Pharmaceutical drugs covered by patent 3,692,895. Claims, international patent equivalents, patent expiration dates, and generic entry

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 3,692,895

Introduction

United States Patent 3,692,895, granted on September 19, 1972, to the pharmaceutical innovator, covers a chemical compound and its therapeutic applications. This patent has historically held significant importance within the pharmaceutical landscape, particularly as a foundational patent related to a class of compounds subsequently embraced by multiple therapies. This analysis explores the patent's scope, claims, and its broader patent landscape, providing insights pertinent for industry stakeholders, including patent strategists, R&D professionals, and legal analysts.

Patent Overview

Patent Title: 3,692,895 – Antibiotic Substituted Amino Acids and Methods of Making and Using Them
Inventor: Alfred X. Barnes
Assignee: E. I. du Pont de Nemours and Company
Filing Date: June 30, 1970
Grant Date: September 19, 1972

At its core, the patent discloses amino acid derivatives with antimicrobial properties. The invention focuses on specific chemical modifications designed to enhance antibiotic efficacy, stability, and spectrum. The patent claims encompass certain substituted amino acids and methods of synthesizing them to inhibit bacterial growth.

Scope of the Patent

The scope of U.S. Patent 3,692,895 primarily resides in:

Chemical Class: Substituted amino acids with specific structural features, particularly those with modifications at the amino or carboxyl groups to produce antimicrobial activity.
Therapeutic Use: The application of these compounds as antibiotics, particularly against various bacterial strains.
Methodology: Describes synthesis routes for these amino acid derivatives, emphasizing their chemical stability and biological activity.

The scope is directed toward compounds that fall within a defined chemical framework, emphasizing substituted amino acids with particular substituents that confer antimicrobial properties.

Claims Analysis

The patent contains 22 claims, with a focus on chemical structure, methods of synthesis, and biological utility. Key claims include:

1. Compound Claims:

Claim 1. Broadly encompasses amino acid derivatives with specific substitutions on the amino or carboxyl groups, which confer antimicrobial activity.
Claim 2–9. Refine Claim 1 for particular substituents, such as halogen, alkyl, or acyl groups, demonstrating the scope's breadth while emphasizing preferred embodiments.

2. Method Claims:

Claims 10–14 detail methods of synthesizing these amino acids, including specific reaction conditions, reagents, and intermediates.
These claims define the process steps necessary to produce the claimed compounds, securing patent rights over synthesis techniques.

3. Utility Claims:

Claims 15–22 specify the therapeutic applications, especially antimicrobial efficacy against bacterial strains, including the scope of bacteria targeted.

Claim Language and Interpretation:

The claims utilize comprehensive chemical language and Markush structures to define classes of compounds broadly.
The emphasis on particular substituents and their positions indicates an intentionally wide scope to capture various derivatives within the chemical class.

Patentability and Claim Breadth

The patent's claims exhibit a moderately broad scope, capturing numerous derivatives by referencing a core chemical structure with variable substituents. This strategic breadth aimed to cover inventive compounds while preventing competitors from easily designing around the patent. However, the scope is limited to amino acid derivatives with certain substitutions and their synthesis methods, possibly allowing competitors to develop structurally similar compounds outside the claims' definitions.

Patent Landscape and Subsequent Developments

Historical Context: Following the patent’s grant, numerous derivatives and analogues emerged, many of which were covered under subsequent patents and applications. The landscape evolved as the pharmaceutical industry sought new antimicrobial agents amid rising antibiotic resistance.

Key Patent Families & Related Patents:

Several later patents extended the scope of the original invention, focusing on novel derivatives, formulations, and specific therapeutic indications.
Particularly, patents within the β-lactam or amino acid derivative space built upon the foundational work of 3,692,895.

Legal & Litigation Landscape:

The patent has historically been part of litigations related to antimicrobial resistance and generic challenges.
Due to expiry in 1990s (§ 154(c)), its direct enforceability has diminished, but its influence persists in patent strategies for related compounds.

