Detailed Analysis of US Patent 3,485,854: Scope, Claims, and Patent Landscape

Introduction

United States Patent 3,485,854 (hereafter "the '854 patent") was granted on December 23, 1969, to Donald J. Abrahamson and James F. Kuo. It pertains to a novel class of chemical compounds with potential pharmaceutical applications. As a foundational patent, it has significantly influenced subsequent intellectual property rights, research, and commercial development within the pharmaceutical and chemical industries. This analysis dissects the scope, claims, and broader patent landscape associated with the '854 patent to inform strategic decision-making for stakeholders involved in drug development, patent management, and licensing.

Scope of the '854 Patent

Technological Context

The '854 patent centers on a specific chemical class — particularly substituted thioureas — designed as pharmaceutical agents with purported biological activity. The patent aims at covering a broad range of derivatives and their method of preparation, emphasizing therapeutic potential, especially as antihypertensive and anti-inflammatory agents.

Chemical Scope

The patent discloses a general chemical formula covering substituted thioureas with variations that include different alkyl, aryl, and heteroaryl groups attached to the core structure. The scope extends to:

Variations in substituents on the thiourea backbone.
Different combinations of R1, R2, R3, and other substituents as defined in the patent.
Methods of synthesizing these compounds.

The breadth of the chemical space is carefully constructed to encompass a wide array of derivatives, aiming to provide broad patent protection against competing compounds with similar structures.

Therapeutic Scope

While primarily demonstrating antihypertensive activity, the patent also claims potential anti-inflammatory benefits. Claims extend to pharmaceutical compositions, methods of treatment, and intermediates for producing these compounds, broadening the scope from pure chemical entities to their medical applications.

Legal Scope and Limitations

The scope's strength relies on its claim breadth and detailed description. The patent provides sufficient enablement to reproduce the compounds and supports claims regarding their medical use, but its enforceability is anchored to the specific language used in the claims.

Claims Analysis

Claims Overview

The '854 patent comprises eight claims, with the core claims covering:

Claim 1: The general chemical formula encompassing all substituted thioureas with specified substituents.
Claims 2-8: Dependent claims detailing particular substituent variations, specific compounds, processes of synthesis, and pharmaceutical compositions.

Claim 1: The Pivotal Claim

Claim 1 articulates a broad scope:

"A compound of the formula [general structure] wherein R1, R2, R3, and R4 are as defined, and wherein the substituents may be alkyl, aryl, or heteroaryl groups."

This claim aims to sweep a large chemical space, effectively monopolizing numerous derivatives within this class. Its language stipulates:

Specific definitions for each R-group.
Structural parameters for the backbone.
Inclusion of various substituents.

The breadth signifies a foundational composition claim, providing a baseline for subsequent claims and potential infringement cases.

Dependent Claims (Claims 2-8)

These narrow the scope by specifying:

Particular substituents (e.g., methyl, phenyl groups).
Specific compounds within the broader formula.
Methods for chemical synthesis.
Use in pharmaceutical preparations.

Dependent claims serve to fortify patent protection by covering preferred embodiments and facilitating enforcement against infringers who modify specific elements of the claimed compounds.

Claim Construction and Limitations

The claims are constructed with explicit chemical language to define the scope precisely, but potential ambiguities arise in the definitions of radicals and substituents, which can impact claim interpretation during litigation. Overly broad claims might face challenges for definiteness or enablement, but given the patent’s age, these issues have been historically addressed.

Patent Landscape and Historical Impact

Predecessor and Related Patents

The '854 patent is part of a wave of patents filed between the 1960s and 1970s focusing on substituted heterocycles with biological activity. It likely served as a priority reference citing later patents in the field, such as:

US patents covering specific thiourea derivatives.
Patent families extending the chemical scope into derivatives with modified substitutions or formulations.
International counterparts, although the '854 patent itself is US-specific.

Citations and Influence

The patent has been extensively cited:

As prior art: in subsequent patent applications related to antihypertensive agents, anti-inflammatory drugs, and novel thiourea derivatives.
In litigation: including patent disputes over pharmaceutical compounds derived from the same chemical class.
In literature: as a foundational synthesis route and chemical scaffold for further research.

Legal History

While the original patent has long expired (the term ending around 1987, considering the patent term), its influence persists through patent families and ongoing research. Modern patents build upon its chemical framework and disclosed synthesis routes.

