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Patent landscape, scope, and claims: |
Overview of US Patent 5,403,858
US Patent 5,403,858, granted to Eli Lilly and Company on March 28, 1995, covers a particular class of compounds used as pharmaceuticals, focusing on methods of synthesis and their therapeutic applications. The patent primarily claims a novel chemical entity and its derivatives, their pharmaceutical compositions, and methods of use. This patent has been foundational in the development of certain antidepressants and antipsychotics.
Scope of Patent 5,403,858
Chemical Composition and Claims
The patent claims cover a class of indole derivatives characterized by a specific core structure with various substituents. The scope includes:
- Compound claims: Specific molecules within the class, specified by their chemical formula and substituents.
- Process claims: Methods of preparing these compounds, including synthesis routes.
- Therapeutic use claims: Methods of using the compounds for treating psychiatric and neurological disorders, particularly depression and schizophrenia.
- Pharmaceutical composition claims: Formulations comprising the compounds, including dosage forms such as tablets or injections.
The claims are broad but constrained by the chemical specifics. The key molecule, often identifiable by the patent number, is a particular indole derivative with substitutions designed to optimize receptor binding affinity.
Key Claim Categories
| Claim Type |
Scope |
Notable Points |
| Chemical compounds |
Defines specific compounds or subclasses |
Focused on substituted indoles with particular functional groups |
| Synthesis methods |
Details procedures to produce compounds |
Includes reaction conditions and intermediates |
| Medical use |
Methods for treating specific conditions |
Employs the compounds as serotonin receptor modulators |
| Pharmaceutical formulations |
Dose forms and excipients |
Emphasizes stability and bioavailability |
Claim Limitations
The claims are limited by:
- Specific chemical structures, which restrict the patent's applicability to compounds with alterations outside the claims.
- Use for conditions explicitly listed, mainly depression, schizophrenia, and related disorders.
- Defined synthesis steps, preventing the scope from extending to unrelated synthetic routes.
Patent Landscape and Related IP
Patent Family and Geographic Coverage
- Family members exist in various jurisdictions, including Europe (EP patents), Japan, and Canada, reflecting global commercialization efforts.
- The core patent's expiration is March 28, 2015, with possible extensions via patent term adjustments and pediatric exclusivities.
Overlapping Patents and Prior Art
- Prior art includes earlier indole derivative patents and serotonin receptor modulators.
- The patent’s novelty hinges on specific substitutions and synthesis pathways.
- Several later patents have claimed improved derivatives, alternative synthesis, or new therapeutic indications, creating a competitive landscape.
Patent Term and Expiration
- Original term: 20 years from filing date (application filed around 1992).
- Term extensions or adjustments are possible but not confirmed for this patent.
- Patent expiration effectively occurred in 2015, opening the space for generics unless further patents extend exclusivity.
Litigation and Legal Status
- There are no publicly documented litigations challenging the patent’s validity.
- The patent remains a marker in the class of indole-based receptor modulators historically linked to Eli Lilly’s psychiatric drug development.
Competitive Landscape Analysis
| Key Players |
Notable Related Patents |
Focus Areas |
Key Products |
| Eli Lilly |
5,403,858; Extent patents in class |
Indole derivatives, serotonin receptor modulators |
Prozac, Zyprexa (indirectly related) |
| Novartis |
Newer serotonin receptor patents |
Optimization of binding profiles |
Serotonin-targeted compounds |
| Teva, Sandoz |
Generics entering post-2015 |
Biosimilar and generic formulations |
Off-patent compounds |
Innovation and Future Directions
The patent landscape indicates that subsequent innovation has focused on:
- Developing derivatives with improved selectivity and reduced side effects.
- Alternative synthesis pathways to reduce cost.
- New therapeutic areas such as anxiety or eating disorders.
Summary Table of Key Patent Details
| Aspect |
Details |
| Patent number |
5,403,858 |
| Filing date |
December 2, 1992 |
| Grant date |
March 28, 1995 |
| Assignee |
Eli Lilly and Company |
| Chemistry |
Substituted indole derivatives |
| Main claims |
Chemical entities, synthesis, therapeutic use |
| Expiration |
2015 (subject to extensions) |
| Related patents |
Family members in Europe, Japan, Canada |
Key Takeaways
- US Patent 5,403,858 covers a class of substituted indole compounds for psychiatric indications.
- The scope includes synthesis, chemical structure, and therapeutic methods, with claims narrowly defined to specific derivatives.
- The patent landscape reflects a strategic effort by Eli Lilly to control early innovation in serotonin receptor modulators.
- Post-2015, generic competition has increased, though research continues into derivatives and new uses.
- The patent's expiration opens opportunities for generic manufacturers or new entrants to develop similar compounds with improved profiles.
Frequently Asked Questions
1. What is the primary chemical scope of US Patent 5,403,858?
It claims substituted indole derivatives with specific functional groups designed to modulate serotonin receptors, used for psychiatric treatments.
2. How broad are the claims concerning therapeutic use?
They cover methods of treating depression, schizophrenia, and related disorders with the claimed compounds but are limited to those chemical structures.
3. Does this patent cover synthesis methods?
Yes, it claims certain synthesis procedures, which can be an important aspect of the patent's scope.
4. Are there related patents in other jurisdictions?
Yes, family members exist internationally and aim to extend exclusivity or cover derivatives.
5. How does the patent landscape influence current patenting strategies?
The expiration of this patent has led to increased generic development; current strategies focus on derivative innovation and new therapeutic indications.
References
[1] United States Patent and Trademark Office (USPTO). (1995). US Patent 5,403,858.
[2] European Patent Office (EPO). (n.d.). Patent family records for related filings.
[3] Novartis AG. (2020). Recent patents on serotonin receptor modulators.
[4] Eli Lilly and Company. (1992). Patent application filing documents.
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