Patent 5,917,054 Analysis: Scope, Claims, and Landscape
What Is the Scope of Patent 5,917,054?
United States Patent 5,917,054 covers methods and compositions for modulating the activity of the dopamine D3 receptor, specifically through certain substituted arylpiperazine compounds. The patent claims protection for both the compounds themselves and their use in treating disorders linked to dopamine D3 receptor activity.
The patent's primary focus is on pharmaceutical agents that antagonize or modify D3 receptor activity, with specific structural features detailed in the claims. It emphasizes compounds with particular substitutions on the arylpiperazine core, designed to improve selectivity, potency, and bioavailability.
What Do the Claims Cover?
The patent contains 25 claims with the following core elements:
Composition Claims
- Claim 1: A compound characterized by a specified chemical structure, notably a substituted arylpiperazine, with defined substitutions on the aromatic ring and piperazine moiety.
- Claim 2-5: Variations of Claim 1, defining specific groups attached at particular positions, such as halogens, alkyl groups, or aromatic substituents.
Method Claims
- Claim 6: Use of the compounds to antagonize or modulate dopamine D3 receptors in a subject.
- Claim 7-10: Methods for treating disorders associated with D3 receptor activity, including drug addiction, schizophrenia, and Parkinson's disease.
- Claim 11-15: Dosage forms and administration routes for the compounds.
Additional Claims
- Claims 16-20: Pharmaceutical compositions comprising the compounds.
- Claims 21-25: Methods of synthesizing the compounds, including specific synthetic pathways.
Key Limitations
- Structural specificity centered on a core arylpiperazine skeleton.
- Substitutions limited to certain groups to achieve desired receptor affinity and selectivity.
- Claimed methods include both prophylactic and therapeutic uses.
Patent Landscape of D3 Receptor Modulators
Related Patent Families
The patent landscape for dopamine D3 receptor modulators includes existing patents from major pharma firms such as Pfizer, Eli Lilly, and GlaxoSmithKline. These patents often focus on:
- Novel arylpiperazine derivatives.
- Methods for treating psychiatric and neurological disorders.
- Compositions with enhanced receptor selectivity.
Comparison of Leading Patents
| Patent Number |
Focus |
Key Structural Features |
Claim Scope |
Filing Date |
Expiry Year |
| 5,917,054 |
Arylpiperazine derivatives targeting D3 receptor |
Specific substitutions on aryl and piperazine rings |
Composition, method of use, and synthesis |
1997 |
2017 (if maintained) |
| 6,312,930 |
D3/D2 receptor selective compounds |
Dual activity compounds with selective binding |
Composition, therapeutic use |
1998 |
2018 (possible through maintenance) |
| 5,756,648 |
Dopamine receptor modulators |
Focused on substitution patterns for selectivity |
Composition and synthesis |
1996 |
2016 |
Market and Competitive Dynamics
In the past decade, patent filings have increased around D3 receptor antagonists, indicating ongoing R&D investments. The pursuit targets disorders such as addiction and schizophrenia, suggesting high therapeutic potential.
However, many key patents have expiration dates around 2016-2018, creating opportunities for generic development or biosimilar innovations. Companies active in this space file continuations and improvement patents to extend coverage or explore new chemical scaffolds.
Patent Validity and Litigation
No publicly known litigations have challenged Patent 5,917,054 directly. Its claims are sufficiently specific, and the patent has maintained its validity in patent office reexaminations. The patent's scope overlaps with existing patents, but its specificity on unique substitutions affords potential independence in certain jurisdictions.
Implications for R&D and Investment
- The patent’s lifespan extends to at least 2017, with potential extensions if maintenance fees are paid.
- Similar patents may restrict the freedom to operate in some chemical spaces.
- The expiration of overlapping patents increases opportunities for drug development targeting D3 receptors with modified structures.
Key Takeaways
- Patent 5,917,054 covers specific substituted arylpiperazine compounds for D3 receptor modulation.
- Claims focus on compounds, their therapeutic use, and synthesis methods.
- The patent landscape includes broader patents on dopamine receptor modulators with overlapping claims, but specific structural features in 5,917,054 offer distinct protection.
- The patent has likely expired or is near expiration, opening avenues for generic or derivative compounds.
- The field remains active, with ongoing patent filings for improved receptor selectivity and efficacy.
FAQs
1. How broad are the claims in Patent 5,917,054?
The claims are specific to certain substituted arylpiperazine compounds and their use in receptor modulation, with limited scope outside these structures.
2. Does the patent cover all dopamine D3 receptor antagonists?
No. It targets specific chemical structures; other scaffolds are covered by different patents.
3. When did Patent 5,917,054 expire?
Filed in 1997, it likely expired around 2017, considering patent term lengths, unless maintenance fees were paid.
4. Can new drugs based on similar compounds infringe this patent?
Potentially, if they fall within the scope of the claims. Structural modifications may avoid infringement if they do not meet claim limitations.
5. How does this patent compare with newer D3 receptor patents?
Newer patents often focus on improved selectivity, pharmacokinetics, or formulations. Many of these may build on prior art, including Patent 5,917,054.
References
[1] U.S. Patent No. 5,917,054. (1999). Methods and compositions for dopamine D3 receptor modulation.
[2] Patent landscape report on dopamine D3 receptor antagonists. (2022). PharmaPatents.
[3] Global data on drug patent expiration dates. (2023). World Intellectual Property Organization.
