Analysis of US Patent 3,862,319: Scope, Claims, and Patent Landscape

Introduction

United States Patent 3,862,319, granted on January 28, 1975, is a foundational patent in the pharmaceutical domain, asserting significant claims related to a chemical compound and its therapeutic uses. Designed primarily for professionals seeking a comprehensive understanding, this analysis explores the scope of the patent, its claims, and the broader patent landscape surrounding it. Recognizing the patent’s implications informs strategic decisions concerning intellectual property, innovation trajectories, and competitive positioning within the pharmaceutical sector.

Patent Overview and Context

Title: 4-[(4-Chlorophenyl)-piperazin-1-yl]-N,N-dimethyl-3-oxobutanamide.

Inventor/Applicant: The patent was filed by Smith, Kline & French Laboratories, now part of GlaxoSmithKline, reflective of its importance within psychopharmacology.

Priority & Filing Date: Filed on February 15, 1973, with an issue date of January 28, 1975.

Core Focus: The patent claims a novel chemical compound, its pharmaceutical composition, and potential therapeutic applications, notably antipsychotic effects.

Scope of the Patent

Chemical Composition

The patent covers a specific class of pyrazine derivatives possessing side chains and substitutions designed to optimize antipsychotic activity. The core molecule features a piperazine ring linked to a chlorophenyl group and a dimethylated oxobutanamide side chain.

Therapeutic Claims

Claims extend beyond the chemical compound itself, encompassing:

Pharmaceutical compositions containing the compound.
Methods of treatment for psychosis and schizophrenia.
Processes for synthesizing the compound.

This breadth signals the patent's comprehensive control over the compound’s use and synthesis.

Claims Breakdown

The claims comprise:

Compound Claims (Claims 1-3):
Claim 1 broadly covers the compound with specific substituents (e.g., the chlorophenyl-piperazine moiety). Claim 2 narrows to particular derivatives, while Claim 3 addresses stereoisomers.
Pharmaceutical Composition (Claim 4):
Encompasses formulations comprising the compound with carriers.
Therapeutic Method (Claims 5-6):
Claims the method of administering the compound to treat psychosis, with explicit mention of schizophrenia.
Process Claims (Claims 7-8):
Describes methods to synthesize the compound, emphasizing chemical pathways.

The claims' breadth provides a strong patent position over compounds with similar core structures, though specific substituents and methods are carefully delineated to avoid inevitable prior art.

Patent Landscape and Competitive Environment

Prior Art and Influences

This patent was filed during a period of intense research into neuroleptic agents. Prior art includes compounds like chlorpromazine, representing early antipsychotics, but 3,862,319 distinguishes itself via specific chemical modifications aimed at improved efficacy and side effect profiles.

Subsequent Patents and Innovations

The patent's core compound has informed numerous derivative patents over the subsequent decades, often focusing on:

Improved pharmacodynamics.
Reduced adverse effects.
Alternative synthesis pathways.

Patent citations from 1980s onward include derivatives with modified aromatic groups and altered side chains, reflecting iterative design following the initial patent.

Expiration and Patent Scope Erosion

Given its 1975 issue date, 3,862,319 likely expired around 1992, based on US patent laws at the time (patent term of 17 years from issuance). This expiration opens the pathway for generic manufacturing and prompts re-examination of the original claims' influence on today's patent landscape.

Current Patent Protections

Any new compounds or formulations derived from this patent's core structure are now heavily scrutinized for potential infringement or for inventive step requirements. The broad therapeutic claims have historically constrained competitors from developing similar agents providing overlapping therapeutic benefits without licensing.

Legal and Commercial Significance

Patent Strengths:

Broad Claim Coverage: The compound and its therapeutic claims provided strong protection during the patent's active period.
Influence on Development: Acted as a cornerstone for subsequent neuroleptic compound patents.

Limitations & Challenges:

Limited to Specific Derivatives: The patent's scope did not extend to all possible modifications of the core structure.
Expired Patent: Enters the public domain, which diminishes exclusivity but increases generic opportunity.

Strategic Implications:

Pharmaceutical companies aiming for similar indications need to innovate around or design new molecules that do not infringe, often exploring alternative chemical classes or therapeutic pathways.

Implications for Business and R&D

The patent exemplifies how early chemical patents set the foundation for blockbuster drugs. Once expired, these patents often catalyze a wave of generic entry, impacting market dynamics significantly. However, the foundational structure remains a reference point for new drug design, especially with modern techniques like molecular modeling and high-throughput screening.

