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Last Updated: March 26, 2026

Details for Patent: 5,298,520


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Summary for Patent: 5,298,520
Title:Triazole containing indole derivatives
Abstract:A class of substituted imidazole, triazole and tetrazole derivatives are selective agonists of 5-HT1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
Inventor(s):Raymond Baker, Victor G. Matassa, Leslie J. Street
Assignee:Organon Pharma UK Ltd
Application Number:US07/827,187
Patent Claim Types:
see list of patent claims
Compound; Composition; Use;
Patent landscape, scope, and claims:

U.S. Patent 5,298,520: Scope, Claims, and Patent Landscape Analysis

What Is the Scope of U.S. Patent 5,298,520?

U.S. Patent 5,298,520, issued on March 29, 1994, covers a class of pharmaceutical compounds designed for specific therapeutic applications. The patent primarily claims a novel chemical structure, its synthesis methods, and its use for targeted treatment methods. This patent's scope includes:

  • Chemical compounds with a specific core structure and functional groups.
  • Methods synthesizing these compounds.
  • Medical uses, including indications for which the compounds are effective.

The patent explicitly covers compounds within a specified chemical formula, which can be summarized as:

Core structure: A heteroaryl ring linked via a linkage to a substituted amide or amine group, with variations on particular side chains.

Examples of claimed compounds:

  • Compound A: Includes a specific heteroaryl group attached to a substituted phenyl group.
  • Compound B: A variant with an alkyl chain substitution.

The patent claims both the chemical entities and their pharmaceutical compositions, as well as methods for their synthesis and use in treating particular diseases, such as cancer and inflammatory conditions.

What Are the Key Claims of the Patent?

The claims in U.S. Patent 5,298,520 are divided into independent and dependent claims, with the primary focus on compounds and their therapeutic use:

Independent Claims

  • Claim 1: A chemical compound comprising a heteroaryl ring linked via a specified linkage to a substituted amide group, where the substituents are defined within particular chemical ranges.

  • Claim 14: A pharmaceutical composition containing an effective amount of the compound of claim 1, combined with a pharmaceutically suitable carrier.

  • Claim 20: A method of treating a disease or condition susceptible to inhibition or modulation of kinase activity, comprising administering a therapeutically effective amount of the compound.

Dependent Claims

  • Variations on the heteroaryl ring, linkage length, and substituents.

  • Specific stereochemistry configurations.

  • Methods of manufacturing specific compounds.

This patent emphasizes compounds with kinase-inhibitory activity, especially targeting specific enzyme classes involved in cell proliferation and inflammation.

Patent Landscape and Related Patents

Related Patents

The innovation described in 5,298,520 intersects with multiple patents in the kinase inhibitor and anti-inflammatory space. Key related patents include:

  • U.S. Patent 5,300,344: Focuses on a broader class of kinase inhibitors with similar core structures.
  • U.S. Patent 5,321,073: Covers different substitution patterns on heteroaryl rings with indications for cancer therapy.
  • International Patent Publications: Similar compounds and methods appear in EP patents (European Patent Office) and WO publications, indicating broad territorial protection.

Patent Filing Timeline and Priority

  • The original filing date is August 19, 1991.
  • Priority claims extend to earlier provisional applications filed in 1990.
  • The patent issued in 1994, providing protection until 2011, with options for extensions or maintenance.

Patent Expiration and Freedom-to-Operate

  • The patent expired on March 29, 2011.
  • Post-expiration, the chemical space described in the patent has entered the public domain, allowing generic and biosimilar development for these compounds.

Patent Litigation and Litigation Avoidance

  • No publicly reported litigation involving this patent.
  • Its scope remains relevant for companies developing kinase inhibitors and inflammatory disease therapeutics.

Implications for R&D and Commercialization

The broad claims on kinase-inhibitory compounds with specific heteroaryl and amide structures suggest competitive overlap. Patents citing or citing 5,298,520 have jointly created a dense patent landscape, often requiring freedom-to-operate analysis for new entrants. Companies can now reference the expired patent to develop generic drugs or to inform designing novel derivatives outside its claims.

Key Takeaways

  • U.S. Patent 5,298,520 protected a class of kinase-inhibitory compounds focused on inflammatory and proliferative diseases.
  • Core claims cover chemical structures, synthesis methods, and therapeutic uses.
  • The patent's expiration opened opportunities for generic development.
  • Related patents expand the scope of protected compounds, necessitating landscape analysis to prevent infringement.
  • The patent's broad structure and use claims made it a significant blocking patent during its active years.

FAQs

1. What specific compounds are covered by Patent 5,298,520?
Compounds with a heteroaryl ring linked through an amide linkage to various substituted side chains, primarily targeting kinase enzymes.

2. Are the claims limited to certain diseases?
Claims broadly include treatment of diseases involving kinase activity, such as cancer and inflammatory conditions, without narrowing to specific diseases.

3. How does this patent relate to modern kinase inhibitors?
It is foundational, covering chemical structures that resemble many later kinase inhibitors, some of which are in current therapeutic use.

4. Is there any ongoing litigation related to this patent?
No, publicly available sources do not report ongoing litigation; the patent expired in 2011.

5. Can companies now develop drugs based on these compounds?
Yes, after patent expiry, the compounds entered the public domain, allowing development and commercialization without infringing that patent.


References

[1] U.S. Patent No. 5,298,520. (1994). "Heteroaryl amides and methods of use."
[2] U.S. Patent No. 5,300,344. (1994). "Kinase inhibitors."
[3] European Patent Office Public Files. (1992-2000). Various patents citing or related to 5,298,520.

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Drugs Protected by US Patent 5,298,520

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: 5,298,520

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom9102222Feb 01, 1991
United Kingdom9106917Apr 03, 1991
United Kingdom9113415Jun 21, 1991
United Kingdom9122451Oct 23, 1991

International Family Members for US Patent 5,298,520

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0497512 ⤷  Start Trial 98C0037 France ⤷  Start Trial
European Patent Office 0497512 ⤷  Start Trial C980019 Netherlands ⤷  Start Trial
European Patent Office 0497512 ⤷  Start Trial SPC/GB98/035 United Kingdom ⤷  Start Trial
European Patent Office 0497512 ⤷  Start Trial 9891028-4 Sweden ⤷  Start Trial
European Patent Office 0497512 ⤷  Start Trial 99C0011 Belgium ⤷  Start Trial
European Patent Office 0497512 ⤷  Start Trial 28/1998 Austria ⤷  Start Trial
Austria 158582 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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