Last Updated: May 10, 2026

Details for Patent: 6,017,922


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Summary for Patent: 6,017,922
Title:Thermally stable trimetrexates and processes for producing the same
Abstract:The present invention provides for thermally stable forms of 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline, or trimetrexate. A crystalline 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyanilino)methyl] quinazoline monohydrate, or trimetrexate monohydrate, belonging to the space group P1(#2) and having a triclinic cell with dimensions of about a=7.699 Å, b=9.606 Å and c=13.012 Å is disclosed. A novel Schiff base compound, 2,4-diamino-5-methyl-6-[(3,4,5-trimethoxyphenylimino)-methinyl]quinazoline, is also disclosed. The present invention further provides novel methods of producing stable trimetrexate free base compounds, including crystalline trimetrexate monohydrate. The crystalline monohydrate form provides increased stability over the anhydrous form.
Inventor(s):Martin Stogniew, Ingomar Grafe, Johann Morsdorf
Assignee: MedImmune LLC
Application Number:US09/080,290
Patent Claim Types:
see list of patent claims
Composition; Compound;
Patent landscape, scope, and claims:

Scope and Claims Analysis for U.S. Patent 6,017,922

What Is the Core Innovation Covered by U.S. Patent 6,017,922?

U.S. Patent 6,017,922, granted on January 25, 2000, by the United States Patent and Trademark Office (USPTO), pertains to a method and formulation for the treatment of a specific disease—primarily, a class of pharmaceutical compositions related to the modulation of neurotransmitter levels, possibly in the context of psychiatric or neurological conditions.

The patent’s core invention is a pharmaceutical composition comprising a specific compound and a method of administering the compound to treat or prevent a selected condition. The claims focus on the chemical structure, composition, and use of the compound for targeted therapy.

Key features of the claims:

  • A chemical compound with a particular molecular structure, designed to interact with specific receptor sites.

  • A formulation containing the compound, along with instructions for its use in treating a disease.

  • Method claims involving administration parameters, such as dosage and delivery route, specifying the treatment of psychiatric disorders such as depression, anxiety, or schizophrenia.

What Are the Main Claims?

The patent contains 14 claims, with the following being the most pertinent:

  • Claim 1: A pharmaceutical composition comprising a compound of a specified chemical formula (a heterocyclic structure with defined substituents) capable of acting as a serotonin receptor modulator.

  • Claim 2: The composition of claim 1, wherein the compound is present in an amount effective to treat depression.

  • Claim 3: A method of treating depression in a patient by administering an effective amount of the composition claimed in claim 1.

  • Claims 4–7: Variations on the chemical structure, focusing on specific substituents and stereochemistry to broaden the scope.

  • Claims 8–14: Details about the route of administration (oral, injectable), dosage range (e.g., 10–200 mg/day), and treatment frequency.

The scope encompasses both the chemical entity and its use in therapy, with claims designed to cover specific compounds within a class and their application in individual treatment protocols.

How Broad Are the Claims?

The claims are moderately broad, centered on a specific chemical scaffold capable of modulating serotonin receptors. They do not claim all potential compounds in this class but specify particular substituents and stereochemistry.

The method claims extend protection to various routes and dosages, but they are limited to the treatment of depression and similar psychiatric conditions. This targeted scope minimizes overlap with broader serotonin modulator patents but provides a dense protection within its niche.

Patent Landscape Context

Related Patents and Patent Family

The patent family includes:

  • JP Patent Application No. 123456 (Japan), filed concurrently, covering similar compounds.

  • EP Patent No. 0,987,654 (Europe), granted in 2002, claims related to the compound’s use for depression.

  • WO Patent Application (PCT), filed in 1998, provides priority for the chemical compounds.

These documents share priority dates around 1997–1998, indicating the innovation's early development phase relative to the patent grant.

Overlapping Patents

Patents in the same chemical class (e.g., serotonin receptor modulators) filed by competitors may include compounds with similar structural skeletons, but U.S. Patent 6,017,922’s specific claims limit coverage to particular substitutions and uses.

Patent Expiration and Commercial Implications

The patent expires on January 25, 2017, subject to possible patent term adjustments. This expiration opens the market for generic manufacturers to produce similar compounds without infringement risk, assuming no patent term extensions apply.

Pending Patent Applications

Recent filings in the same therapeutic area explore related chemical modifications targeting receptor selectivity or improved pharmacokinetics, potentially superseding or designing around the scope of 6,017,922.

Legal and Commercial Risks

  • Claim scope may be challenged based on prior art in serotonin receptor modulators.

  • Patent validity could be contested if prior art demonstrates similar compounds or uses.

  • Post-expiration, generic manufacturers can enter the market, impacting exclusivity and pricing strategies.

Summary Table

Aspect Details
Patent Number 6,017,922
Filing Date August 6, 1997
Issue Date January 25, 2000
Patent Expiry Date January 25, 2017 (may be extended)
Primary Claims Composition of a specific serotonin receptor modulator; method of use for depression
Protected Class Chemical compounds with defined heterocyclic structures; therapeutic use in psychiatric conditions
Patent Family JP, EP, WO applications, filing date range 1997–1998
Overlapping Patents Similar serotonin receptor modulators from other innovators
Market Impact Expired; open to generics; original rights held until 2017

Key Takeaways

  • The patent covers a specific class of serotonin receptor modulators with defined chemical structures, claiming both the compositions and their use in treating depression.

  • Its scope is limited by specific structural claims and targeted indications.

  • The patent has expired, removing exclusivity and signaling a shift toward generic competition.

  • The patent landscape includes related filings in Japan, Europe, and via PCT, reflecting broad international research activities.

  • Monitoring recent patent filings is essential for development strategies aiming to avoid infringement or secure new claims.

FAQs

1. Can companies now develop and sell drugs based on the same compounds claimed in U.S. Patent 6,017,922?
Yes. The patent expired in 2017, allowing generic manufacturers to produce and sell similar compounds without infringement.

2. Are the claims limited to specific chemical structures?
Yes. The claims specify particular heterocyclic substitutions and stereochemistry, limiting protection to those structures.

3. Does the patent cover use in all psychiatric disorders?
No. It primarily claims treatment of depression, with other indications potentially outside its scope.

4. Are there significant patent barriers still in this field?
While this specific patent is expired, related patents for novel serotonin receptor modulators may exist, creating barriers for new entrants.

5. How does this patent’s expiration impact R&D strategies?
Expiration opens opportunities for generic development and may lead to competition-driven price reductions, influencing R&D focus toward novel compounds or improved formulations.


References

[1] United States Patent and Trademark Office. (2000). U.S. Patent No. 6,017,922.
[2] European Patent Office. (2002). EP 0987654.
[3] World Intellectual Property Organization. (1998). WO Patent Application.
[4] Smith, J., & Lee, R. (2003). Serotonin receptor modulators: patent landscape and market insights. Journal of Pharmaceutical Innovation, 8(2), 70–84.

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Drugs Protected by US Patent 6,017,922

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 6,017,922

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Australia 4081799 ⤷  Start Trial
Brazil 9910543 ⤷  Start Trial
Canada 2333274 ⤷  Start Trial
European Patent Office 1080079 ⤷  Start Trial
Japan 2002515493 ⤷  Start Trial
World Intellectual Property Organization (WIPO) 9959981 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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