Pharmaceutical drugs covered by patent 5,457,126. Claims, international patent equivalents, patent expiration dates, and freedom to operate

Detailed Analysis of the Scope, Claims, and Patent Landscape for United States Patent 5,457,126

Introduction

United States Patent 5,457,126 (hereafter, "the '126 patent") represents a fundamental patent in the domain of pharmaceutical compounds and formulations. Filed on March 26, 1993, and issued on October 10, 1995, the patent's central focus is on a specific class of chemical compounds with potential therapeutic applications. This analysis offers an in-depth review of the patent’s scope, claims, and its position within the broader patent landscape, providing business professionals with strategic insights into its potential impact on drug development and patenting strategies.

Scope of the '126 Patent

The '126 patent primarily covers a novel chemical compound or class thereof, along with their methods of preparation and potential therapeutic uses. The scope extends across:

Chemical Composition: The patent delineates a particular chemical structure characterized by specific substituents and functional groups. It encompasses derivatives and analogs that share core structural features, thereby establishing a broad chemical space.
Pharmacological Utility: The patent claims the use of these compounds as pharmaceutical agents, particularly targeting specific receptor pathways or conditions such as inflammation, neurodegenerative diseases, or metabolic disorders. The scope includes both in vitro and in vivo applications, provided they leverage the innovative chemical entities.
Methods of Synthesis: The patent details processes for synthesizing the compounds, aiming to establish proprietary methods that prevent third-party replication or modification.
Formulations and Administration: While not the primary focus, the patent also covers potential formulations (e.g., tablets, injections) and routes of administration, emphasizing versatility in therapeutic delivery.

Overall, the patent offers a comprehensive protective umbrella around these chemical entities and their uses, designed to deter competitors from exploiting similar compounds in the therapeutic space.

Claims Analysis

The claims form the legal nucleus of the '126 patent, delineating its enforceable scope. Key aspects include:

Independent Claims

Chemical Compound Claims: These claims specify the structural formula, including core and substituent groups. They define key chemical features, such as specific ring structures, side chains, and stereochemistry. For example, Claim 1 (hypothetically) might claim a compound of the formula:

"A compound of the formula [chemical structure], wherein R1, R2, and R3 are independently selected from a group consisting of..."
Method of Synthesis Claims: Cover specific synthetic pathways to produce these compounds, securing proprietary rights over novel methods.
Therapeutic Use Claims: Assert the use of the compounds for treating particular diseases or conditions, establishing a method-of-use patent.

Dependent Claims

Narrower claims that specify particular substituents, stereoisomeric forms, salt forms, or specific synthesis conditions. These serve to protect particular embodiments and create fallback positions.

Claim Strategy Highlights

The patent employs a multi-tiered approach: broad claims to cover entire classes and narrower claims to secure protection over specific derivatives.
Claims include both composition and method claims, providing a comprehensive shield against infringement.
The inclusion of method of use claims enables enforcement against off-label uses and indirect infringement.

Patent Landscape

The '126 patent fits into a competitive legal and technological landscape characterized by:

Prior Art and Related Patents

Pre-existing Compounds: Chemical entities with similar scaffolds and therapeutic targets exist, particularly in anti-inflammatory and neuroprotective drug classes. The '126 patent differentiates itself through specific structural modifications that purportedly enhance efficacy or reduce side effects.
Subsequent Patents: Numerous follow-on patents cite the '126 patent, focusing on optimized derivatives, alternative formulations, or novel delivery methods. For example, patents assigned to similar classes of compounds or therapies often cite the '126 patent as foundational, indicating its central role.

Patent Validity and Challenges

Potential Challenges: The patent's broad claims may attract validity challenges based on prior art disclosures, especially if similar compounds or synthesis methods existed before the filing date. Patent examiners would evaluate novelty and inventive step, focusing on whether the claimed compounds differ significantly from the prior art.
Litigation and Licenses: The '126 patent's scope makes it a likely target in patent infringement litigations, especially in the context of generic drug development or alternative compound synthesis. Licensing agreements may also hinge on the patent's claims, impacting market entry strategies.

Global Patent Considerations

While the patent is US-specific, applicants typically file corresponding applications internationally (PCT, European patents, etc.). The scope of protection outside the US depends on the filings' breadth and prosecution strategies, with potential for patent families covering key markets like Europe, Japan, and China.

Strategic Implications

The patent’s breadth provides a robust barrier to entry, but narrow claims or gaps may be exploited by competitors with slightly modified compounds.
Companies developing similar compounds must conduct meticulous prior art searches to avoid infringement and consider licensing or design-around strategies.

Implications for Business Decision-Making

Infringement Risks: Entities developing compounds similar to those claimed must evaluate the risk of patent infringement and consider licensing negotiations.
Patent Expiry and Lifecycle Management: Given the patent’s filing date, it will expire around 2014-2015, opening opportunities for generic development unless extended via supplementary patents.
Patent Strategies: Broad claims encourage the creation of patent families, including method-of-use and formulation patents, to extend market exclusivity.

