United States Patent 4,267,179: A Detailed Analysis of Scope, Claims, and Patent Landscape
Introduction
United States Patent 4,267,179, titled "Heterocyclic derivatives of (4-phenylpiperazin-1-yl)alkylamines," is a significant patent in the pharmaceutical industry, particularly in the development of antifungal drugs. This patent, granted to Janssen Pharmaceutical NV, is crucial for understanding the intellectual property landscape surrounding itraconazole, a broad-spectrum antifungal agent.
Patent Overview
Publication and Priority
The patent was published on May 5, 1981, with the application number US06/020,383. It is part of a broader family of patents related to heterocyclic derivatives, which are essential in the synthesis of various pharmaceutical compounds[4].
Inventors and Assignees
The patent was assigned to Janssen Pharmaceutica N.V., a Belgian pharmaceutical company known for its innovative drug development. The inventors listed on the patent are key figures in the development of itraconazole and other related compounds.
Claims and Scope
Independent Claims
The patent includes several claims, but the primary focus is on the independent claims that define the novel compounds and their uses. The claims cover:
- Chemical Structure: The patent describes heterocyclic derivatives of (4-phenylpiperazin-1-yl)alkylamines, specifically highlighting the substitution of the aryloxy-moiety with a 4-phenylpiperazinyl group[4].
- Synthesis: The claims include methods for synthesizing these compounds, which involve reactive ester residues and specific chemical reactions.
- Therapeutic Use: The patent claims the therapeutic use of these compounds, particularly as antifungal agents.
Dependent Claims
Dependent claims further specify the scope of the invention by detailing various aspects such as:
- Specific Compounds: The patent lists preferred compounds where the 4-phenylpiperazinyl function is attached to the phenoxymethyl moiety in the para position.
- Substituents: It specifies the types of substituents that can be used, such as halo groups (fluoro, chloro, bromo, and iodo) and lower alkyl groups (methyl, ethyl, etc.)[4].
Patent Landscape
Regulatory Extensions
Patents like U.S. 4,267,179 can be subject to regulatory extensions under 35 U.S.C. § 156, which allows for the extension of patent terms due to delays in FDA approval. This is particularly relevant for pharmaceutical patents, as seen in other related patents where extensions were granted to account for regulatory review periods[2].
Litigation and Enforcement
The patent has been involved in significant litigation, such as the case of Janssen Pharmaceutical NV v. Eon Labs Manufacturing, Inc., where Janssen enforced its patent rights against a generic drug manufacturer. This case highlights the importance of patent protection in the pharmaceutical industry and the legal battles that can ensue when generic manufacturers attempt to enter the market[1].
Patent Analytics and Claim Coverage
To fully understand the scope and claims of U.S. 4,267,179, patent analytics tools can be employed. These tools help in categorizing patents by claims and scope concepts, making it easier to identify gaps in coverage and future design opportunities. For instance, a Claim Coverage Matrix can show which patents and claims are actively protecting the intellectual property related to itraconazole and where opportunities or gaps exist[3].
Impact on the Pharmaceutical Industry
Development of Itraconazole
The patent played a crucial role in the development of itraconazole, which is marketed under the brand name SPORANOX. Itraconazole is a broad-spectrum antifungal agent used to treat various fungal infections. The patent's claims and scope ensured that Janssen maintained exclusive rights to this drug, allowing for significant market dominance[1].
Generic Competition
The expiration of the patent and subsequent attempts by generic manufacturers to enter the market have been a subject of litigation. The case against Eon Labs highlights the challenges generic manufacturers face when trying to bypass the original patent holder's rights. This competition is critical in the pharmaceutical industry, as it affects drug prices and availability[1].
Key Takeaways
- Patent Scope: U.S. 4,267,179 covers heterocyclic derivatives of (4-phenylpiperazin-1-yl)alkylamines, including their synthesis and therapeutic use.
- Regulatory Extensions: The patent term can be extended due to FDA approval delays, which is common in pharmaceutical patents.
- Litigation: The patent has been involved in significant litigation to protect its claims against generic manufacturers.
- Patent Analytics: Tools like Claim Coverage Matrix are essential for understanding the patent landscape and identifying gaps or opportunities.
- Industry Impact: The patent has been pivotal in the development and market dominance of itraconazole, a broad-spectrum antifungal agent.
FAQs
What is the primary compound covered by U.S. Patent 4,267,179?
The primary compound covered is itraconazole, a broad-spectrum antifungal agent.
How does the patent protect Janssen's intellectual property?
The patent protects Janssen's intellectual property by granting exclusive rights to the synthesis and therapeutic use of itraconazole and related compounds.
What is the significance of regulatory extensions under 35 U.S.C. § 156?
Regulatory extensions under 35 U.S.C. § 156 allow for the extension of patent terms due to delays in FDA approval, which is crucial for pharmaceutical patents.
How does patent analytics help in understanding the patent landscape?
Patent analytics tools, such as Claim Coverage Matrix, help in categorizing patents by claims and scope concepts, identifying gaps in coverage, and highlighting future design opportunities.
What was the outcome of the litigation between Janssen and Eon Labs?
The litigation resulted in a temporary restraining order preventing Eon Labs from marketing its generic version of itraconazole until the patent infringement case was resolved[1].
Sources
- Janssen Pharmaceutical NV v. Eon Labs Manufacturing, Inc. - Casetext
- Extension Under 35 U.S.C. 156(e)(1) - United States Patent and Trademark Office
- Patent Analytics - Schwegman, Lundberg & Woessner, P.A.
- US4267179A - Heterocyclic derivatives of (4-phenylpiperazin-1-yl)alkylamines - Google Patents
