United States Patent 8,987,463: A Detailed Analysis of Scope and Claims
Introduction
United States Patent 8,987,463, titled "Methods of synthesizing factor Xa inhibitors," is a significant patent in the pharmaceutical industry, particularly in the field of anticoagulant drugs. This patent, assigned to Portola Pharmaceuticals, Inc., describes novel methods for synthesizing factor Xa inhibitors, which are crucial for preventing and treating thrombotic disorders.
Background
Factor Xa is a key enzyme in the coagulation cascade, and inhibitors of this enzyme are used to prevent blood clots. The patent in question focuses on the synthesis of betrixaban, a specific factor Xa inhibitor, and its pharmaceutically acceptable salts.
Patent Overview
Publication Number and Authority
The patent number is US8987463B2, and it was granted by the United States Patent and Trademark Office (USPTO)[4].
Prior Art and Legal Status
The patent is active, with an expiration date based on the patent term. The prior art keywords include "compound," "betrixaban," "formula," "salt," and "acid," indicating the patent's focus on specific chemical compounds and their synthesis methods[4].
Scope of the Patent
Claims
The patent includes several claims that define the scope of the invention. These claims cover:
- Methods of Synthesis: The patent describes methods for synthesizing a compound of Formula II, which is a factor Xa inhibitor, and its pharmaceutically acceptable salts. This includes the conversion of the compound to a maleate salt of betrixaban, which has excellent crystallinity, thermal, and hydrolytic stability, and purity[4].
- Compositions and Methods: The claims also include compositions and methods that involve the recited elements but do not exclude other elements that do not materially alter the novel characteristics of the claimed invention. Terms like "consisting essentially of" and "consisting of" are used to define the scope of the compositions and methods[4].
Embodiments
The patent outlines various embodiments of the invention, including:
- Gram and Kilogram Scale Synthesis: The methods described are applicable on both a gram and kilogram scale, making the process scalable for industrial production[4].
- Pharmaceutically Acceptable Salts: The patent emphasizes the synthesis of pharmaceutically acceptable salts, such as the maleate salt of betrixaban, which is crucial for the drug's efficacy and stability[4].
Claims Analysis
Dependency and Scope
The claims are structured to ensure that the invention is broadly protected while allowing for variations that do not alter the essential characteristics. For example, the use of "consisting essentially of" allows for the inclusion of other elements that do not significantly change the claimed invention[4].
Novelty and Non-Obviousness
The patent claims must meet the criteria of novelty and non-obviousness. The unique synthesis methods and the specific properties of the maleate salt of betrixaban ensure that the invention is novel and not obvious to those skilled in the art[4].
Patent Landscape
Related Patents and Applications
The patent landscape for factor Xa inhibitors is complex, with multiple patents and applications filed by various pharmaceutical companies. The USPTO's Patent Public Search tool and the Global Dossier service can be used to identify related patents and applications, including those from other IP5 Offices[1].
Citation Data
The Common Citation Document (CCD) application can provide a single point of access to citation data related to this patent, consolidating prior art cited by all participating IP5 Offices. This helps in understanding the broader patent landscape and potential overlaps or conflicts[1].
Practical Implications
Industrial Application
The methods described in the patent are designed for industrial-scale production, making them practically significant for pharmaceutical manufacturing. The scalability and stability of the synthesized compounds are critical for ensuring consistent quality in drug production[4].
Regulatory Compliance
Compliance with regulatory requirements is essential. The patent's focus on pharmaceutically acceptable salts and the stability of these compounds aligns with regulatory standards for drug approval. This ensures that the synthesized compounds meet the necessary safety and efficacy criteria[4].
Expert Insights
Industry experts and legal practitioners often emphasize the importance of detailed patent claims and the need for clarity in defining the scope of the invention. For example, Andrei Iancu, former Undersecretary of Commerce for IP and Director of the USPTO, has highlighted the significance of robust patent claims in protecting intellectual property[5].
Statistics and Trends
The USPTO's Patent Claims Research Dataset provides insights into patent scope and claims trends. This dataset, which includes detailed information on claims from US patents granted between 1976 and 2014, can help in understanding the broader trends in patent claims and their impact on the pharmaceutical industry[3].
Key Takeaways
- Novel Synthesis Methods: The patent introduces novel methods for synthesizing factor Xa inhibitors, particularly betrixaban and its pharmaceutically acceptable salts.
- Scalability: The methods are scalable for industrial production, ensuring consistent quality in drug manufacturing.
- Regulatory Compliance: The patent focuses on synthesizing compounds that meet regulatory standards for safety and efficacy.
- Patent Landscape: The patent is part of a complex landscape of related patents and applications, requiring careful analysis using tools like the Global Dossier and CCD.
FAQs
Q: What is the main focus of United States Patent 8,987,463?
A: The main focus is on methods for synthesizing factor Xa inhibitors, specifically betrixaban and its pharmaceutically acceptable salts.
Q: How does the patent ensure scalability in production?
A: The patent describes methods that are applicable on both a gram and kilogram scale, making the process scalable for industrial production.
Q: What is the significance of the maleate salt of betrixaban?
A: The maleate salt of betrixaban has excellent crystallinity, thermal, and hydrolytic stability, and purity, making it a preferred form for pharmaceutical use.
Q: How can one search for related patents and applications?
A: Tools like the USPTO's Patent Public Search, Global Dossier, and Common Citation Document (CCD) can be used to identify related patents and applications.
Q: What are the regulatory implications of this patent?
A: The patent ensures that the synthesized compounds meet regulatory standards for safety and efficacy, which is crucial for drug approval.
Sources
- USPTO - Search for patents: "How to Conduct a Preliminary U.S. Patent Search: A Step by Step Strategy."
- USA.gov - U.S. Patent and Trademark Office: "U.S. Patent and Trademark Office (USPTO)."
- USPTO - Patent Claims Research Dataset: "Patent Claims Research Dataset."
- Google Patents - US8987463B2: "Methods of synthesizing factor Xa inhibitors."
- ACUS - U.S. Patent Small Claims Court: "U.S. Patent Small Claims Court Study."
