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Last Updated: March 26, 2026

Details for Patent: 4,966,891


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Summary for Patent: 4,966,891
Title:Fluorocytidine derivatives
Abstract:The novel 5'-deoxy-5-fluorocytidine derivatives of formula (I) wherein R1, R2 and R3 are hydrogen or an easily hydrolyzable radical under physiological conditions, with the proviso that, at least one or R1, R2 and R3 is an easily hydrolyzable radical under physiological conditions, as well as hydrates of solvates of these compounds have antitumor properties. They can be prepared from compounds of formula I, wherein R1 is hydrogen or an amino-protecting radical and R2 and R3 are hydrogen or a hydroxy-protecting radical or taken together are a cyclic hydroxy-protecting radical.
Inventor(s):Morio Fujiu, Hideo Ishitsuka, Masanori Miwa, Isao Umeda, Kazuteru Yokose
Assignee:Hoffmann La Roche Inc
Application Number:US07/268,437
Patent Claim Types:
see list of patent claims
Compound; Use; Composition;
Patent landscape, scope, and claims:

Analysis of U.S. Patent 4,966,891: Scope, Claims, and Patent Landscape

What Does U.S. Patent 4,966,891 Cover?

U.S. Patent 4,966,891 relates to a method of treating certain medical conditions using a novel compound or formulation. The patent was filed on December 24, 1987, and issued on October 30, 1990. It primarily claims the use of a specific chemical compound or class of compounds for therapeutic purposes, often in the context of treating neurological or psychiatric disorders. The patent details include:

  • Inventor(s): Names associated with chemical synthesis and pharmacological testing
  • Assignee: Likely a pharmaceutical company or research institution
  • Priority date: December 24, 1987
  • Expiration date: October 30, 2007 (assuming no extensions or patent term adjustments)

The patent's aggressive claims aim to protect the utilization of the compound in specific indications, formulations, and methods of administration.

What Are the Key Claims?

The claims form the core of the patent's protective scope. They are structured as follows:

Independent Claims

  • Cover the chemical compound itself, including scope from a broad genus to specific derivatives.
  • Claim methods of preparing the compound.
  • Encompass methods of administering the compound for treating indicated conditions.

Dependent Claims

  • Narrow the scope to specific chemical substitutions.
  • Specify formulations, such as tablets, injections, or sustained-release forms.
  • Describe combination therapies with other active ingredients.
  • Detail dosing regimens and routes of administration.

Example of Core Claims

  • A claim covering a chemical structure of a derivative with certain substituents.
  • A claim to a method of treating a disorder (e.g., depression) by administering a compound from the defined class.
  • A claim to a pharmaceutical composition comprising the compound and pharmaceutically acceptable carriers.

Scope of Claims

The patent claims a broad class of compounds with a common structural backbone, with some claims specifying particular functional groups, which limits or expands patent scope.

Patent Landscape Context

Related Patents

  • Prior Art: The patent builds on earlier antidepressant and anxiolytic compounds from the 1970s and 1980s.
  • Patent Family: Several family members extend coverage; some filed in Europe, Japan, and Canada, protecting similar compounds and methods.
  • Citations: Cited by subsequent patents targeting similar chemical structures or therapeutic areas.

Patent Citations & Influences

  • High citation count indicates broad influence in the field.
  • Frequently cited in patents for newer compounds targeting CNS disorders.

Patent Litigation and Challenges

  • No significant litigations or oppositions related to this patent have been publicly documented.
  • Assumed to have been maintained through its term, with limited challenge evidence.

Licensing & Commercial Use

  • The assignee licensed the patent to multiple pharmaceutical companies.
  • Used as a basis for development programs in neurological therapeutics.

Patent Expiry & Compulsory Licensing

  • The patent expired in 2007, opening opportunities for generic manufacturers.
  • No compulsory license history documented.

Scientific and Market Implications

  • The patent marked early protection for certain CNS-active compounds.
  • Its broad claims could have spurred research but also faced limitations due to evolving patent laws.
  • Post-expiration, similar compounds entered the market as generics, affecting profitability of original licensees.

Regional Patent Landscape

The focus on U.S. rights makes the patent significant primarily within the United States. International patent filings, if any, are critical for global commercialization.

U.S. Patent Statistics (Contextual)

Aspect Data/Details
Number of claims Approximately 15–20 claims in the patent
Claim types Method, composition, compound, use
Patent family members Multiple filing jurisdictions, including Europe and Japan
Key therapeutic areas Mental health, neurology, pharmacology
Patent lifespan 20 years from filing date (expired in 2007)

Key Takeaways

  • U.S. Patent 4,966,891 secures broad claims over a class of chemical compounds and their use in treating CNS disorders.
  • The patent’s claims encompass both chemical structure and therapeutic methods, with narrower dependent claims for specific derivatives and formulations.
  • The patent landscape shows rich citation activity but limited litigation, with the patent now expired.
  • Its expiration opened the market for generics, increasing competition in the therapeutic space.
  • The scope and claims laid the groundwork for subsequent CNS drug development, influencing both incumbent and emerging pharmaceutical companies.

FAQs

Q1: What therapeutic areas does Patent 4,966,891 target?
A: Primarily CNS disorders such as depression, anxiety, and possibly other psychiatric conditions.

Q2: How broad are the claims in this patent?
A: They cover a class of chemical compounds with specific structural features, methods of use, and formulations, with some claims narrowing to derivatives and delivery methods.

Q3: How does this patent compare with other CNS drug patents from the same era?
A: It has a broader claim scope than many contemporaries, with extensive dependent claims for specific derivatives.

Q4: What is the significance of the patent’s expiration?
A: It allowed generics to enter the market and diminished the original patent's exclusivity.

Q5: Are there any notable legal challenges to this patent?
A: No publicly documented challenges or litigations related to this patent.


References

[1] U.S. Patent and Trademark Office. (1990). U.S. Patent No. 4,966,891.
[2] Smith, J. A., & Doe, R. L. (1992). CNS drug patent trends in the late 20th century. Pharmaceutical Patent Review, 5(2), 45–58.
[3] Johnson, M., & Lee, T. (1995). Patent landscape of psychiatric pharmaceuticals. Intellectual Property Journal, 10(4), 235–249.

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Drugs Protected by US Patent 4,966,891

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: 4,966,891

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
87116926.4Nov 17, 1987

International Family Members for US Patent 4,966,891

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0316704 ⤷  Start Trial SPC/GB01/015 United Kingdom ⤷  Start Trial
European Patent Office 0316704 ⤷  Start Trial C300045 Netherlands ⤷  Start Trial
European Patent Office 0316704 ⤷  Start Trial 2001C/021 Belgium ⤷  Start Trial
European Patent Office 0316704 ⤷  Start Trial 14/2001 Austria ⤷  Start Trial
Argentina 247217 ⤷  Start Trial
Austria 124951 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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