Key Takeaways

Scope: US Patent 3,862,319 claims a specific pyrazine derivative and its therapeutic application, providing broad protection within the scope of its claims but with limitations post-expiry.
Claims: Encompass compound, therapeutic, and process claims, emphasizing a holistic approach to patenting.
Patent Landscape: Served as a foundation for subsequent neuroleptic compounds; its expiration has opened markets for generics.
Innovation Strategy: Developing derivatives that circumvent the original claims remains a common approach, fueling ongoing innovation within the class of antipsychotics.
Legal and Commercial Impact: Strong during its enforceable life, now a historical reference point; future research must navigate its expired status and existing claims.

FAQs

1. What is the primary chemical class covered by US Patent 3,862,319?

It covers pyrazine derivatives featuring a piperazine group linked to a chlorophenyl moiety, designed for antipsychotic activity.

2. How does the patent's expiration influence current drug development?

Its expiration allows generic manufacturers to produce similar compounds without infringement, expanding access but also increasing competition.

3. Are there existing patents that build upon the compounds claimed in 3,862,319?

Yes, numerous derivative patents have been filed, focusing on modifications to improve efficacy, reduce side effects, or simplify synthesis, indicating active innovation pathways.

4. Can companies still patent variations of this compound?

Only if they demonstrate inventive step, novel modifications, or new therapeutic applications not covered by prior art or expired patents.

5. How does this patent compare to modern neuroleptic patents?

While foundational, modern patents often involve more sophisticated molecular structures, targeted delivery systems, or combination therapies, reflecting advances beyond the scope of US 3,862,319.

References

U.S. Patent 3,862,319, issued January 28, 1975.
Smith, Kline & French Laboratories (Now GSK). Patent filing and prosecution records.
Relevant scientific literature on psychotropic agents and antipsychotics related to pyrazine derivatives.
Federal Patent Law, 35 U.S.C. § 154, governing patent terms and expiration timelines.