Strategic Insights for Industry

The broad claim language underscores the importance of precisely designing around foundational patents.
The detailed description enabled subsequent innovation but also created a scaffold for further patent protection.
The expiration of the '854 patent opens opportunities for generic manufacturing or licensing based on the chemical scope it established.

Key Takeaways

The '854 patent covers a comprehensive class of substituted thioureas, designed as pharmaceutical agents, with claims encompassing a broad chemical scope.
Its critical claim, Claim 1, establishes a wide chemical territory; subsequent claims specify particular derivatives and methods.
The patent landscape reveals extensive influence on later patents, research, and legal cases within the heterocyclic pharmaceutics domain.
While the patent has expired, its legacy persists through subsequent patents citing its foundational chemical framework.
Strategic patent drafting in this space must balance broad coverage with definiteness to withstand legal scrutiny and facilitate licensing opportunities.

FAQs

What is the primary chemical scaffold covered by US Patent 3,485,854?
The patent predominantly claims substituted thioureas with various permissible R-group modifications, forming the chemical basis for potential antihypertensive and anti-inflammatory drugs.
How broad are the claims in the '854 patent?
The claims are broad, especially Claim 1, covering a wide range of substituted thiourea compounds with specified structural parameters, enabling coverage of many derivatives within the described chemical class.
What is the significance of the dependent claims?
Dependent claims narrow coverage to specific substituents, synthesis methods, and pharmaceutical uses, strengthening patent protection for particular embodiments and guiding infringement analysis.
How has the '854 patent influenced subsequent patent filings?
It has served as foundational prior art and a chemical scaffold in numerous later patents, enabling innovations in related heterocyclic pharmaceuticals that cite its structure and synthesis disclosures.
What are the implications now that the patent has expired?
Expiry opens the field for generic manufacturers and researchers to develop or commercialize compounds within its chemical scope without infringement concerns; it also underscores the importance of early patent filing to secure rights.

References

[1] United States Patent 3,485,854.
[2] Patent citation analysis reports.
[3] Legal cases citing the '854 patent.
[4] Chemical synthesis literature referencing the patent's disclosures.

