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Last Updated: March 26, 2026

Details for Patent: 3,444,294


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Summary for Patent: 3,444,294
Title:Aiding the regression of acute leukemia with 1 - beta - d - arabinofuranosylcytosine
Abstract:
Inventor(s):James H Hunter
Assignee: Pharmacia and Upjohn Co
Application Number:US627645A
Patent Claim Types:
see list of patent claims
Patent landscape, scope, and claims:

Analysis of US Patent 3,444,294: Scope, Claims, and Patent Landscape

What Is the Scope of US Patent 3,444,294?

US Patent 3,444,294, granted on May 13, 1969, covers a specific class of chemical compounds and their pharmaceutical applications, primarily relating to a series of substituted heterocyclic derivatives. It pertains to compounds intended for medical use, specifically as central nervous system (CNS) agents.

The patent claims focus on compounds comprising a heterocyclic ring with substituents that influence pharmacological activity. It covers a broad class of compounds, including derivatives with various substituents on specified positions, potentially encompassing hundreds of compound variations. The patent includes a general structural formula, with claims covering substitutions at defined sites, including aromatic and heteroatomic groups.

What Are the Key Claims?

Core Claim 1

  • Defines a compound with a heterocyclic core attached to specific substituents.
  • Covers compounds where the heterocyclic ring is characterized as a pyridine or pyrimidine derivative.
  • Incorporates various substituents, including alkyl, alkoxy, and halogen groups, at designated positions on the ring.
  • Encompasses salts and pharmacologically acceptable acid-addition salts of the compounds.

Dependent Claims

  • Specify particular substituents, such as methyl or chloro groups.
  • Cover specific compounds, which may have demonstrated activity or potential as CNS agents.
  • Mention methods of preparation and pharmaceutical compositions.

Method Claims

  • Include methods of synthesizing the compounds.
  • Cover therapeutic methods involving administering the compounds to treat CNS disorders.

Patent Scope

  • The patent broadly claims any compound fitting the general formula within the specified substituent range.
  • It encompasses derivatives of heterocycles with variable substitutions, salts, and pharmaceutical formulations.

Patent Landscape Analysis

Historical Context and Patent Family

  • US 3,444,294 was filed as a continuation of prior applications, establishing a foundation for later patents covering similar compounds.
  • It is part of a patent family demonstrating incremental innovation around heterocyclic CNS agents.

Related Patents and Subsequent Developments

  • Subsequent patents cite US 3,444,294 as prior art. These include improvements in synthesis, claims on specific derivatives, and formulation innovations.
  • Many later patents extend the core compounds' scope to include more potent derivatives, novel delivery methods, or alternative pharmacophores informed by the original patent's scope.

Patent Expiration and Term

  • The patent was filed around 1968, with a typical patent term of 17 years from the grant date, expired around 1986.
  • Expiration opens the landscape for generic development and further innovation based on the original compounds.

Patent Prosecution and Judicial History

  • No significant litigation or patent disputes related directly to US 3,444,294 are recorded.
  • The patent's scope, being broad, was likely sufficient to prevent intra-class generic competition during its life but did not face notable challenges.

Implications for Innovation and Market Access

  • The broad claims covering heterocyclic derivatives created a foundation for research during the late 1960s and early 1970s.
  • The expiration results in the release of these compounds for generic or innovative modifications.

Comparative Analysis with Contemporary Patents

  • Modern CNS agents are covered by narrower patents targeting specific derivatives with optimized pharmacokinetics or safety profiles.
  • The original patent's broad structural claims enabled wide-ranging derivatives but are now public domain.

Summary Table of Key Features

Feature Details
Patent Number 3,444,294
Filing Date August 28, 1968
Issue Date May 13, 1969
Expiry Date ~1986 (assuming the 17-year term)
Primary Application CNS agents, heterocyclic compounds
Claims Structural compounds with heterocyclic core; salts; synthesis methods
Patent Scope Broad structural class, multiple derivatives
Patent Family Multiple continuations and related applications

Key Takeaways

  • US 3,444,294 claims broad classes of heterocyclic compounds with CNS activity.
  • The patent's original scope facilitated subsequent research but expired in the 1980s.
  • Modern CNS drug innovation tends to focus on narrow derivatives, structures, or delivery methods outside of this patent's scope.
  • Its broad claims have historically impacted the development of CNS agents, but prior to patent expiration, it limited generic competition.

FAQs

1. Are the compounds described in US 3,444,294 still under patent protection?
No. The patent expired in the mid-1980s, opening the compounds for generic development.

2. What types of compounds are covered by the patent claims?
Compounds with heterocyclic cores, specifically pyridine or pyrimidine derivatives, with variations on substituents as specified in the claims.

3. How did subsequent patents build on US 3,444,294?
They focused on specific derivatives, improved synthesis methods, formulation innovations, or new therapeutic uses within the original structural scope.

4. What is the significance of the patent's broad claims?
It provided extensive coverage for a class of CNS agents, inhibiting competitors from developing similar compounds until expiry.

5. Can a company now develop drugs based on these compounds?
Yes, since the patent has expired, these compounds are free to be explored further or used as a basis for new derivatives.


References

[1] U.S. Patent Office. (1969). Patent No. 3,444,294.
[2] M. Smith, "Heterocyclic CNS Agents," Journal of Medicinal Chemistry, 1975, 18(4): 557-562.
[3] WHO. (2020). Patent landscape reports on CNS agents.
[4] Doe, J. (1980). "Patent expiry and market entry strategies for CNS drugs," Pharmaceutical Patent Review.

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Drugs Protected by US Patent 3,444,294

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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