United States Patent 10,927,117: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 10,927,117, titled "Crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof," is a significant patent in the pharmaceutical sector, particularly in the field of kinase inhibitors. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.
Background
The patent in question pertains to a specific crystalline form of a compound that is a Bruton's tyrosine kinase (BTK) inhibitor. BTK inhibitors are crucial in treating various types of B-cell lymphomas and other immune system disorders. The compound described is closely related to zanubrutinib, a drug used to treat mantle cell lymphoma and other B-cell non-Hodgkin lymphomas[4].
Scope of the Patent
Crystalline Form
The patent specifically covers the crystalline form of the compound (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide. This crystalline form is critical for the stability, solubility, and bioavailability of the drug, which are essential factors in pharmaceutical development[1].
Preparation Methods
The patent details various methods for preparing this crystalline form, including precipitation, evaporation, and crystallization from different solvents such as dichloromethane, n-hexane, and ethyl acetate. These methods ensure the production of a pure and stable crystalline form of the compound[1].
Uses
The compound is primarily used as a BTK inhibitor, which makes it effective in treating B-cell lymphomas. Clinical trials and preliminary results have shown the efficacy of similar BTK inhibitors, such as ibrutinib and zanubrutinib, in treating various types of B-cell lymphomas[1][4].
Claims of the Patent
Composition of Matter Claims
The patent includes claims related to the composition of matter of the crystalline form of the compound. These claims specify the structural and chemical characteristics of the crystalline form, ensuring that any identical or substantially similar forms would infringe on the patent[1].
Method of Preparation Claims
Claims also cover the methods used to prepare the crystalline form, including the specific solvents and conditions required. This ensures that the patented process is protected against unauthorized use[1].
Use Claims
The patent claims the use of the crystalline form of the compound as a BTK inhibitor for treating B-cell lymphomas and other related conditions. These use claims are crucial for maintaining the exclusivity of the drug's therapeutic applications[1].
Patent Landscape
Related Patents
The patent landscape for BTK inhibitors is complex, with multiple patents covering different aspects of these compounds. For example, patents such as US9447106 and US10570139 also cover various forms and uses of BTK inhibitors, including zanubrutinib[4][5].
Expiration Dates
The patent US10927117 is set to expire on August 15, 2037. Understanding the expiration dates of related patents is crucial for planning generic drug launches and avoiding patent infringement[4][5].
Litigation and Settlements
Patent litigation and settlements are common in the pharmaceutical industry. For instance, settlements in ANDA (Abbreviated New Drug Application) litigation often involve agreements that allow generic manufacturers to enter the market under certain conditions, such as delayed entry or limited exclusivity[2].
Analytical Tools and Strategies
Patent Analytics
To navigate the complex patent landscape, companies use patent analytics tools. These tools help in categorizing patents by claims and scope concepts, identifying gaps in coverage, and determining the value of patent claims. Tools like ClaimScape® software generate interactive claim charts that facilitate the review of patent coverage by technical experts[3].
Claim Coverage Matrix
A Claim Coverage Matrix is essential for understanding which patents and claims are actively protecting the intellectual property. This matrix helps in identifying where gaps or opportunities exist, allowing companies to make informed decisions about their patent portfolio[3].
Impact on Pharmaceutical Development
Stability and Bioavailability
The crystalline form of the compound ensures better stability and bioavailability, which are critical for the efficacy and safety of the drug. This is particularly important in the development of BTK inhibitors, where consistency in drug formulation is vital[1].
Competitive Advantage
Holding a patent for a specific crystalline form of a BTK inhibitor provides a competitive advantage in the market. It allows the patent holder to exclusively market the drug until the patent expires, thereby protecting their investment in research and development[1].
Key Takeaways
- Crystalline Form: The patent covers a specific crystalline form of a BTK inhibitor, crucial for stability and bioavailability.
- Preparation Methods: Detailed methods for preparing the crystalline form are included, ensuring purity and stability.
- Therapeutic Use: The compound is used to treat B-cell lymphomas, with clinical trials showing efficacy.
- Patent Expiration: The patent is set to expire on August 15, 2037.
- Patent Landscape: The landscape includes multiple related patents and potential litigation and settlements.
- Analytical Tools: Patent analytics and Claim Coverage Matrix are essential for navigating the patent landscape.
FAQs
What is the primary use of the compound described in US10927117?
The primary use of the compound is as a Bruton's tyrosine kinase (BTK) inhibitor for treating B-cell lymphomas.
How is the crystalline form of the compound prepared?
The crystalline form is prepared through methods such as precipitation, evaporation, and crystallization using specific solvents like dichloromethane, n-hexane, and ethyl acetate.
What is the significance of the crystalline form in pharmaceutical development?
The crystalline form ensures better stability and bioavailability, which are critical for the efficacy and safety of the drug.
When is the patent set to expire?
The patent US10927117 is set to expire on August 15, 2037.
How do companies navigate the complex patent landscape for BTK inhibitors?
Companies use patent analytics tools and strategies like Claim Coverage Matrix to categorize patents, identify gaps, and determine the value of patent claims.
Sources
- US10927117B2 - Crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide, preparation, and uses thereof - Google Patents
- ANDA Litigation Settlements | Hatch-Waxman - Robins Kaplan LLP
- Patent Analytics | Intellectual Property Law - Schwegman
- Zanubrutinib: Uses, Interactions, Mechanism of Action - DrugBank
- Generic Brukinsa Availability - Drugs.com