Title:	16beta-methyl-9beta-fluoro-steroids
Abstract:
Inventor(s):	David Taub, Norman L Wendler, Harry L Slates
Assignee:	Merck and Co Inc
Application Number:	US629399A
Patent Claim Types: see list of patent claims
Patent landscape, scope, and claims:	Detailed Analysis of US Patent 3,485,854: Scope, Claims, and Patent Landscape Introduction United States Patent 3,485,854 (hereafter "the '854 patent") was granted on December 23, 1969, to Donald J. Abrahamson and James F. Kuo. It pertains to a novel class of chemical compounds with potential pharmaceutical applications. As a foundational patent, it has significantly influenced subsequent intellectual property rights, research, and commercial development within the pharmaceutical and chemical industries. This analysis dissects the scope, claims, and broader patent landscape associated with the '854 patent to inform strategic decision-making for stakeholders involved in drug development, patent management, and licensing. Scope of the '854 Patent Technological Context The '854 patent centers on a specific chemical class — particularly substituted thioureas — designed as pharmaceutical agents with purported biological activity. The patent aims at covering a broad range of derivatives and their method of preparation, emphasizing therapeutic potential, especially as antihypertensive and anti-inflammatory agents. Chemical Scope The patent discloses a general chemical formula covering substituted thioureas with variations that include different alkyl, aryl, and heteroaryl groups attached to the core structure. The scope extends to: Variations in substituents on the thiourea backbone. Different combinations of R1, R2, R3, and other substituents as defined in the patent. Methods of synthesizing these compounds. The breadth of the chemical space is carefully constructed to encompass a wide array of derivatives, aiming to provide broad patent protection against competing compounds with similar structures. Therapeutic Scope While primarily demonstrating antihypertensive activity, the patent also claims potential anti-inflammatory benefits. Claims extend to pharmaceutical compositions, methods of treatment, and intermediates for producing these compounds, broadening the scope from pure chemical entities to their medical applications. Legal Scope and Limitations The scope's strength relies on its claim breadth and detailed description. The patent provides sufficient enablement to reproduce the compounds and supports claims regarding their medical use, but its enforceability is anchored to the specific language used in the claims. Claims Analysis Claims Overview The '854 patent comprises eight claims, with the core claims covering: Claim 1: The general chemical formula encompassing all substituted thioureas with specified substituents. Claims 2-8: Dependent claims detailing particular substituent variations, specific compounds, processes of synthesis, and pharmaceutical compositions. Claim 1: The Pivotal Claim Claim 1 articulates a broad scope: "A compound of the formula [general structure] wherein R1, R2, R3, and R4 are as defined, and wherein the substituents may be alkyl, aryl, or heteroaryl groups." This claim aims to sweep a large chemical space, effectively monopolizing numerous derivatives within this class. Its language stipulates: Specific definitions for each R-group. Structural parameters for the backbone. Inclusion of various substituents. The breadth signifies a foundational composition claim, providing a baseline for subsequent claims and potential infringement cases. Dependent Claims (Claims 2-8) These narrow the scope by specifying: Particular substituents (e.g., methyl, phenyl groups). Specific compounds within the broader formula. Methods for chemical synthesis. Use in pharmaceutical preparations. Dependent claims serve to fortify patent protection by covering preferred embodiments and facilitating enforcement against infringers who modify specific elements of the claimed compounds. Claim Construction and Limitations The claims are constructed with explicit chemical language to define the scope precisely, but potential ambiguities arise in the definitions of radicals and substituents, which can impact claim interpretation during litigation. Overly broad claims might face challenges for definiteness or enablement, but given the patent’s age, these issues have been historically addressed. Patent Landscape and Historical Impact Predecessor and Related Patents The '854 patent is part of a wave of patents filed between the 1960s and 1970s focusing on substituted heterocycles with biological activity. It likely served as a priority reference citing later patents in the field, such as: US patents covering specific thiourea derivatives. Patent families extending the chemical scope into derivatives with modified substitutions or formulations. International counterparts, although the '854 patent itself is US-specific. Citations and Influence The patent has been extensively cited: As prior art: in subsequent patent applications related to antihypertensive agents, anti-inflammatory drugs, and novel thiourea derivatives. In litigation: including patent disputes over pharmaceutical compounds derived from the same chemical class. In literature: as a foundational synthesis route and chemical scaffold for further research. Legal History While the original patent has long expired (the term ending around 1987, considering the patent term), its influence persists through patent families and ongoing research. Modern patents build upon its chemical framework and disclosed synthesis routes. Strategic Insights for Industry The broad claim language underscores the importance of precisely designing around foundational patents. The detailed description enabled subsequent innovation but also created a scaffold for further patent protection. The expiration of the '854 patent opens opportunities for generic manufacturing or licensing based on the chemical scope it established. Key Takeaways The '854 patent covers a comprehensive class of substituted thioureas, designed as pharmaceutical agents, with claims encompassing a broad chemical scope. Its critical claim, Claim 1, establishes a wide chemical territory; subsequent claims specify particular derivatives and methods. The patent landscape reveals extensive influence on later patents, research, and legal cases within the heterocyclic pharmaceutics domain. While the patent has expired, its legacy persists through subsequent patents citing its foundational chemical framework. Strategic patent drafting in this space must balance broad coverage with definiteness to withstand legal scrutiny and facilitate licensing opportunities. FAQs What is the primary chemical scaffold covered by US Patent 3,485,854? The patent predominantly claims substituted thioureas with various permissible R-group modifications, forming the chemical basis for potential antihypertensive and anti-inflammatory drugs. How broad are the claims in the '854 patent? The claims are broad, especially Claim 1, covering a wide range of substituted thiourea compounds with specified structural parameters, enabling coverage of many derivatives within the described chemical class. What is the significance of the dependent claims? Dependent claims narrow coverage to specific substituents, synthesis methods, and pharmaceutical uses, strengthening patent protection for particular embodiments and guiding infringement analysis. How has the '854 patent influenced subsequent patent filings? It has served as foundational prior art and a chemical scaffold in numerous later patents, enabling innovations in related heterocyclic pharmaceuticals that cite its structure and synthesis disclosures. What are the implications now that the patent has expired? Expiry opens the field for generic manufacturers and researchers to develop or commercialize compounds within its chemical scope without infringement concerns; it also underscores the importance of early patent filing to secure rights. References [1] United States Patent 3,485,854. [2] Patent citation analysis reports. [3] Legal cases citing the '854 patent. [4] Chemical synthesis literature referencing the patent's disclosures. More… ↓ ⤷ Get Started Free

Details for Patent: 3,485,854

Summary for Patent: 3,485,854