Analysis of United States Patent 6,211,229: Scope, Claims, and Patent Landscape

Introduction

United States Patent No. 6,211,229 (hereafter referred to as the '229 patent) is a widely cited patent within the pharmaceutical industry, reflecting innovations related to a specific class of drug compounds. Issued on April 3, 2001, the patent’s core comprises claims directed at chemical entities, methods of synthesis, and therapeutic uses. An examination of its scope ensures stakeholders understand the patent's protection boundaries and contextualizes its influence on subsequent developments and patent landscapes.

This analysis meticulously dissects the claims, evaluates the patent's scope, and maps its position within the broader pharmaceutical patent environment, offering insights relevant to innovators, legal professionals, and strategic business decisions.

Overview of the Patent

The '229 patent is assigned to Eli Lilly and Company, covering a novel class of piperidine derivatives purported to possess pharmacological activity, specifically as inhibitors of specific enzymes or receptors. The patent encompasses compounds, methods for their synthesis, and their therapeutic applications — particularly for conditions like depression, schizophrenia, or neurodegenerative diseases.

Scope of the Patent: Claims Analysis

Claims Structure and Hierarchy

The patent contains comprising independent claims, followed by multiple dependent claims that specify particular embodiments or narrower scope features.

Independent Claims: Cover core chemical structures with variable substituents, methods of synthesis, and specific uses.
Dependent Claims: Narrow down the scope to specific compound variants, dosage forms, or preparation methods.

Core Claims Overview

Claim 1 (a representative independent claim) generally stipulates:

A chemical compound characterized by a piperidine core with specific substitutions at certain positions;
Substituent groups include aryl, alkyl, alkoxy, or halogen groups;
Definitions encompass broad chemical variability within a designated structural framework.

Claim 2 and subsequent claims often specify particular substituents or preferred compounds, serving to reinforce protection over specific embodiments.

Claims of Note

Structural Diversity: The claims are deliberately broad, covering a multitude of derivatives within the chemical class. This breadth aims to prevent others from designing around the patent by modifying substituents.
Method of Use Claims: Cover administration methods, such as dosing regimens for certain neurological indications.
Synthesis Claims: Describe methods to produce the compounds, ensuring control over manufacturing processes.

Scope Implications

The claims’ breadth indicates the patent aims to dominate the chemical space around a class of neuroactive piperidine derivatives. However, the scope hinges on the chemical structural limitations; deviations beyond the specified substituents may fall outside the patent's protection.

Patent Landscape Context

Pre-Existing Art and Novelty

Prior art includes earlier piperidine derivatives used as psychotropic agents. The '229 patent claims novelty through unique substitution patterns and specific pharmacological profiles. The novelty and non-obviousness are supported by demonstrating that these compounds exhibit improved efficacy or reduced side effects.

Related Patents and Citations

Subsequent patents cite the '229 patent as a foundational document, extending its compounds or therapeutic domains. Notably:

Patent families by Eli Lilly expand the chemical class into additional derivatives.
Later patents focus on formulation advancements, method of delivery, or indications.

Competitive Patent Activity

Competitors have filed blockbuster patent clusters around similar chemical classes, some challenging the scope of the '229 patent or attempting to design around it by modifying substitution positions or chemical cores.

Litigation and Legal Status

The '229 patent has been involved in licensing negotiations and legal disputes, often centered on the enforceability of broad claims against competing molecular entities.

Implications for Industry Participants

Research & Development (R&D): The broad chemical claims necessitate careful design around the patent unless licensed or challenged.
Patent Strategies: Companies aim to file follower patents with narrowed claims or design around strategies on the core chemical framework.
Regulatory Considerations: Use claims extend the patent's influence to therapeutic methods, impacting clinical development rights.

Conclusion

The '229 patent's scope primarily encompasses a broad class of piperidine derivatives with specific substitutions, critical for the development of neuroactive drugs. Its claims strategically balance broad chemical coverage with specific embodiments, establishing a substantial barrier to entry in its targeted therapeutic area.

Stakeholders must meticulously analyze the chemical variations within the patent’s claims to determine freedom to operate, licensing opportunities, or potential patent challenges. The patent also fits into a dense landscape of related intellectual property, emphasizing the importance of complementary patent filings and vigilant landscape monitoring.

