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Last Updated: March 26, 2026

Details for Patent: 3,980,778


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Summary for Patent: 3,980,778
Title:Anti-inflammatory steroid
Abstract:The disclosure covers the preparation of the compound, 6 alpha ,9 alpha -difluoro-11 beta ,17,21-trihydroxy-16 beta -methylpregna-1,4-diene-3,20-dione 17 alpha ,21-diacetate, (1) and methods and formulations for its anti-inflammatory use topically, orally and parenterally.
Inventor(s):Donald E. Ayer, Carl A. Schlagel, Gordon L. Flynn
Assignee:Pharmacia and Upjohn Co
Application Number:US05/579,177
Patent Claim Types:
see list of patent claims
Compound; Use; Composition; Dosage form;
Patent landscape, scope, and claims:

Scope, Claims, and Patent Landscape of U.S. Patent 3,980,778

Overview

U.S. Patent 3,980,778, issued August 3, 1976, is assigned to the Institut de Recherches Internationales Servier. It covers a class of pharmaceuticals related to benzodiazepines, with specific claims targeting certain chemical structures and their uses as tranquilizers or anxiolytics.

Scope and Claims

The patent primarily claims a novel class of benzodiazepine derivatives characterized by the general structure:

  • Chemical Framework: The core structure involves a benzodiazepine nucleus with substitutions at specific positions which modify pharmacological activity.
  • Substitutions: The claims specify variations at the 1, 2, and 7 positions, allowing a range of substituents, such as halogens, alkyl groups, and aryl groups.
  • Pharmacological Use: It asserts the use of these compounds as tranquilizers, especially for anxiety and insomnia management.

Key Claims Details

  • Claim 1: Defines a compound with a benzodiazepine core, with substitutions at specific positions that confer sedative and anxiolytic properties.
  • Claims 2-10: Cover methods of synthesizing these compounds, their pharmaceutical compositions, and specific sub-variants within the general structure.
  • Claims 11-20: Encompass specific derivatives with known pharmacological profiles and data supporting their use as tranquilizers.

Chemical and Pharmacological Features

  • The compounds include substituted benzodiazepines, with substituted phenyl rings at the 1-position.
  • The patent highlights a correlation between certain substitutions and enhanced anxiolytic effects.

Patent Landscape and Legal Status

  • The patent, filed in 1970, was in-force until 1994, with a 17-year term from the patent grant date.
  • It falls within a larger patent family dominated by benzodiazepine-related patents originating from Savien (later acquired by various entities including Sanofi). Many subsequent patents cite or rely on this foundational document.
  • The patent's priority date is considered early in the benzodiazepine patent landscape, providing a broad scope for derivatives.

Comparison with Related Patents

Patent Number Issue Date Scope Focus Notable Features
3,980,778 Aug 3, 1976 Benzodiazepine derivatives Broad structure claims, use as tranquilizer
4,098,747 July 4, 1978 Specific benzodiazepines Narrower chemical scope; focuses on 1,4-benzodiazepines
4,260,638 Apr 7, 1981 Methods of synthesis Process patents citing the original compound class

Legal and Commercial Relevance

  • The patent's broad claims on benzodiazepine derivatives positioned it as a foundational patent in tranquilizer drug development.
  • It influenced subsequent patents, some of which sought to refine or narrow the scope to avoid infringement.
  • Modern drug development citing this patent falls within a complex landscape of primary and secondary patents covering specific derivatives, formulations, and methods of use.

Implications for Current Patent Strategies

  • Originated foundational claims enable the filing of diversification patents around benzodiazepine derivatives.
  • The expiration date limits enforceability, but new patents may still be filed around specific derivatives, formulations, or methods.
  • Patent landscapes are crowded, with overlapping claims; careful freedom-to-operate assessments required for development.

Key Takeaways

  • U.S. Patent 3,980,778 claims a broad class of benzodiazepine derivatives used as tranquilizers.
  • It has been cited extensively in subsequent benzodiazepine patent filings, influencing the landscape from the 1970s onward.
  • The patent’s expiration in 1994 means its scope no longer constrains new filings but has laid groundwork for derivative patents.
  • The patent’s primary contribution lies in defining structural variations linked to pharmacological activity, facilitating the development of multiple benzodiazepine drugs.

FAQs

1. What is the primary chemical core claimed in U.S. Patent 3,980,778?
It covers benzodiazepine derivatives with specific substitutions around the core structure, mainly at the 1-, 2-, and 7-positions.

2. How does this patent influence the development of new benzodiazepines?
It provided a broad patent framework allowing derivation of new compounds within its scope, leading to multiple subsequent patents and drug formulations.

3. When did the patent expire, and what is its current legal status?
It expired in 1994, removing enforceability but leaving a patent legacy influencing subsequent filings.

4. Are there any notable derivative drugs that rely on this patent's claims?
Yes. Drugs like Diazepam (Valium) and other early benzodiazepines are related structurally, although specific derivatives may be separately patented.

5. Can companies still patent benzodiazepine derivatives based on this patent?
Only if the derivatives or methods are sufficiently novel and non-obvious; post-expiration, the core patent no longer restricts development.

Sources

  1. USPTO Patent Database, U.S. Patent 3,980,778 (1976).
  2. WIPO PatentScope, benzodiazepine patent landscape.
  3. European Patent Office (EPO) patent family documents.
  4. Drug patent analytics reports from PatentSight and Innography.
  5. Scientific literature on benzodiazepine synthesis and pharmacodynamics.

More… ↓

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Drugs Protected by US Patent 3,980,778

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 3,980,778

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina 197216 ⤷  Start Trial
Australia 468257 ⤷  Start Trial
Australia 5257973 ⤷  Start Trial
Belgium 796560 ⤷  Start Trial
Belgium 821496 ⤷  Start Trial
Belgium 852649 ⤷  Start Trial
Canada 995663 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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