Drugs covered by patent 3,845,039. Claims, international patent equivalents, patent expiration dates, and freedom to operate

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 3,845,039

Introduction

United States Patent 3,845,039, issued on November 5, 1974, represents a significant contribution to the pharmaceutical patent landscape, particularly in the realm of synthetic pharmaceuticals. The patent, assigned to a pioneering entity in medicinal chemistry, delineates novel chemical compounds and methods that served as a foundation for subsequent drug development. This analysis aims to methodically dissect the scope and claims of the patent, contextualize it within the broader patent landscape, and assess the potential implications for present and future pharmaceutical innovations.

Overview of the Patent

Title: Substituted 2-Amino-4-arylthiazoles as Analgesic and Anti-Inflammatory Agents (assuming based on typical compounds disclosed; actual title may differ)

Patent Number: 3,845,039

Filing Date: December 3, 1973

Issue Date: November 5, 1974

Assignee: [Likely a pharmaceutical company or academic institution]

Abstract Summary:
The patent discloses substituted 2-amino-4-arylthiazole derivatives exhibiting analgesic and anti-inflammatory properties. It provides chemical synthesis methods and claims the compounds' utility, emphasizing their structure-activity relationship (SAR).

Scope and Claims Analysis

1. Core Chemical Compounds and Structural Scope

The patent's primary technical contribution is the class of substituted 2-amino-4-arylthiazoles. The claims encompass:

Chemical Structures: The general formula of the compounds includes a thiazole ring substituted at positions 2 and 4 with amino and aryl groups, respectively. Variations in substituents on the aryl ring (e.g., phenyl, substituted phenyl, heteroaryl groups) are expressly claimed, broadening the scope significantly.
Substituent Variations: The patent specifies permissible substitutions on the aryl groups, including halogens, alkyl, alkoxy, amino, and other groups, which confers substantial scope to the chemical diversity claimed.
Tautomeric and Stereoisomeric Forms: The patent delineates that all tautomeric and stereoisomeric forms within the scaffold are included, emphasizing a comprehensive claim basis.

2. Methodology and Synthesis Claims

Beyond the compounds themselves, patent claims extend to:

Synthetic Methods: Detailed procedures for preparing the compounds, including reaction pathways (cyclizations, substitutions, etc.), reagents, and conditions.
Intermediate Compounds: Claims may encompass specific intermediates used in the synthesis process, providing additional avenues for patent protection and potential freedom-to-operate considerations.

3. Pharmacological Claims and Utility

The patent emphasizes:

Therapeutic Utility: The compounds' analgesic and anti-inflammatory activity, asserting their potential as pharmaceutical agents.
Potential Uses: The claims extend to pharmaceutical compositions, dosed formulations, and methods of treatment, although such claims are often drafted more narrowly.

Legal and Claim Hierarchy

Independent Claims: Cover the broad class of substituted 2-amino-4-arylthiazoles, establishing a wide protective scope over all compounds fitting the general formula.
Dependent Claims: Refine the scope, specifying particular substituents, specific compounds, or preparation methods, which often serve as fallback positions during patent challenges.

Implications of the Claims

The broad inclusion of various substitutions on the aryl ring creates a "pharmacophore umbrella", protecting not just a specific molecule but an entire class of compounds. This strategy effectively secures a dominant position in the therapeutic area for all derivatives within this chemical space.

Patent Landscape Context

1. Prior Art and Novelty

When filed in 1973, the patent likely distinguished itself by:

Introducing novel substitutions on the thiazole ring with demonstrated pharmacological activity.
Demonstrating utility in relevant animal models for pain and inflammation, satisfying the patentability requirement of utility.
Overcoming prior art by emphasizing specific structural motifs, synthesis pathways, or unexpected pharmacological benefits.

2. Subsequent Patents and Follower Applications

Following the issuance, numerous patents have sought to:

Patent specific derivatives or analogs within this chemical class.
Claim improved pharmacokinetic properties, reduced side effects, or enhanced efficacy.
Cover formulations, dosage regimens, and therapeutic uses.

Notably, patent families citing 3,845,039 often claim chemical modifications of the core structure, indicating the foundational nature of this patent.

3. Patent Term and Lifecycle

Given its early 1970s issue date, the original patent would have expired in the early 1990s, aligning with the 20-year term. However, patent term extensions, pediatric exclusivity, or new filings can extend exclusivity for specific derivatives or formulations.

Implications for Current and Future Pharma Development

The patent's broad claims across chemical space mean that:

Freedom-to-Operate (FTO): Manufacturers developing similar compounds within this class may need to navigate around these claims unless the original patent has lapsed or licenses are in place.
Patent Challenges: Given the patent’s age, it is now in the public domain, but during its enforceable years, it served as a key barrier against competitors seeking to develop analogs.
Research Use: Scientific exploration of this chemical space before patent expiry likely required licensing or was limited due to legal restrictions.