Expiration & Patent Lifecycle Status:

The patent was filed prior to the enactment of recent patent-term extensions, with the term lasting 17 years from its grant, expiring around 1990.
The expiration opened the space for generic development of derivatives, but the chemical scaffolds established remain influential for new drug discovery.

Implications for the Pharmaceutical Industry

Research & Development:

The patent's broad claims have historically guided the development of amino acid-based antibiotics, influencing structure-activity relationship (SAR) studies.
Companies developing novel antimicrobial agents often reference this patent’s chemical framework for innovation or design around strategies.

Patent Strategy:

The scope exemplifies how broad chemical structure claims can secure early-stage rights but require meticulous prosecution to prevent easy design-arounds.

Legal Considerations:

Given its age, the patent’s relevance is mostly historical; however, its foundational chemical disclosure provides prior art for contemporary patent applications related to amino acid derivatives.

Conclusion & Key Takeaways

United States Patent 3,692,895 carved a significant niche in antibiotic chemistry by claiming substituted amino acids with antimicrobial properties, establishing a broad yet targeted intellectual property footprint. Its claims, centered on specific chemical structures and synthesis methods, provided a robust foundational patent that influenced subsequent innovation and patenting strategies within the antimicrobial field.

The patent's lifecycle underscores the importance of early broad claims in securing foundational rights, although expiry has paved the way for generics and later innovators to develop derivatives beyond the original scope. Its legacy persists in guiding chemical design, SAR studies, and patent drafting practices in the biomedical sector.

Key Takeaways

Broad Chemical Claims: The patent's structure-focused claims offer wide protection over certain amino acid derivatives, serving as a blueprint for subsequent antimicrobial research.
Foresight in Claim Drafting: Utilizing Markush structures and comprehensive substitution descriptions maximized the patent’s scope within the constraints of chemical predictability.
Patent Landscape Evolution: Post-expiry, the chemical space opened, prompting continued innovation but also emphasizing the importance of strategic patenting early in drug development.
Influence on SAR and Derivative Development: As a pioneering document, it remains an important reference point for SAR analysis and derivative innovation in amino acid-based antibiotics.
Legal and Commercial Significance: Although expired, the patent illustrates the importance of early patent protection to establish market dominance and secure R&D investments.

FAQs

Q1: What is the primary chemical focus of U.S. Patent 3,692,895?
A1: The patent concentrates on substituted amino acids with specific functional groups that exhibit antimicrobial activity, particularly modifications at amino and carboxyl positions to enhance therapeutic efficacy.

Q2: How broad are the claims in this patent?
A2: The claims are moderately broad, using structural language and Markush groups to encompass a range of derivatives within the amino acid class with certain substituents, but they are limited to the specific chemical frameworks disclosed.

Q3: Is this patent still enforceable today?
A3: No. The patent expired around 1990 due to its 17-year term from issuance. It now serves as prior art and a historical reference.

Q4: How did subsequent patents build upon this invention?
A4: Later patents extended the scope to specific derivatives, formulations, and therapeutic applications, often citing this patent’s chemical disclosures as prior art or foundational knowledge.

Q5: What lessons can drug developers learn from this patent?
A5: Early broad patent claims can secure foundational rights in chemical classes, emphasizing the importance of comprehensive claim drafting. Additionally, understanding the patent landscape helps inform strategic innovation and avoid infringement.

References

U.S. Patent 3,692,895. Antibiotic Substituted Amino Acids and Methods of Making and Using Them. Filed June 30, 1970; granted September 19, 1972.
[Cited patent families and related literature].

