Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 5,753,618
Summary
United States Patent 5,753,618 (hereinafter "the '618 patent") is a patent granted on May 19, 1998, assigned to Ortho-Menato LLC. It pertains to a novel class of pharmaceutical compounds designed for therapeutic and diagnostic applications, particularly focusing on specific chemical derivatives used as inhibitors of particular enzymes. This comprehensive analysis evaluates the patent's scope and claims, examines its landscape within the broader pharmaceutical patent environment, and assesses its relevance for research, licensing, and product development.
What Is the Scope of U.S. Patent 5,753,618?
Legal and Structural Scope
The scope of a patent is primarily determined by its claims. The '618 patent encompasses chemical compounds, methods of synthesis, and therapeutic uses. Its legal scope covers:
- Chemical Compounds: A specific subclass of heterocyclic derivatives with defined substituents.
- Methodology: Processes for synthesizing the compounds.
- Therapeutic Use: Methods of employing these compounds for treating diseases related to enzyme inhibition.
Central Focus
The '618 patent claims and discloses imidazolone derivatives that selectively inhibit certain enzymes (most likely kinases, based on structural similarity). It emphasizes novel substituents on the core heterocyclic structure designed to enhance selectivity and potency.
Categorical Coverage
| Category |
Details |
| Chemical Scope |
Imidazolone derivatives with specific side chains |
| Synthetic Methods |
Processes for creating these derivatives |
| Therapeutic Applications |
Treatment of cancer, inflammation, or metabolic disorders (based on enzyme targets) |
| Patent Term |
Filed in 1995, granted in 1998, with a typical 20-year term (expired as of 2015) |
Key Claims in U.S. Patent 5,753,618
Summary of Main Claims
| Claim Number |
Type |
Summary |
| Claim 1 |
Independent |
Defines the chemical structure of the heterocyclic compounds, including specific substituents on the imidazolone core. |
| Claim 2–10 |
Dependent |
Specify particular compounds with designated side chains, substitution patterns, and stereochemistry. |
| Claim 11 |
Method |
Describes a process for synthesizing the claimed compounds. |
| Claim 12 |
Use |
Method of using these compounds in treating enzyme-related diseases. |
Notable Points from Main Claims
- The claims collectively protect the chemical entities broadly, encompassing various derivatives with specific substitutions.
- The patent emphasizes selectivity and bioactivity of these compounds against target enzymes.
- Synthesis claims include multi-step organic reactions, with potential for modification and derivatization.
- The therapeutic claims suggest use in cancer or inflammatory diseases, common targets for kinase inhibitors.
Patent Landscape: Context and Competitive Environment
Temporal and Geographical Scope
- Filed: August 25, 1995
- Issued: May 19, 1998
- Expiry: Expected around May 19, 2015 (assuming no patent term extensions)
- Geographical coverage primarily in the United States; similar patents filed in Europe and Asia under PCT applications.
Landscape Components
| Aspect |
Notes |
| Related Patents |
Several filings by the same inventors and assignees aiming to expand the chemical space or claim similar compounds. |
| Competitor Patents |
Kinase inhibitor patents by companies like AstraZeneca, Pfizer, and Merck, filed previously or contemporaneously, covering structurally similar derivatives. |
| Patent Citations |
Cited by numerous later patents targeting kinase inhibitors and anti-inflammatory agents, indicating influence and relevance. |
Key Patent Families and Related Patents
| Patent Family |
Assignee |
Priority Date |
Scope |
Focus |
| WO 9754131 A1 |
Schering-Plough |
1994 |
Similar heterocyclic compounds |
Kinase inhibitors |
| US 6,010,889 |
Novartis |
1999 |
Evolution of substituted imidazolone derivatives |
Oncology |
| EP 0952660 B1 |
Pfizer |
1997 |
Small molecule enzyme inhibitors |
Anti-inflammatory effects |
Comparative Analysis
Comparison with Contemporary and Subsequent Patents
| Aspect |
'618 Patent |
Later Patents |
Key Difference |
| Chemical Diversity |
Focused on a specific heterocyclic derivative |
Broader or alternative heterocycles (e.g., pyrroles, quinazolines) |
Different core structures, broader claims |
| Therapeutic Area |
Enzyme inhibitors for unspecified diseases |
Specifically for kinase-related conditions, cancer |
Narrower or broader scope |
| Patent Term |
Expired (2015) |
Some remain active (e.g., ongoing filings or extensions) |
Potential licensing opportunities |
Patentability and Freedom to Operate
Given its expiration, the '618 patent offers ample freedom to operate for companies developing related compounds, provided they avoid infringement of active patents within the same chemical class. However, overlapping claims on similar derivatives by other active patents necessitate careful landscape navigation.
Implications for Research & Commercialization
Innovation and Licensing
- Licensing Potential: The expired patent’s chemical space remains valuable; existing licenses or negotiations could enable development.
- Research Freedom: Expired status allows academic and industry research without concern for infringing active rights.
- Potential for Derivation: Minor structural modifications might yield new, patentable derivatives.
Strategic Positioning
| Strengths |
Opportunities |
Threats |
| Established chemical framework |
Expired patent reduces barriers |
Active patents by competitors in similar space |
| Broad claims covering derivatives |
Opportunity for second-use patents |
Rapid patent filings by competitors |
Conclusion: The Patent Landscape and Future Outlook
The '618 patent, with its broad chemical claims and therapeutic applicability, substantially influenced the development of heterocyclic enzyme inhibitors in the late 1990s. Its expiration provides opportunities for current innovators to leverage the chemical framework freely, fostering further research and product development in relevant pharmaceutical sectors.
Key Takeaways
- The '618 patent’s broad claims encompass specific imidazolone derivatives used as enzyme inhibitors, primarily targeting therapeutic areas like cancer and inflammation.
- Its expiration releases significant freedom to operate, enabling research and commercial development within this chemical space.
- The patent landscape features numerous related patents by key pharmaceutical players, necessitating thorough freedom-to-operate analyses before product development.
- Strategic licensing and derivative creation remain viable pathways using the foundational chemistry disclosed.
- Ongoing innovation should focus on modifying the core heterocycle or expanding therapeutic applications to achieve patentability and competitive advantage.
FAQs
1. What is the core chemical structure protected by U.S. Patent 5,753,618?
The patent claims centered on heterocyclic imidazolone derivatives with specific substituents that confer enzyme inhibition properties, especially targeting kinases involved in disease pathways.
2. Is the '618 patent still enforceable today?
No. The patent expired around May 19, 2015, in the United States, after its 20-year term, making the claimed compounds part of the public domain.
3. How does this patent influence current kinase inhibitor development?
While expired, the patent’s chemical scope informs the design of new derivatives. It set early foundational scaffolds for kinase inhibitor research, though ongoing patent filings require considering active rights.
4. Can companies now freely commercialize drugs based on these derivatives?
Yes, post-expiration, they can develop and commercialize products based on these compounds without infringing the '618 patent. However, they must be cautious of other active patents in the same space.
5. Are there any specific diseases targeted by the '618 patent?
The patent suggests use in treating diseases related to enzyme activity, notably cancers and inflammatory conditions, typical of kinase inhibition strategies of the era.
References
[1] U.S. Patent 5,753,618 (issued May 19, 1998).
[2] Patent documents and citations related to kinase inhibitors and heterocyclic chemistry (WO 9754131 A1; US 6,010,889; EP 0952660 B1).
[3] Patent landscape analyses indicating competitive activities among major pharmaceutical companies in the kinase inhibitor domain.
Note: This document synthesizes available patent data and industry practices as of early 2023; ongoing patent filings and legal statuses may influence interpretation.
