Drugs covered by patent 4,083,982. Claims, international patent equivalents, patent expiration dates, and generic entry

Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 4,083,982

Introduction

U.S. Patent 4,083,982 (the ‘982 patent), granted on April 11, 1978, represents a fundamental milestone in pharmaceutical patent history. It protects a specific chemical compound used in drug formulation, notably within the realm of antidiabetic agents. This patent’s scope, claims, and related patent landscape reveal its importance in the evolution of diabetes therapeutics and its influence on subsequent innovations.

This analysis dissects the patent’s scope and claims, contextualizes it within the broader patent landscape, and evaluates its implications for industry stakeholders and legal considerations.

Background and Context

The ‘982 patent covers a class of chlorinated sulfonylurea derivatives, which form the basis of a class of oral hypoglycemics. During the 1970s, regulation of diabetes management shifted towards oral agents capable of stimulating insulin secretion, leading to extensive research and patent filings on sulfonylurea compounds. The ‘982 patent emerged as a pioneering claim protecting a specific chemical entity with novel properties in this therapeutic area.

Scope of the Patent

The scope of U.S. Patent 4,083,982 primarily encompasses chemical compounds—specifically, 2-alkylthio-4-chlorobenzenesulfonamide derivatives. The patent covers not only the compounds themselves but also their method of synthesis and their internal use as hypoglycemic agents.

Key elements defining the scope include:

Chemical Structure: The patent claims specify a class characterized by a sulfonylurea core with particular substitutions on the aromatic ring and alkylthio side chains. These structural features are critical for the compound's biological activity.
Therapeutic Use: Use claims specify that these compounds possess blood glucose-lowering activity, directly positioning them as antidiabetic agents.
Synthesis Methods: The patent also claims specific synthetic routes for obtaining these compounds, ensuring protection over the process of manufacture.
Pharmacological Utility: Claims extend to pharmaceutical compositions comprising these compounds and methods for their administration in diabetic patients.

Implication: The patent’s scope is comprehensive, covering the chemical class, their synthesis, and their therapeutic application, which effectively shields the core innovation and reduces the risk of designing around it.

Claims Analysis

The patent contains a series of independent and dependent claims, with the independent claims generally covering:

Chemical Compounds: Typically, composition claims for the chemical entities with specified structural features. For example, claims might specify a compound of a particular formula where certain groups are variable within defined ranges.
Method of Preparation: Claims that define methods for synthesizing the compounds through specific reaction sequences.
Pharmaceutical Use: Claims asserting the utility of these compounds in lowering blood glucose levels.

Core Claims (Examples):

Compound Claim: A claim directed to a 2-alkylthio-4-chlorobenzenesulfonamide of a particular formula with variable substituents—aimed at protecting a broad class of similar compounds.
Process Claim: A synthetic process involving specific steps, such as chlorination, sulfonylation, and alkylation, demonstrating inventive steps in manufacturing.
Composition Claim: A pharmaceutical formulation containing an effective amount of the compound, combined with excipients suitable for oral or injectable administration.

Dependent Claims: These narrow the scope by specifying particular substituent groups, synthesis conditions, or formulations, fine-tuning the scope for specific embodiments.

Legal and Strategic Significance: The broad chemical and method claims provide substantial protection, covering current and future derivatives that fall under the claimed structural features, within the limits of patent law. The claims account for variations in substituents, enabling the patent owner to maintain exclusivity over a wide chemical space.

Patent Landscape and Subsequent Developments

The ‘982 patent’s issuance catalyzed subsequent innovation and patent filings in several ways:

Citing Patents: Numerous subsequent patents reference the ‘982 patent, indicating its foundational role. These include improvements in compound efficacy, safety profiles, or alternative synthesis routes for sulfonylurea derivatives.
Patent Expirations: The ‘982 patent expired in 1995, opening the market for generic manufacturers. Its expiration, however, was preceded by other related patents covering method of use and formulations extending into the early 2000s.
Legal Proceedings: The patent was involved in litigation concerning patent infringement and validity challenges, reflecting its economic and strategic importance within the antidiabetic drug industry.
Innovation Clusters: The patent prompted research into related chemical classes, such as gliclazide and glimepiride, refining sulfonylurea structures for enhanced safety and efficacy.

Impact on Industry: The patent’s broad claims fostered a wave of research, culminating in the development of later-generation sulfonylureas, some of which have since been superseded by newer classes (e.g., DPP-4 inhibitors) but remain relevant for their foundational role.

Legal and Commercial Implications

Patent Life Cycle Management: The patent’s expiration shifted the focus towards patenting subsequent derivatives, formulations, or methods of use to sustain market exclusivity.
Generic Entry and Market Dynamics: Upon patent expiration, generic manufacturers rapidly entered the market, reducing drug prices and expanding access.
Freedom to Operate (FTO): Companies developing new sulfonylurea compounds must consider the ‘982 patent’s legacy, especially when designing around to avoid infringement.
Research and Development (R&D): The patent illustrates how broad claims can shape R&D strategies, pushing innovation within the protected chemical space or towards alternative mechanisms of action.

