United States Patent 8,546,428: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
The United States Patent 8,546,428, titled "Fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol," is a significant patent in the pharmaceutical domain. This patent, issued to Janssen Pharmaceutica NV, pertains to a specific compound and its pharmaceutical compositions, which are crucial in the treatment of mycobacterial infections, including tuberculosis.
Patent Overview
Inventors and Assignees
The patent was invented by Jean François Alexandre Lucas, Wim Albert Alex Aelterman, Yolande Lydia Lang, Sigrid Carl Maria Stokbroekx, Carina Leys, Peter Jozef Maria Van Remoortere, and Anne Faure. It is assigned to Janssen Pharmaceutica NV, a subsidiary of Johnson & Johnson[2].
Patent Issue and Expiration Dates
The patent was issued on October 1, 2013, and is set to expire on March 19, 2029[2].
Scope of the Patent
Active Ingredient
The patent focuses on the fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol. This compound is known as bedaquiline, a diarylquinoline antimycobacterial drug that inhibits mycobacterial ATP synthase by binding to subunit c of the enzyme[4].
Pharmaceutical Compositions
The patent includes pharmaceutical compositions that use the fumarate salt as the active ingredient. These compositions can be formulated in various dosage forms, such as tablets, and may include additional ingredients like wetting agents, binding agents, disintegrants, and lubricants[1].
Claims of the Patent
Independent Claims
The patent contains multiple independent claims that define the scope of the invention. These claims include:
- The fumarate salt of the specified compound.
- Pharmaceutical compositions comprising the fumarate salt.
- Methods for preparing these pharmaceutical compositions.
- Specific formulations and dosage forms of the drug[1].
Dependent Claims
Dependent claims further specify the details of the independent claims, such as the types of excipients used, the methods of preparation, and the specific characteristics of the pharmaceutical compositions[1].
Patent Landscape
Related Patents
The patent is part of a broader patent landscape related to bedaquiline. Another relevant patent is US 7,498,343, which also pertains to bedaquiline and its formulations. This patent is set to expire on December 1, 2026[2].
Exclusivity
In addition to patent protection, the FDA has granted exclusivity to the manufacturer, which provides exclusive marketing rights. This exclusivity can run concurrently with the patent but is a separate statutory provision[2].
Patent Scope Metrics
Independent Claim Length and Count
Research on patent scope metrics suggests that the length and count of independent claims can be indicative of the patent's breadth and complexity. Narrower claims, as seen in this patent, are often associated with a higher probability of grant and a shorter examination process[3].
Manufacturing and Formulation
Preparation Methods
The patent describes various methods for preparing the pharmaceutical compositions, including mixing, granulation, and film coating. These methods ensure the stability and efficacy of the drug[1].
Excipients and Additives
The compositions may include a range of excipients such as polyethylene glycol, microcrystalline cellulose, croscarmellose sodium, and magnesium stearate. These additives enhance the drug's performance and patient compliance[1].
Therapeutic Use
Mycobacterial Infections
Bedaquiline, the active ingredient, is specifically designed to treat mycobacterial infections, including multi-drug resistant tuberculosis. It works by inhibiting the ATP synthase enzyme, which is essential for the energy production of mycobacteria[4].
Regulatory Status
FDA Approval
The drug was approved by the FDA, and as of the current date, there is no therapeutically equivalent generic version available in the United States[2].
Economic and Legal Implications
Patent Expiration and Generic Competition
The expiration of the patent in 2029 will open the market to generic competition, potentially reducing the cost of the drug and increasing accessibility. However, until then, Janssen Pharmaceutica NV retains exclusive rights to manufacture and market bedaquiline[2].
Litigation and Patent Quality
The patent's scope and claims have been carefully defined to avoid issues of patent quality and litigation. The narrower claims and clear definitions help in maintaining the patent's validity and reducing potential legal disputes[3].
Key Takeaways
- The patent covers the fumarate salt of bedaquiline and its pharmaceutical compositions.
- It includes detailed methods for preparation and formulation.
- The drug is crucial for treating mycobacterial infections, including multi-drug resistant tuberculosis.
- The patent expires in 2029, after which generic versions may become available.
- The patent's scope is well-defined to ensure clarity and avoid legal issues.
Frequently Asked Questions (FAQs)
What is the active ingredient covered by US Patent 8,546,428?
The active ingredient is the fumarate salt of (alpha S, beta R)-6-bromo-alpha-[2-(dimethylamino)ethyl]-2-methoxy-alpha-1-naphthalenyl-beta-phenyl-3-quinolineethanol, known as bedaquiline.
What is the therapeutic use of bedaquiline?
Bedaquiline is used to treat mycobacterial infections, including multi-drug resistant tuberculosis.
When does the patent expire?
The patent is set to expire on March 19, 2029.
Are there any generic versions of bedaquiline available?
As of the current date, there are no therapeutically equivalent generic versions of bedaquiline available in the United States.
What are the key components of the pharmaceutical compositions covered by the patent?
The compositions include the fumarate salt of bedaquiline along with various excipients such as polyethylene glycol, microcrystalline cellulose, and magnesium stearate.
Sources Cited
- US8546428B2 - Fumarate salt of (alpha S, beta R) - Google Patents
- Generic Sirturo Availability - Drugs.com
- Patent Claims and Patent Scope - Hoover Institution
- Bedaquiline: Uses, Interactions, Mechanism of Action - DrugBank
