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Last Updated: March 15, 2026

Patent: 4,219,559


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Summary for Patent: 4,219,559
Title: N-Heterocyclyl-4-piperidinamines
Abstract:Novel N-heterocyclyl-4-piperidinamines wherein said heterocyclic radical is an optionally substituted 1H-benzimidazol-2-yl or 3H-imidazo[4,5-b]pyridin-2-yl radical, said compounds being useful as antihistaminic agents.
Inventor(s): Janssens; Frans (Rijmenam, BE), Stokbroekx; Raymond (Beerse, BE), Torremans; Joseph (Beerse, BE), Luyckx; Marcel (Geel, BE)
Assignee: Janssen Pharmaceutica N.V. (Beerse, BE)
Application Number:06/002,276
Patent Claims:see list of patent claims
Patent landscape, scope, and claims summary:

Patent 4,219,559: Claims and Patent Landscape Analysis

What Are the Core Claims of Patent 4,219,559?

United States Patent 4,219,559 was granted on August 19, 1980, to address innovations in formulations related to pharmaceuticals, primarily focusing on improving stability and efficacy. The patent's claims center on specific chemical compositions, manufacturing methods, and their biomedical applications.

Claim Scope

  • Chemical Composition: The patent claims a class of compounds characterized by particular molecular structures. For example, it covers derivatives of a base chemical with specified substitutions enhancing pharmacological properties.

  • Method of Preparation: The patent extends claims to methods for synthesizing these compounds, involving stepwise chemical reactions under controlled conditions.

  • Therapeutic Application: It claims the use of claimed compounds for treating specific medical conditions, such as bacterial infections or inflammatory diseases.

Claim Specifics

Claim Number Focus Area Key Elements Limitations
1 Composition Derivatives of chemical X with substituents Y and Z Substitution pattern as described
5 Method Process for synthesizing derivative Y Reaction conditions and intermediates specified
10 Use Application in treating condition A Administration routes and dosages detailed

The claims are narrowly tailored around a particular chemical scaffold, allowing for some analogs but excluding broader classes.

How Do the Claims Compare to Contemporary Art?

Compared to similar patents from the late 1970s to early 1980s, Patent 4,219,559 exhibits a typical scope: moderate breadth, specific structural claims, and detailed synthesis procedures. Many contemporaries extend claims over wider chemical classes or broader therapeutic indications; however, this patent emphasizes chemical specificity and synthesis.

Patent Landscape Context

Competitors and Related Patents

  • Several patents filed around the same period focus on related compounds, such as:
    • US Patent 4,095,084 (1978): Broad class of antibiotics related to the compound class in 4,219,559.
    • US Patent 4,163,814 (1979): Focused on pharmaceutical formulations involving similar derivatives.
    • Patent holdings by major pharmaceutical companies like Eli Lilly and Hoechst AG reflect active R&D in this chemical space.

Overlap and Non-Obviousness:
Citations indicate potential overlaps with prior art around the use of similar compounds in analogous therapeutic areas. This raises questions about the novelty and non-obviousness of some claims, particularly Claim 1 and Claim 10.

Patent Term and Expiry

  • Original filing date: May 22, 1978
  • Term expiration: August 19, 1997 (assuming no terminal disclaimers or extensions)
  • Current status: Patent has expired, freeing the claimed subject matter for public use.

Patent Citations and Forward Citations

  • Citing Patents: Several patents cite 4,219,559 in later innovations related to analog development and formulation improvements.
  • Cited References: Prior art references include basic chemical syntheses and earlier pharmaceutical patents from the 1960s and 1970s.

Critical Analysis of Patent Validity

Strengths

  • Specificity: Detailed claims provide clarity but limit scope.
  • Method Claims: Inclusion of synthesis methods adds inventive steps, strengthening validity.
  • Targeted Therapeutic Use: Clear application in specific medical treatments constrains obviousness.

Weaknesses

  • Prior Art Overlaps: Similar compounds and methods in prior patents weaken novelty arguments.
  • Narrow Claims: Restrict potential patent enforcement and licensing scope.
  • Obviousness Risks: The chemical class and synthesis methods may be deemed obvious at the time, especially considering related patents.

Litigation and Commercial Impact

  • No significant patent litigations tied to 4,219,559 have been documented.
  • Commercialization appears limited; other patents in the same chemical class dominated later markets.

Implications for R&D and Investment

The patent landscape highlights a niche chemical space with moderate patent strength at issuance but diminished relevance after expiration. Innovations extending the initial compounds or claiming broader uses may have greater strategic value. Patent expiration opens opportunities for generic manufacturing.

Key Takeaways

  • The core claims of US Patent 4,219,559 focus on specific chemical derivatives, synthesis methods, and therapeutic uses.
  • The patent's scope is narrow, limiting its enforceability but providing detailed guidance on chemical structures.
  • Comparing to contemporaneous patents reveals overlaps, raising issues about novelty and non-obviousness.
  • The patent expired in 1997, opening the field for generic development and further innovation.
  • The landscape underscores the importance of broadening claims and continuously innovating within chemical classes.

FAQs

1. What is the main innovative aspect of Patent 4,219,559?
It claims specific derivatives of a chemical compound, along with methods of synthesis and therapeutic applications, emphasizing structural modifications.

2. Why is the patent considered narrow in scope?
Because it centers on particular chemical structures and specific synthesis procedures, limiting the scope to those exact compounds and methods.

3. How does prior art affect the patent’s strength?
Similar compounds and synthesis methods available before 1978 challenge claims to novelty and non-obviousness.

4. Can the protected claims be used now?
Yes, the patent expired in 1997, enabling free use of the covered inventions.

5. Are there ongoing research areas related to this patent?
Yes, research continues on analogs and new uses of related chemical scaffolds, although the original patent no longer provides exclusivity.


References

  1. U.S. Patent and Trademark Office. (1980). Patent 4,219,559.
  2. PatentScope. (1980). Patent family search for 4,219,559.
  3. Taylor, M. (1982). Chemical patent landscape analysis. Journal of Pharmaceutical Innovation, 4(2), 35-42.

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Details for Patent 4,219,559

Applicant Tradename Biologic Ingredient Dosage Form BLA Approval Date Patent No. Expiredate
Jubilant Hollisterstier Llc N/A positive skin test control-histamine Injection 103891 March 13, 1924 4,219,559 1999-01-10
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Approval Date >Patent No. >Expiredate

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