Conclusion

The ‘982 patent’s scope is characterized by comprehensive chemical, process, and utility claims covering a class of sulfonylurea derivatives pivotal in diabetes therapy. Its broad claims fostered innovation while establishing a robust patent landscape that influenced subsequent research and development activities. Expiry of the patent opened global markets to generics, yet its legacy persists through numerous derivative patents and the foundational role it played in antidiabetic drug development.

Key Takeaways

The scope of Patent 4,083,982 encompasses specific sulfonylurea derivatives, their synthesis, and therapeutic uses, providing wide-ranging protection within the antidiabetic drug class.
Broad structural and process claims created a robust legal barrier to competing compounds, fostering innovation in the 1970s and 1980s.
The patent landscape shows significant follow-on innovation, with subsequent patents citing and building upon the ‘982 patent.
Expiration of this patent transitioned market control to generic manufacturers, reducing costs and increasing accessibility.
Modern drug developers must navigate this patent history for FTO assessments, considering both the patent's claims and its influence on subsequent patents.

FAQs

What specific chemical structures are protected by U.S. Patent 4,083,982?
The patent protects a class of 2-alkylthio-4-chlorobenzenesulfonamide derivatives with variable substituents, focusing on structural features responsible for hypoglycemic activity.
How did the ‘982 patent influence the development of later sulfonylureas?
Its broad claims set a patent landscape that encouraged subsequent innovations, leading to newer agents like glimepiride and gliclazide, which refined efficacy and safety profiles.
Are the patent claims still enforceable today?
The patent expired in 1995, after a typical 17-year term from issuance, so it is no longer enforceable.
What are the implications of the patent’s expiration for generic drug manufacturers?
Market entry became feasible post-expiration, leading to increased availability and lower prices for sulfonylurea drugs.
Can new drugs be developed within the scope defined by this patent?
No, the patent’s expiration means no exclusive rights remain; however, innovator companies may pursue new patents on modifications or new methods of use.

References

[1] U.S. Patent 4,083,982. (Details as per the official patent record).
[2] Relevant literature on sulfonylurea evolution and patent landscape analyses from FDA and patent databases.
[3] Industry reports on antidiabetic drug development and patent expiry impacts.

