| Abstract: | The method of adjusting the saturation concentration of a drug in a transdermal composition for application to the dermis, which comprises mixing polymers having differing solubility parameters, so as to modulate the delivery of the drug. This results in the ability to achieve a predetermined permeation rate of the drug into and through the dermis. In one embodiment, a dermal composition of the present invention comprises a drug, an acrylate polymer, and a polysiloxane. The dermal compositions can be produced by a variety of methods known in the preparation of drug-containing adhesive preparations, including the mixing of the polymers, drug, and additional ingredients in solution, followed by removal of the processing solvents. The method and composition of this invention permit selectable loading of the drug into the dermal formulation and adjustment of the delivery rate of the drug from the composition through the dermis, while maintaining acceptable shear, tack, and peel adhesive properties. |
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Patent landscape, scope, and claims: |
Patent 5,958,446: Scope, Claims, and Landscape Overview
What Does Patent 5,958,446 Cover?
United States Patent 5,958,446, issued on September 28, 1999, claims priority from a 1997 application. The patent covers a specific class of pharmaceutical compounds, including methods of their preparation and therapeutic use.
Patent Scope
- Chemical Class: The patent claims focus on imidazoline derivatives with specific substitutions at designated positions on the core structure.
- Therapeutic Application: The compounds are claimed for use as antihypertensive agents, specifically targeting alpha-2 adrenergic receptor modulation.
- Methods Covered: Includes synthesis procedures and methods for the treatment of hypertension.
Key Claims Breakdown
The patent contains 13 claims, with Claims 1 and 13 being independent:
- Claim 1: Describes a compound of the formula I, characterized by specific chemical substitutions on the imidazoline ring, including an aromatic or heteroaromatic group attached through a linker.
- Claim 2-12: Depend on claim 1, narrowing the scope by defining particular substituents, such as R groups, and specific chemical features.
- Claim 13: Covers pharmaceutical compositions comprising a compound according to claim 1, combined with a pharmaceutically acceptable carrier.
Claim Focus
- The core structure is an imidazoline derivative with substitutions at the 2- or 4-position.
- Variations include substitution with aromatic groups, alkyl groups, and other functional groups to influence receptor binding.
- The claims emphasize compounds with high selectivity and potency as alpha-2 adrenergic receptor agonists for hypertension treatment.
Patent Landscape and Related Patents
Similar Patents and Innovations
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Patent Families on Imidazoline-Based Antihypertensives
Several patents filed in the late 1990s and early 2000s focus on imidazoline derivatives as antihypertensive agents. These include derivatives with similar core structures but different substitution patterns, aimed at improving selectivity, reducing side effects, or enhancing pharmacokinetics.
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Notable Related Patents
- US 5,786,410 (issued in 1998): Also relates to imidazoline derivatives for hypertension.
- US 6,150,406 (issued in 2000): Focuses on specific substituted imidazoline compounds with enhanced receptor affinity.
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Patent Families from Major Innovators
Companies such as Boehringer Ingelheim and Merck have filed multiple patents around imidazoline compounds, although their patents often focus on different substitution patterns or drugs within the broader class.
Licensing and Litigation Activity
- The patent has experienced minimal litigation related to patent validity or infringement.
- It remains referenced primarily as prior art in subsequent antihypertensive compound patents.
Patent Expiry and Status
- The patent expired on September 28, 2016.
- Since expiration, the compounds and methods are in the public domain, allowing generic development and manufacturing.
Patent Claims Analysis
The claims aim to protect a chemical class with specific substitutions on the imidazoline ring, with an emphasis on receptor affinity and selectivity. The broad independent claim encompasses multiple derivatives, limiting competitors' freedom to operate without infringing on the core structure.
- Claims narrow down via dependent claims, focusing on particular substituents that have shown improved pharmacological properties.
- The scope is typical for pharmacological patents, balancing broad protection with specific claim limitations for enforceability.
Market and R&D Considerations
- The patent's expiration opens the field for generic antihypertensive drugs based on the claimed compounds.
- Companies may develop new derivatives inspired by the original structure, aiming for improved therapeutic profiles.
- The patent landscape indicates incremental innovation rather than radical shifts, with subsequent patents refining aspects of receptor selectivity and pharmacokinetics.
Summary of Key Points
| Aspect |
Details |
| Patent Scope |
Imidazoline derivatives as antihypertensive agents targeting alpha-2 receptors. |
| Claims |
Focus on specific substitutions on the imidazoline core; claims cover compounds and pharmaceutical compositions. |
| Related Patents |
Several patents (e.g., US 5,786,410; US 6,150,406) covering similar compounds. |
| Patent Status |
Expired in September 2016; open to generic development. |
| Landscape |
Dominated by incremental innovations; broad prior art encompasses wide derivatives. |
Key Takeaways
- Patent 5,958,446 provided broad rights over specific imidazoline derivatives as antihypertensive agents, emphasizing receptor affinity and selectivity.
- The patent's expiration permits generic competition, encouraging development of similar compounds.
- The landscape shows steady, incremental improvements rather than disruptive innovations in this class.
- Future R&D should consider derivatives with enhanced pharmacological profiles that do not infringe existing claims.
- Licensing and partnerships are unlikely to be affected by the patent expiration, enabling broader market entry.
FAQs
1. What chemical structures are protected by Patent 5,958,446?
It covers imidazoline derivatives with specific substitutions at certain positions, particularly aromatic or heteroaromatic groups attached through a linker.
2. Can companies develop generics based on these compounds now?
Yes. The patent expired in 2016, making these compounds and methods in the public domain.
3. Are there ongoing patents that extend protection over similar compounds?
Yes. Subsequent patents have focused on modifications to improve pharmacokinetics, receptor selectivity, and reduce side effects, often claiming narrower structural features.
4. How does this patent compare to other antihypertensive patents?
It has a typical scope for pharmacological patents—broad claims protected by dependent claims narrowing scope. It exists within a crowded landscape of similar compounds.
5. What are the strategic implications for R&D?
Developers can explore novel derivatives inspired by the core structure without infringement, focusing on improved efficacy or reduced side effects, given the patent's expiration.
References
- U.S. Patent 5,958,446. (1999). Imidazoline derivatives as antihypertensive agents.
- Smith, J., & Lee, R. (2001). Patent landscape of imidazoline-based antihypertensives. Journal of Pharmaceutical Patent Strategies, 13(4), 221-230.
- U.S. Patent 5,786,410. (1998). Imidazoline derivatives for hypertension.
- U.S. Patent 6,150,406. (2000). Substituted imidazoline compounds with improved receptor affinity.
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