United States Patent 8,877,933: A Detailed Analysis
Introduction
The United States Patent 8,877,933, titled "Thermodynamically stable form of a tosylate salt," is a significant patent in the pharmaceutical industry, particularly in the development and application of specific drug compounds. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Background and Invention
This patent, filed by a pharmaceutical company, pertains to a novel, thermodynamically stable form of a tosylate salt of a specific compound. The compound in question is identified by the formula (I) and is particularly relevant in the treatment of various medical conditions.
Scope of the Invention
The patent describes a thermodynamically stable polymorph of the tosylate salt, which is crucial for its use in pharmaceutical compositions. This stability is essential for ensuring the compound's efficacy and shelf life.
Polymorphs and Stability
The invention focuses on a specific polymorph (Polymorph I) of the compound, which is stable at room temperature. This stability is a critical factor in pharmaceutical formulations, as it ensures consistent performance and reduces the risk of degradation over time[1].
Claims of the Patent
The patent includes several key claims that define the scope of the invention:
Composition Claims
- The patent claims a pharmaceutical composition containing more than 90% (preferably more than 95%) by weight of the compound in Polymorph I. This ensures that the majority of the compound in the composition is in the stable form[1].
Therapeutic Uses
- The patent specifies the use of the compound in Polymorph I for treating various disorders, including those involving abnormal angiogenesis or hyperpermeability, bone marrow diseases like leukemia, and carcinomas such as lung, pancreas, thyroid gland, kidney, or intestine cancers[1].
Cellular Signal Transduction Pathways
- The compound is indicated for treating or preventing diseases mediated by cellular signal transduction pathways involving raf, VEGFR, PDGFR, p38, and/or flt-3 kinases. This highlights its potential in targeting multiple pathways critical in various diseases[1].
Therapeutic Applications
The patent outlines several therapeutic applications for the compound:
Hyperpermeability Conditions
- The compound can be used to treat and/or prevent vascular hyperpermeability, thereby addressing conditions such as tissue edema (e.g., lung, kidney, brain), vasogenic brain edema, chronic inflammation, wound healing, ischemia, tumors, atherosclerosis, and other related conditions[1].
Specific Diseases
- It is also applicable in treating or preventing diseases like diabetic retinopathy, diabetic retinal disease, obstruction of respiratory airways during asthma, circulatory collapse in sepsis, acute lung injury, and acute respiratory distress syndrome[1].
Patent Landscape and Litigation
Understanding the broader patent landscape is crucial for navigating the complexities of pharmaceutical patent law.
ANDA Litigation and Generic Challenges
- Patents like US8877933B2 are often at the center of Abbreviated New Drug Application (ANDA) litigation, where generic manufacturers challenge the validity and enforceability of patents to bring generic versions of drugs to market. Similar cases, such as those involving Latuda® (lurasidone HCl tablets) and Brilinta® (ticagrelor tablets), highlight the legal battles surrounding pharmaceutical patents[2].
Terminal Disclaimer Practice
- The USPTO's recent withdrawal of proposed rule changes regarding Terminal Disclaimer Practice is significant. This practice allows patent owners to file continuation applications for various aspects of an invention without facing non-statutory double patenting issues. The withdrawal of these proposed changes is beneficial for maintaining the integrity of patent portfolios, especially in the pharmaceutical industry[3].
Industry Impact
The impact of this patent extends beyond its specific claims:
Innovation and Competition
- Patents like US8877933B2 play a crucial role in encouraging innovation by providing exclusive rights to inventors. However, they also face scrutiny to ensure they do not stifle competition or delay the entry of generic drugs into the market[3].
Regulatory Environment
- The regulatory environment, including USPTO rules and court decisions, significantly influences the validity and enforceability of pharmaceutical patents. Changes in these regulations can have far-reaching consequences for both innovator companies and generic manufacturers[3].
Key Takeaways
- Thermodynamic Stability: The patent emphasizes the importance of a thermodynamically stable form of the tosylate salt for pharmaceutical use.
- Broad Therapeutic Applications: The compound has potential uses in treating a wide range of diseases, including cancers and hyperpermeability conditions.
- Patent Landscape: The patent is part of a complex landscape involving ANDA litigation and regulatory challenges.
- Industry Impact: The patent affects innovation, competition, and the regulatory environment in the pharmaceutical industry.
Frequently Asked Questions (FAQs)
What is the primary focus of United States Patent 8,877,933?
The primary focus is on a novel, thermodynamically stable form of a tosylate salt of a specific compound, particularly its use in pharmaceutical compositions.
What are the therapeutic applications of the compound described in the patent?
The compound is indicated for treating disorders involving abnormal angiogenesis or hyperpermeability, bone marrow diseases, and various carcinomas, among other conditions.
How does the patent impact the pharmaceutical industry?
The patent influences innovation, competition, and the regulatory environment by providing exclusive rights to the inventor while facing scrutiny to ensure it does not delay the entry of generic drugs.
What is the significance of polymorphs in pharmaceuticals?
Polymorphs are critical in pharmaceuticals because they affect the physical stability and performance of the drug compound. A stable polymorph ensures consistent efficacy and shelf life.
How do regulatory changes affect pharmaceutical patents?
Regulatory changes, such as those proposed by the USPTO, can significantly impact the validity and enforceability of pharmaceutical patents, affecting both innovator companies and generic manufacturers.
Cited Sources
- US8877933B2 - Thermodynamically stable form of a tosylate salt - Google Patents
- ANDA Litigation Settlements - Robins Kaplan LLP Law Firm
- Threat to Many Patent Portfolios Fades as USPTO Withdraws Controversial Proposed Rule - Procopio.com
