United States Patent 7,037,917: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 7,037,917, titled "HIV replication inhibiting pyrimidines," is a significant patent in the field of antiretroviral therapy, particularly for the treatment of HIV. This patent, issued on May 2, 2006, and assigned to Janssen Pharmaceutica N.V., covers a class of compounds known as pyrimidinyl derivatives that inhibit HIV replication.
Inventors and Assignees
The patent lists several inventors, including Bart De Corte, Marc Rene De Jonge, Jan Heeres, Chih Yung Ho, Paul Adriaan Jan Janssen, Robert W. Kavash, Lucien Mara Henricus Koymans, Michael Joseph Kukla, Donald William Ludovici, Koen Jeanne Alfons Van Aken, and Koenraad Jozef Lodewijk Marcel Andries. The assignee is Janssen Pharmaceutica N.V., a subsidiary of Johnson & Johnson[2].
Patent Scope and Claims
The patent encompasses 32 claims, which include the active ingredient etravirine, pharmaceutical formulations containing etravirine, combinations of etravirine with other retroviral compounds, and methods of using these formulations. The claims are divided into several categories:
Compound Claims
Claims 1-5, 9, 11, 15, 21, 22, and 26-32 specifically claim etravirine and its various forms, including pharmaceutically acceptable salts and solvates[2].
Formulation Claims
These claims cover pharmaceutical formulations that include etravirine, often in combination with other antiretroviral agents. The formulations can be tailored for different administration routes, such as oral or parenteral[4].
Method Claims
The patent also includes claims for methods of treating HIV infection using etravirine, either alone or in combination with other antiretroviral drugs[2].
Chemical Structure and Composition
The compounds claimed in the patent are pyrimidinyl derivatives, characterized by specific structural elements such as amino, alkyl, and cyano groups. These compounds are designed to inhibit the reverse transcriptase enzyme of HIV, thereby preventing viral replication[1][2].
Pharmaceutical Formulations
One of the key aspects of this patent is the development of pharmaceutical formulations that enhance the bioavailability and stability of etravirine. For example, a formulation described in a related patent (US8703786B2) includes etravirine dissolved in a mixture of 1-methyl-2-pyrrolidinone, Labrasol, and water, which significantly improves the drug's oral bioavailability compared to the commercially available Intelence® Tablet formulation[4].
Bioavailability and Stability
The formulations developed under this patent have been shown to be stable over extended periods at room temperature and exhibit superior bioavailability. For instance, a pharmacokinetic study demonstrated that the new formulation had over 40-fold superior bioavailability compared to the Intelence® Tablet[4].
Patent Term and Extensions
The original expiration date of the patent was November 5, 2019. However, Janssen Pharmaceutica N.V. petitioned for and was granted an extension of the patent term by 404 days to December 13, 2020, under 35 U.S.C. §156(d) and 37 C.F.R. §1.740[2].
Patent Landscape and Impact
The patent landscape surrounding US7037917B2 is complex, with multiple related patents and applications. This patent is part of a broader portfolio of intellectual property related to HIV treatments, reflecting the ongoing research and development in antiretroviral therapy.
Related Patents
Other patents, such as US8703786B2, build upon the foundational work of US7037917B2 by focusing on specific formulations and uses of etravirine. These patents collectively contribute to the advancement of HIV treatment options[4].
Industry Impact
The issuance and maintenance of this patent have significant implications for the pharmaceutical industry, particularly in the area of HIV treatment. It underscores the importance of intellectual property in driving innovation and ensuring that new treatments are developed and made available to patients.
Metrics for Patent Scope
Research on patent scope, such as the work by Alan C. Marco et al., highlights the importance of metrics like independent claim length and independent claim count in assessing patent breadth and quality. These metrics can help in understanding the scope and impact of patents like US7037917B2[3].
Regulatory and Legal Aspects
The patent has undergone various regulatory and legal processes, including a request for a certificate of correction to add an inventor and a terminal disclaimer to disclaim the terminal part of the statutory term beyond the expiration date of a related patent[2].
Conclusion
United States Patent 7,037,917 is a pivotal patent in the field of HIV treatment, covering the active ingredient etravirine and its formulations. The patent's scope, claims, and related formulations have significantly contributed to the advancement of antiretroviral therapy. Understanding the patent landscape and the metrics used to assess patent scope provides valuable insights into the innovation and regulatory environment surrounding such critical medical treatments.
Key Takeaways
- Active Ingredient: The patent covers etravirine, a second-generation non-nucleoside reverse transcriptase inhibitor.
- Formulations: The patent includes claims for various pharmaceutical formulations that enhance the bioavailability and stability of etravirine.
- Method Claims: Methods of treating HIV infection using etravirine alone or in combination with other antiretroviral agents are claimed.
- Patent Term: The patent term was extended to December 13, 2020.
- Impact: The patent has a significant impact on the development and availability of HIV treatments.
Frequently Asked Questions (FAQs)
What is the main compound covered by US7037917B2?
The main compound covered by this patent is etravirine, a non-nucleoside reverse transcriptase inhibitor used in the treatment of HIV.
What are the key formulations described in the patent?
The patent describes pharmaceutical formulations that include etravirine, often in combination with solvents and surfactants to enhance bioavailability and stability.
How was the bioavailability of etravirine improved?
The bioavailability of etravirine was significantly improved through the development of a formulation that includes 1-methyl-2-pyrrolidinone, Labrasol, and water, showing over 40-fold superior bioavailability compared to the Intelence® Tablet.
What is the significance of the patent term extension?
The patent term extension to December 13, 2020, allowed Janssen Pharmaceutica N.V. to maintain exclusive rights to etravirine for a longer period, ensuring continued innovation and investment in HIV treatment.
How does this patent impact the pharmaceutical industry?
This patent impacts the pharmaceutical industry by protecting the intellectual property related to etravirine, encouraging further research and development in antiretroviral therapy, and ensuring that new treatments are made available to patients.
Cited Sources:
- US7037917B2 - HIV replication inhibiting pyrimidines - Google Patents
- Application for Extension of U.S. Patent No. 7,037,917 - Regulations.gov
- Patent Claims and Patent Scope - Hoover Institution
- US8703786B2 - Etravirine formulations and uses thereof - Google Patents
