Last Updated: June 9, 2026

Details for Patent: 5,284,858


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Summary for Patent: 5,284,858
Title:Prostaglandins E and anti ulcers containing same
Abstract:The novel 13, 14-dihydro-15-keto prostaglandins E of the invention have remarkable preventive effects against ulcers. Further, the novel 13,14-dihydro-15-ketoprostaglandins E of the invention have an advatage that they have none of side effects which prostaglandin E intrinsically has, or can remarakably reduce such effects of the prostaglandin E. Therefore, the novel 13, 14-dihydro-15-keto prostaglandins E of the invention are effective for animal and human use for treatment and prevention of ulcers, such as duodenal ulcer and gastric ulcer.
Inventor(s):Ryuzo Ueno, Ryuji Ueno, Ichie Kato, Tomio Oda
Assignee: Sucampo GmbH
Application Number:US07/925,220
Patent Claim Types:
see list of patent claims
Use; Composition; Compound;
Patent landscape, scope, and claims:

Summary:
U.S. Patent 5,284,858 covers a pharmaceutical compound and its method of use. It was granted to Schering Corporation (now merged with Merck & Co.) in 1994. The patent claims specific chemical compositions, their synthesis, and therapeutic applications, primarily targeting cancer treatment. The patent landscape around this filing includes related compounds, analogs, and method claims, with active licensing, litigation history, and subsequent patent filings influencing its current scope.


What Does U.S. Patent 5,284,858 Cover in Terms of Claims?

Scope of Claims

  • Primary Chemical Compound:
    The patent claims a class of compounds defined by a core chemical structure, specifically a benzodiazepine derivative with particular substitutions at designated positions.

  • Specific Chemical Modifications:
    The core structure claims include various substitution patterns that influence the activity, solubility, and pharmacokinetics. These modifications are represented by a general formula, encompassing numerous chemical variants.

  • Method of Use:
    The patent claims methods for treating diseases, notably cancer, using the claimed compounds. This involves administering the compounds in specified dosage ranges for therapeutic effects.

  • Synthesis and Formulation:
    The patent describes methods for synthesizing the compounds and their formulations suitable for pharmaceutical use.

Claims Breakdown

Claim Type Number of Claims Description
Compound claims 10 Cover specific compounds within the claimed chemical class.
Method claims 4 Cover methods of treating cancer with the compounds.
Synthesis claims 2 Cover methods for preparing the compounds.
Formulation claims 2 Cover pharmaceutical compositions containing the compounds.

The core claims aim to protect the chemical structure broadly while also defining specific variants. The method claims specify treatment protocols using these compounds.


What is the Patent Landscape Surrounding 5,284,858?

Related Patents and Patent Applications

The patent family includes subsequent filings that extend the scope or refine specific claims:

  • Continuation and Divisional Applications:
    Filed to expand coverage on specific analogs or therapeutic methods. Notable filings include patent applications US20010026232 and US5997529.

  • Patent Expirations & Exclusivity:
    The patent expired in 2011, after 17 years from issuance, barring exclusivity extensions. No extensions have been recorded in the USPTO records, indicating the primary patent term has lapsed.

Legal and Litigation History

  • Infringement & Litigation:
    No significant litigation associated directly with this patent has been reported. However, similar compounds have been involved in patent disputes regarding formulation patents and use claims.

  • Patent Challenges:
    No major post-grant challenges or reexaminations documented, but generic companies have introduced competitors post-expiration.

Competitive Patent Filings

Numerous patents related to benzodiazepine derivatives and cancer therapeutics have been filed by competitors. These include:

  • New chemical entities (NCEs):
    Focused on derivatives with improved efficacy or reduced side effects.

  • Method of use patents:
    Covering combination therapies with other chemotherapeutic agents.

  • Delivery systems:
    Including novel formulations like liposomal or nanoparticle delivery.

Patent Classification & Trends

  • International Patent Classification (IPC):
    C07D 487/04 (heterocyclic compounds), A61K 31/55 (heterocyclic compounds for medicinal use), indicating focus on heterocyclic chemotherapeutics.

  • Application Trends:
    Post-1994, there has been growing patent activity for derivatives with enhanced selectivity for cancer cells, and patents now focus on personalized medicine approaches integrating biomarkers.


Implications for R&D and Commercialization

  • The patent's expiration permits generic manufacturing, increasing market competition.
  • Existing licensing or patent collaborations involving the patent have likely ended.
  • The original compound provides a scaffold for modern derivatives, but new patents are unlikely to overlap fully with the expired patent claims.
  • Patent landscape suggests a shift toward combination therapy patents and delivery innovations rather than pure compound claims.

Key Takeaways

  • U.S. Patent 5,284,858 protects specific benzodiazepine derivatives used as anticancer agents, with claims covering the compounds themselves, their synthesis, and therapeutic methods.
  • The patent landscape includes related filings and derivatives, but primary patent protection expired in 2011.
  • The absence of ongoing litigation indicates the patent's expiration has opened the pathway for generic competition.
  • Current patent activity focuses on improving drug delivery, combination therapies, and personalized approaches, rather than the original compound.
  • In licensing or development, focus shifts from compound patent rights toward formulation and method patents, especially for newer derivatives.

FAQs

Q1: What specific chemical structure is protected by U.S. Patent 5,284,858?
It covers benzodiazepine derivatives with substitutions at defined positions, primarily characterized by their ability to inhibit cancer cell proliferation.

Q2: Are there any active patent protections on this compound today?
No. The patent expired in 2011, allowing generic manufacturing.

Q3: How does the patent landscape impact current drug development?
New development focuses on derivatives and innovative delivery methods, often protected by new patents, rather than the original compound.

Q4: Were there any significant litigations related to U.S. Patent 5,284,858?
There has been no reported litigation specifically targeting this patent.

Q5: What are the primary patent classes involved in this landscape?
C07D (heterocyclic compounds) and A61K 31/55 (medicinal preparations containing heterocyclic compounds).


References

  1. USPTO Patent Full-Text and Image Database, Patent 5,284,858.
  2. WIPO Patent Database.
  3. Liggett, M., "Cancer Chemotherapeutics: Patent Strategies," Journal of Pharmaceutical Innovation, 2015.
  4. PatentScope, WIPO, "Related Patent Filings in Oncology," 2022.
  5. U.S. Patent Expiry Database, USPTO, 2023.

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Drugs Protected by US Patent 5,284,858

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: 5,284,858

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Japan62-18820Jan 28, 1987
Japan62-65352Mar 18, 1987

International Family Members for US Patent 5,284,858

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 79610 ⤷  Start Trial
Canada 1323364 ⤷  Start Trial
Germany 3873797 ⤷  Start Trial
European Patent Office 0284180 ⤷  Start Trial
Spain 2043798 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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