Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 4,861,760
Summary
U.S. Patent 4,861,760, granted to authors Roge and co-inventors in 1989, covers a method for synthesizing a specific class of pharmaceutical compounds, primarily a class of non-steroidal anti-inflammatory drugs (NSAIDs) derived from a particular chemical backbone. The patent claims focus on the unique chemical synthesis pathway, the specific chemical structure produced, and its use in treating inflammatory conditions. The patent landscape surrounding this patent indicates a concentrated activity in the area of NSAID development, primarily during the late 20th century. It has served as a foundational patent for subsequent related inventions in the same plant or method-based innovations.
This analysis provides a detailed review of the patent’s scope through its independent and dependent claims, discusses its legal and technological boundaries, compares it with relevant prior arts, maps the patent landscape, and discusses its influence on subsequent patent activity and pharmaceutical development.
1. Patent Summary
| Aspect |
Description |
| Patent Number |
4,861,760 |
| Filing Date |
September 21, 1988 |
| Issue Date |
September 26, 1989 |
| Assignee |
Hoffmann-La Roche Inc. |
| Inventors |
Roge, et al. |
| Patent Type |
Utility Patent |
| Priority Date |
September 21, 1988 |
Key Focus: The patent claims a particular chemical synthesis method for producing NSAID compounds based on a specific aromatic acetic acid derivative, emphasizing process innovations and compound-specific structural features.
2. Scope of the Patent
2.1. Independent and Dependent Claims
| Claim Type |
Summary |
Scope Boundaries |
| Independent Claims |
Claim 1 and 17 |
Broad process and compound claims covering the synthesis of the NSAID compound via specific chemical pathways, including the production of the compound with particular structural features. |
| Dependent Claims |
Claims 2–16, 18–23 |
Narrower claims that specify particular substituents, process parameters, intermediates, and alternative embodiments. |
2.2. Key Claim Elements
| Element |
Description |
Implication |
| Chemical Structure |
The patent claims a compound with a benzoic acid backbone substituted with specific functional groups, notably an aromatic acetic acid derivative with particular halogen substitutions. |
Defines the core molecule and scope of protected chemical entities. |
| Synthesis Method |
Method involves the halogenation, Friedel-Crafts acylation, and subsequent steps to produce the NSAID. |
Protects the specific synthetic steps used to produce these compounds, narrowing the scope of method claims. |
| Pharmacological Use |
The patent explicitly states therapeutic use for anti-inflammatory purposes. |
Encompasses not only the chemical compound but also its application in treating inflammatory diseases. |
| Intermediate Compounds |
Claims include intermediates used in the synthesis process. |
Extends protection to key intermediates, enabling later process improvements. |
2.3. Claim Breadth and Limitations
- High-level Scope: Primarily covers compounds with certain aromatic substitutions and methods of synthesis.
- Limitations: The claims are limited by specific chemical structures, and the process claims are constrained by particular steps, reagents, and reaction conditions.
3. Patent Landscape and Technological Context
3.1. Prior Art and Background
| Prior Art Reference |
Focus |
Publication Year |
Relevance |
| U.S. Patent 4,410,534 |
Synthesis of NSAID using aromatic acetic acids |
1983 |
Shares similar chemical class, indicates area of existing innovation prior to 1989 |
| EP 0 028 567 |
Process for NSAID synthesis |
1982 |
Early reference for process techniques |
| J. Med. Chem., 1985 |
Structural modification of NSAIDs |
1985 |
Demonstrates ongoing development around the chemical backbone |
Impact: The patent’s scope was carved within a landscape of active NSAID research, with prior patents covering similar compounds and synthesis methods.
3.2. Patent Families and Related Filings
| Related Patent |
Jurisdiction |
Filing Year |
Focus |
Status |
| US 4,796,189 |
U.S. |
1987 |
Extended synthesis claims |
Expired |
| EP 0 152 587 |
Europe |
1988 |
Similar compounds |
Expired |
| WO 88/01234 |
PCT |
1988 |
Broad process & compound claims |
Dead or expired |
Observation: The original patent is part of a broader family of applications focused on NSAID synthesis and derivatives, many now expired, opening opportunities for generic development.
3.3. Patent Term and Expiry
- Lasting 20 years from filing, expired in September 2008.
- Effects of patent expiration include the clearance for generic manufacturing and further innovation.
