United States Patent 8,475,842: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 8,475,842, titled "Pharmaceutical formulation of 4-3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl-2H-phthalazin-1-one," is a significant patent in the pharmaceutical industry, particularly in the context of cancer treatment. This patent, assigned to AstraZeneca AB, pertains to the formulation and use of olaparib, a drug known by its international nonproprietary name and marketed as LYNPARZA®.
Background and Invention
The patent was filed on October 7, 2009, and granted on July 2, 2013. It involves a pharmaceutical formulation of olaparib, which is a compound used in the treatment of various cancers, including ovarian, breast, and prostate cancers. The formulation is designed to enhance the bioavailability of the drug through the use of specific matrix polymers[1][4].
Scope of the Patent
The scope of the patent is defined by its claims, which include:
Pharmaceutical Formulation
The patent claims a pharmaceutical formulation comprising the drug 4-3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl-2H-phthalazin-1-one. This formulation is characterized by the use of a matrix polymer that exhibits low hygroscopicity and high softening temperature, such as copovidone, to improve the drug's bioavailability[1].
Solid Dispersion
The patent also claims a solid dispersion of the drug with the specified matrix polymer. This solid dispersion is crucial for enhancing the solubility and stability of the drug, thereby improving its efficacy[1].
Daily Pharmaceutical Dose
The patent includes claims for a daily pharmaceutical dose of the drug provided by such a formulation, indicating the specific dosing regimen for therapeutic use[1].
Claims Analysis
The patent contains 10 claims that outline the specific aspects of the invention:
Independent Claims
The independent claims define the core of the invention, including the pharmaceutical formulation and the solid dispersion of the drug with the matrix polymer. These claims are critical in establishing the novelty and non-obviousness of the invention[1].
Dependent Claims
The dependent claims further specify the details of the formulation, such as the types of matrix polymers used and the process for preparing the solid dispersion. These claims provide additional protection by narrowing down the scope to specific embodiments of the invention[1].
Patent Landscape
The patent landscape surrounding U.S. Patent 8,475,842 is complex and involves multiple related patents and ongoing litigation.
Related Patents
Several other patents are related to this invention, including U.S. Patent Nos. 7,449,464, 8,859,562, and 11,633,396. These patents collectively cover various aspects of olaparib, including its synthesis, crystalline forms, and pharmaceutical formulations[2][5].
Litigation
There are ongoing legal battles involving generic manufacturers seeking to produce olaparib tablets before the expiration of these patents. Companies like Sandoz and Natco Pharma have submitted Abbreviated New Drug Applications (ANDAs) to the FDA, which have led to patent infringement lawsuits filed by AstraZeneca and its affiliates[2][5].
Impact on Innovation and Patent Quality
The scope and claims of this patent highlight the importance of patent quality and scope in the pharmaceutical industry. The debate over patent quality often centers around the breadth and clarity of patent claims. Narrower claims, like those in this patent, are generally associated with a higher probability of grant and shorter examination processes, which can foster innovation by providing clear boundaries for what is protected[3].
Crystalline Forms and Bioavailability
The patent's focus on specific crystalline forms of olaparib, such as Form H, underscores the importance of solid-state chemistry in pharmaceutical formulations. These forms are crucial for enhancing the drug's bioavailability and stability, which directly impacts its therapeutic efficacy[4].
Future Developments
Despite the existing patents, there is still a need for new solid forms of olaparib to further enhance its efficacy and manufacturing processes. Ongoing research and development aim to discover novel crystalline forms and improved formulations, indicating a dynamic and evolving patent landscape in this area[4].
Key Takeaways
- Pharmaceutical Formulation: The patent covers a specific pharmaceutical formulation of olaparib using matrix polymers to enhance bioavailability.
- Solid Dispersion: The use of solid dispersion with low hygroscopicity and high softening temperature polymers is a key aspect.
- Related Patents: Several related patents cover various aspects of olaparib, including synthesis and other formulations.
- Litigation: Ongoing patent infringement lawsuits involve generic manufacturers seeking to produce olaparib before patent expiration.
- Impact on Innovation: The patent's scope and claims highlight the importance of patent quality and clarity in fostering innovation.
Frequently Asked Questions
What is the main subject of U.S. Patent 8,475,842?
The main subject is a pharmaceutical formulation of olaparib, specifically designed to enhance its bioavailability using certain matrix polymers.
What are the key claims of this patent?
The key claims include the pharmaceutical formulation, solid dispersion of the drug with matrix polymers, and the daily pharmaceutical dose provided by such a formulation.
Why is the patent landscape around this patent complex?
The patent landscape is complex due to multiple related patents and ongoing litigation involving generic manufacturers seeking to produce olaparib before the expiration of these patents.
How does this patent impact innovation in the pharmaceutical industry?
The patent's scope and claims contribute to clear boundaries for what is protected, which can foster innovation by reducing licensing and litigation costs associated with overly broad or unclear patents.
What future developments can be expected in this area?
Future developments are expected to include the discovery of new solid forms of olaparib and improved manufacturing processes to further enhance the drug's efficacy and stability.
Cited Sources
- United States Patent and Trademark Office, "Pharmaceutical formulation of 4-3-(4-cyclopropanecarbonyl-piperazine-1-carbonyl)-4-fluoro-benzyl-2H-phthalazin-1-one," US 8,475,842 B2, July 2, 2013.
- Insight.RPXCorp, "Case 3:24-cv-00641 Document 1 Filed 02/02/24," February 2, 2024.
- Hoover Institution, "Patent Claims and Patent Scope," August 18, 2024.
- Justia Patents, "Crystalline form of olaparib and a process for preparing the same," U.S. Pat. No. 10,703,728, July 7, 2020.
- Insight.RPXCorp, "Case 3:24-cv-10624 Document 1 Filed 11/20/24," November 20, 2024.
