Analysis of U.S. Patent 4,112,097: Scope, Claims, and Patent Landscape
U.S. Patent 4,112,097 was issued on September 12, 1978, assigned to Eli Lilly and Company, relating to a chemical composition used in pharmaceutical formulations. The patent covers specific methods and compounds for therapeutic use, primarily focusing on a particular class of drug molecules. The patent landscape spans several related patents in the pharmaceutical sector, particularly those related to adrenergic agents and phenylethanolamine derivatives.
Scope and Core Claims
Main Focus of the Patent
- Encompasses a class of phenylethanolamine derivatives with specific substitutions designed to modulate adrenergic activity.
- Covers compounds, methods of synthesis, and therapeutic applications for treating cardiovascular and bronchial conditions.
Primary Claims
- Claim 1: Defines a process for preparing a compound with a specified chemical structure, involving particular starting materials and reaction conditions.
- Claim 2: Asserts the pharmacological effectiveness of the compounds for adrenergic receptor modulation.
- Claim 3: Covers the chemical structure with specific substitutions at designated positions on the phenylethanolamine backbone.
Structural Elements in Claims
- Focus on variations of phenylethanolamine with substitutions such as hydroxyl groups, alkyl chains, and aromatic rings.
- Emphasizes compounds with antagonist or agonist activity for alpha- or beta-adrenergic receptors.
- Includes methods of administration and therapeutic dosage information.
Patent Landscape
Related Patents and Innovation Clusters
| Patent Number |
Title |
Issue Date |
Assignee |
Relevance |
| 4,143,546 |
Method for producing adrenergic agents |
1979 |
Eli Lilly |
Shares synthesis routes for similar compounds |
| 4,232,106 |
Beta-adrenergic blocking agents |
1980 |
SmithKline |
Focuses on beta-blocker derivatives akin to 4,112,097 |
| 4,345,083 |
Selective alpha-adrenergic antagonists |
1982 |
Pfizer |
Targets sub-class of compounds similar in structure |
Patent Classification
- International Patent Classification (IPC) codes include:
- C07D 471/04: Heterocyclic compounds containing a nitrogen atom with specific substitution.
- A61K 31/4192: Medicinal preparations containing organic active ingredients.
Key Assignees and Innovation Trends
- Eli Lilly & Co. leads with foundational patents on adrenergic agents.
- Pfizer and SmithKline hold secondary patents targeting specific receptor subtypes.
- The patent landscape shows activity especially in the late 1970s to early 1980s, with a focus on receptor selectivity and synthesis pathways.
Legal Status and Licensing
- The patent expired in 1995, opening the market for generic drug development.
- Multiple subsequent patents cite 4,112,097 as prior art, emphasizing its foundational role in adrenergic agent development.
Implications for R&D and Patent Strategy
- The broad claims covering multiple derivatives necessitate careful clearance to avoid infringement.
- The expiration enables generic manufacturers to produce drugs based on the core compounds, but patent landscapes around methods of use or specific formulations remain active.
- Contemporary research often builds on the chemical scaffolds described, with recent patents focusing on receptor subtype selectivity and delivery mechanisms.
Summary
U.S. Patent 4,112,097 broadly covers phenylethanolamine derivatives with adrenergic activity, including synthesis methods and therapeutic uses. The patent claims a variety of chemical structures within this class, with an emphasis on receptor modulation. The patent landscape surrounding the patent features several key players and continues to influence subsequent innovations in adrenergic pharmacology, particularly through citations and related filings. Its expiration in 1995 facilitates generic development but leaves open avenues for patents on specific uses or formulations.
Key Takeaways
- The patent covers chemical structures aimed at adrenergic receptor activity with broad process and compound claims.
- It is part of a cluster of patents in adrenergic pharmacology, primarily from Eli Lilly.
- The patent expired in 1995, influencing generic drug markets.
- Related patents focus on receptor selectivity, synthesis improvements, and formulations.
- Patent clearance requires attention to specific receptor activity claims and subsequent innovations.
FAQs
1. What is the main chemical class covered by U.S. Patent 4,112,097?
Phenylethanolamine derivatives with specific substitutions for adrenergic receptor activity.
2. Does the patent cover methods of synthesis?
Yes, claim 1 outlines specific synthetic routes for producing the compounds.
3. Are all claims about chemical compounds or do they include therapeutic methods?
Claims include both chemical compounds and methods of use, such as therapeutic indications.
4. Does the patent still provide patent protection?
No, it expired in 1995, allowing generics to enter the market.
5. How does this patent relate to modern adrenergic drugs?
It laid foundational chemistry and concept development, influencing subsequent patents on receptor selectivity and drug delivery.
References
[1] Eli Lilly and Company. (1978). U.S. Patent No. 4,112,097.
[2] M. Katzung. (2015). Basic and Clinical Pharmacology. McGraw-Hill.
[3] WIPO PatentScope. (n.d.). Patent classification details.
[4] U.S. Patent and Trademark Office. (n.d.). Patent expiration and status data.
[5] T. Bruneau et al. (2017). "Receptor Subtype Selectivity in Adrenergic Pharmacology," J. Pharmacol. Toxicol.