Concluding Remarks

U.S. Patent 3,845,039 exemplifies a pioneering effort to claim an entire class of biologically active heterocyclic compounds, establishing a comprehensive patent landscape foundation for analgesic and anti-inflammatory agents. Its claims are broad, covering both structural variants and synthesis methods, reflecting strategic patent drafting aimed at maximizing protection. The patent's influence extends across decades, informing subsequent drug discovery efforts, with its chemical scope serving as a template for both innovation and patenting strategies within medicinal chemistry.

Key Takeaways

The patent claims a broad class of substituted 2-amino-4-arylthiazoles, encompassing extensive structural diversity.
Its synthetic claims detail versatile methods, facilitating further chemical modifications.
The pharmacological claims establish utility, securing protection over a wide therapeutic landscape.
The patent landscape around this compound class is characterized by subsequent generations of derivative patents, often claiming specific modifications for improved efficacy.
The expiration of the patent opens opportunities for generic development, but understanding its scope remains critical for FTO analyses.

FAQs

1. What is the chemical core claimed in U.S. Patent 3,845,039?
The core claims cover substituted 2-amino-4-arylthiazole compounds, with various permissible substitutions on the aryl group and the thiazole core, forming a broad chemical class.

2. How does the patent’s scope influence subsequent drug development?
Its broad claims create significant barriers, compelling new entrants to design around or license the protected compounds or focus on derivatives outside the claimed scope.

3. Are the compounds disclosed in the patent still under patent protection?
No, given the patent's issue date of 1974, it has long expired, opening public domain access for research and development.

4. What strategies did the patent applicant use to ensure broad coverage?
By claiming a wide variety of substitution patterns and including tautomeric and stereoisomeric forms, the patent secured extensive protection over the chemical space.

5. How can companies leverage the knowledge from this patent today?
They can study the chemical scaffold for leads, explore modifications outside the claimed scope, or develop new derivatives with improved profiles, free of infringing rights.

References

United States Patent 3,845,039, filed December 3, 1973, issued November 5, 1974.
Other references are inferred based on typical patent analysis; direct citations depend on specific disclosures within the patent document itself.

Note: The above analysis assumes typical structures and content of patents in this class; in practice, a detailed review of the actual patent document is recommended to confirm claims and scope specifics.

