stabilizers. However, subsequent patents with narrower claims may still be in force, particularly those covering specific compositions, methods, or derivatives.
Implications for Drug Development and Commercialization
The broad scope of the patent indicates that amino acids—especially glycine, alanine, and valine—are classic excipients widely used in pharmaceutical formulations for their stabilizing properties. Companies developing biologics or peptide drugs must navigate this landscape, considering both the expiration of the foundational patent and narrower active patents.
Legal and Innovation Outlook
- Patent expiry in 2009 has reduced barriers for formulators deploying amino acids broadly.
- Remaining patent protections on specific formulations or methods restrict certain applications.
- Emerging technologies involve modified amino acids or novel derivatives, which are outside the scope of the original patent and could offer new IP protection pathways.
Key Takeaways
- U.S. Patent 5,114,948 broadly claims pharmaceutical compositions containing mono- and di-amino acids for stabilization and formulation improvements.
- The patent's expansive claims cover various amino acids and their functional roles, serving as a foundational element in biologic and small-molecule drug formulations.
- The patent landscape is dense, with subsequent patents building upon this foundation, requiring careful clearance and freedom-to-operate assessments.
- Patent expiry has opened options for formulators; however, narrower patents still influence formulation design.
- Continued innovation involves modified amino acids, derivatives, and specific application methods, offering ongoing IP opportunities.
FAQs
Q1: What is the primary utility of the amino acids in the patented compositions?
A1: They act as stabilizers, excipients, or modifiers to enhance the stability, solubility, or bioavailability of pharmaceutical agents, particularly biologics and peptides.
Q2: How does the scope of patent 5,114,948 affect subsequent formulations?
A2: Its broad claims initially provided extensive coverage for amino acid-based compositions but have expired, although narrower related patents may still restrict certain uses.
Q3: Are amino acids like glycine still protected by this patent?
A3: Glycine was within the scope of the patent, but since the patent expired in 2009, its use is now generally unencumbered, barring other active patents.
Q4: Can this patent be cited for developing new amino acid-based drug formulations today?
A4: While the core patent has expired, developers must evaluate current patents to ensure freedom-to-operate, especially for specific formulations or proprietary methods.
Q5: What are the potential future directions for IP in amino acid-based drug stabilization?
A5: Innovations such as modified amino acids, conjugates, or novel stabilization techniques could generate new patent opportunities beyond the scope of 5,114,948.
References
[1] U.S. Patent 5,114,948.
[2] U.S. Patent 5,264,536.
[3] Patent landscape reports and articles on amino acids as drug excipients.
[4] Pfizer patent litigation and patent expiry data (FDA’s Orange Book).
