United States Patent 8,617,598: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 8,617,598, issued on December 31, 2013, pertains to specific pharmaceutical compositions, particularly those involving everolimus, a macrolide compound. This patent is crucial for understanding the intellectual property landscape in the pharmaceutical industry, especially regarding formulations of everolimus.
Overview of the Patent
Patent Description
The patent describes pharmaceutical compositions in the form of dispersible tablets that include a solid dispersion of everolimus, a disintegrant, and colloidal silicon dioxide. Everolimus is an inhibitor of the mammalian target of rapamycin (mTOR) and is used as an antineoplastic and immunosuppressant agent[2][4].
Key Components
- Everolimus: The active pharmaceutical ingredient, which is a macrolide compound.
- Solid Dispersion: A formulation technique that enhances the solubility and bioavailability of everolimus.
- Disintegrant: An excipient that helps in the rapid disintegration of the tablet in the gastrointestinal tract.
- Colloidal Silicon Dioxide: An excipient that improves the flowability and stability of the formulation[1][2].
Scope of the Patent
Claims
The patent includes several claims that define the scope of protection:
- Composition Claims: These claims cover the specific formulation of everolimus in a solid dispersion with a disintegrant and colloidal silicon dioxide.
- Method Claims: These claims cover the methods of preparing these pharmaceutical compositions.
- Use Claims: These claims cover the therapeutic uses of the compositions, such as inhibiting the growth of non-malignant solid tumors of the brain[2].
Therapeutic Applications
The patent specifies the use of everolimus in treating various conditions, including non-malignant solid tumors of the brain. This indicates a broad therapeutic scope for the patented compositions[2].
Patent Landscape
Related Patents
The patent landscape surrounding US 8,617,598 includes other patents related to everolimus and similar macrolide compounds:
- US 20200093804 A1: This patent describes pharmaceutical compositions of everolimus using hot melt extrusion (HME) grade hydroxypropyl methylcellulose, which is another formulation technique to enhance the bioavailability of everolimus[4].
- US 20120289536 A1: This patent also deals with pharmaceutical compositions comprising colloidal silicon dioxide, similar to the '598 patent, but may have different formulation specifics[5].
Litigation and Enforcement
The '598 patent has been involved in litigation, particularly in a case where Novartis AG alleged infringement by Mylan for filing an Abbreviated New Drug Application (ANDA) for everolimus tablets. This highlights the importance of this patent in protecting Novartis's intellectual property[2].
Claim Coverage and Scope Concepts
Claim Analysis
To understand the full scope of the patent, a detailed claim analysis is necessary. This involves categorizing claims by scope concepts, which can help in identifying gaps or opportunities in the patent landscape. Tools like ClaimScape® software can be used to generate interactive claim charts that facilitate this analysis[3].
Scope Concepts
- High-Value Claims: These are claims that are highly relevant to the current products and technologies of the company.
- Medium-Value Claims: These indicate potential future directions or technologies.
- Low-Value Claims: These may not be worth maintaining and can be identified through thorough analysis[3].
Impact on Pharmaceutical Industry
Formulation Innovations
The patent promotes innovations in pharmaceutical formulations, particularly in enhancing the bioavailability and stability of everolimus. This is crucial for improving patient outcomes and compliance.
Intellectual Property Protection
The '598 patent serves as a significant barrier to entry for generic manufacturers, protecting Novartis's investment in research and development. It also underscores the importance of patent analytics in managing and leveraging intellectual property in the pharmaceutical sector[2][3].
Key Takeaways
- Specific Formulation: The patent covers a specific formulation of everolimus in a solid dispersion with a disintegrant and colloidal silicon dioxide.
- Therapeutic Use: The compositions are used for treating non-malignant solid tumors of the brain and other conditions.
- Litigation: The patent has been involved in significant litigation, highlighting its importance in protecting intellectual property.
- Patent Landscape: The patent is part of a broader landscape that includes other related patents on everolimus formulations.
- Innovation: The patent promotes innovations in pharmaceutical formulations, enhancing bioavailability and stability.
FAQs
Q: What is the main active ingredient in the pharmaceutical compositions described in US 8,617,598?
A: The main active ingredient is everolimus, an inhibitor of the mammalian target of rapamycin (mTOR).
Q: What are the key excipients mentioned in the patent?
A: The key excipients include a disintegrant and colloidal silicon dioxide.
Q: What is the therapeutic use of the compositions described in the patent?
A: The compositions are used for inhibiting the growth of non-malignant solid tumors of the brain and other therapeutic applications.
Q: Has the '598 patent been involved in any litigation?
A: Yes, the patent has been involved in litigation, particularly in a case where Novartis AG alleged infringement by Mylan.
Q: How does the patent impact the pharmaceutical industry?
A: The patent promotes innovations in pharmaceutical formulations and protects Novartis's intellectual property, serving as a barrier to entry for generic manufacturers.
Sources
- US8617598B2 - Pharmaceutical compositions comprising colloidal silicon dioxide - Google Patents
- in the united states district court for the district of delaware novartis ... - Insight.RPXCorp
- Patent Analytics | Intellectual Property Law - SLWIP
- US20200093804A1 - Pharmaceutical composition of everolimus - Google Patents
- US20120289536A1 - Pharmaceutical Compositions Comprising Colloidal Silicon Dioxide - Google Patents