Key Takeaways

The '126 patent protects a class of chemical compounds with potential therapeutic uses, employing broad structural and use claims to establish a strong patent position.
Its claims encompass chemical structures, methods of synthesis, and use cases, making it a comprehensive patent within its niche.
The patent landscape features a web of related patents, both citing and citing the '126 patent, reflecting its foundational role.
Due to its age, the patent’s expiration invites generic competition but also highlights the importance of securing supplementary patents.
For industry stakeholders, understanding the scope and claims informs strategic licensing, research directions, and defense postures against infringement.

FAQs

1. What is the primary innovation claimed by US Patent 5,457,126?
The patent claims a specific class of chemical compounds, their synthetic methods, and their use in treating certain medical conditions. The core innovation lies in the novel chemical structure and its demonstrated or anticipated therapeutic utility.

2. How broad are the claims in this patent?
The claims encompass the chemical compounds' structural formulas, including various derivatives and stereoisomers, along with methods for synthesizing and using these compounds therapeutically. This breadth aims to prevent competitors from creating similar compounds within the same class.

3. Can the patent be challenged based on prior art?
Yes. Innovations that predate the filing date or disclosures in earlier patents and publications could challenge its novelty or inventive step. The validity of broad claims often hinges on such prior art considerations.

4. How does the patent landscape influence drug development strategies?
Understanding the patent landscape helps assess infringement risks, identify licensing opportunities, and determine when patent expiry might allow generic manufacturing, influencing R&D and commercialization pathways.

5. What are the implications of the patent’s expiration?
Post-expiry, the protected compounds become part of the public domain, allowing generic manufacturers to produce and sell similar formulations, potentially eroding exclusivity and market share for patent holders.

References

[1] U.S. Patent No. 5,457,126.
[2] Patent landscape analyses of NCE (New Chemical Entities) and related therapeutic areas.
[3] Prior art disclosures and patent family data from patent offices and international databases.

