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Patent landscape, scope, and claims: |
Scope, Claims, and Patent Landscape for US Patent 4,863,742
What Does US Patent 4,863,742 Cover?
US Patent 4,863,742, granted on September 5, 1989, pertains to a class of pharmaceutical compounds classified as substituted 1,2,4-benzothiadiazine 1,1-dioxide derivatives. The patent claims cover chemical structures, synthesis methods, and their use as antihypertensive agents.
Key features:
- The patent describes a chemical scaffold with various substituents attached to a benzothiadiazine core.
- The compounds are intended for the treatment of hypertension by acting as calcium channel blockers.
- Claims include specific compounds, such as certain aryl substituted derivatives, and methods for their preparation.
How Broad Are the Patent Claims?
US 4,863,742 has a broad scope within the chemical class. The claim set includes:
- Compound Claims: Cover multiple chemical variations, including the core structure with various substituents, side chains, and functional groups.
- Method Claims: Encompass methods of synthesizing these derivatives.
- Use Claims: Cover the therapeutic application as antihypertensives.
Notable points:
- The patent explicitly claims substituted benzothiadiazine derivatives with a wide range of substituents, effectively creating a chemical space of thousands of potential compounds.
- The claims extend over derivatives with specific substitution patterns on the aromatic rings, broadening the scope to include structurally related compounds.
This broad claim scope provides extensive patent protection over related chemical entities and synthesis processes.
Patent Claims Breakdown
The core claims are classified into:
-
Chemical Structure Claims:
- Covering compounds where the benzothiadiazine ring is substituted at particular positions with aromatic or alkyl groups.
- Variations include different heteroatoms, substituent groups, and functionalizations.
-
Synthesis Method Claims:
- Methods involve specific chemical reactions, such as cyclizations, substitutions, or oxidations, to generate the compounds.
-
Therapeutic Use Claims:
- Method claims for use as antihypertensive agents, specifically calcium channel blockers.
Claim Example (paraphrased):
"A compound of the formula [structure], wherein R1 and R2 are selected from various specified groups, providing antihypertensive activity."
This formulation covers a range of derivatives, effectively encompassing many molecules with similar chemical backbones.
Patent Landscape and Related Patents
Historical context (post-1989):
- Multiple patents have cited or built upon US 4,863,742, often focusing on derivatives with improved potency, selectivity, or pharmacokinetic profiles.
- No recent patents that are direct duplicates exist post-2000; however, derivatives and analogs continue to be patented targeting calcium channel blockade.
Key related patents:
| Patent Number |
Title |
Filing Date |
Focus |
Cited By (most recent) |
| US 5,192,741 |
Benzothiadiazine derivatives as calcium channel blockers |
1990 |
Specific derivatives with enhanced activity |
Multiple (2010s) |
| US 6,287,843 |
Substituted benzothiadiazine compounds |
1999 |
Optimized pharmaceutical formulations |
US patents citing US 4,863,742 |
| WO 1990/008583 |
Benzothiadiazine derivatives for hypertension |
1990 |
Similar structural class, international patent |
Updated international applications |
Patent expiration and freedom-to-operate:
- US 4,863,742 expired in 2007 due to age, allowing unrestricted commercial use of the described compounds.
- However, newer patents may cover specific derivatives with improved profiles.
Research and patent activity:
- The landscape shows continuous activity in derivative synthesis, indicating ongoing interest.
- Parallel filings focus on derivatives with enhanced pharmacological properties.
Implications for R&D and Commercialization
- The broad scope of US 4,863,742 provides foundational coverage over a significant chemical class of calcium channel blockers.
- Strategic pipelines should consider derivatives outside the scope or protected by newer patents.
- Patent expiration opens opportunities to develop generic formulations or new indications with existing derivatives.
Key Takeaways
- US 4,863,742 claims a broad class of substituted benzothiadiazine derivatives active as antihypertensives.
- Claims include chemical structures, synthesis methods, and therapeutic uses, creating extensive patent coverage.
- The patent landscape continues to evolve with subsequent patents refining or extending the chemical space.
- The patent expired in 2007, but related derivatives remain active in research and patent filings.
- Companies may explore non-infringing derivatives, formulation patents, or new therapeutic indications to innovate around existing patents.
FAQs
Q1: How broad are the chemical claims in US 4,863,742?
The claims cover a wide range of substituted benzothiadiazine derivatives, effectively encompassing thousands of related chemical structures within the core scaffold.
Q2: Is the patent still enforceable?
No. US 4,863,742 expired in 2007, removing its enforceability; however, derivative patents may still apply.
Q3: What are the main therapeutic claims?
The patent claims the compounds' use as antihypertensive agents, primarily via calcium channel blockade.
Q4: Are there any subsequent patents that build on US 4,863,742?
Yes. Multiple patents focus on derivatives with improved efficacy, pharmacokinetics, or formulations. These often cite US 4,863,742 as prior art.
Q5: How can a competitor avoid infringing on older patents like US 4,863,742?
They can design structurally different compounds outside the scope of the claims, seek new therapeutic uses, or develop novel synthesis methods not covered by the patent.
References
- U.S. Patent 4,863,742
- Patent Citation Data (e.g., US 5,192,741, US 6,287,843)
- Scientific literature on benzothiadiazine derivatives and calcium channel blockers
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