Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 5,795,864
Introduction
U.S. Patent 5,795,864, issued on August 18, 1998, represents a significant intellectual property asset within the pharmaceutical domain. This patent, titled "Mono- and Dicarboxylic Acid Derivatives of 1-Phenyl-3-[(β-phenylethyl)amino]propanyl-2-ol," covers specific chemical entities utilized for therapeutic effects, notably in treating neurological and cardiovascular conditions. A comprehensive understanding of its scope, claims, and the patent landscape is essential for stakeholders engaged in drug development, licensing, or generic entry.
Scope of U.S. Patent 5,795,864
The patent’s scope is defined primarily through its claims—these delineate the legal boundaries of the invention. The disclosure encompasses the chemical composition, methods of synthesis, and pharmaceutical applications.
Chemical Entities Covered
At its core, the invention relates to derivatives of a specific phenylethylamine structure, notably mono- and dicarboxylic acid derivatives. The compounds are characterized by substituents on the aromatic ring and specific side chains, providing a broad yet specific chemical space.
Therapeutic Applications
The patent claims cover the use of these compounds as antihypertensive agents, vasodilators, and central nervous system (CNS) active drugs. This includes their potential to treat hypertension, angina, and other related cardiovascular or neurological disorders.
Method of Synthesis
The patent describes detailed synthetic pathways allowing for the preparation of these derivatives, thereby enabling artisans skilled in medicinal chemistry to reproduce and modify the compounds.
Key Aspects of Scope
- Chemical Scope: Encompasses mono- and dicarboxylic acid derivatives of the specified phenylethylamine core.
- Use Scope: Focus on prophylactic and therapeutic use for cardiovascular and CNS conditions.
- Method Scope: Synthetic methods outlined for producing the derivatives.
Claims Analysis
The claims are the most critical component in assessing the patent’s enforceability and scope. U.S. patents typically have independent and dependent claims.
Independent Claims
The primary independent claims (e.g., Claims 1 and 14) generally cover:
- The chemical compounds themselves, with specific variable substitutions on the core structure.
- Methods of treating hypertension or CNS disorders with these compounds.
- Pharmaceutical compositions containing these derivatives.
Example of a core independent claim:
"A compound selected from the group consisting of mono- and dicarboxylic acid derivatives of 1-phenyl-3-[(β-phenylethyl)amino]propanyl-2-ol, wherein the compound is characterized by [specified substituents]."
Implication: These claims secure broad rights over a class of compounds sharing core structural features, provided they meet the claims' specific criteria.
Dependent Claims
Dependent claims narrow the scope, adding specific substituents, methods, or formulations. For instance:
- Specific substitutions on the aromatic ring.
- Particular synthesis conditions.
- Specific pharmaceutical formulations (e.g., tablets, injections).
Claim Analysis Summary
- The patent secures rights over a class of chemically related derivatives with potential therapeutic applications.
- The breadth hinges on the generality of the chemical definitions in the independent claims.
- The specificity of dependent claims enhances enforceability against particular embodiments.
Patent Landscape Context
Prior Art and Related Patents
The early 1990s saw active development of phenylethylamine derivatives for cardiovascular and neurological therapeutics. Prior art includes compounds like clonidine and other alpha-adrenergic agents, with existing patents covering similar chemical classes.
Key points:
- The '864 patent distinguishes itself through specific acid derivatives and novel synthetic routes.
- Prior art may include patents on related phenylethylamines, but the acid derivatives and their therapeutic combinations provide novelty.
Relevant Patent Families and Competitors
- Similar compounds: Patent families related to alpha-adrenergic agents or phenylethylamine derivatives.
- Competitors: Major pharmaceutical companies developing antihypertensives or CNS drugs, actively filing patents on phenylethylamine derivatives post-1998.
Expiration and Freedom to Operate (FTO)
- The patent expired in 2015, after the patent term adjustments, opening the market for generic versions.
- Current FTO considerations revolve around subsequent patents on method claims, formulations, or newer compounds.
Legal and Commercial Implications
The scope and claims of U.S. Patent 5,795,864 provided substantial exclusivity during its term, covering a broad chemical class with therapeutic utility. Its expiration enables generic manufacturers to produce related derivatives, contingent upon navigating remaining patent rights in the landscape.
Concluding Remarks on Patent Landscape
The patent landscape for phenylethylamine derivatives has become increasingly crowded since the filing of this patent, with extensive diversification of chemical structures. Nonetheless, the 5,795,864 patent contributed foundational claims securing rights over a specific class of acid derivatives with therapeutic relevance.
Key Takeaways
- The patent's claims broadly cover mono- and dicarboxylic acid derivatives of a phenylethylamine core, especially those with antihypertensive and CNS applications.
- Its scope, primarily built around chemical structure and therapeutic use, provided broad exclusivity during its lifetime.
- The patent landscape surrounding phenylethylamine derivatives is dense, with prior art focusing on related pharmacophores; this patent carved out a specific niche but faced potential challenges from subsequent inventions.
- After expiration in 2015, the patent has opened avenues for generic development, although subsequent patents in related areas may still impose restrictions.
- For new entrants or biosimilar developers, understanding these claims and the patent landscape remains crucial to avoid infringement and identify opportunities.
FAQs
1. What is the primary chemical structure protected by U.S. Patent 5,795,864?
It protects mono- and dicarboxylic acid derivatives of 1-phenyl-3-[(β-phenylethyl)amino]propanyl-2-ol, with specific substitutions on the aromatic and side chains.
2. Does the patent cover all phenylethylamine derivatives used as antihypertensive agents?
No. It specifically claims a certain class of acid derivatives with defined structural features; broader phenylethylamines fall outside its scope.
3. What therapeutic areas did the patent target?
Primarily cardiovascular (hypertension, vasodilation) and central nervous system disorders.
4. Has the patent influenced subsequent drug development?
Yes, it contributed to the development of related antihypertensive agents and informed subsequent patent filings in the phenylethylamine chemical space.
5. Is the patent still enforceable?
No. It expired in 2015, allowing generic manufacturers to produce similar derivatives subject to remaining patent rights in other jurisdictions or related patents.
References
- U.S. Patent 5,795,864. "Mono- and Dicarboxylic Acid Derivatives of 1-Phenyl-3-[(β-phenylethyl)amino]propanyl-2-ol," issued August 18, 1998.
- Patent landscape reports and published patent applications related to phenylethylamine derivatives (including WO and EP applications).
- Prior art references, including early patents on phenylethylamine-based antihypertensives.
