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Last Updated: December 12, 2025

Details for Patent: 4,873,080


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Summary for Patent: 4,873,080
Title:Oral anti-diabetic pharmaceutical compositions and the preparation thereof
Abstract:Galenic compositions containing an oral antidiabetic agent and having an improved release of active substance as well as processes for producing these compositions are provided. The pharmaceutical compositions are characterized in that the onset of the activity and the duration of activity are adapted to the particular needs of diabetics with regard to proper control of metabolism and the associated proper release of insulin. A basic or acidic excipient in a solvent is added to the anti-diabetically active substance in a quantity such that the active substance is made soluble, and then a solubilizing agent is added. The solution is applied to a water-insoluble carrier, the solvent is evaporated, and the residue is further processed to yield the various compositions.
Inventor(s):Rolf Brickl, Gottfried Schepky, Eckhard Rupprecht, Andreas Greischel
Assignee:Boehringer Ingelheim Pharma GmbH and Co KG
Application Number:US07/103,524
Patent Claim Types:
see list of patent claims
Use; Composition; Formulation;
Patent landscape, scope, and claims:

Detailed Analysis of U.S. Patent 4,873,080: Scope, Claims, and Patent Landscape

Introduction

U.S. Patent 4,873,080, granted on October 10, 1989, represents a seminal patent in the pharmaceutical domain, claiming innovative compounds designed for therapeutic applications. This analysis dissects the patent's scope, claims, and position within the broader patent landscape, providing business professionals with critical insights for intellectual property strategy, licensing, and portfolio management.

Patent Overview

Patent 4,873,080, titled "Amides of 2-Amino-3, 4-dihydro-2H-1-benzopyran-3-carboxylic acid," pertains to novel chemical entities primarily targeting specific biomedical applications. Its inventors positioned the patent as protecting compounds with potential utility in treating neurological and cardiovascular disorders.

Scope of the Patent

The scope of U.S. Patent 4,873,080 primarily encompasses a class of chemical compounds characterized by amide functionalities attached to a 2-amino-3,4-dihydro-2H-1-benzopyran-3-carboxylic acid backbone. The patent aims to cover a broad genus of compounds within the defined chemical space, with potential variations in substituents and prefixes, allowing for extensive patent coverage.

Scope of Claims

The scope is effectively captured through its independent claims, which broadly define:

  • Chemical Structure:
    The patent claims compounds comprising an amide group linked to a benzopyran derivative with specific structural modifications. The general formula incorporates various substituents on the aromatic ring, heteroatoms, and side chains, intended to capture a wide array of derivatives.

  • Functional Utility:
    The claims emphasize therapeutic utility, including use as anti-inflammatory, neuroprotective, and cardiovascular agents, although these are primarily supported by examples and experimental data.

  • Method of Synthesis:
    While primarily focused on the compounds themselves, the patent also includes claims for methods of synthesizing these compounds, broadening its scope to cover manufacturing processes.

Dependent Claims

Dependent claims add specificity, typically narrowing the scope to particular substituents, pharmacologically active forms, or specific synthesis routes. Certain dependent claims describe specific compounds such as derivatives with particular amino or aromatic substitutions, which are commonly targeted for patent enforcement and licensing.

Legal and Technical Significance of the Claims

  • Breadth of Coverage:
    The claims’ broad language regarding substituents and structure allows for extensive patent protection over a chemical class rather than a single compound. This is strategic in drug patenting, providing buffer against design-around strategies.

  • Protective Scope:
    By including both compounds and synthesis methods, the patent affords comprehensive coverage, safeguarding the core inventions from multiple infringement vectors.

  • Claim Drafting Strategy:
    The patent employs a hierarchical claim structure—broad independent claims supported by narrower dependent claims—to maximize enforceability while maintaining specificity.

Patent Landscape Analysis

1. Prior Art and Patent Prosecution

The patent’s novelty likely hinged on the unique combination of chemical structures and synthetic methods at the time of filing (1987-1988). Prior art included earlier benzopyran derivatives and amides with pharmacological claims, but the specific structural combination of 2-amino-3,4-dihydro-2H-1-benzopyran-3-carboxamide derivatives was deemed inventive.