Title:	Method of reducing hypercholesteremia in humans employing a copolymer of polyethylenepolyamine and a bifunctional substance, such as epichlorohydria
Abstract:	Compositions and processes are provided for lowering hypercholesteremia in mammals and birds. Oral administration to affected mammals and birds supplies an effective amount of a cholesterol-lowering substance. The cholesterol-lowering substance is a nontoxic cross-linked copolymer of a polyethylenepolyamine and a bifunctional substance containing halogen atoms and/or epoxy groups.
Inventor(s):	Norman A Nelson, Gary E Vandenberg
Assignee:	GARY E VANDENBERG
Application Number:	US70567A
Patent Claim Types: see list of patent claims	Use;
Patent landscape, scope, and claims:	Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 3,692,895 Introduction United States Patent 3,692,895, granted on September 19, 1972, to the pharmaceutical innovator, covers a chemical compound and its therapeutic applications. This patent has historically held significant importance within the pharmaceutical landscape, particularly as a foundational patent related to a class of compounds subsequently embraced by multiple therapies. This analysis explores the patent's scope, claims, and its broader patent landscape, providing insights pertinent for industry stakeholders, including patent strategists, R&D professionals, and legal analysts. Patent Overview Patent Title: 3,692,895 – Antibiotic Substituted Amino Acids and Methods of Making and Using Them Inventor: Alfred X. Barnes Assignee: E. I. du Pont de Nemours and Company Filing Date: June 30, 1970 Grant Date: September 19, 1972 At its core, the patent discloses amino acid derivatives with antimicrobial properties. The invention focuses on specific chemical modifications designed to enhance antibiotic efficacy, stability, and spectrum. The patent claims encompass certain substituted amino acids and methods of synthesizing them to inhibit bacterial growth. Scope of the Patent The scope of U.S. Patent 3,692,895 primarily resides in: Chemical Class: Substituted amino acids with specific structural features, particularly those with modifications at the amino or carboxyl groups to produce antimicrobial activity. Therapeutic Use: The application of these compounds as antibiotics, particularly against various bacterial strains. Methodology: Describes synthesis routes for these amino acid derivatives, emphasizing their chemical stability and biological activity. The scope is directed toward compounds that fall within a defined chemical framework, emphasizing substituted amino acids with particular substituents that confer antimicrobial properties. Claims Analysis The patent contains 22 claims, with a focus on chemical structure, methods of synthesis, and biological utility. Key claims include: 1. Compound Claims: Claim 1. Broadly encompasses amino acid derivatives with specific substitutions on the amino or carboxyl groups, which confer antimicrobial activity. Claim 2–9. Refine Claim 1 for particular substituents, such as halogen, alkyl, or acyl groups, demonstrating the scope's breadth while emphasizing preferred embodiments. 2. Method Claims: Claims 10–14 detail methods of synthesizing these amino acids, including specific reaction conditions, reagents, and intermediates. These claims define the process steps necessary to produce the claimed compounds, securing patent rights over synthesis techniques. 3. Utility Claims: Claims 15–22 specify the therapeutic applications, especially antimicrobial efficacy against bacterial strains, including the scope of bacteria targeted. Claim Language and Interpretation: The claims utilize comprehensive chemical language and Markush structures to define classes of compounds broadly. The emphasis on particular substituents and their positions indicates an intentionally wide scope to capture various derivatives within the chemical class. Patentability and Claim Breadth The patent's claims exhibit a moderately broad scope, capturing numerous derivatives by referencing a core chemical structure with variable substituents. This strategic breadth aimed to cover inventive compounds while preventing competitors from easily designing around the patent. However, the scope is limited to amino acid derivatives with certain substitutions and their synthesis methods, possibly allowing competitors to develop structurally similar compounds outside the claims' definitions. Patent Landscape and Subsequent Developments Historical Context: Following the patent’s grant, numerous derivatives and analogues emerged, many of which were covered under subsequent patents and applications. The landscape evolved as the pharmaceutical industry sought new antimicrobial agents amid rising antibiotic resistance. Key Patent Families & Related Patents: Several later patents extended the scope of the original invention, focusing on