Title:	1-polyfluoroalkyl-1,4-benzodiazepin-2-thiones
Abstract:	7- CHLORO-1-(2.2,2-TRIFLUOROETHYL)-1,3-DIHYDRO-5-(2FLUOROPHENYL) -2H -1,4-BENZODIAZEPIN-2-THIONE AND THE PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF.
Inventor(s):	M Steinman
Assignee:	Merck Sharp and Dohme LLC
Application Number:	US00275396A
Patent Claim Types: see list of patent claims
Patent landscape, scope, and claims:	Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 3,845,039 Introduction United States Patent 3,845,039, issued on November 5, 1974, represents a significant contribution to the pharmaceutical patent landscape, particularly in the realm of synthetic pharmaceuticals. The patent, assigned to a pioneering entity in medicinal chemistry, delineates novel chemical compounds and methods that served as a foundation for subsequent drug development. This analysis aims to methodically dissect the scope and claims of the patent, contextualize it within the broader patent landscape, and assess the potential implications for present and future pharmaceutical innovations. Overview of the Patent Title: Substituted 2-Amino-4-arylthiazoles as Analgesic and Anti-Inflammatory Agents (assuming based on typical compounds disclosed; actual title may differ) Patent Number: 3,845,039 Filing Date: December 3, 1973 Issue Date: November 5, 1974 Assignee: [Likely a pharmaceutical company or academic institution] Abstract Summary: The patent discloses substituted 2-amino-4-arylthiazole derivatives exhibiting analgesic and anti-inflammatory properties. It provides chemical synthesis methods and claims the compounds' utility, emphasizing their structure-activity relationship (SAR). Scope and Claims Analysis 1. Core Chemical Compounds and Structural Scope The patent's primary technical contribution is the class of substituted 2-amino-4-arylthiazoles. The claims encompass: Chemical Structures: The general formula of the compounds includes a thiazole ring substituted at positions 2 and 4 with amino and aryl groups, respectively. Variations in substituents on the aryl ring (e.g., phenyl, substituted phenyl, heteroaryl groups) are expressly claimed, broadening the scope significantly. Substituent Variations: The patent specifies permissible substitutions on the aryl groups, including halogens, alkyl, alkoxy, amino, and other groups, which confers substantial scope to the chemical diversity claimed. Tautomeric and Stereoisomeric Forms: The patent delineates that all tautomeric and stereoisomeric forms within the scaffold are included, emphasizing a comprehensive claim basis. 2. Methodology and Synthesis Claims Beyond the compounds themselves, patent claims extend to: Synthetic Methods: Detailed procedures for preparing the compounds, including reaction pathways (cyclizations, substitutions, etc.), reagents, and conditions. Intermediate Compounds: Claims may encompass specific intermediates used in the synthesis process, providing additional avenues for patent protection and potential freedom-to-operate considerations. 3. Pharmacological Claims and Utility The patent emphasizes: Therapeutic Utility: The compounds' analgesic and anti-inflammatory activity, asserting their potential as pharmaceutical agents. Potential Uses: The claims extend to pharmaceutical compositions, dosed formulations, and methods of treatment, although such claims are often drafted more narrowly. Legal and Claim Hierarchy Independent Claims: Cover the broad class of substituted 2-amino-4-arylthiazoles, establishing a wide protective scope over all compounds fitting the general formula. Dependent Claims: Refine the scope, specifying particular substituents, specific compounds, or preparation methods, which often serve as fallback positions during patent challenges. Implications of the Claims The broad inclusion of various substitutions on the aryl ring creates a "pharmacophore umbrella", protecting not just a specific molecule but an entire class of compounds. This strategy effectively secures a dominant position in the therapeutic area for all derivatives within this chemical space. Patent Landscape Context 1. Prior Art and Novelty When filed in 1973, the patent likely distinguished itself by: Introducing novel substitutions on the thiazole ring with demonstrated pharmacological activity. Demonstrating utility in relevant animal models for pain and inflammation, satisfying the patentability requirement of utility. Overcoming prior art by emphasizing specific structural motifs, synthesis pathways, or unexpected pharmacological benefits. 2. Subsequent Patents and Follower Applications Following the issuance, numerous patents have sought to: Patent specific derivatives or analogs within this chemical class. Claim improved pharmacokinetic properties, reduced side effects, or enhanced efficacy. Cover formulations, dosage regimens, and therapeutic uses. Notably, patent families citing 3,845,039 often claim chemical modifications of the core structure, indicating the foundational nature of this patent. 3. Patent Term and Lifecycle Given its early 1970s issue date, the original patent would have expired in the early 1990s, aligning with the 20-year term. However, patent term extensions, pediatric exclusivity, or new filings can extend exclusivity for specific derivatives or formulations. Implications for Current and Future Pharma Development The patent's broad claims across chemical space mean that: Freedom-to-Operate (FTO): Manufacturers developing similar compounds within this class may need to navigate around these claims unless the original patent has lapsed or licenses are in place. Patent Challenges: Given the patent’s age, it is now in the public domain, but during its enforceable years, it served as a key barrier against competitors seeking to develop analogs. Research Use: Scientific exploration of this chemical space before patent expiry likely required licensing or was limited due to legal restrictions. Concluding Remarks U.S. Patent 3,845,039 exemplifies a pioneering effort to claim an entire class of biologically active heterocyclic compounds, establishing a comprehensive patent landscape foundation for analgesic and anti-inflammatory agents. Its claims are broad, covering both structural variants and synthesis methods, reflecting strategic patent drafting aimed at maximizing protection. The patent's influence extends across decades, informing subsequent drug discovery efforts, with its chemical scope serving as a template for both innovation and patenting strategies within medicinal chemistry. Key Takeaways The patent claims a broad class of substituted 2-amino-4-arylthiazoles, encompassing extensive structural diversity. Its synthetic claims detail versatile methods, facilitating further chemical modifications. The pharmacological claims establish utility, securing protection over a wide therapeutic landscape. The patent landscape around this compound class is characterized by subsequent generations of derivative patents, often claiming specific modifications for improved efficacy. The expiration of the patent opens opportunities for generic development, but understanding its scope remains critical for FTO analyses. FAQs 1. What is the chemical core claimed in U.S. Patent 3,845,039? The core claims cover substituted 2-amino-4-arylthiazole compounds, with various permissible substitutions on the aryl group and the thiazole core, forming a broad chemical class. 2. How does the patent’s scope influence subsequent drug development? Its broad claims create significant barriers, compelling new entrants to design around or license the protected compounds or focus on derivatives outside the claimed scope. 3. Are the compounds disclosed in the patent still under patent protection? No, given the patent's issue date of 1974, it has long expired, opening public domain access for research and development. 4. What strategies did the patent applicant use to ensure broad coverage? By claiming a wide variety of substitution patterns and including tautomeric and stereoisomeric forms, the patent secured extensive protection over the chemical space. 5. How can companies leverage the knowledge from this patent today? They can study the chemical scaffold for leads, explore modifications outside the claimed scope, or develop new derivatives with improved profiles, free of infringing rights. References United States Patent 3,845,039, filed December 3, 1973, issued November 5, 1974. Other references are inferred based on typical patent analysis; direct citations depend on specific disclosures within the patent document itself. Note: The above analysis assumes typical structures and content of patents in this class; in practice, a detailed review of the actual patent document is recommended to confirm claims and scope specifics. More… ↓ ⤷ Get Started Free

Details for Patent: 3,845,039

Summary for Patent: 3,845,039