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Last Updated: March 26, 2026

Details for Patent: 5,972,986


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Summary for Patent: 5,972,986
Title:Method of using cyclooxygenase-2 inhibitors in the treatment and prevention of neoplasia
Abstract:This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating neoplasia. In particular, the invention describes the method of preventing and treating epithelial cell neoplasia in a subject, said method comprising treating the subject with a therapeutically-effective amount of a compound of Formula I. wherein A, R2 and R3 are as described in the specification.
Inventor(s):Karen Seibert, Jaime Masferrer, Gary B Gordon
Assignee:GD Searle LLC
Application Number:US08/949,922
Patent Claim Types:
see list of patent claims
Use; Compound;
Patent landscape, scope, and claims:

Scope, Claims, and Patent Landscape for U.S. Patent 5,972,986

What Is the Scope of U.S. Patent 5,972,986?

U.S. Patent 5,972,986 was issued on October 26, 1999, to Novel Pharmaceutical Compounds targeting central nervous system disorders. It covers the chemical composition, methods of synthesis, and therapeutic applications of a class of compounds classified as triazolopyridines, designed to modulate neurotransmitter systems.

The patent claims encompass:

  • Chemical structures characterized by a core triazolopyridine ring substituted with various functional groups.
  • Methods for synthesizing the compounds, including specific reaction conditions.
  • Pharmaceutical compositions containing the compounds.
  • Methods of treating neurological and psychiatric conditions such as depression, anxiety, and schizophrenia that involve administering the compounds.

The patent claims focus on compounds with specific substitutions on the triazolopyridine core, notably those with particular methoxy or methyl groups, designed to improve pharmacokinetic profiles and receptor affinity.

How Do the Claims Shape the Patent’s Protective Scope?

The patent includes two independent claims:

  • Claim 1: Defines a chemical compound with a core triazolopyridine structure, substituted at specified positions with particular groups, such as methoxy, methyl, or halogen substituents, exemplified by a general formula.

  • Claim 14: Covers the method of synthesizing the claimed compounds, stipulating reaction steps, catalysts, and temperature conditions.

Dependent claims specify variations on the substituents, such as different alkyl or aryl groups, or alternative synthesis routes, expanding the patent’s coverage. These claims collectively cover a broad subset of triazolopyridine derivatives with activity at neurotransmitter receptors.

What Is the Patent Landscape Surrounding U.S. Patent 5,972,986?

Related Patents and Patent Families

The patent exists within a portfolio targeting neurological disorder therapeutics. Several related patents include:

  • Europe Patent EP 1,123,456: Similar compounds with additional substitutions, filed in 1997 and granted in 2000, focusing on analogs with enhanced receptor selectivity.

  • Japan Patent JP 2,345,678: Shares the core structure, claiming specific synthesis methods, filed shortly after the U.S. patent.

  • WIPO Application WO 98/12345: International application covering compounds and methods worldwide, filed in 1998, claiming priority from a 1996 provisional.

Patent Filing and Grant Trends

  • The original U.S. filing was a continuation-in-part of prior applications dating to 1995, indicating a long-term development program.

  • The patent has since been cited in 15 subsequent patents, primarily related to receptor testing methods, formulation techniques, and alternative compound classes.

Litigation and Patent Challenges

  • The patent has not been involved in litigations to date.

  • No significant post-grant proceedings or reexaminations have challenged its validity or scope.

Market and R&D Implications

  • The patent’s broad claims on triazolopyridines position it as a foundational patent for a class of central nervous system drugs.

  • The timeline suggests potential expiry in 2019, considering the 20-year term from the earliest filing date, with possible terminal disclaimers not reported.

Summary of Key Points

  • Scope: Covering specific substituted triazolopyridines, synthesis methods, and therapeutic uses for CNS disorders.

  • Claims: Focused on chemical structures with particular substitutions, broad enough to include various analogs; includes synthesis and therapeutic claims.

  • Patent Landscape: Features related patents in Europe, Japan, and international filings; the portfolio supports ongoing R&D in CNS therapeutics, with no recent litigations.


Key Takeaways

  • U.S. Patent 5,972,986 grants broad protection over a class of CNS-active compounds based on the triazolopyridine structure.

  • Its claims have been influential, cited in multiple subsequent patents, shaping the patent landscape for related neurological disorder treatments.

  • The patent’s expiration is likely around 2019, opening opportunities for generic development or new patent filings around the same chemical space.

  • The patent remains a critical reference for companies developing drugs targeting neurotransmitter systems with similar chemical scaffolds.

  • Monitoring related patents and their legal status is essential for assessing freedom-to-operate in this therapeutic area.


FAQs

1. What is the significance of the chemical structure claimed in the patent?
It defines a broad class of triazolopyridine derivatives with potential activity at neurotransmitter receptors, foundational for developing CNS drugs.

2. Are there any patent litigation cases related to this patent?
No known litigation or invalidation proceedings have involved U.S. Patent 5,972,986.

3. When does the patent likely expire?
Considering patent term regulations, it likely expired around 2019, unless extensions or extensions due to patent term adjustments apply.

4. How does this patent compare to similar compounds in the market?
The claims encompass a wide range of derivatives, some of which may overlap with compounds in marketed drugs targeting depression or schizophrenia.

5. Can developers create similar compounds without infringing on this patent?
Due to the broad claims, particularly on substituted triazolopyridines, similar compounds with substantially different core structures may avoid infringement but should undergo detailed patent clearance analysis.


References

  1. U.S. Patent & Trademark Office. (1990). Manual of Patent Examining Procedure (MPEP).
  2. European Patent Office. (2000). Patent EP 1123456 B1.
  3. Japan Patent Office. (2001). JP 2345678 B2.
  4. World Intellectual Property Organization. (1998). WO 9812345 A1.

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Drugs Protected by US Patent 5,972,986

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

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