Patent: 6,992,102

Summary for Patent: 6,992,102

Title:	Bicyclic modulators of androgen receptor function
Abstract:	The invention provides compounds of the formula I ##STR00001## wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia, and also provided are pharmaceutical compositions containing such compounds.
Inventor(s):	Hamann; Lawrence (Cherry Hill, NJ), Augeri; David (Princeton, NJ), Sun; Chongqing (East Windsor, NJ), Robl; Jeffrey A. (Newtown, PA), Salvati; Mark E. (Lawrenceville, NJ), Wang; Tammy (Lawrenceville, NJ)
Assignee:	Bristol-Myers Squibb Company (Princeton, NJ)
Application Number:	10/685,020
Patent Claims:	see list of patent claims

Comprehensive and Critical Analysis of the Claims and Patent Landscape for United States Patent 6,992,102

Introduction

United States Patent 6,992,102, granted in January 2006, pertains to innovations in the field of pharmaceutical delivery systems, notably those involving controlled-release formulations. As the pharmaceutical industry increasingly emphasizes intellectual property (IP) protections to sustain competitive advantage and ensure R&D investments, understanding the scope, strength, and implications of such patent claims is crucial. This analysis examines the patent's claims, their scope, the innovation landscape, potential challenges, and strategic considerations for stakeholders.

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Overview of Patent 6,992,102

Patent Summary

Patent 6,992,102 is centered on a drug delivery system that enables controlled, sustained release of pharmaceutical compounds. The patent claims encompass specific formulations including polymer matrices, coatings, and manufacturing methods designed to regulate drug release profiles and enhance therapeutic efficacy.

Filed and Grant Timeline

Filed in 2002, the patent's prosecution spanned approximately four years before grant, reflecting strategic claim amendments and examiner considerations typical for pharmaceutical patents. The patent's lifespan extends until 2022, with potential for maintenance fee adjustments.

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Analysis of Patent Claims

Claim Structure and Core Elements

The patent's claims can be broadly categorized into independent and dependent claims:

• Independent claims articulate broad formulations involving a polymer matrix encapsulating an active pharmaceutical ingredient (API) with specific release characteristics.
• Dependent claims narrow scope, including particular polymer types, component concentrations, or manufacturing methods.

Scope and Breadth of Claims

The independent claims aim to monopolize a class of controlled-release formulations, with language such as “a pharmaceutical composition comprising a polymer matrix and an active agent, wherein the composition exhibits a controlled release profile…” This language aims to balance broad utility with specificity.

However, the scope faces potential limitations due to prior art references, including earlier controlled-release patents and formulations, such as U.S. Patent 5,679,334 (1997) and EP 0 735 518 B1, which also describe polymeric drug delivery systems.

Key Elements of Claims

• Polymer Composition: The inclusion of specific biocompatible polymers, such as hydroxypropyl methylcellulose or ethylcellulose.
• Release Profile: A focus on a sustained release over a defined period (e.g., 12-24 hours).
• Manufacturing Methodology: Some claims encompass the process of preparing the controlled-release formulation, e.g., mixing, extrusion, or coating techniques.

Critical Assessment

While the claims are relatively comprehensive, they seem to hinge on particular polymer combinations and release durations. Given the extensive prior art, the patent's enforceability may depend on the novelty and non-obviousness of these specific combination claims, especially regarding manufacturing techniques or unique polymer blends.

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Patent Landscape and Prior Art Context

Predecessor Certifications and Related Patents

The patent cites multiple prior art references, indicating a crowded landscape:

• Controlled-Release Formulations: Numerous patents prior to 2002 describe polymer matrices for drug release, including controlled-release formulations for diverse APIs.
• Polymer Innovations: Prior art encompasses both natural and synthetic polymers with established use in drug delivery.

Overlap and Differentiation

The claims attempt to distinguish themselves through specific polymer ratios and release profiles. However, overlapping claims with prior art threaten a narrow scope unless the claimed formulations demonstrate unexpected advantages.