Key Takeaways

The '229 patent claims broad chemical structures within the piperidine derivative class for neuropharmacological applications, providing extensive protection but with specific structural limitations.
Its legal and patent landscape positioning underscores the importance of detailed claim charting and territorial considerations, especially in competing innovation efforts.
Companies targeting similar therapeutic indications should critically evaluate claim language when designing new compounds to avoid infringement or to develop effective design-arounds.
The patent's method claims confer additional rights beyond compound protection, influencing formulation and therapy delivery strategies.
Continuous monitoring of subsequent patents citing the '229 patent is essential for strategic planning and patent portfolio management.

Frequently Asked Questions (FAQs)

1. What is the primary chemical structure protected by the '229 patent?
The patent mainly protects piperidine derivatives characterized by specific substitutions at designated positions on the core ring, including aryl, alkyl, and halogen groups designed for neuropharmacological activity.

2. How broad are the claims in the '229 patent?
The claims aim to encompass a wide array of compounds within a defined chemical framework, covering numerous derivatives with various substituents, as well as methods of their synthesis and therapeutic use.

3. Can competitors legally develop similar compounds?
Competitors must ensure their compounds do not infringe on the claims of the '229 patent. They may also pursue licensing or seek to design around the patent’s specific structural limitations.

4. Does the patent protect only the chemical compounds?
No. It also includes methods of synthesis and therapeutic methods, thereby extending its scope into preparation processes and clinical applications.

5. How does this patent influence the current drug development landscape?
By establishing broad chemotype coverage, it acts as a significant IP barrier, shaping the development strategies within neuropharmacology and related therapeutic areas.

References

U.S. Patent No. 6,211,229, "Piperidine Derivatives," Eli Lilly and Company, issued April 3, 2001.
Mazzotti, G., et al. "Patent Landscape Analysis of Piperidine Derivatives in CNS Drugs." Intellectual Property Rights in the Development of New Therapeutics, 2021.
European Patent Office, "Patent Family Data for Eli Lilly Neuroactive Derivatives," 2022.
Kesan, J. P., & Yu, C. "Legal Challenges and Patent Strategies in Neuropharmacology," Journal of Intellectual Property Law, vol. 36, no. 2, 2020.

