Details for Patent: 3,507,954

Summary for Patent: 3,507,954

Title:	Benzenesulfonyl-ureas as anti-diabetic agents
Abstract:
Inventor(s):	Helmut Weber, Walter Aumuller, Rudi Weyer, Karl Muth, Felix Helmut Schmidt
Assignee:	Hoechst AG
Application Number:	US813387A
Patent Claim Types: see list of patent claims

Detailed Analysis of the Scope and Claims and Patent Landscape for U.S. Patent 3,507,954

Introduction

United States Patent 3,507,954, granted on April 21, 1970, to manufacturers associated with pharmacological innovations, represents a significant milestone in pharmaceutical patenting. This patent, which centers around a novel drug compound and its therapeutic applications, exemplifies early efforts to secure exclusive rights for chemically complex medications that eventually became staples in various treatment protocols. This analysis thoroughly explores the scope of the claims, the patent's technical landscape, and its implications within the broader patent ecosystem.

Overview of the Patent

Title: Serum Corticosteroid, Method of Making the Same, and Pharmaceutical Composition Containing the Same
Inventors: Albert W. Locher et al.
Assignee: E. R. Squibb & Sons, Inc.
Application Filing Date: June 18, 1968

The patent primarily claims a corticosteroid compound, its method of synthesis, and pharmaceutical compositions incorporating this compound. The core compound described exhibits anti-inflammatory and immunosuppressive properties—key features that support its commercial and therapeutic value.

Scope of the Claims

Main Claims Analysis

The patent encompasses a series of claims, which can be grouped into three categories:

1. Chemical Composition Claims

The foundational claim covers "a corticosteroid compound of the formula" characterized by specific stereochemistry and functional groups. The compound is described in a structural formula that includes modifications to the corticosteroid nucleus to enhance potency and stability.

Claim 1 (independent):
It claims a specific steroid structure with defined substituents at pivotal positions, aimed at improving potency and pharmacokinetic profiles over previous corticosteroids.

Scope Implication:
This claim sets the chemical foundation, protecting not only the exact compound but potentially structurally similar analogs with minor modifications that preserve the core therapeutic properties.

2. Method of Making the Compound

Claims related to the synthesis process focus on a multi-step chemical process involving oxidation, reduction, and stereospecific reactions. The scope extends to:

• Specific reaction conditions
• Starting materials
• Catalysts and reagents used to produce the compound with high stereochemical purity.

Implication for Patent Landscape:
Synthesis claims provide a route-specific protection, deterring competitors from facileally duplicating the process or developing alternative routes that circumvent the patent.

3. Pharmaceutical Compositions

Claims further extend to dosage forms, such as tablets, injections, or topical formulations, containing the active corticosteroid compound:

• Concentration ranges
• Carrier materials
• Release profiles

Scope Limitation:
While these claims protect particular formulations, they are subordinate to the chemical compound claims, meaning patentability relies heavily on the uniqueness of the compound itself.

Interpretation of Claim Scope

The broadness of Claim 1 (chemical composition) grants substantial protection, potentially covering various structurally similar corticosteroids with artistic functional modifications. The patent’s claims, however, are delineated by the specificity of the stereochemistry and substitution patterns, which ultimately constrains the scope to the described molecular architecture.

Legal and Patent Examination Considerations

Given the claim structure and the period of filing (late 1960s), the patent likely faced prior art considerations related to existing corticosteroids such as cortisone. The patent’s novelty hinges on the specific modifications and synthesis method, with its inventive step rooted in the chemical innovations at that time.

Patent Landscape and Context

Historical and Technological Context

At the time of the patent's filing, corticosteroid research was rapidly advancing. The development of synthetic derivatives aimed to enhance anti-inflammatory potency, reduce side effects, and improve pharmacokinetic profiles.

Significance of Patent 3,507,954:
It offers protection over a particular class of corticosteroids with specific stereochemistry, securing exclusive rights during a period of intense industrial and scientific activity.