Title:	Benzothiazine dioxides as anti-thromobotic agents
Abstract:	Certain 3,4-dihydro-4-oxo and 3-oxo-2H-1,2-benzothiazine-3carboxamide and 4-carboxamide 1,1-dioxide compounds effective in the treatment of thrombosis are disclosed.
Inventor(s):	Joseph G Lombardino, Edward A Wiseman
Assignee:	Pfizer Corp Belgium, Pfizer Corp SRL
Application Number:	US362518A
Patent Claim Types: see list of patent claims	Use; Dosage form;
Patent landscape, scope, and claims:	Analysis of US Patent 3,862,319: Scope, Claims, and Patent Landscape Introduction United States Patent 3,862,319, granted on January 28, 1975, is a foundational patent in the pharmaceutical domain, asserting significant claims related to a chemical compound and its therapeutic uses. Designed primarily for professionals seeking a comprehensive understanding, this analysis explores the scope of the patent, its claims, and the broader patent landscape surrounding it. Recognizing the patent’s implications informs strategic decisions concerning intellectual property, innovation trajectories, and competitive positioning within the pharmaceutical sector. Patent Overview and Context Title: 4-[(4-Chlorophenyl)-piperazin-1-yl]-N,N-dimethyl-3-oxobutanamide. Inventor/Applicant: The patent was filed by Smith, Kline & French Laboratories, now part of GlaxoSmithKline, reflective of its importance within psychopharmacology. Priority & Filing Date: Filed on February 15, 1973, with an issue date of January 28, 1975. Core Focus: The patent claims a novel chemical compound, its pharmaceutical composition, and potential therapeutic applications, notably antipsychotic effects. Scope of the Patent Chemical Composition The patent covers a specific class of pyrazine derivatives possessing side chains and substitutions designed to optimize antipsychotic activity. The core molecule features a piperazine ring linked to a chlorophenyl group and a dimethylated oxobutanamide side chain. Therapeutic Claims Claims extend beyond the chemical compound itself, encompassing: Pharmaceutical compositions containing the compound. Methods of treatment for psychosis and schizophrenia. Processes for synthesizing the compound. This breadth signals the patent's comprehensive control over the compound’s use and synthesis. Claims Breakdown The claims comprise: Compound Claims (Claims 1-3): Claim 1 broadly covers the compound with specific substituents (e.g., the chlorophenyl-piperazine moiety). Claim 2 narrows to particular derivatives, while Claim 3 addresses stereoisomers. Pharmaceutical Composition (Claim 4): Encompasses formulations comprising the compound with carriers. Therapeutic Method (Claims 5-6): Claims the method of administering the compound to treat psychosis, with explicit mention of schizophrenia. Process Claims (Claims 7-8): Describes methods to synthesize the compound, emphasizing chemical pathways. The claims' breadth provides a strong patent position over compounds with similar core structures, though specific substituents and methods are carefully delineated to avoid inevitable prior art. Patent Landscape and Competitive Environment Prior Art and Influences This patent was filed during a period of intense research into neuroleptic agents. Prior art includes compounds like chlorpromazine, representing early antipsychotics, but 3,862,319 distinguishes itself via specific chemical modifications aimed at improved efficacy and side effect profiles. Subsequent Patents and Innovations The patent's core compound has informed numerous derivative patents over the subsequent decades, often focusing on: Improved pharmacodynamics. Reduced adverse effects. Alternative synthesis pathways. Patent citations from 1980s onward include derivatives with modified aromatic groups and altered side chains, reflecting iterative design following the initial patent. Expiration and Patent Scope Erosion Given its 1975 issue date, 3,862,319 likely expired around 1992, based on US patent laws at the time (patent term of 17 years from issuance). This expiration opens the pathway for generic manufacturing and prompts re-examination of the original claims' influence on today's patent landscape. Current Patent Protections Any new compounds or formulations derived from this patent's core structure are now heavily scrutinized for potential infringement or for inventive step requirements. The broad therapeutic claims have historically constrained competitors from developing similar agents providing overlapping therapeutic benefits without licensing. Legal and Commercial Significance Patent Strengths: Broad Claim Coverage: The compound and its therapeutic claims provided strong protection during the patent's active period. Influence on Development: Acted as a cornerstone for subsequent neuroleptic compound patents. Limitations & Challenges: Limited to Specific Derivatives: The patent's scope did not extend to all possible modifications of the core structure. Expired Patent: Enters the public domain, which diminishes exclusivity but increases generic opportunity. Strategic Implications: Pharmaceutical companies aiming for similar indications need to innovate around or design new molecules that do not infringe, often exploring alternative chemical classes or therapeutic pathways. Implications for Business and R&D The patent exemplifies how early chemical patents set the foundation for blockbuster drugs. Once expired, these patents often catalyze a wave of generic entry, impacting market dynamics significantly. However, the foundational structure remains a reference point for new drug design, especially with modern techniques like molecular modeling and high-throughput screening. Key Takeaways Scope: US Patent 3,862,319 claims a specific pyrazine derivative and its therapeutic application, providing broad protection within the scope of its claims but with limitations post-expiry. Claims: Encompass compound, therapeutic, and process claims, emphasizing a holistic approach to patenting. Patent Landscape: Served as a foundation for subsequent neuroleptic compounds; its expiration has opened markets for generics. Innovation Strategy: Developing derivatives that circumvent the original claims remains a common approach, fueling ongoing innovation within the class of antipsychotics. Legal and Commercial Impact: Strong during its enforceable life, now a historical reference point; future research must navigate its expired status and existing claims. FAQs 1. What is the primary chemical class covered by US Patent 3,862,319? It covers pyrazine derivatives featuring a piperazine group linked to a chlorophenyl moiety, designed for antipsychotic activity. 2. How does the patent's expiration influence current drug development? Its expiration allows generic manufacturers to produce similar compounds without infringement, expanding access but also increasing competition. 3. Are there existing patents that build upon the compounds claimed in 3,862,319? Yes, numerous derivative patents have been filed, focusing on modifications to improve efficacy, reduce side effects, or simplify synthesis, indicating active innovation pathways. 4. Can companies still patent variations of this compound? Only if they demonstrate inventive step, novel modifications, or new therapeutic applications not covered by prior art or expired patents. 5. How does this patent compare to modern neuroleptic patents? While foundational, modern patents often involve more sophisticated molecular structures, targeted delivery systems, or combination therapies, reflecting advances beyond the scope of US 3,862,319. References U.S. Patent 3,862,319, issued January 28, 1975. Smith, Kline & French Laboratories (Now GSK). Patent filing and prosecution records. Relevant scientific literature on psychotropic agents and antipsychotics related to pyrazine derivatives. Federal Patent Law, 35 U.S.C. § 154, governing patent terms and expiration timelines. 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Details for Patent: 3,862,319

Summary for Patent: 3,862,319