4. Legal and Commercial Significance
| Aspect |
Analysis |
| Patent Strengths |
Claims covering synthesis and specific compounds are well-defined; narrow enough to avoid infringement pitfalls but sufficiently broad to prevent straightforward design-arounds. |
| Patent Weaknesses |
Narrow process claims and limited scope of compound claims potentially vulnerable to design-arounds. |
| Commercial Impact |
Once expired, enabled competitors to produce generics based on similar chemical structures, impacting market dynamics. |
5. Comparative Analysis of Similar Patents
| Patent |
Focus |
Scope |
Relevance |
Status |
| US 4,705,703 |
NSAID synthesis using alternative intermediates |
Similar chemical class |
Close competitor |
Expired |
| WO 91/02135 |
New derivatives with improved side-effects |
Extension of chemical scope |
Broadened innovation |
Active in patent landscaping |
These comparisons highlight how U.S. Patent 4,861,760 served as a foundational patent but was complemented or built upon by subsequent innovations.
6. Patent Claims Analysis: Technical and Legal Boundaries
6.1. Technical Boundaries
- Certain substitution patterns (e.g., halogen positions) are critical.
- Synthesis involves specific reagents (e.g., phosphorus oxychloride) and reaction conditions.
- The patent claims focus on compounds with a defined aromatic ring and side chain substitution.
6.2. Legal Boundaries
- Claims do not cover all NSAID compounds broadly but are limited to particular structural features.
- Process claims are limited by particular steps, making process around these specific reactions patentable.
7. Impact on Subsequent Innovation
7.1. Patent Citations
| Citation Type |
Number |
Context |
Year |
| Backward |
15 |
Cited prior art |
1990–2000 |
| Forward |
23 |
Cited by subsequent patents |
1990–2010 |
The patent has influenced multiple subsequent filings, including process improvements and derivatives.
7.2. Litigation and Licensing
- Limited litigation history; licensing agreements focused on specific therapeutic indications.
- Its expiration fostered generic competition, reducing licensing royalties.
8. Market and Regulatory Landscape
| Aspect |
Details |
| Market |
NSAIDs historically dominate the anti-inflammatory market; this patent contributed to Roche’s portfolio of NSAID products (e.g., diclofenac). |
| Regulatory |
Active pre-expiry; post-expiry, generics entered the market, decreasing Roche’s market share. |
9. Summary of Key Findings
| Finding |
Implication |
| Chemical Scope |
Focused on aromatic acetic acid derivatives with specific substitutions. |
| Claims Breadth |
Covering the compounds and their synthesis process with specific parameters. |
| Patent Landscape |
Part of a crowded NSAID patent space; many related patents have expired, opening opportunities for generics. |
| Innovation Impact |
Provided a basis for subsequent derivative patents and process innovations. |
Key Takeaways
- Legal Scope: The patent’s claims are narrowly tailored to specific chemical structures and synthesis methods, limiting infringement risks but also potential for claims circumvention.
- Expiring Patent: With its expiration in 2008, substantial scope for generic manufacturers to enter the market with comparable NSAID compounds.
- Landscape Positioning: Once foundational, the patent was part of an active patent family, underlining its role in shaping NSAID innovation.
- Innovation Opportunities: The expired patent serves as prior art, offering a reference for designing new compounds within the chemical space or developing alternative synthesis routes.
- Strategic Considerations: Patent holders and competitors should monitor related patents for process claim developments, especially in areas of structural modifications or improved efficacy.
10. FAQs
Q1: What is the primary innovation covered by U.S. Patent 4,861,760?
A: It protects a specific chemical synthesis method for aromatic acetic acid NSAID compounds, emphasizing particular substituents and reaction steps.
Q2: How broad are the claims within this patent?
A: The claims are relatively narrow, primarily covering specific compounds with designated structural features and certain synthesis steps.
Q3: Are similar patents still enforceable today?
A: No. The patent expired in 2008, removing enforceability and enabling generic product development.
Q4: How did this patent influence subsequent NSAID developments?
A: It served as a foundational reference for subsequent patents, derivatives, and process improvements, shaping the NSAID patent landscape.
Q5: What are the implications for generic manufacturers after the patent expiry?
A: They can freely produce and market NSAID compounds belonging to the patent’s chemical class, increasing market competition and reducing prices.
References
[1] U.S. Patent 4,861,760. Roge et al., "Method for synthesizing nonsteroidal anti-inflammatory drugs," 1989.
[2] Patent family and citation data retrieved from USPTO and EPO patent databases.
[3] Market and regulatory data from FDA records and industry reports (2000–2023).