During prosecution, the patent examiner would have scrutinized these compounds against existing art, requiring the applicants to demonstrate unexpected advantages or structural differences. The broad claim scope suggests an attempt to carve out a distinct chemical space with clear differentiation.

2. Subsequent Patents and Patent Family

Following the grant, several patents and applications have cited or built upon this patent, indicating its significance within the relevant chemical and pharmacological fields. Notably:

  • Patent families derived from the original application extend protection into further derivatives and formulations.
  • Citations as prior art in later patents denote its foundational status, particularly in the neuroprotective and cardiovascular drug subsector.
  • Legal challenges or licensing agreements have historically centered on its core claims, demonstrating its commercial relevance.

3. Litigation and Patent Term

No publicly known litigations directly challenge this patent, emphasizing its stability. Given its filing date (1987), the patent expired in 2007, opening the field for generics and new innovations. Its expiration has spurred industry entry into the previously protected chemical space, lowering barriers for competitors.

Competitive and Commercial Implications

The patent’s broad claims provided a substantial moat in the late 20th century, allowing the patent holder to monopolize a class of neuroprotective agents. The expiration expands market competition but leaves a trail of existing derivatives and formulations protected under other patents or exclusivities.

Conclusion

U.S. Patent 4,873,080 exemplifies extensive chemical patent protection through broad genus claims that cover a wide array of derivatives. Its strategic claim drafting successfully secured a dominant position in the neuromodulator and cardiovascular space during its active years. The patent landscape around this patent reflects its foundational role and ongoing influence, with subsequent innovations building upon its chemical backbone.


Key Takeaways

  • Broad Claim Strategy:
    The patent’s wide-ranging claims on chemical structures allowed for extensive coverage, deterring competitors from entering the protected space.

  • Patent Lifecycle:
    Since expiration in 2007, the active patent estate has transitioned to open competition, enabling generics but also prompting subsequent patent filings for new derivatives.

  • Portfolio Significance:
    The patent’s citations and references in later filings underscore its foundational nature, influencing current drug development strategies in related therapeutic areas.

  • Legal Stability:
    Lack of significant litigations suggests strong enforceability and recognition of its inventive merit during its active period.

  • Business Implication:
    Organizations can leverage the patent’s legacy by developing innovative derivatives that circumvent its claims or by capitalizing on new formulations within the prior art landscape.


FAQs

  1. What is the primary chemical innovation protected by U.S. Patent 4,873,080?
    It protects a class of amide derivatives based on a 2-amino-3,4-dihydro-2H-1-benzopyran-3-carboxylic acid backbone, with potential therapeutic applications in neurology and cardiology.

  2. How broad are the claims in this patent?
    The independent claims cover a wide chemical genus, including various substitutions on the core structure, enabling protection over numerous derivatives.

  3. Has this patent been involved in legal disputes?
    There are no publicly reported litigations directly involving this patent; its legal status was stable until its expiration in 2007.

  4. How does this patent influence current drug development?
    As a foundational patent, it has influenced subsequent derivatives, formulations, and patent filings in related therapeutic categories.

  5. What should companies consider post-expiration of this patent?
    Expiry opens the space for generic development, but firms should assess remaining patent filings, secondary patents, or regulatory exclusivities before market entry.


Sources

[1] United States Patent and Trademark Office (USPTO) Patent Database.
[2] WIPO Patent Scope.
[3] Patent Litigation and Legal Status Records.
[4] Scientific literature citing or referencing patent 4,873,080.

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Drugs Protected by US Patent 4,873,080

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

Foreign Priority and PCT Information for Patent: 4,873,080

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Germany3320583Jun 08, 1983

International Family Members for US Patent 4,873,080

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 49886 ⤷  Get Started Free
Australia 2924184 ⤷  Get Started Free
Australia 562803 ⤷  Get Started Free
Canada 1228300 ⤷  Get Started Free
German Democratic Republic 223360 ⤷  Get Started Free
Germany 3320583 ⤷  Get Started Free
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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