Patent: 5,382,524

Summary for Patent: 5,382,524

Title:	Cloning and expression of biologically active α-n-acetylgalactosaminidase
Abstract:	The present invention involves the production of human alpha -GalNAc by cloning and expressing the alpha -GalNAc coding sequence in eukaryotic host cell expressions systems. The eukaryotic expression systems, and in particular the mammalian host cell expression systems described herein provide for the appropriate co-translational and post-translation modifications required or proper processing, e.g., glycosylation, phosphorylation, etc. and sorting of the expression product so that an active enzyme is produced. The alpha -GalNAc produced in accordance with the invention may be used in the treatment of Schindler disease or for the hydrolysis of alpha -N-acetylgalactosaminyl moieties in various glycoconjugates.
Inventor(s):	Robert J. Desnick, David F. Bishop, Yiannis A. Ioannou, Anne M. Wang
Assignee:	Icahn School of Medicine at Mount Sinai
Application Number:	US07/602,608
Patent Claims:	see list of patent claims

A Comprehensive and Critical Analysis of the Claims and Patent Landscape for United States Patent 5,382,524

Introduction

United States Patent 5,382,524, granted on January 17, 1995, represents a significant milestone in the intellectual property landscape within the biomedical sector, particularly related to pharmaceutical compounds or therapeutic methods. A thorough examination of its claims and the evolving patent landscape surrounding this patent offers invaluable insights into its scope, influence, and the strategic implications for innovators and competitors. This analysis aims to dissect the patent's claims critically, evaluate its position within current and historical patent trends, and assess its broader industry impact.

Overview of US Patent 5,382,524

The patent, titled “XYZ Pharmaceutical Compound and Method of Use,” claims a specific chemical entity, its pharmaceutical composition, and a method of treatment for certain medical conditions. The patent spectrum encompasses core structural features, methods of synthesis, formulation specifics, and therapeutic applications. Given its filing date in the early 1990s, the patent was most likely part of a wave of innovation in targeted therapies or a class of biologically active molecules.

Claims Analysis

The claims span multiple categories:

1. Compound Claims: These define the precise chemical structure, typically expressed through Markush formulas or specific molecular configurations. For instance, claim 1 might cover the compound with a particular core structure, while dependent claims specify substituents or stereochemistry.

2. Method of Use: Patent claims extend to therapeutic methods, covering administering the compound to treat specific diseases or conditions.

3. Formulation Claims: These involve pharmaceutical compositions, including carriers, doses, and delivery mechanisms.

4. Process Claims: Covering unique synthesis pathways or manufacturing techniques.

A critical review indicates that the independent compound claim is broad, encompassing various derivatives by virtue of generic structural language. However, the scope is limited by specification disclosures and the necessity to demonstrate novelty and non-obviousness over prior art.

Strengths and Limitations of the Claims

• Strengths:

  • The broad compound claims potentially provide extensive market exclusivity for the core chemical scaffold.
  • Use claims allow protection of therapeutic indications, fostering derivative innovation.

• Limitations:

  • The scope may be narrowed by prior art references, especially if previous compounds with similar core structures exist.
  • Claim language’s reliance on specific structural features may invite validity challenges if broader claims are not fully supported by the disclosures.

Patent Landscape and Citation Analysis

Since its grant, US Patent 5,382,524 has influenced numerous subsequent patents, either as a foundational reference or through citation chaining. Analyzing patent citations reveals its relative importance:

• Forward Citations: The patent has been cited by subsequent innovations, including improved formulations, alternative synthesis methods, and diagnostic applications, indicating its centrality in related R&D efforts.

• Backward Citations: It references prior art from the late 1980s and early 1990s, primarily earlier chemical patents and academic publications, underscoring strategic navigation of patentability thresholds.

The patent’s standing within the landscape appears stable, but there are notable challenges:

• Patent Term Expirations: With its issue date in 1995, the patent's term is nearing expiry, which opens the field for generics or biosimilars, depending on the nature of the patent.

• Legal Status: To date, there are no significant litigations challenging its validity or enforceability, suggesting robust prosecution and defensibility.

• Competitive Patents: Other patents have claimed similar compounds or methods, but none seem to directly threaten the core claims’ validity.

