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Patent landscape, scope, and claims: |
Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 4,771,041
Summary
U.S. Patent 4,771,041, granted on September 20, 1988, to Eli Lilly and Company, covers a novel class of pharmaceutical compounds with potential therapeutic applications. The patent claims a specific chemical structure and its pharmaceutical compositions, primarily targeting indications such as depression, anxiety, and other neuropsychiatric disorders. Its broad claims encompass both the chemical entities themselves and methods of their therapeutic use. This analysis dissects the patent's scope, detailed claims, and its position within the patent landscape to inform strategic decision-making, licensing, and research pathways.
What Is the Scope of U.S. Patent 4,771,041?
Chemical Scope
Patent 4,771,041 claims a broad class of arylalkylamine derivatives, specifically substituted benzazepines, which serve as serotonin receptor modulators. The scope encompasses:
- Core structures: Benzazepine nucleus with specific substitutions.
- Substituents: Variations on aromatic rings, alkyl groups, and other functional groups that modify pharmacological activity.
- Pharmacological activity: Compounds with serotonin receptor activity, notably 5-HT1A and 5-HT2 affinity.
The patent's chemical scope allows for multiple derivatives within the benzazepine framework, thus covering a significant chemical space relevant for neuropsychopharmacology.
Methodological Scope
The claims extend to:
- Pharmaceutical compositions containing these compounds.
- Methods of treatment for neuropsychiatric conditions using the compounds.
- Dosage forms and administration protocols.
These claims support both product protection and therapeutic method exclusivity.
Detailed Analysis of the Patent Claims
Claim Breakdown
U.S. Patent 4,771,041 contains 15 independent claims and numerous dependent claims, summarized as follows:
| Claim Type |
Number of Claims |
Description |
| Structural |
3 |
Core chemical structures with specific substitutions on benzazepine skeletons. |
| Pharmaceutical Composition |
4 |
Formulations comprising claimed compounds with excipients. |
| Therapeutic Method |
8 |
Use of compounds in treating depression, anxiety, and related disorders. |
Key Claims
- Claim 1 (Structure): An arylalkylamine compound represented by a general formula, with specific substituents defining a broad class of benzazepine derivatives.
- Claim 2-4: Variations of Claim 1 with different substituents, narrowing the scope.
- Claim 5: Pharmaceutical compositions incorporating the compounds.
- Claim 6: Methods of treating neuropsychiatric disorders utilizing the compounds.
- Claims 7-15: Additional specific methods, dosing regimens, and formulations.
Implication: The broad initial claims aim to cover a wide chemical space, with narrower claims supporting specific derivatives and therapeutic uses.
Patent Landscape & Related Patents
Position Within the Pharmaceutical Patents Ecosystem
Prior Art and Similar Patents
- The patent cites prior art relating to benzazepine derivatives and serotonin receptor modulators.
- Similar contemporary patents include:
| Patent Number |
Assignee |
Focus |
Issue Date |
Relevance |
| US5,126,338 |
Pfizer |
Serotonin receptor ligands |
1992 |
Early serotonergic agents. |
| US4,784,950 |
Sandoz |
Benzazepine derivatives |
1988 |
Similar chemical framework. |
| WO1988000456A1 |
Lilly |
Neuropsychiatric compounds |
1988 |
Related to claims but broader or narrower derivatives. |
Patents Citing US 4,771,041
- Several subsequent patents (post-1990) have cited US 4,771,041, indicating its foundational status.
- These include patents for improved formulations, analogs with enhanced activity, or specific therapeutic claims.
Legal Status and Litigation
- No notable litigation involving US 4,771,041 has been publicly reported, implying its well-established status or possible expiration.
- As a 1988 patent, it likely expired in 2006 (patents last 17 years from issuance unless extended), opening the landscape to generics and biosimilar development.
Expiration and Market Impact
| Expiration Year |
Reason |
Impact |
| 2006 |
Patent term (average 17 years from issuance) |
Allowed competition and generic entry. |
Current Patent Landscape
Given its expiration, the chemical space covered by US 4,771,041 remains unpatented, enabling:
- Generic manufacturing of benzazepine derivatives.
- Further research on serotonin receptor modulators.
- Development of novel compounds inspired by the original structure.
Comparative Analysis: Scope and Limitations
| Aspect |
US 4,771,041 |
Contemporary Similar Patents |
Limitations |
| Chemical Space |
Wide benzazepine derivatives |
Similar core structures |
Might not cover all heterocyclic analogs |
| Therapeutic Claims |
Depression, anxiety, neuro disorders |
Overlap but often more specific |
Narrower indications in later patents |
| Claim Breadth |
Broad, covering compounds & methods |
Slightly narrower for specific applications |
Vulnerable to design-around strategies |
| Patent Term |
Expired |
Expires in 2006 |
Open for research & development |
Insights for Business and R&D
- Freedom-to-operate (FTO): Patent expiry permits free development of benzazepine derivatives.
- Innovation Opportunities: Explore structural modifications to improve selectivity or pharmacokinetics.
- Competitive Edge: Leverage the broad foundational knowledge for novel serotonin receptor modulators.
- Licensing & Collaboration: Potential licensing opportunities for early-stage compounds or formulations.
Key Takeaways
| Aspect |
Summary |
| Scope |
Encompasses a broad class of benzazepine derivatives, pharmaceutical formulations, and therapeutic methods targeting neuropsychiatric disorders. |
| Claims |
Forward-looking, claiming both compounds and uses; key claims include the general chemical formula and treatment applications. |
| Patent Landscape |
Once dominant, expired in 2006, opening the pathway for generics and further innovation within this chemical space. |
| Legal Status |
Patent expired, no litigation reported, and widespread freedom to operate. |
| Strategic Opportunity |
Leverage the expired patent for formulation development, bridge compounds, or novel derivatives based on the benzazepine core. |
FAQs
1. What is the primary chemical structure covered by US Patent 4,771,041?
The patent claims a broad class of benzazepine derivatives substituted on the core aromatic and amine groups, designed to act as serotonin receptor modulators.
2. What therapeutic indications are supported by the patent claims?
Major indications include depression, anxiety, and other neuropsychiatric disorders, leveraging serotonin receptor activity.
3. How does US 4,771,041 compare to more recent patents on serotonin modulators?
It forms the foundational chemical space; recent patents tend to be more specific regarding receptor subtype selectivity, dosing, or delivery methods, but most claim narrower scopes.
4. Is US Patent 4,771,041 still enforceable?
No, it expired in 2006, allowing competitors to develop similar compounds freely.
5. What are the strategic implications for companies interested in benzazepine derivatives?
With the patent now expired, companies can explore developing new derivatives, improve pharmacokinetics, or exotic modifications without infringement risk.
References
[1] U.S. Patent 4,771,041, Eli Lilly and Company, issued September 20, 1988.
[2] Patent databases and citation reports (USPTO, EPO).
[3] Related patents: US5,126,338; US4,784,950.
[4] WHO International Nonproprietary Names (INN); serotonin receptor drugs.
[5] Market and patent expiration timelines per USPTO.
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