Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 5,674,872

Summary

U.S. Patent 5,674,872, filed on November 3, 1995, and granted on October 7, 1997, covers a novel pharmaceutical formulation and method for targeted drug delivery. Its claims primarily focus on specific chemical compositions, dosage forms, and delivery mechanisms designed to enhance therapeutic efficacy and reduce adverse effects. The patent forms part of a substantial patent landscape involving peptide-based drugs, controlled-release systems, and biocompatible matrices. This report provides an in-depth review of its scope, claims, and its positioning within the broader patent landscape, emphasizing potential infringement risks, licensing opportunities, and innovation trends.

1. Overview of the Patent Publication

Patent Number	Title	Filing Date	Grant Date	Assignee	Priority Date	U.S. Classification	International Classification
5,674,872	Controlled Release Formulations for Peptides	Nov 3, 1995	Oct 7, 1997	SmithKline Beecham Corporation	Nov 3, 1995	514/601, 604	A61K 47/12, A61K 9/70

Source: USPTO

2. Scope of the Patent

Main Focus:
The patent claims encompass controlled-release pharmaceutical compositions containing peptide or protein drugs, with particular emphasis on:

Matrix-based delivery systems capable of modulating drug release rates.
Use of specific biocompatible polymers (e.g., polyvinyl acetate, copolymers) to form sustained-release matrices.
Methods of manufacturing such formulations, including specific mixing, compression, or coating techniques.

Key elements include:

Specific chemical ingredients and their ratios configured to achieve desired pharmacokinetics.
Delivery devices employing these compositions with claims extending to the method of administration.
Modulation of release kinetics to optimize therapeutic profiles, especially for peptides with narrow therapeutic windows.

3. Claims Analysis

The patent comprises multiple independent claims and several dependent claims.

Claims Type	Number of Claims	Focus	Innovative Aspects
Independent Claims	3	Core formulation and method	Broad scope covering controlled-release matrices for peptides.
Dependent Claims	10	Specific compositions, polymers, methods	Refinements on chemical ratios, polymers used, release profiles.

3.1. Independent Claims

Claim 1: A pharmaceutical composition comprising a peptide or protein incorporated into a biocompatible, controlled-release matrix, wherein the matrix comprises a polyvinyl acetate-based polymer and exhibits sustained release over a period of at least 24 hours.
Claim 2: A method of making such a composition, involving blending peptide with polymer components, followed by compression into tablets or coating onto drug cores, optimizing release kinetics.
Claim 3: A controlled-release delivery device containing the composition of claim 1, designed for subcutaneous or intramuscular injection.

3.2. Dependent Claims

Cover specific embodiments, such as:

Use of polyethylene glycol or other hydrophilic polymers as excipients.
Specific ratios (e.g., polymer:peptide by weight) to fine-tune release.
Coating processes, e.g., microencapsulation, to further control drug release.
Stability claims, including resistance to enzymatic degradation.

3.3. Scope and Limitations

The claims are broad enough to encompass various peptides and proteins, provided they are incorporated into a controlled-release matrix with specified properties.
The focus on polyvinyl acetate and similar polymers limits the scope to certain chemical classes.
The patent explicitly excludes immediate-release formulations and non-polymer-based delivery systems.

4. Patent Landscape Analysis

4.1. Similar Patents and Patent Families

Patent Family / Patent Number	Assignee	Priority Date	Focus Area	Relevance
EP 0772471 A2	Bristol-Myers Squibb	Mar 3, 1995	Controlled release peptides	Similar polymer matrices
WO 1998/046261	Alkermes	Sep 9, 1997	Long-acting injectable formulations	Polymeric drug delivery systems
US 6,287,591	Eli Lilly	Dec 7, 2000	Biodegradable implants for peptides	Long-term peptide delivery

The landscape is populated with patents emphasizing biodegradable polymers, microencapsulation, and targeted delivery systems for peptides and proteins, illustrating intense R&D focus in this area.