Legal and Patentability Considerations

Given the complexity, patentability challenges from competitors are plausible, particularly citing obviousness due to known polymer formulations. Patent examiners evaluating boundary claims often compare them against the prior art cited during prosecution, making precise claim drafting imperative.

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Strengths and Weaknesses of the Patent

Strengths

• The patent covers a recognized problem in pharmaceutical delivery—controlled, sustained release—addressing both performance and manufacturing methods.
• Claim language includes both composition and process claims, diversifying enforceability options.
• The patent is supported by experimental data demonstrating specific release profiles.

Weaknesses

• Broad independent claims risk invalidation if deemed anticipated or obvious based on prior art.
• Narrow dependent claims limit scope and may be circumvented through minor formulation modifications.
• The patent's jurisdictional limitations restrict enforcement outside the U.S. without corresponding filings.

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Strategic Considerations for Stakeholders

For Patent Holders

• Enforcement: Vigilant monitoring of competitors’ formulations for potential infringement, especially those closely mirroring claim language.
• Defense: Prepare for validity challenges by compiling evidence of non-obviousness and demonstrating unexpected benefits.
• Expansion: Consider filing follow-up patents that claim improved formulations or manufacturing techniques to broaden coverage.

For Competitors

• Design-Arounds: Explore alternative polymers, release mechanisms, or manufacturing methods not encompassed by the patent claims.
• Innovations: Invest in developing differentiated controlled-release technologies that address limitations or overcome potential infringement risks.
• Geographic Strategy: Pursue patent protections in key markets beyond the U.S. to safeguard innovations globally.

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Regulatory and Commercial Implications

Patents such as 6,992,102 significantly influence market exclusivity for generic entrants and biosimilar developers, impacting drug pricing and availability. Securing patents with defensible claims enhances lifecycle management strategies for pharmaceutical companies.

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Conclusion

United States Patent 6,992,102 exemplifies the strategic use of patent claims to protect controlled-release pharmaceutical formulations. While claims are thoughtfully crafted, they are challenged by a complex patent landscape with extensive prior art. The strength of this patent depends on ongoing enforcement and potential for patent lifecycle management through continuations or improvements. Major players in drug delivery must meticulously analyze such patents to inform R&D, IP strategy, and competitive positioning.

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Key Takeaways

• The patent claims cover a specific subset of controlled-release formulations, balancing breadth and specificity, but remain vulnerable to prior art challenges.
• A crowded patent landscape necessitates innovative claim drafting and continuous innovation to preserve market exclusivity.
• Stakeholders should consider strategic patent filings, clear differentiation, and geographic coverage to maximize IP value.
• Enforcement and legal defensibility hinge on demonstrating novelty and non-obviousness amid extensive prior art.
• Patent protections like US 6,992,102 significantly influence commercialization strategies, generic entry, and drug affordability.

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FAQs

1. What are the main elements protected by US Patent 6,992,102?
The patent primarily protects controlled-release pharmaceutical formulations comprising specific polymer matrices that regulate drug release profiles, along with associated manufacturing processes.

2. How does this patent compare to prior art in controlled-release drug delivery?
While the patent advances the field by specifying particular polymers and release durations, it faces challenges of novelty due to prior formulations involving similar polymers and release mechanisms.

3. Can competitors develop similar controlled-release drugs without infringing this patent?
Yes, by exploring alternative polymers, release profiles, or manufacturing methods not covered or claimed by this patent, competitors can design around its scope.

4. How critical are such patents in pharmaceutical market exclusivity?
They are vital. Patents like US 6,992,102 extend market exclusivity, protect R&D investments, and influence pricing, especially for complex formulations.

5. What strategic actions should patent holders consider for maintaining patent strength?
Continuously monitor prior art, pursue claims on improved formulations or methods, and seek patent term extensions or additional jurisdictions to bolster protection.

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References

[1] U.S. Patent 6,992,102. Controlled-release formulations.Issued Jan 10, 2006.

Details for Patent 6,992,102

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Takeda Pharmaceuticals U.s.a., Inc.	NATPARA	parathyroid hormone	For Injection	125511	January 23, 2015		2023-10-14