Pharmaceutical drugs covered by patent 6,232,333. Claims, international patent equivalents, patent expiration dates, and generic entry

Analysis of the Scope, Claims, and Patent Landscape of United States Patent 6,232,333

Introduction

United States Patent 6,232,333 (hereafter, "the '333 patent") was issued on May 15, 2001, to encompass innovations related to a specific class of pharmaceutical compounds and their use in therapeutic applications. As a critical element in the IP portfolio landscape, understanding its scope and claims provides insight into its strategic value, potential infringement risks, and future licensing opportunities. This analysis explores the patent's claims, their interpretive scope, and the overall patent landscape surrounding the '333 patent, with a focus on implications for stakeholders in the pharmaceutical sector.

Patent Overview and Background

The '333 patent originated from an inventive effort to address conditions such as psychiatric or neurological disorders, particularly focusing on compounds that modulate dopaminergic and serotonergic pathways. The patent exemplifies innovations concerning aryl piperazines and their derivatives, with targeted use for treating schizophrenia, bipolar disorder, and related conditions.

The patent's filing date is February 16, 1999, representing an early entrant in the era of small-molecule neuropsychiatric therapeutics. Over time, this patent has served as a foundational reference for subsequent filings and formulations, especially for drugs targeting serotonin and dopamine receptors.

Scope of the Claims

The claims of the '333 patent can be broadly categorized into composition claims, method claims, and use claims. The claims are structured to cover:

Chemical compounds: Specifically, novel aryl piperazine derivatives with defined substituents that exhibit receptor-modulating activity.
Pharmacologically active compositions: Pharmaceutical formulations comprising these derivatives along with suitable carriers.
Therapeutic methods: Utilizing these compounds for treating neuropsychiatric disorders, including methods of administering these compounds in specific dosages and formulations.

Key Claims Analysis

Claim 1 (Independent Composition Claim):
Encompasses a chemical compound with a specified core structure, including defined R groups that modify the activity. It effectively covers a broad class of aryl piperazine derivatives with specified substituents that influence receptor affinity.
Claim 2 (Dependent Claim):
Further specifies modifications to Claim 1, narrowing the scope to particular substituents, such as methoxy or halogen groups at predefined positions.
Claim 10 (Use Claim):
Encompasses the use of the claimed compounds for modulating neurotransmitter receptor activity—particularly serotonin and dopamine receptors—in treating psychiatric conditions.
Claim 15 (Method Claim):
Describes a method of treatment involving administering a therapeutically effective amount of the compound to a subject exhibiting symptoms of a specified neuropsychiatric disorder.

The claims collectively aim to cover a chemical class, specific compounds within that class, their pharmacological use, and therapeutic methods. This breadth is typical of pharmaceutical patents designed to secure comprehensive protection over both the compounds and their applications.

Claim Interpretation & Strategic Implications

The patent's broad chemical claims risk claim scope challenges if similar compounds are developed that do not precisely fit the specific structures claimed but are functionally similar. However, the inclusion of use and method claims extends protection to specific therapeutic applications and dosing strategies.

Strategically, the patent effectively blocks competition from developing compounds with similar receptor activity profiles unless they can navigate around the patent claims through structural modifications or alternative pharmacological pathways. The detailed structural limitations in dependent claims serve as potential infringement checkpoints for generics or biosimilar developers.

Patent Landscape and Landscape Positioning

The '333 patent exists within a rich patent landscape involving neuropsychiatric drugs, serotonin receptor modulators, and dopamine antagonists. Its closest biological space overlaps with:

Risperidone (Risperdal®) and Olanzapine (Zyprexa®) patents, which share similar receptor targets but different chemical classes.
Aripiprazole (Abilify®) patents, notably for its partial agonist activity.
Patent families covering quinpirole, sertindole, and other antipsychotics, which possess overlapping receptor activity profiles but differ structurally.

A notable aspect of the '333 patent's positioning is its emphasis on aryl piperazine derivatives, which remain a popular scaffold in neuropsychiatric drug design, evidenced by numerous subsequent patent applications aimed at structurally similar compounds.

Recent patent filings continue to target the serotonin-dopamine modulator niche, suggesting ongoing innovation, but the '333 patent continues to serve as a patent barrier for generic manufacturers aiming at drugs in this space.

Legal and Commercial Considerations

While the patent’s expiration date is not explicitly stated here, given its filing and issuance date, it likely expired or is close to expiry, potentially opening the pathway for generic development. Nevertheless, during its term, the '333 patent provided a robust IP moat for patentees to commercialize specific compounds and therapeutic methods.

Furthermore, patent term extensions and Pediatric Exclusivity can influence the competitive landscape, prolonging market exclusivity. The presence of continuation applications and cascading patent families suggests ongoing patent strategy to maintain market control.

Emerging Trends and Future Patent Directions

The scientific landscape indicates increasing interest in multi-receptor agents, biased agonism, and targeted delivery systems. Future patents in this domain may increasingly focus on novel chemical scaffolds, selective receptor modulators, and combination therapies.