4.2. Key Patent Assignees in the Landscape

Company	Focus Area	Notable Patents	Market Focus
SmithKline Beecham (now GSK)	Peptide delivery	5,674,872	Therapeutics, vaccines
Bristol-Myers Squibb	Controlled release formulations	EP 0772471	Oncology, immunology
Eli Lilly	Injectable peptides	US 6,287,591	Diabetes, hormonal therapies
Alkermes	Long-acting injectables	WO 1998/046261	CNS, metabolic disorders

4.3. Patent Term and Expiry

Filing date: Nov 3, 1995
Estimated expiration: Nov 3, 2015 (considering patent term adjustments or extensions)
Given the expiration, the patent is now in the public domain; however, its claims may still shape current patent applications and formulations.

5. Notable Challenges and Opportunities

5.1. Patent Litigation and Freedom-to-Operate (FTO)

The broad claims covering peptide matrices suggest potential infringement risks for developers of similar formulations.
FTO analyses reveal that subsequent patents covering biodegradable polymers (e.g., PLGA-based systems) may or may not encroach upon this patent's scope, depending on composition specifics.

5.2. Innovation Trends

Shifting focus toward biodegradable polymers for short- and long-term peptide release.
Increasing interest in implantable systems, microcapsules, and nanomaterials.
Regulatory push for biosimilar and generic versions leveraging expired patents.

6. Comparative Analysis: Similar Patents and Technological Differentiators

Patent	Differentiator	Patent Status	Relevance to 5,674,872
EP 0772471 A2	Use of specific copolymer blends	Granted	Similar controlled-release matrix
WO 1998/046261	Microencapsulation techniques	Granted	Similar drug delivery approach
US 6,287,591	Biodegradation profile	Granted	Different material focus but related drug delivery concept

7. Regulatory and Policy Context

The Food and Drug Administration (FDA) encourages innovation in sustained-release formulations, with clear pathways for approval.
Patent data indicates an active R&D environment, with shifting emphasis towards biodegradable and nanotechnology-based systems.

8. Concluding Remarks

U.S. Patent 5,674,872 delineates a broad yet specific approach to peptide delivery, emphasizing controlled-release matrices, especially polymer-based systems. Its claims set a precedent during the late 1990s, influencing subsequent innovations in peptide therapeutics. Given its expiration, the patent no longer poses infringement risks but continues to impact formulation strategies and patent drafting in the field.

Key Takeaways

Scope: Focuses on polymer-based controlled-release peptide formulations, with specific compositions and manufacturing methods.
Claims: Broad enough to cover multiple delivery systems but limited to polymer matrices with defined characteristics.
Patent Landscape: Shares thematic similarities with patents from BMS, Eli Lilly, and Alkermes; provides foundational principles for controlled-release peptide drugs.
Strategic Implication: Developers should assess related patents for freedom-to-operate, especially in polymeric delivery systems.
Innovation Trend: Moving towards bioerodable polymers and nanotechnologies, expanding patent landscapes.

5. FAQs

Q1: Does U.S. Patent 5,674,872 still provide enforceable patent rights?
A: No. Since it was filed in 1995 and granted in 1997, it has likely expired around 2015, assuming no patent term adjustments. Its claims now are part of the public domain.

Q2: How broad are the claims concerning peptide therapeutics?
A: The claims broadly encompass peptides and proteins incorporated into controlled-release matrices using specified polymers, providing considerable scope for various therapeutic agents.

Q3: What are common alternatives to the polymer matrices described in this patent?
A: Biodegradable polymers such as PLGA, lipid-based systems, and nanocarriers are common alternatives now, with many protected by subsequent patents.

Q4: Can new formulations be developed based on this patent?
A: Yes, especially since it's likely expired; however, care must be taken to avoid infringing any ongoing patent rights covering specific polymers or methods.

Q5: How does this patent influence current drug formulation strategies?
A: It laid foundational principles for controlled-release peptide formulations, influencing subsequent innovations and patent filings in sustained-release drug systems.

References

United States Patent and Trademark Office (USPTO). Patent No. 5,674,872. Filed Nov 3, 1995; granted Oct 7, 1997.
European Patent EP 0772471 A2.
WO 1998/046261.
US Patent 6,287,591.
FDA Guidance on Sustained-Release Formulations. (2019).

Details for Patent: 5,674,872

Summary for Patent: 5,674,872