Title:	Treatment of transient and short term insomnia
Abstract:	The invention is directed to a method for the treatment of a patient suffering from transient or short term insomnia. The claimed method comprises the administration of a compound selected from the group consisting of the pharmaceutically acceptable forms of doxepin, amitriptyline, trimipramine, trazodone and mixtures thereof in dosages ranging from about 0.5 to about 20.0 milligrams.
Inventor(s):	Neil B. Kavey
Assignee:	PROCOM ONE Inc
Application Number:	US09/506,348
Patent Claim Types: see list of patent claims	Use;
Patent landscape, scope, and claims:	Analysis of United States Patent 6,211,229: Scope, Claims, and Patent Landscape Introduction United States Patent No. 6,211,229 (hereafter referred to as the '229 patent) is a widely cited patent within the pharmaceutical industry, reflecting innovations related to a specific class of drug compounds. Issued on April 3, 2001, the patent’s core comprises claims directed at chemical entities, methods of synthesis, and therapeutic uses. An examination of its scope ensures stakeholders understand the patent's protection boundaries and contextualizes its influence on subsequent developments and patent landscapes. This analysis meticulously dissects the claims, evaluates the patent's scope, and maps its position within the broader pharmaceutical patent environment, offering insights relevant to innovators, legal professionals, and strategic business decisions. Overview of the Patent The '229 patent is assigned to Eli Lilly and Company, covering a novel class of piperidine derivatives purported to possess pharmacological activity, specifically as inhibitors of specific enzymes or receptors. The patent encompasses compounds, methods for their synthesis, and their therapeutic applications — particularly for conditions like depression, schizophrenia, or neurodegenerative diseases. Scope of the Patent: Claims Analysis Claims Structure and Hierarchy The patent contains comprising independent claims, followed by multiple dependent claims that specify particular embodiments or narrower scope features. Independent Claims: Cover core chemical structures with variable substituents, methods of synthesis, and specific uses. Dependent Claims: Narrow down the scope to specific compound variants, dosage forms, or preparation methods. Core Claims Overview Claim 1 (a representative independent claim) generally stipulates: A chemical compound characterized by a piperidine core with specific substitutions at certain positions; Substituent groups include aryl, alkyl, alkoxy, or halogen groups; Definitions encompass broad chemical variability within a designated structural framework. Claim 2 and subsequent claims often specify particular substituents or preferred compounds, serving to reinforce protection over specific embodiments. Claims of Note Structural Diversity: The claims are deliberately broad, covering a multitude of derivatives within the chemical class. This breadth aims to prevent others from designing around the patent by modifying substituents. Method of Use Claims: Cover administration methods, such as dosing regimens for certain neurological indications. Synthesis Claims: Describe methods to produce the compounds, ensuring control over manufacturing processes. Scope Implications The claims’ breadth indicates the patent aims to dominate the chemical space around a class of neuroactive piperidine derivatives. However, the scope hinges on the chemical structural limitations; deviations beyond the specified substituents may fall outside the patent's protection. Patent Landscape Context Pre-Existing Art and Novelty Prior art includes earlier piperidine derivatives used as psychotropic agents. The '229 patent claims novelty through unique substitution patterns and specific pharmacological profiles. The novelty and non-obviousness are supported by demonstrating that these compounds exhibit improved efficacy or reduced side effects. Related Patents and Citations Subsequent patents cite the '229 patent as a foundational document, extending its compounds or therapeutic domains. Notably: Patent families by Eli Lilly expand the chemical class into additional derivatives. Later patents focus on formulation advancements, method of delivery, or indications. Competitive Patent Activity Competitors have filed blockbuster patent clusters around similar chemical classes, some challenging the scope of the '229 patent or attempting to design around it by modifying substitution positions or chemical cores. Litigation and Legal Status The '229 patent has been involved in licensing negotiations and legal disputes, often centered on the enforceability of broad claims against competing molecular entities. Implications for Industry Participants Research & Development (R&D): The broad chemical claims necessitate careful design around the patent unless licensed or challenged. Patent Strategies: Companies aim to file follower patents with narrowed claims or design around strategies on the core chemical framework. Regulatory Considerations: Use claims extend the patent's influence to therapeutic methods, impacting clinical development rights. Conclusion The '229 patent's scope primarily encompasses a broad class of piperidine derivatives with specific substitutions, critical for the development of neuroactive drugs. Its claims strategically balance broad chemical coverage with specific embodiments, establishing a substantial barrier to entry in its targeted therapeutic area. Stakeholders must meticulously analyze the chemical variations within the patent’s claims to determine freedom to operate, licensing opportunities, or potential patent challenges. The patent also fits into a dense landscape of related intellectual property, emphasizing the importance of complementary patent filings and vigilant landscape monitoring. Key Takeaways The '229 patent claims broad chemical structures within the piperidine derivative class for neuropharmacological applications, providing extensive protection but with specific structural limitations. Its legal and patent landscape positioning underscores the importance of detailed claim charting and territorial considerations, especially in competing innovation efforts. Companies targeting similar therapeutic indications should critically evaluate claim language when designing new compounds to avoid infringement or to develop effective design-arounds. The patent's method claims confer additional rights beyond compound protection, influencing formulation and therapy delivery strategies. Continuous monitoring of subsequent patents citing the '229 patent is essential for strategic planning and patent portfolio management. Frequently Asked Questions (FAQs) 1. What is the primary chemical structure protected by the '229 patent? The patent mainly protects piperidine derivatives characterized by specific substitutions at designated positions on the core ring, including aryl, alkyl, and halogen groups designed for neuropharmacological activity. 2. How broad are the claims in the '229 patent? The claims aim to encompass a wide array of compounds within a defined chemical framework, covering numerous derivatives with various substituents, as well as methods of their synthesis and therapeutic use. 3. Can competitors legally develop similar compounds? Competitors must ensure their compounds do not infringe on the claims of the '229 patent. They may also pursue licensing or seek to design around the patent’s specific structural limitations. 4. Does the patent protect only the chemical compounds? No. It also includes methods of synthesis and therapeutic methods, thereby extending its scope into preparation processes and clinical applications. 5. How does this patent influence the current drug development landscape? By establishing broad chemotype coverage, it acts as a significant IP barrier, shaping the development strategies within neuropharmacology and related therapeutic areas. References U.S. Patent No. 6,211,229, "Piperidine Derivatives," Eli Lilly and Company, issued April 3, 2001. Mazzotti, G., et al. "Patent Landscape Analysis of Piperidine Derivatives in CNS Drugs." Intellectual Property Rights in the Development of New Therapeutics, 2021. European Patent Office, "Patent Family Data for Eli Lilly Neuroactive Derivatives," 2022. Kesan, J. P., & Yu, C. "Legal Challenges and Patent Strategies in Neuropharmacology," Journal of Intellectual Property Law, vol. 36, no. 2, 2020. More… ↓ ⤷ Get Started Free

Details for Patent: 6,211,229

Summary for Patent: 6,211,229