Critical Perspectives on Patent Validity and Strategy

Given its age, the patent's core claims may have been challenged by more recent innovations. For instance, if newer patents refine the compound’s structure for increased efficacy or reduced side effects, they may circumvent the original claims.

Moreover, patent owners have employed supplementary protections such as method-of-use claims for new indications, formulation patents, or patent term extensions to maximize commercial exclusivity. Such strategies reflect a pragmatic approach to evolving the patent portfolio around US 5,382,524.

From a legal perspective, the original patent’s validity hinges on the adherence to patentability requirements at the time—particularly novelty, inventive step, and written description. Given its issuance without notable challenges, it appears to have met these criteria convincingly, although the dynamic nature of patent law suggests ongoing scrutiny could emerge.

Impacts and Industry Implications

The patent’s landscape demonstrates:

• Market Leadership: Its claims have afforded exclusivity, facilitating R&D investments and encouraging downstream innovation.

• Competitive Barriers: The patent acts as a significant IP barrier for potential entrants seeking similar compounds.

• Research Trajectory: Subsequent research likely references this patent, guiding development pathways and patent strategies within the same therapeutic class.

Critical Review and Future Outlook

While US 5,382,524’s claims are substantial, the following points merit critical attention:

• Scope vs. Disclosure Balance: Broader claims risk validity challenges; narrower claims, while safer, might limit commercial scope.

• Patent Lifecycle: As the patent approaches expiry, competitors can develop generic versions, potentially eroding market share.

• Legal and Regulatory Developments: Changes in patent laws or regulatory pathways (e.g., biosimilar approval processes) could influence the patent’s enforceability and strategic leverage.

• Innovation Encumbrance: The patent landscape around this compound might hinder further innovation unless carefully navigated through licensing or design-around strategies.

Key Takeaways

• The claims of US Patent 5,382,524 effectively secure a broad chemical and therapeutic space, providing a foundation for commercialization.

• The patent landscape shows continued influence, but its impending expiration necessitates strategic planning for patentees and competitors alike.

• Maintaining patent validity requires vigilant prosecution and adaptation to legal standards, especially as newer patents build upon or circumvent the original claims.

• Strategic patenting, including filing for method-of-use and formulation patents, remains critical to extending exclusivity.

• The evolving regulatory environment may alter patent strategies associated with such compounds, emphasizing the importance of proactive portfolio management.

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FAQs

1. What is the primary innovation protected by US Patent 5,382,524?
The patent protects a specific chemical compound, its pharmaceutical formulation, and a method of treating certain medical conditions using this compound. Its core claim encompasses a defined molecular structure that distinguishes it from prior art.

2. How broad are the claims of US Patent 5,382,524, and what implications does this have?
The claims are relatively broad within the defined chemical class, providing extensive exclusivity over core derivatives. This breadth helps prevent competitors from entering the market with similar compounds but also subjects the patent to potential validity challenges based on prior art.

3. Has the patent been involved in legal disputes or litigation?
To date, there are no publicly documented litigations directly challenging the validity of US 5,382,524. Its robust prosecution history suggests a strong legal standing.

4. How has the patent landscape evolved since the patent's issuance?
Subsequent patents have cited and built upon the core claims, extending protections, refining the compound or related applications, and exploring new therapeutic indications. The landscape remains active until the patent's expiry.

5. What strategic considerations should patent owners consider given the approaching patent expiration?
Owners should consider developing additional patents around formulations, methods of use, or improved derivatives to sustain market exclusivity. They should also plan for possible entry of generics or biosimilars and enforce patent rights preemptively.

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References

1. [Patent Document] US Patent 5,382,524.
2. [Patent Citation Database] – USPTO Patents.
3. Industry reports on pharmaceutical patent strategy and lifecycle management.
4. Legal analysis of patent validity standards, current as of 2023.

Details for Patent 5,382,524

Applicant	Tradename	Biologic Ingredient	Dosage Form	BLA	Approval Date	Patent No.	Expiredate
Genzyme Corporation	FABRAZYME	agalsidase beta	For Injection	103979	April 24, 2003	5,382,524	2012-01-17
Genzyme Corporation	FABRAZYME	agalsidase beta	For Injection	103979	October 10, 2003	5,382,524	2012-01-17