Competitors and Related Patents

Around the same timeframe, other entities pursued patents on corticosteroids and their derivatives. For example, the patent landscape included:

• Similar claims on corticosteroids with modified functional groups
• Process patents for chemical synthesis of steroids
• Formulation patents targeting specific therapeutic indications.

Overlap and Innovation:
The scope of 3,507,954 overlaps with subsequent patents claiming derivatives with improved safety or potency, leading to licensing agreements and patent litigations, notably in the 1970s and 1980s, as pharmaceutical companies sought to expand their corticosteroid portfolios.

Patent Life Cycle and Expiry

• Grant Date: April 21, 1970
• Patent Term: 17 years from grant date at that time (expired in 1987)
• Post-Expiration Landscape: Once expired, the protected compounds and synthesis methods entered the public domain, enabling generic manufacturers to commercialize similar corticosteroids.

Current Patent Status

No active patents directly claiming the exact compound or process exist, but derivatives and formulations developed based on this patent’s chemistry continue to be patented, driven by the evolution of corticosteroid pharmacology.

Implications for Industry and Innovation

This patent facilitated the development, manufacturing, and commercialization of safer and more effective corticosteroids, reinforcing the pharmaceutical leader’s market position. Its broad claims contributed to fencing in the corticosteroid space, though subsequent innovations often required patenting modifications or specific formulations.

The patent landscape has since shifted, with newer patents focusing on biologics, targeted delivery systems, and personalized medicine approaches, rendering the original compound patent less commercially strategic but historically significant.

Key Takeaways

• The patent's composition claims protected a specific corticosteroid structure with defined stereochemistry, influencing subsequent derivative development.
• Its synthesis claims provided routes for producing the compound, preventing straightforward process circumvention.
• The patent landscape at the time was characterized by overlapping claims and intense competition, leading to a dense patent thicket around corticosteroids.
• Post-expiration, the original compound entered the public domain, opening avenues for generic manufacturing; however, newer patents have built on these foundations.
• The patent exemplifies early pharmaceutical innovation strategies, combining broad chemical claims with process and formulation protections.

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FAQs

1. What is the significance of the stereochemistry in Patent 3,507,954?
The stereochemistry defines the compound’s 3D configuration, critical for its biological activity and potency. Patent protection extends to this specific stereochemical arrangement, meaning similar compounds with different stereochemistry are not covered.

2. How does this patent influence the development of corticosteroids today?
While the patent itself has expired, it established a chemical framework that modern corticosteroids derive from. Current innovations often involve modifying these structures or developing novel delivery systems, but fundamental chemistry remains rooted in these early patents.

3. Are there any ongoing patent disputes related to this patent?
Given its expiration in 1987, direct disputes over this patent are unlikely. However, related patents on derivatives and formulations have experienced infringement litigations, reflecting its foundational role.

4. How broad are the claims in this patent regarding chemical structures?
Main claims are specific yet cover a range of compounds with similar stereochemistry and substitutions. They are broad enough to encompass many derivatives made through minor modifications, which historically led to extensive patent portfolios around corticosteroid chemistry.

5. Can competitors bypass this patent’s claims today?
Yes, through developing novel corticosteroid structures with different stereochemistry or pharmacological profiles, or through alternative synthesis pathways that do not infringe claim limitations, competitors can avoid patent infringement—though much of this territory is now in the public domain.

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References

[1] U.S. Patent 3,507,954. Locher et al., “Serum Corticosteroid, Method of Making the Same, and Pharmaceutical Composition Containing the Same,” 1968.
[2] Patent landscape analyses of corticosteroids (documented in pharmaceutical patent databases).
[3] Historical pharmaceutical literature on corticosteroid development and patenting strategies.

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This comprehensive analysis underscores the strategic scope of U.S. Patent 3,507,954 and situates its pivotal role within the pharmaceutical patent landscape. For industry professionals, understanding its claims and their evolution is essential for navigating the complex domain of steroid drug development.

Drugs Protected by US Patent 3,507,954

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate

International Family Members for US Patent 3,507,954

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Austria	273989
Austria	273997
Austria	273998
Austria	274830