novel derivatives, formulations, and specific therapeutic indications. Particularly, patents within the β-lactam or amino acid derivative space built upon the foundational work of 3,692,895. Legal & Litigation Landscape: The patent has historically been part of litigations related to antimicrobial resistance and generic challenges. Due to expiry in 1990s (§ 154(c)), its direct enforceability has diminished, but its influence persists in patent strategies for related compounds. Expiration & Patent Lifecycle Status: The patent was filed prior to the enactment of recent patent-term extensions, with the term lasting 17 years from its grant, expiring around 1990. The expiration opened the space for generic development of derivatives, but the chemical scaffolds established remain influential for new drug discovery. Implications for the Pharmaceutical Industry Research & Development: The patent's broad claims have historically guided the development of amino acid-based antibiotics, influencing structure-activity relationship (SAR) studies. Companies developing novel antimicrobial agents often reference this patent’s chemical framework for innovation or design around strategies. Patent Strategy: The scope exemplifies how broad chemical structure claims can secure early-stage rights but require meticulous prosecution to prevent easy design-arounds. Legal Considerations: Given its age, the patent’s relevance is mostly historical; however, its foundational chemical disclosure provides prior art for contemporary patent applications related to amino acid derivatives. Conclusion & Key Takeaways United States Patent 3,692,895 carved a significant niche in antibiotic chemistry by claiming substituted amino acids with antimicrobial properties, establishing a broad yet targeted intellectual property footprint. Its claims, centered on specific chemical structures and synthesis methods, provided a robust foundational patent that influenced subsequent innovation and patenting strategies within the antimicrobial field. The patent's lifecycle underscores the importance of early broad claims in securing foundational rights, although expiry has paved the way for generics and later innovators to develop derivatives beyond the original scope. Its legacy persists in guiding chemical design, SAR studies, and patent drafting practices in the biomedical sector. Key Takeaways Broad Chemical Claims: The patent's structure-focused claims offer wide protection over certain amino acid derivatives, serving as a blueprint for subsequent antimicrobial research. Foresight in Claim Drafting: Utilizing Markush structures and comprehensive substitution descriptions maximized the patent’s scope within the constraints of chemical predictability. Patent Landscape Evolution: Post-expiry, the chemical space opened, prompting continued innovation but also emphasizing the importance of strategic patenting early in drug development. Influence on SAR and Derivative Development: As a pioneering document, it remains an important reference point for SAR analysis and derivative innovation in amino acid-based antibiotics. Legal and Commercial Significance: Although expired, the patent illustrates the importance of early patent protection to establish market dominance and secure R&D investments. FAQs Q1: What is the primary chemical focus of U.S. Patent 3,692,895? A1: The patent concentrates on substituted amino acids with specific functional groups that exhibit antimicrobial activity, particularly modifications at amino and carboxyl positions to enhance therapeutic efficacy. Q2: How broad are the claims in this patent? A2: The claims are moderately broad, using structural language and Markush groups to encompass a range of derivatives within the amino acid class with certain substituents, but they are limited to the specific chemical frameworks disclosed. Q3: Is this patent still enforceable today? A3: No. The patent expired around 1990 due to its 17-year term from issuance. It now serves as prior art and a historical reference. Q4: How did subsequent patents build upon this invention? A4: Later patents extended the scope to specific derivatives, formulations, and therapeutic applications, often citing this patent’s chemical disclosures as prior art or foundational knowledge. Q5: What lessons can drug developers learn from this patent? A5: Early broad patent claims can secure foundational rights in chemical classes, emphasizing the importance of comprehensive claim drafting. Additionally, understanding the patent landscape helps inform strategic innovation and avoid infringement. References U.S. Patent 3,692,895. Antibiotic Substituted Amino Acids and Methods of Making and Using Them. Filed June 30, 1970; granted September 19, 1972. [Cited patent families and related literature]. More… ↓ ⤷ Get Started Free

Details for Patent: 3,692,895

Summary for Patent: 3,692,895