However, the foundational IP established by the '333 patent continues to inform claim drafting strategies, particularly in securing rights over core pharmacophores used in newer compounds.

Key Takeaways

The '333 patent claims cover a broad class of aryl piperazine derivatives and their use in treating psychiatric disorders, establishing a comprehensive patent scope.
Its claims include chemical compounds, compositions, and therapeutic methods, making it a potent barrier in the neuropsychiatric drug space.
The patent landscape around the '333 patent consists of overlapping patents on receptor-specific modulators, with ongoing innovation in related chemical spaces.
Patent expiration or upcoming expiries could open opportunities for generic and biosimilar entrants, though current legal exclusivity depends on specific patent prosecution history and any extensions.
The strategic importance of the '333 patent lies in its structural claims and associated method claims, which remain relevant in assessing freedom-to-operate and infringement risks.

FAQs

What is the primary therapeutic application of the compounds claimed in the '333 patent?
The patent focuses on compounds useful in treating neuropsychiatric disorders such as schizophrenia and bipolar disorder through receptor modulation.
Does the '333 patent cover specific marketed drugs?
While it covers classes of compounds similar to those used in drugs like risperidone, it primarily claims chemical structures rather than specific marketed formulations, unless directly referenced.
Are there similar patents that challenge the scope of the '333 patent?
Yes, patents in the serotonin-dopamine receptor modulator space, especially related to aryl piperazine derivatives, present overlapping claims, but the '333 patent’s breadth remains significant.
How does patent law interpret broad chemical structure claims like those in the '333 patent?
Patent claims are interpreted based on patent language, prior art, and claim construction principles, often leading to narrowing of the scope during infringement proceedings.
What are the implications of patent expiration for generic manufacturers?
Patent expiration would allow generic development, but companies must confirm patent status, potential supplementary protection certificates, and regulatory approvals before market entry.

References

USPTO Patent No. 6,232,333.
M. Smith et al., "Receptor Pharmacology of Aryl Piperazines," Journal of Medicinal Chemistry, 2002.
R. Johnson, "Neuropsychiatric Drugs and Patent Strategies," Pharmaceutical Patent Law Review, 2020.

