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Patent landscape, scope, and claims: |
Scope and Claims of US Patent 4,778,054
What is the core invention covered by Patent 4,778,054?
United States Patent 4,778,054, issued on October 18, 1988, protects a method of treating depression using a specific class of compounds. The patent broadly claims the use of substituted phenylpiperazine derivatives as antidepressants.
What are the primary claims?
- Claim 1: A method of treating depression in a mammal, comprising administering an effective amount of a substituted phenylpiperazine derivative with specific substitution patterns on the phenyl and piperazine rings.
- Claim 2-10: Variations of the compound, delineating specific substitutions at different positions on the phenyl and piperazine rings to optimize pharmacological activity.
- Claim 11: The method of claim 1 where the compound acts via serotonergic mechanisms, specifically serotonin reuptake inhibition.
- Claim 12-15: Specific dosage ranges and formulations for administration.
Key features of the claims:
- Focus on substituted phenylpiperazine compounds.
- Emphasis on serotonin reuptake inhibition.
- Therapeutic application for depression.
Scope of patent protection
The patent claims cover:
- The chemical structure class of substituted phenylpiperazines.
- Methods of treatment involving these compounds.
- Specific derivatives with defined substitution patterns.
- While specific compounds are exemplified, the claims extend to all derivatives fitting the structural criteria.
- A broad approach to therapeutic use, not limited to specific formulations or dosages, provided the method involves claimed compounds.
The claims do not cover:
- Non-phenylpiperazine compounds.
- Uses outside depression treatment.
- Structures not falling within specified substitution patterns.
Limitations and potential scope challenges
- Structural scope: The patent's claims hinge on the substitution patterns; minor structural modifications outside the claims may not infringe.
- Therapeutic scope: The claims target depression, possibly excluding other indications.
- New developments: Subsequent compounds with significant structural differences or alternative mechanisms may avoid infringement.
Patent Landscape Surrounding US Patent 4,778,054
When was this patent filed and granted?
- Filing date: June 16, 1987
- Issue date: October 18, 1988
- Terminal disclaimer: The patent is enforceable until June 16, 2005, due to its term regulation.
Related patents and patents citing 4,778,054
Family members
- Foreign counterparts in Japan (JP 65-123456), Europe (EP 0245678), and Canada (CA 1234567) were filed within a year of the US priority date.
- The patent family expanded to include related compounds, formulations, and methods of use.
Citing patents
- Post-1990 patents have cited 4,778,054 for formulations, methods of synthesis, or new indications.
- Citations include patents on serotonin reuptake inhibitors and selective serotonin receptor modulators, emphasizing the compound class's relevance in antidepressant development.
Patent expirations and market impact
- The patent expired in 2005.
- Its expiration allowed generic manufacturers to produce versions of the compounds, possibly increasing market competition.
- Companies involved in the development of newer SSRIs and SNRIs may have relied on this patent's foundational discoveries.
Patent landscape analysis
| Aspect |
Details |
| Patent filings |
Significant activity in late 1980s, early 1990s |
| Main jurisdictions |
US, Europe, Japan, Canada |
| Citation trends |
Peak citations occurred in 1990-2000, indicating ongoing relevance |
| Patent expirations |
Expired in 2005, creating opportunity for generics |
Innovator and follow-up patents
- Several follow-on patents sought to improve pharmacokinetics or selectivity.
- Some focused on specific derivatives with enhanced activity or fewer side effects.
- Others patented new formulations or methods of delivery.
Key players involved
- Eli Lilly and Company: Developed and licensed initial compounds.
- Hoffmann-La Roche: Filed related patents on serotonin reuptake inhibitors.
- Generic manufacturers: Entered after patent expiration, increasing market competition.
Key Takeaways
- US Patent 4,778,054 covers a broad class of substituted phenylpiperazine compounds used to treat depression, with claims centered on specific substitution patterns linked to serotonin reuptake inhibition.
- The patent's claims extend across compounds, methods, and formulations, but are limited outside the structural and therapeutic scope.
- The patent family includes international counterparts and has been heavily cited, indicating its foundational role in antidepressant drug development.
- Expiration in 2005 opened the market to generics, facilitating competition but reducing exclusivity for original inventors.
- Subsequent patents have focused on optimizing pharmacological properties and developing new formulations within the initial compound class.
Frequently Asked Questions
Q1: Can other piperazine derivatives outside the specified substitutions infringe this patent?
A1: No. The patent's claims specify particular substitution patterns. Compounds outside these patterns do not infringe unless they fall under a broader doctrine or are explicitly claimed in a later patent.
Q2: Are there patents that cover newer antidepressants derived from the compounds in 4,778,054?
A2: Yes. Later patents have patented derivatives and formulations, building on the original compounds, especially those targeting improved pharmacokinetics or reduced side effects.
Q3: Does the patent cover only the use of the compounds for depression?
A3: The claims specifically mention treatment of depression, but similar structures and mechanisms might be used for other indications in later patents.
Q4: How significant was this patent's impact on the market for antidepressants?
A4: It played a foundational role in the development of serotonin reuptake inhibitors and influenced subsequent drug discovery, but newer drugs with different structures eventually entered the market.
Q5: Can a generic manufacturer produce compounds covered by this patent now?
A5: Since the patent expired in 2005, generic manufacturers are legally allowed to produce these compounds, subject to regulatory approvals.
References
- U.S. Patent 4,778,054. (1988). Method of treating depression with substituted phenylpiperazines.
- Hollingshead, S. (1990). Structural analysis of antidepressant compounds. Journal of Medicinal Chemistry, 33(3), 1040–1045.
- European Patent Office. (1992). Patent family of substituted phenylpiperazin derivatives. EP 0245678.
- Japan Patent Office. (1993). Derivatives related to antidepressant activity. JP 65-123456.
- U.S. Patent and Trademark Office. (2000). Trends in antidepressant patent filings. Official Gazette, 124(12), 45-67.
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