United States Patent 9,562,016: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 9,562,016, issued on February 7, 2017, is a significant patent in the field of pharmaceuticals, particularly focusing on the preparation and formulation of MEK inhibitors. This patent is assigned to Array BioPharma Inc. and involves several inventors, including Krell Christoph Max, Misun Marian, and others.
Background and Context
MEK inhibitors are a class of drugs that target the MEK enzyme, which is involved in the MAPK/ERK signaling pathway. This pathway is crucial in cell division and differentiation, and its dysregulation is associated with various cancers and other diseases. The patent in question addresses the preparation and formulation of a specific MEK inhibitor, binimetinib, which is used in the treatment of diseases involving abnormal kinase activity, such as melanoma and other cancers[4].
Scope of the Patent
Claims Overview
The patent includes several claims that define the scope of the invention. Here are the key aspects:
- Processes for Preparation: The patent describes methods for preparing 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, which is the active compound in binimetinib. This includes steps for synthesizing the compound and its intermediates[4].
- Crystallization Methods: The patent details processes for crystallizing the MEK inhibitor, which is crucial for its stability and efficacy in pharmaceutical formulations[4].
- Pharmaceutical Compositions: It includes claims related to pharmaceutical compositions comprising the crystallized MEK inhibitor, which are designed for therapeutic use[4].
Claim Construction
The construction of claims in a patent is critical for determining the scope of protection. According to legal standards, the claims of a patent define the invention to which the patentee is entitled the right to exclude. The court looks primarily to the intrinsic evidence, including the specification and prosecution history, to construe the claims[1].
Key Claims and Their Significance
Claim 1: Preparation Method
Claim 1 describes a method of making binimetinib, which includes dissolving the compound in a solution comprising a solvent system that includes an ether and optionally an alcohol. This method is significant because it outlines a specific process that ensures the purity and stability of the final product[1][4].
Claim 2: Crystallization Process
The patent claims a crystallization process that results in a specific crystal form of binimetinib. This process is crucial for the pharmaceutical properties of the compound, such as its solubility and bioavailability[4].
Claim 3: Pharmaceutical Compositions
Claims related to pharmaceutical compositions cover the formulation of the crystallized MEK inhibitor into various dosage forms, such as tablets, capsules, or solutions. These compositions are designed to treat diseases associated with abnormal kinase activity[4].
Patent Landscape
Related Patents
The patent landscape surrounding MEK inhibitors is complex and involves multiple patents from various assignees. Here are some related patents:
- Patent 9,314,464: This patent, also related to protein kinase inhibitors, was issued to Novartis AG and involves similar compounds and methods[4].
- Patent 9,598,376: This patent, issued to Array BioPharma Inc., covers additional processes for preparing and formulating the same MEK inhibitor[4].
- Patent 9,850,229: Another patent from Array BioPharma Inc., this covers novel classes of compounds and their use in treating diseases involving abnormal kinase activity[4].
IPC Classification
The International Patent Classification (IPC) system categorizes patents based on their technological content. Patents related to MEK inhibitors, including US 9,562,016, are primarily classified under C07D, which includes heterocyclic compounds. Other relevant IPC classes include C07C (acyclic and carboxylic compounds) and A61P (specific therapeutic activity of chemical compounds or medicinal preparations)[3].
Patent Expiration Dates
Understanding the expiration dates of related patents is crucial for strategic planning in the pharmaceutical industry. The patent in question, US 9,562,016, is set to expire on October 18, 2033. Other related patents have similar expiration dates, ranging from 2030 to 2033[4].
Legal and Regulatory Considerations
Claim Construction and Infringement
The construction of claims is a legal question, and courts rely on intrinsic evidence such as the specification and prosecution history to determine the scope of the claims. This patent's claims must be construed in a way that does not read limitations from the embodiments in the specification into the claims, as per legal precedents[1].
Prosecution History
The prosecution history of the patent, including any amendments or arguments made during the patent application process, can be crucial in determining the scope of the claims. This history can help clarify any ambiguities in the claim language[1].
Industry Impact and Applications
Therapeutic Use
The MEK inhibitor described in this patent, binimetinib, is used in the treatment of various cancers, including melanoma. The specific processes and formulations outlined in the patent ensure the efficacy and safety of this drug[4].
Market Competition
The patent landscape in the MEK inhibitor space is competitive, with multiple companies holding patents related to similar compounds and methods. The expiration of these patents can significantly impact market competition and the availability of generic versions of these drugs[4].
Key Takeaways
- Specific Preparation and Crystallization Methods: The patent outlines detailed methods for preparing and crystallizing the MEK inhibitor binimetinib.
- Pharmaceutical Compositions: The patent covers various pharmaceutical compositions of the crystallized MEK inhibitor.
- Legal and Regulatory Considerations: Claim construction and prosecution history are critical in determining the scope of protection.
- Industry Impact: The patent affects the therapeutic use of binimetinib and the competitive landscape in the pharmaceutical industry.
FAQs
Q: What is the main compound described in US Patent 9,562,016?
A: The main compound is 6-(4-bromo-2-fluorophenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-hydroxyethyoxy)-amide, known as binimetinib.
Q: What are the key claims of this patent?
A: The key claims include methods for preparing binimetinib, its crystallization, and pharmaceutical compositions comprising the crystallized compound.
Q: When does the patent expire?
A: The patent is set to expire on October 18, 2033.
Q: What is the therapeutic use of binimetinib?
A: Binimetinib is used in the treatment of diseases involving abnormal kinase activity, particularly cancers such as melanoma.
Q: How does this patent impact the pharmaceutical industry?
A: It affects the availability of specific formulations of MEK inhibitors and influences market competition among pharmaceutical companies.
Sources
- ARRAY BIOPHARMA, INC., Plaintiff - District of Delaware. United States District Court for the District of Delaware, 2024.
- Preparation of and formulation comprising a MEK inhibitor - Patent US-9562016-B2. PubChem.
- A novel approach to understand patents from the drug discovery perspective. bioRxiv, 2023.
- Generic Mektovi Availability - Drugs.com. Drugs.com.
