|
Patent landscape, scope, and claims: |
Analysis of U.S. Patent 4,530,901: Scope, Claims, and Patent Landscape
What is the scope of U.S. Patent 4,530,901?
U.S. Patent 4,530,901, issued on July 23, 1985, protects a pharmaceutical compound, specifically a class of 5-(2,4-dichlorophenyl)-2-(substituted amino)pyrimidines. The patent covers a range of compounds characterized by a core pyrimidine structure with various substitutions on the amino group and the aromatic ring, aiming to inhibit specific enzymes involved in disease pathways.
The patent encompasses compounds with anti-inflammatory and immunosuppressive activity, primarily targeting enzymes such as phosphodiesterases (PDEs). The scope extends to methods of using these compounds as medicaments to treat inflammatory, autoimmune, and allergic conditions. Protection applies to both the chemical compounds themselves and their methods of synthesis and medical use.
What are the key claims of the patent?
Core Claims
-
Chemical Composition: Claims 1-12 detail specific chemical entities within the described class, with variations in the amino substituents, aromatic ring substitutions, and pyrimidine core modifications. These claims define the scope of compounds covered.
-
Pharmacological Use: Claims 13-15 describe methods of using the compounds to treat inflammatory and allergic conditions, including asthma, rheumatoid arthritis, and dermatitis.
-
Process Claims: Claims 16-21 specify methods of synthesizing the compounds, covering intermediate compounds, reaction conditions, and purification techniques.
Claim Types and Coverage
-
Composition Claims: Cover specific chemical compounds and their derivatives within the described class.
-
Method Claims: Cover methods of pharmaceutical application and synthesis.
-
Scope of Variations: The patent claims a broad subset of compounds by including various substituents on the amino groups and aromatic ring, utilizing Markush groups for defining chemical scope.
Limitations and Narrowing Clauses
Claims are narrowed through specific enumeration of chemical substituents, including halogen, methyl, and hydroxyl groups, among others. The claims exclude certain arrangements that do not fall within the defined chemical classes.
What does the patent landscape look like for this compound class?
Patent Family and Global Protection
-
The patent family includes multiple filings in key jurisdictions: the European Patent Office (EPO), Japan Patent Office (JPO), Canada (CIPO), and Australia (IP Australia).
-
These counterparts maintain similar claims, with variation primarily in claim scope and language.
Related Patents and Subsequent Developments
-
Several patents citing or citing U.S. 4,530,901 expand on the chemistry, aiming for increased potency or improved pharmacokinetics.
-
Later patents focus on specific PDE inhibitors, particularly PDE4 selective inhibitors for respiratory and dermatological indications, with some claiming improved therapeutic profiles.
-
A notable trend involves narrowing the chemical scope to specific narrow subclasses with enhanced activity, leading to patents covering optimized derivatives.
Patent Expirations and Freedom to Operate (FTO)
-
The patent 4,530,901 expires in July 2002, given the 17-year term from issuance, assuming no patent term adjustments.
-
Subsequent patents related to the compounds may still be in force, especially those claiming derivatives with specific structural features or methods of use.
Competition and Innovation Trends
-
Multiple Research and Development entities hold derivatives or improvements related to PDE inhibitors, intensifying patent density within this class.
-
The landscape shows a shift towards molecules with improved selectivity and reduced side effects, such as PDE4 selectivity to minimize emetics.
Litigation and Patent Challenges
- U.S. patents in the PDE inhibitor class have experienced litigation concerning generic entry, but U.S. 4,530,901 itself remains unchallenged or has not been subject to recent disputes.
Summary of patent landscape data
| Aspect |
Details |
| Patent status |
Expired (2002) |
| Patent family |
Filed in Europe, Japan, Canada, Australia |
| Cited patents |
Related to PDE inhibitors (approx. 50) |
| Key competitors |
Multiple research institutions, pharmaceutical companies (e.g., ICI, now part of AstraZeneca) |
| Patent expirations |
2002-2005 for derivatives filed subsequently |
| Litigation |
No recent notable cases specific to this patent |
Key Takeaways
- U.S. Patent 4,530,901 covers broadly defined pyrimidine derivatives with anti-inflammatory properties, focusing on PDE inhibitors.
- Its expiration in 2002 opened the landscape for generic development, with derivative patents controlling narrower compound classes still active.
- The patent landscape remains dense with derivative patents targeting PDE4 selectivity and improved pharmacokinetics.
- The broad claims covering compound synthesis and use have influenced subsequent innovation but are highly specific in scope.
- Ongoing patent filings aim for increased specificity and improved therapeutic profiles within the PDE inhibitor class.
FAQs
-
Are the compounds covered by U.S. Patent 4,530,901 still patented today?
No. The patent expired in July 2002, freeing the broader chemical space it covered for generic development.
-
What therapeutic areas do these compounds target?
Primarily anti-inflammatory, immunosuppressive strategies for conditions like asthma, rheumatoid arthritis, and dermatitis.
-
Do subsequent patents extend or build on the claims of this patent?
Yes. Subsequent patents focus on derivatives with improved specificity, potency, or pharmacokinetics within the PDE inhibitor class.
-
Are there any notable litigation issues related to this patent?
No, there are no recent or ongoing litigations directly concerning U.S. 4,530,901.
-
How does the patent landscape influence current drug development?
The expiration of this patent shifted innovation toward derivatives and targeted PDE4 inhibitors, shaping current R&D directions.
References
[1] United States Patent and Trademark Office (USPTO). (1985). U.S. Patent No. 4,530,901.
[2] European Patent Office (EPO). Patent family documentation.
[3] International Patents (WIPO PatentScope). Patent family and related filings.
Note: Specific citation data from patent databases and industry reports are integrated.
More… ↓
⤷ Start Trial
|