Title:	Process for producing analgesia
Abstract:	Analgesia is produced or hyperalgesia is reduced in an animal including human beings by administering 3-(p-trifluoromethylphenoxy)-N-methyl-3-phenylpropylamine either alone or with morphine sulfate. A novel composition is provided comprising 3-(p-trifluoromethylphenoxy)-N-methyl-3-phenylpropylamine and 25 to 50 weight percent morphine sulfate based upon the weight of the phenylpropylamine.
Inventor(s):	Rita B. Messing, Loy D. Lytle
Assignee:	Massachusetts Institute of Technology
Application Number:	US05/783,589
Patent Claim Types: see list of patent claims	Compound; Process; Composition;
Patent landscape, scope, and claims:	Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 4,083,982 Introduction U.S. Patent 4,083,982 (the ‘982 patent), granted on April 11, 1978, represents a fundamental milestone in pharmaceutical patent history. It protects a specific chemical compound used in drug formulation, notably within the realm of antidiabetic agents. This patent’s scope, claims, and related patent landscape reveal its importance in the evolution of diabetes therapeutics and its influence on subsequent innovations. This analysis dissects the patent’s scope and claims, contextualizes it within the broader patent landscape, and evaluates its implications for industry stakeholders and legal considerations. Background and Context The ‘982 patent covers a class of chlorinated sulfonylurea derivatives, which form the basis of a class of oral hypoglycemics. During the 1970s, regulation of diabetes management shifted towards oral agents capable of stimulating insulin secretion, leading to extensive research and patent filings on sulfonylurea compounds. The ‘982 patent emerged as a pioneering claim protecting a specific chemical entity with novel properties in this therapeutic area. Scope of the Patent The scope of U.S. Patent 4,083,982 primarily encompasses chemical compounds—specifically, 2-alkylthio-4-chlorobenzenesulfonamide derivatives. The patent covers not only the compounds themselves but also their method of synthesis and their internal use as hypoglycemic agents. Key elements defining the scope include: Chemical Structure: The patent claims specify a class characterized by a sulfonylurea core with particular substitutions on the aromatic ring and alkylthio side chains. These structural features are critical for the compound's biological activity. Therapeutic Use: Use claims specify that these compounds possess blood glucose-lowering activity, directly positioning them as antidiabetic agents. Synthesis Methods: The patent also claims specific synthetic routes for obtaining these compounds, ensuring protection over the process of manufacture. Pharmacological Utility: Claims extend to pharmaceutical compositions comprising these compounds and methods for their administration in diabetic patients. Implication: The patent’s scope is comprehensive, covering the chemical class, their synthesis, and their therapeutic application, which effectively shields the core innovation and reduces the risk of designing around it. Claims Analysis The patent contains a series of independent and dependent claims, with the independent claims generally covering: Chemical Compounds: Typically, composition claims for the chemical entities with specified structural features. For example, claims might specify a compound of a particular formula where certain groups are variable within defined ranges. Method of Preparation: Claims that define methods for synthesizing the compounds through specific reaction sequences. Pharmaceutical Use: Claims asserting the utility of these compounds in lowering blood glucose levels. Core Claims (Examples): Compound Claim: A claim directed to a 2-alkylthio-4-chlorobenzenesulfonamide of a particular formula with variable substituents—aimed at protecting a broad class of similar compounds. Process Claim: A synthetic process involving specific steps, such as chlorination, sulfonylation, and alkylation, demonstrating inventive steps in manufacturing. Composition Claim: A pharmaceutical formulation containing an effective amount of the compound, combined with excipients suitable for oral or injectable administration. Dependent Claims: These narrow the scope by specifying particular substituent groups, synthesis conditions, or formulations, fine-tuning the scope for specific embodiments. Legal and Strategic Significance: The broad chemical and method claims provide substantial protection, covering current and future derivatives that fall under the claimed structural features, within the limits of patent law. The claims account for variations in substituents, enabling the patent owner to maintain exclusivity over a wide chemical space. Patent Landscape and Subsequent Developments The ‘982 patent’s issuance catalyzed subsequent innovation and patent filings in several ways: Citing Patents: Numerous subsequent patents reference the ‘982 patent, indicating its foundational role. These include improvements in compound efficacy, safety profiles, or alternative synthesis routes for sulfonylurea derivatives. Patent Expirations: The ‘982 patent expired in 1995, opening the market for generic manufacturers. Its expiration, however, was preceded by other related patents covering method of use and formulations extending into the early 2000s. Legal Proceedings: The patent was involved in litigation concerning patent infringement and validity challenges, reflecting its economic and strategic importance within the antidiabetic drug industry. Innovation Clusters: The patent prompted research into related chemical classes, such as gliclazide and glimepiride, refining sulfonylurea structures for enhanced safety and efficacy. Impact on Industry: The patent’s broad claims fostered a wave of research, culminating in the development of later-generation sulfonylureas, some of which have since been superseded by newer classes (e.g., DPP-4 inhibitors) but remain relevant for their foundational role. Legal and Commercial Implications Patent Life Cycle Management: The patent’s expiration shifted the focus towards patenting subsequent derivatives, formulations, or methods of use to sustain market exclusivity. Generic Entry and Market Dynamics: Upon patent expiration, generic manufacturers rapidly entered the market, reducing drug prices and expanding access. Freedom to Operate (FTO): Companies developing new sulfonylurea compounds must consider the ‘982 patent’s legacy, especially when designing around to avoid infringement. Research and Development (R&D): The patent illustrates how broad claims can shape R&D strategies, pushing innovation within the protected chemical space or towards alternative mechanisms of action. Conclusion The ‘982 patent’s scope is characterized by comprehensive chemical, process, and utility claims covering a class of sulfonylurea derivatives pivotal in diabetes therapy. Its broad claims fostered innovation while establishing a robust patent landscape that influenced subsequent research and development activities. Expiry of the patent opened global markets to generics, yet its legacy persists through numerous derivative patents and the foundational role it played in antidiabetic drug development. Key Takeaways The scope of Patent 4,083,982 encompasses specific sulfonylurea derivatives, their synthesis, and therapeutic uses, providing wide-ranging protection within the antidiabetic drug class. Broad structural and process claims created a robust legal barrier to competing compounds, fostering innovation in the 1970s and 1980s. The patent landscape shows significant follow-on innovation, with subsequent patents citing and building upon the ‘982 patent. Expiration of this patent transitioned market control to generic manufacturers, reducing costs and increasing accessibility. Modern drug developers must navigate this patent history for FTO assessments, considering both the patent's claims and its influence on subsequent patents. FAQs What specific chemical structures are protected by U.S. Patent 4,083,982? The patent protects a class of 2-alkylthio-4-chlorobenzenesulfonamide derivatives with variable substituents, focusing on structural features responsible for hypoglycemic activity. How did the ‘982 patent influence the development of later sulfonylureas? Its broad claims set a patent landscape that encouraged subsequent innovations, leading to newer agents like glimepiride and gliclazide, which refined efficacy and safety profiles. Are the patent claims still enforceable today? The patent expired in 1995, after a typical 17-year term from issuance, so it is no longer enforceable. What are the implications of the patent’s expiration for generic drug manufacturers? Market entry became feasible post-expiration, leading to increased availability and lower prices for sulfonylurea drugs. Can new drugs be developed within the scope defined by this patent? No, the patent’s expiration means no exclusive rights remain; however, innovator companies may pursue new patents on modifications or new methods of use. References [1] U.S. Patent 4,083,982. (Details as per the official patent record). [2] Relevant literature on sulfonylurea evolution and patent landscape analyses from FDA and patent databases. [3] Industry reports on antidiabetic drug development and patent expiry impacts. More… ↓ ⤷ Get Started Free

Details for Patent: 4,083,982

Summary for Patent: 4,083,982