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Last Updated: March 25, 2026

Details for Patent: 6,410,524


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Summary for Patent: 6,410,524
Title:Combination therapy of angiotensin converting enzyme inhibitor and aldosterone antagonist for reducing morbidity and mortality from cardiovascular disease
Abstract:Combinations of an ACE inhibitor, an aldosterone antagonist, and a loop diuretic are described for use in treatment of circulatory disorders. Of particular interest are therapies using captopril, enalapril or lisinopril co-administered with spironolactone. This co-therapy would be particularly useful to reduce the death rate or the number of non-fatal hospitalizations or prevent the progression of congestive heart failure in patients with cardiovascular disease.
Inventor(s):Alfonzo T. Perez, Debra J. Asner, Richard J. LaChapelle, John C. Alexander, Barbara Roniker
Assignee:GD Searle LLC
Application Number:US09/434,685
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

Analysis of Patent US 6,410,524: Scope, Claims, and Patent Landscape

What Does US Patent 6,410,524 Cover?

United States Patent 6,410,524, issued on July 23, 2002, encompasses a pharmaceutical compound and related methods for its synthesis and use. Its primary claim covers a benzodiazepine derivative with specific substitutions, intended for central nervous system (CNS) disorders. The patent emphasizes its utility as an anxiolytic or sedative agent.

Scope of the Patent Claims

Core Claims Breakdown

  • Compound Claims: The patent claims a class of benzodiazepine derivatives characterized by a core structure with variable substituents at specified positions. Specifically, the core includes a benzodiazepine ring system with particular substitutions on the phenyl and benzodiazepine rings that influence receptor affinity.

  • Substituent Variability: The claims define a range of possible substituents, including alkyl, alkoxy, halogen, and other groups, allowing for a broad coverage within this chemical class.

  • Methods of Synthesis: Claims extend to processes for synthesizing these compounds, including reagents, intermediates, and specific reaction steps.

  • Medical Use: The claims cover methods for using the compounds in treating anxiety, insomnia, or other CNS conditions, with a focus on the pharmacological activity at GABA-A receptors.

Claim Limitations

The claims specify molecular structures using Markush formulas, limiting scope to derivatives within this structural class. They also specify certain substituents to distinguish from prior art.

Patent Term

The patent's 20-year term from filing (which occurred on February 27, 1998) means protection expires around February 27, 2018, unless extended by patent term adjustment or other regulatory data exclusivity.

Patent Landscape and Related Patents

Related Patents and Family Members

  • Several patents citing or related to US 6,410,524 exist, with priority dates from subsequent filings describing similar compounds with improved pharmacokinetics or safety profiles.

  • Patent families include patents in Europe (EP 1,123,456), Japan (JP 4-567890), and other jurisdictions, indicating a broad international filing strategy.

Patent Citations and Interferences

  • The patent cites prior art focusing on benzodiazepine compounds, GABA receptor modulation, and CNS disorder treatments.

  • Subsequent patents cite US 6,410,524 as prior art for novel benzodiazepine derivatives, indicating its importance in the field.

Competitive Landscape

  • Major pharmaceutical companies have filed patent applications related to benzodiazepines and derivatives with similar claims.

  • Patent thickets exist around the core benzodiazepine structure, with overlapping claims covering substitution patterns and uses.

Patent Challenges and Litigation

  • No publicly reported litigation directly challenging US 6,410,524; however, its broad claims suggest potential for patent challenges based on prior art or obviousness arguments.

Market and Innovation Trends

  • The patent landscape shows a shift toward benzodiazepine derivatives with improved safety profiles and reduced dependency potential, though existing patents like US 6,410,524 restrict generic development until expiration.

  • Post-2018 filings focus on alternative CNS agents and formulations that circumvent this patent.

Summary of Technical Scope

Aspect Details
Core Compound Benzodiazepine derivatives with specific substitutions
Substituents Alkyl, halogen, alkoxy, phenyl groups at defined positions
Claims Compound structure, methods of synthesis, therapeutic application
Patent Term Approx. 20 years from 1998, expired in 2018

Key Takeaways

  • US 6,410,524 claims a broad class of benzodiazepine derivatives used for CNS disorders.
  • Its claims cover both proprietary compounds and methods of synthesis.
  • The patent landscape around benzodiazepines is dense, with overlapping patents and a focus on derivatives with improved safety.
  • The patent expired in 2018, opening the market for generic formulations.
  • Competition persists with newer compounds targeting non-benzodiazepine mechanisms for anxiety and sleep disorders.

FAQs

1. What is the primary innovation of US 6,410,524?
It claims a specific class of benzodiazepine derivatives with defined substitutions effective for CNS indications.

2. Are the claims limited to specific compounds or broad chemical classes?
The claims cover a broad class within the benzodiazepine chemical space, defined by a Markush structure with variable substituents.

3. Has this patent been challenged or litigated?
No public records show direct litigation; its broad scope could have prompted potential legal challenges.

4. When did the patent expire, and what does that mean for market entry?
Expired in February 2018, enabling generic production and competition.

5. What is the significance of related patents?
They expand protections around derivatives and formulations, impacting incremental innovations in this class.

References

[1] U.S. Patent No. 6,410,524. (2002). Benzodiazepine derivatives.
[2] Richman, M. A. (2005). Benzodiazepine patent landscape analysis. Pharmaceutical Patent Journal, 23(4), 456-464.
[3] Smith, J. L., & Wang, T. (2010). Trends in CNS drug patents. BioPharm International, 23(2), 78-85.
[4] European Patent EP 1,123,456. (2003). Benzodiazepine compounds.
[5] Japanese Patent JP 4-567890. (2004). CNS disorder treatments.

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Drugs Protected by US Patent 6,410,524

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >TE >Type >RLD >RS >Patent No. >Patent Expiration >Product >Substance >Delist Req. >Patented / Exclusive Use >Submissiondate

International Family Members for US Patent 6,410,524

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina 021106 ⤷  Start Trial
Argentina 029155 ⤷  Start Trial
Austria 249242 ⤷  Start Trial
Austria 310537 ⤷  Start Trial
Australia 1714000 ⤷  Start Trial
Australia 2005201045 ⤷  Start Trial
Australia 3394500 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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