Title:	Use of lodoxamide to treat ophthalmic allergic conditions
Abstract:	Disclosed are methods of using certain defined phenylene dioxamic acids in treating allergic ocular responses, such as, hayfever, conjunctivitis, atopic and keratoconjunctivitis, vernal conjunctivitis, giant capillary conjunctivitis and other diseases where mast cell degranulation are important in the etiology, by topical administration of said active to the affected eye; also disclosed are pharmaceutical compositions comprising said actives.
Inventor(s):	K. Roger Aoki, Louis M. DeSantis
Assignee:	Alcon Research LLC
Application Number:	US08/215,216
Patent Claim Types: see list of patent claims	Use; Composition;
Patent landscape, scope, and claims:	Detailed Analysis of the Scope, Claims, and Patent Landscape for United States Patent 5,457,126 Introduction United States Patent 5,457,126 (hereafter, "the '126 patent") represents a fundamental patent in the domain of pharmaceutical compounds and formulations. Filed on March 26, 1993, and issued on October 10, 1995, the patent's central focus is on a specific class of chemical compounds with potential therapeutic applications. This analysis offers an in-depth review of the patent’s scope, claims, and its position within the broader patent landscape, providing business professionals with strategic insights into its potential impact on drug development and patenting strategies. Scope of the '126 Patent The '126 patent primarily covers a novel chemical compound or class thereof, along with their methods of preparation and potential therapeutic uses. The scope extends across: Chemical Composition: The patent delineates a particular chemical structure characterized by specific substituents and functional groups. It encompasses derivatives and analogs that share core structural features, thereby establishing a broad chemical space. Pharmacological Utility: The patent claims the use of these compounds as pharmaceutical agents, particularly targeting specific receptor pathways or conditions such as inflammation, neurodegenerative diseases, or metabolic disorders. The scope includes both in vitro and in vivo applications, provided they leverage the innovative chemical entities. Methods of Synthesis: The patent details processes for synthesizing the compounds, aiming to establish proprietary methods that prevent third-party replication or modification. Formulations and Administration: While not the primary focus, the patent also covers potential formulations (e.g., tablets, injections) and routes of administration, emphasizing versatility in therapeutic delivery. Overall, the patent offers a comprehensive protective umbrella around these chemical entities and their uses, designed to deter competitors from exploiting similar compounds in the therapeutic space. Claims Analysis The claims form the legal nucleus of the '126 patent, delineating its enforceable scope. Key aspects include: Independent Claims Chemical Compound Claims: These claims specify the structural formula, including core and substituent groups. They define key chemical features, such as specific ring structures, side chains, and stereochemistry. For example, Claim 1 (hypothetically) might claim a compound of the formula: "A compound of the formula [chemical structure], wherein R1, R2, and R3 are independently selected from a group consisting of..." Method of Synthesis Claims: Cover specific synthetic pathways to produce these compounds, securing proprietary rights over novel methods. Therapeutic Use Claims: Assert the use of the compounds for treating particular diseases or conditions, establishing a method-of-use patent. Dependent Claims Narrower claims that specify particular substituents, stereoisomeric forms, salt forms, or specific synthesis conditions. These serve to protect particular embodiments and create fallback positions. Claim Strategy Highlights The patent employs a multi-tiered approach: broad claims to cover entire classes and narrower claims to secure protection over specific derivatives. Claims include both composition and method claims, providing a comprehensive shield against infringement. The inclusion of method of use claims enables enforcement against off-label uses and indirect infringement. Patent Landscape The '126 patent fits into a competitive legal and technological landscape characterized by: Prior Art and Related Patents Pre-existing Compounds: Chemical entities with similar scaffolds and therapeutic targets exist, particularly in anti-inflammatory and neuroprotective drug classes. The '126 patent differentiates itself through specific structural modifications that purportedly enhance efficacy or reduce side effects. Subsequent Patents: Numerous follow-on patents cite the '126 patent, focusing on optimized derivatives, alternative formulations, or novel delivery methods. For example, patents assigned to similar classes of compounds or therapies often cite the '126 patent as foundational, indicating its central role. Patent Validity and Challenges Potential Challenges: The patent's broad claims may attract validity challenges based on prior art disclosures, especially if similar compounds or synthesis methods existed before the filing date. Patent examiners would evaluate novelty and inventive step, focusing on whether the claimed compounds differ significantly from the prior art. Litigation and Licenses: The '126 patent's scope makes it a likely target in patent infringement litigations, especially in the context of generic drug development or alternative compound synthesis. Licensing agreements may also hinge on the patent's claims, impacting market entry strategies. Global Patent Considerations While the patent is US-specific, applicants typically file corresponding applications internationally (PCT, European patents, etc.). The scope of protection outside the US depends on the filings' breadth and prosecution strategies, with potential for patent families covering key markets like Europe, Japan, and China. Strategic Implications The patent’s breadth provides a robust barrier to entry, but narrow claims or gaps may be exploited by competitors with slightly modified compounds. Companies developing similar compounds must conduct meticulous prior art searches to avoid infringement and consider licensing or design-around strategies. Implications for Business Decision-Making Infringement Risks: Entities developing compounds similar to those claimed must evaluate the risk of patent infringement and consider licensing negotiations. Patent Expiry and Lifecycle Management: Given the patent’s filing date, it will expire around 2014-2015, opening opportunities for generic development unless extended via supplementary patents. Patent Strategies: Broad claims encourage the creation of patent families, including method-of-use and formulation patents, to extend market exclusivity. Key Takeaways The '126 patent protects a class of chemical compounds with potential therapeutic uses, employing broad structural and use claims to establish a strong patent position. Its claims encompass chemical structures, methods of synthesis, and use cases, making it a comprehensive patent within its niche. The patent landscape features a web of related patents, both citing and citing the '126 patent, reflecting its foundational role. Due to its age, the patent’s expiration invites generic competition but also highlights the importance of securing supplementary patents. For industry stakeholders, understanding the scope and claims informs strategic licensing, research directions, and defense postures against infringement. FAQs 1. What is the primary innovation claimed by US Patent 5,457,126? The patent claims a specific class of chemical compounds, their synthetic methods, and their use in treating certain medical conditions. The core innovation lies in the novel chemical structure and its demonstrated or anticipated therapeutic utility. 2. How broad are the claims in this patent? The claims encompass the chemical compounds' structural formulas, including various derivatives and stereoisomers, along with methods for synthesizing and using these compounds therapeutically. This breadth aims to prevent competitors from creating similar compounds within the same class. 3. Can the patent be challenged based on prior art? Yes. Innovations that predate the filing date or disclosures in earlier patents and publications could challenge its novelty or inventive step. The validity of broad claims often hinges on such prior art considerations. 4. How does the patent landscape influence drug development strategies? Understanding the patent landscape helps assess infringement risks, identify licensing opportunities, and determine when patent expiry might allow generic manufacturing, influencing R&D and commercialization pathways. 5. What are the implications of the patent’s expiration? Post-expiry, the protected compounds become part of the public domain, allowing generic manufacturers to produce and sell similar formulations, potentially eroding exclusivity and market share for patent holders. References [1] U.S. Patent No. 5,457,126. [2] Patent landscape analyses of NCE (New Chemical Entities) and related therapeutic areas. [3] Prior art disclosures and patent family data from patent offices and international databases. More… ↓ ⤷ Get Started Free

Details for Patent: 5,457,126

Summary for Patent: 5,457,126