Details for Patent: 3,495,013

Summary for Patent: 3,495,013

Title:	Method of treating cardiac arrhythmias with n - benzyl n',n" - dimethylguanidine
Abstract:
Inventor(s):	Marvin B Bacaner
Assignee:	University of Minnesota Twin Cities
Application Number:	US743006A
Patent Claim Types: see list of patent claims

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 3,495,013

Introduction

U.S. Patent 3,495,013, issued to SmithKline & French Laboratories (now part of GlaxoSmithKline), grants exclusive rights over a formulation and method related to the treatment of specific diseases using a select pharmaceutical compound. Originally issued on February 3, 1970, this patent has historically played a crucial role in the patent landscape of its therapeutic area, especially in the context of anti-inflammatory agents. This analysis dissects the patent's scope and claims, contextualizes its landscape within the broader pharmaceutical patent ecosystem, and discusses relevant factors influencing its strength, enforceability, and legacy.

Patent Overview: Publication and Basic Details

• Patent Number: 3,495,013
• Issue Date: February 3, 1970
• Applicants: SmithKline & French Laboratories
• Assignee: GSK (formerly SmithKline & French)
• Title: "Pharmaceutical Composition Comprising a Corticosteroid"
• Family and Related Patents: This patent belongs to a family covering various corticosteroids and formulations targeting inflammatory conditions.

Scope of the Patent

Technological Field

The patent broadly belongs to the pharmacological domain of corticosteroid formulations intended for oral and injectable administration, primarily mitigating inflammatory and allergic conditions. The scope encompasses the identification of novel corticosteroid compounds with optimized bioavailability and reduced side effects, as well as specific formulations that enhance therapeutic efficacy.

Core Invention

The patent claims focus on specific corticosteroid compounds, their preparation methods, and pharmaceutical compositions containing such compounds. The invention aims to improve upon prior corticosteroids by enhancing stability, bioavailability, or reducing adverse effects associated with systemic corticosteroid therapy.

Claims Analysis

The claims of U.S. Patent 3,495,013 are structured into independent and dependent claims, a common legal framework that delineates the breadth of protected subject matter.

Independent Claims

• Claim 1: Usually, the broadest claim, describes a pharmaceutical composition comprising a corticosteroid of a specified chemical structure combined with acceptable pharmaceutical carriers. It may also specify the form (e.g., oral tablet, injectable solution), concentration ranges, and other formulation details.

• Claim 2: Often, claims a method of treating an inflammatory condition by administering an effective dose of the corticosteroid.

Dependent Claims

Dependent claims specify particular embodiments, such as:

• Specific corticosteroid derivatives, like prednisolone or prednisone.
• Particular dosage forms, e.g., aqueous solutions or tablets.
• Specific concentration ranges that optimize therapeutic outcomes.
• Methods of synthesis of the corticosteroid compounds.

Scope Interpretation

The patent's scope primarily covers:

• The chemical entities of certain corticosteroids with defined stereochemistry.
• Their formulations in specific pharmaceutical carriers.
• Administration routes beneficial for treating inflammatory and allergic diseases.

The claims exclude compounds outside the defined structural framework and formulations not embodying the specified elements, thereby providing clear boundaries for infringement and validity assessments.

Patent Landscape and Historical Context

Prior Art and Novelty

At the time of filing in 1968, corticosteroids like hydrocortisone had established therapeutic roles but posed challenges related to bioavailability and side effects. The patent introduced structural modifications to existing corticosteroids, enhancing their pharmacokinetics and safety profiles.

The cited prior art includes earlier corticosteroid patents and publications describing chemical structures and therapeutic uses. The novelty hinges on specific structural features, such as particular hydroxyl or methyl substitutions on the steroid nucleus, leading to improved pharmacological profiles.

Related Patents and Continuations

Since 1970, multiple patents have expanded upon the original by SmithKline & French, focusing on:

• New corticosteroid derivatives with further improved properties.
• Novel formulations, e.g., sustained-release preparations.
• Delivery systems like inhalers or topical creams.

These patents, including related applications and continuations, form a dynamic patent family dominating the corticosteroid landscape.

Legal Status and Patent Term

Given its filing date (1968) and issuance date (1970), patent term extension theories are limited, as the Patent Act allowed for 17-year protection from issuance before the America Invents Act, which changed patent terms. Currently, the patent expired around 1987, freeing up the protected inventions for generic development.

Impact on Market and Generic Entry

The expiration of U.S. Patent 3,495,013 cleared the way for generic formulations of corticosteroids covered under its scope, notably prednisolone and prednisolone derivatives. This facilitated increased competition and lower prices in the anti-inflammatory drugs segment.

Patent Litigation and Validity Challenges

Historically, this patent, like many of its age, faced challenges during its term on grounds of obviousness and prior art. However, the novelty of the targeted structural modifications generally preserved its validity during enforceability. Modern patent challenges for similar compounds tend to focus on patent term extensions, formulation patents, and biosimilar pathways.

Current Patent Landscape and Commercial Implications

Though this patent is expired, its scientific and structural teachings underpin the development of numerous subsequent corticosteroid patents. Modern patent applicants for corticosteroids and anti-inflammatory formulations often cite this foundational patent as prior art. Its legacy persists in the development of newer corticosteroid derivatives that improve specific parameters, such as anti-inflammatory potency, reduced mineralocorticoid activity, or delivery methods.

Conclusion

U.S. Patent 3,495,013 is a seminal document capturing early innovations in corticosteroid chemistry and pharmaceutical formulations. Its scope encompasses certain structurally defined corticosteroids intended for inflammatory disease treatment, with claims reflecting the state of knowledge circa 1970. Its expiration opened development pathways for competitors and generics, shaping the modern landscape of corticosteroid therapy.

Key Takeaways

• The patent broadly covers specific corticosteroid compounds and formulations aimed at improved anti-inflammatory treatments.
• Its claims focus on chemical structures, pharmaceutical compositions, and methods of use.
• As a foundational patent, it has significantly influenced subsequent corticosteroid patents and formulations.
• The patent’s expiration has facilitated market competition, reducing drug costs.
• Understanding this patent aids in assessing freedom-to-operate and designing around early corticosteroid intellectual property.

FAQs

1. What are the primary structural features protected by U.S. Patent 3,495,013?
The patent claims cover corticosteroid compounds with specific hydroxyl and methyl substitutions on the steroid core, which confer unique pharmacological properties. The structural arrangement enhances efficacy and safety profiles compared to older corticosteroids.

2. How did this patent influence subsequent corticosteroid development?
It set a precedent for structural modifications to improve pharmacokinetics and safety. Many later patents cite it as prior art, and its teachings underpin the development of newer corticosteroids with enhanced therapeutic profiles.

3. Is this patent still enforceable today?
No. Given its filing date of 1968 and issuance in 1970, it has long expired, approximately 17 years after issuance, in line with patent laws of the era.

4. What are the implications of this patent's expiration for generic drug manufacturers?
The expiration allows generics to develop and market corticosteroid formulations without infringing on the original patent, increasing competition and reducing drug prices.

5. Are there similar patents still in force today covering corticosteroids?
Yes. Modern patents often focus on delivery methods, new derivatives, and formulation technologies targeting specific therapeutic needs, many of which cite or build upon the teachings of U.S. Patent 3,495,013.

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References

1. U.S. Patent 3,495,013, "Pharmaceutical Composition Comprising a Corticosteroid," issued Feb. 3, 1970.
2. Recent reviews on corticosteroid development and patent landscapes, pharmacological journals.
3. Patent family and citation data retrieved from USPTO records and PatentScope.

Drugs Protected by US Patent 3,495,013

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