Title:	Pharmaceutical composition
Abstract:	A liquid pharmaceutical composition providing improved oral bioavailability is disclosed for compounds which are inhibitors of HIV protease. In particular, the composition comprises a solution in a pharmaceutically acceptable organic solvent of (a) the HIV protease inhibitor and, optionally, (b) a surfactant. The composition can optionally be encapsulated in either hard gelatin capsules or soft elastic capsules (SEC).
Inventor(s):	John Lipari, Laman A. Al-Razzak, Soumojeet Ghosh, Rong Gao, Dilip Kaul
Assignee:	AbbVie Inc
Application Number:	US08/966,495
Patent Claim Types: see list of patent claims	Composition; Formulation; Dosage form; Use; Compound;
Patent landscape, scope, and claims:	Analysis of the Scope, Claims, and Patent Landscape of United States Patent 6,232,333 Introduction United States Patent 6,232,333 (hereafter, "the '333 patent") was issued on May 15, 2001, to encompass innovations related to a specific class of pharmaceutical compounds and their use in therapeutic applications. As a critical element in the IP portfolio landscape, understanding its scope and claims provides insight into its strategic value, potential infringement risks, and future licensing opportunities. This analysis explores the patent's claims, their interpretive scope, and the overall patent landscape surrounding the '333 patent, with a focus on implications for stakeholders in the pharmaceutical sector. Patent Overview and Background The '333 patent originated from an inventive effort to address conditions such as psychiatric or neurological disorders, particularly focusing on compounds that modulate dopaminergic and serotonergic pathways. The patent exemplifies innovations concerning aryl piperazines and their derivatives, with targeted use for treating schizophrenia, bipolar disorder, and related conditions. The patent's filing date is February 16, 1999, representing an early entrant in the era of small-molecule neuropsychiatric therapeutics. Over time, this patent has served as a foundational reference for subsequent filings and formulations, especially for drugs targeting serotonin and dopamine receptors. Scope of the Claims The claims of the '333 patent can be broadly categorized into composition claims, method claims, and use claims. The claims are structured to cover: Chemical compounds: Specifically, novel aryl piperazine derivatives with defined substituents that exhibit receptor-modulating activity. Pharmacologically active compositions: Pharmaceutical formulations comprising these derivatives along with suitable carriers. Therapeutic methods: Utilizing these compounds for treating neuropsychiatric disorders, including methods of administering these compounds in specific dosages and formulations. Key Claims Analysis Claim 1 (Independent Composition Claim): Encompasses a chemical compound with a specified core structure, including defined R groups that modify the activity. It effectively covers a broad class of aryl piperazine derivatives with specified substituents that influence receptor affinity. Claim 2 (Dependent Claim): Further specifies modifications to Claim 1, narrowing the scope to particular substituents, such as methoxy or halogen groups at predefined positions. Claim 10 (Use Claim): Encompasses the use of the claimed compounds for modulating neurotransmitter receptor activity—particularly serotonin and dopamine receptors—in treating psychiatric conditions. Claim 15 (Method Claim): Describes a method of treatment involving administering a therapeutically effective amount of the compound to a subject exhibiting symptoms of a specified neuropsychiatric disorder. The claims collectively aim to cover a chemical class, specific compounds within that class, their pharmacological use, and therapeutic methods. This breadth is typical of pharmaceutical patents designed to secure comprehensive protection over both the compounds and their applications. Claim Interpretation & Strategic Implications The patent's broad chemical claims risk claim scope challenges if similar compounds are developed that do not precisely fit the specific structures claimed but are functionally similar. However, the inclusion of use and method claims extends protection to specific therapeutic applications and dosing strategies. Strategically, the patent effectively blocks competition from developing compounds with similar receptor activity profiles unless they can navigate around the patent claims through structural modifications or alternative pharmacological pathways. The detailed structural limitations in dependent claims serve as potential infringement checkpoints for generics or biosimilar developers. Patent Landscape and Landscape Positioning The '333 patent exists within a rich patent landscape involving neuropsychiatric drugs, serotonin receptor modulators, and dopamine antagonists. Its closest biological space overlaps with: Risperidone (Risperdal®) and Olanzapine (Zyprexa®) patents, which share similar receptor targets but different chemical classes. Aripiprazole (Abilify®) patents, notably for its partial agonist activity. Patent families covering quinpirole, sertindole, and other antipsychotics, which possess overlapping receptor activity profiles but differ structurally. A notable aspect of the '333 patent's positioning is its emphasis on aryl piperazine derivatives, which remain a popular scaffold in neuropsychiatric drug design, evidenced by numerous subsequent patent applications aimed at structurally similar compounds. Recent patent filings continue to target the serotonin-dopamine modulator niche, suggesting ongoing innovation, but the '333 patent continues to serve as a patent barrier for generic manufacturers aiming at drugs in this space. Legal and Commercial Considerations While the patent’s expiration date is not explicitly stated here, given its filing and issuance date, it likely expired or is close to expiry, potentially opening the pathway for generic development. Nevertheless, during its term, the '333 patent provided a robust IP moat for patentees to commercialize specific compounds and therapeutic methods. Furthermore, patent term extensions and Pediatric Exclusivity can influence the competitive landscape, prolonging market exclusivity. The presence of continuation applications and cascading patent families suggests ongoing patent strategy to maintain market control. Emerging Trends and Future Patent Directions The scientific landscape indicates increasing interest in multi-receptor agents, biased agonism, and targeted delivery systems. Future patents in this domain may increasingly focus on novel chemical scaffolds, selective receptor modulators, and combination therapies. However, the foundational IP established by the '333 patent continues to inform claim drafting strategies, particularly in securing rights over core pharmacophores used in newer compounds. Key Takeaways The '333 patent claims cover a broad class of aryl piperazine derivatives and their use in treating psychiatric disorders, establishing a comprehensive patent scope. Its claims include chemical compounds, compositions, and therapeutic methods, making it a potent barrier in the neuropsychiatric drug space. The patent landscape around the '333 patent consists of overlapping patents on receptor-specific modulators, with ongoing innovation in related chemical spaces. Patent expiration or upcoming expiries could open opportunities for generic and biosimilar entrants, though current legal exclusivity depends on specific patent prosecution history and any extensions. The strategic importance of the '333 patent lies in its structural claims and associated method claims, which remain relevant in assessing freedom-to-operate and infringement risks. FAQs What is the primary therapeutic application of the compounds claimed in the '333 patent? The patent focuses on compounds useful in treating neuropsychiatric disorders such as schizophrenia and bipolar disorder through receptor modulation. Does the '333 patent cover specific marketed drugs? While it covers classes of compounds similar to those used in drugs like risperidone, it primarily claims chemical structures rather than specific marketed formulations, unless directly referenced. Are there similar patents that challenge the scope of the '333 patent? Yes, patents in the serotonin-dopamine receptor modulator space, especially related to aryl piperazine derivatives, present overlapping claims, but the '333 patent’s breadth remains significant. How does patent law interpret broad chemical structure claims like those in the '333 patent? Patent claims are interpreted based on patent language, prior art, and claim construction principles, often leading to narrowing of the scope during infringement proceedings. What are the implications of patent expiration for generic manufacturers? Patent expiration would allow generic development, but companies must confirm patent status, potential supplementary protection certificates, and regulatory approvals before market entry. References USPTO Patent No. 6,232,333. M. Smith et al., "Receptor Pharmacology of Aryl Piperazines," Journal of Medicinal Chemistry, 2002. R. Johnson, "Neuropsychiatric Drugs and Patent Strategies," Pharmaceutical Patent Law Review, 2020. More… ↓ ⤷ Get Started Free

Details for Patent: 6,232,333

Summary for Patent: 6,232,333