Detailed Analysis of the Scope and Claims of United States Patent 8,653,260
Introduction
United States Patent 8,653,260, titled "Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists," was issued on February 18, 2014, to Merck Sharp & Dohme Corp. This patent is crucial in the field of pharmaceuticals, particularly for the treatment of diseases mediated by the activation of β3-adrenoceptors.
Background of the Invention
The patent addresses the function of the lower urinary tract, which involves the storage and periodic release of urine. This process is regulated by a complex interplay of neural pathways and the autonomic nervous system, affecting the contractile state of bladder and urethral muscles. β3-adrenergic receptors play a significant role in this regulation, making them a target for therapeutic interventions, especially for conditions like overactive bladder[1].
Scope of the Patent
Compounds and Formulations
The patent describes a series of hydroxymethyl pyrrolidine compounds, specifically those of Formula (I), which are designed to act as agonists for β3-adrenergic receptors. These compounds are part of a broader class of pharmaceutical compositions intended for the treatment or prevention of diseases mediated by the activation of these receptors[4].
Therapeutic Applications
The primary therapeutic application of these compounds is in the treatment of overactive bladder, characterized by symptoms such as urge urinary incontinence, urgency, and frequency. The activation of β3-adrenergic receptors helps in relaxing the detrusor muscle, thereby reducing the frequency and urgency of urination[1][2].
Claims of the Patent
Independent Claims
The patent includes several independent claims that define the scope of the invention. These claims cover:
- The specific chemical structures of the hydroxymethyl pyrrolidine compounds.
- Pharmaceutical compositions containing these compounds.
- Methods of using these compounds for the treatment or prevention of diseases mediated by β3-adrenoceptor activation[4].
Dependent Claims
Dependent claims further specify the invention by detailing various aspects such as:
- Specific substituents and functional groups on the pyrrolidine ring.
- Different formulations and dosage forms of the pharmaceutical compositions.
- Methods of synthesis and purification of the compounds[4].
Patent Landscape
Related Patents and Applications
The patent is part of a series of related applications and patents, including U.S. Patent No. 8,247,415, which also deals with β3-adrenergic receptor agonists. These patents collectively form a robust intellectual property portfolio for Merck Sharp & Dohme Corp. in the area of urinary tract disorders[1][2].
Regulatory Approvals and Extensions
The approval of GEMTESA (vibegron), a drug indicated for the treatment of overactive bladder and related to the patents in question, has significant implications. The FDA's approval and subsequent patent term restoration applications highlight the regulatory pathway and the importance of these patents in protecting the intellectual property of the drug[2].
Patent Term and Expiration
The patent is set to expire on April 2, 2029. However, the patent term may be extended due to regulatory review periods, as governed by the Generic Animal Drug and Patent Term Restoration Act. The FDA and USPTO collaborate to determine the eligibility and extent of such extensions[2].
Impact on Innovation and Competition
The scope and claims of this patent influence innovation in the pharmaceutical industry by setting a standard for β3-adrenergic receptor agonists. The patent's breadth and specificity can affect licensing and litigation costs, potentially impacting the development of similar drugs by other companies. The absence of generic versions of GEMTESA currently underscores the patent's protective role[3][5].
Key Metrics for Patent Scope
Metrics such as independent claim length and independent claim count can be used to measure the scope of this patent. These metrics help in assessing the breadth and clarity of the patent claims, which are crucial for determining the patent's validity and its impact on innovation[3].
Expert Insights and Statistics
Industry experts emphasize the importance of precise and clear patent claims to avoid disputes and encourage innovation. For instance, the approval of GEMTESA and the associated patent term restoration highlight the complex interplay between regulatory approvals and patent protection. Statistics on the regulatory review period, such as the 1,483 and 1,433 days sought for patent term extension, illustrate the extensive process involved in bringing such drugs to market[2].
Illustrative Examples
The specific example of GEMTESA (vibegron) approved by the FDA demonstrates the practical application of the compounds described in the patent. This drug's success in treating overactive bladder symptoms underscores the therapeutic potential of β3-adrenergic receptor agonists[2].
"The approval of GEMTESA represented the first permitted commercial marketing or use of the product," highlighting the significance of this patent in bringing new treatments to market[2].
Conclusion
United States Patent 8,653,260 is a pivotal patent in the field of pharmaceuticals, particularly for the treatment of overactive bladder and related urinary tract disorders. The patent's scope, claims, and regulatory landscape collectively protect a significant innovation in β3-adrenergic receptor agonists, influencing both the therapeutic landscape and the competitive environment within the pharmaceutical industry.
Key Takeaways
- Compounds and Formulations: The patent describes hydroxymethyl pyrrolidine compounds as β3-adrenergic receptor agonists.
- Therapeutic Applications: Primary use is in treating overactive bladder symptoms.
- Claims: Cover specific chemical structures, pharmaceutical compositions, and methods of use.
- Patent Landscape: Part of a broader portfolio related to urinary tract disorders.
- Regulatory Approvals: Associated with FDA approvals and potential patent term extensions.
- Impact on Innovation: Influences licensing, litigation, and the development of similar drugs.
FAQs
What is the primary therapeutic application of the compounds described in US Patent 8,653,260?
The primary therapeutic application is in the treatment of overactive bladder, characterized by symptoms such as urge urinary incontinence, urgency, and frequency.
Who is the assignee of US Patent 8,653,260?
The assignee is Merck Sharp & Dohme Corp.
What is the expiration date of US Patent 8,653,260?
The patent is set to expire on April 2, 2029, although it may be extended due to regulatory review periods.
How does the patent impact innovation in the pharmaceutical industry?
The patent influences innovation by setting standards for β3-adrenergic receptor agonists, affecting licensing and litigation costs, and impacting the development of similar drugs.
Is there a generic version of GEMTESA available?
No, there is currently no therapeutically equivalent generic version of GEMTESA available in the United States[5].
Cited Sources
- United States Patent and Trademark Office, "US8653260B2 - Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists," February 18, 2014.
- Federal Register, "Federal Register/Vol. 89, No. 41/Thursday, February 29, 2024/Notices," February 29, 2024.
- Hoover Institution, "Patent Claims and Patent Scope," August 2016.
- Google Patents, "US8653260B2 - Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists."
- Drugs.com, "Generic Gemtesa Availability," November 6, 2024.
