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Last Updated: March 26, 2026

Details for Patent: 5,693,675


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Summary for Patent: 5,693,675
Title:Alkylated amine polymers
Abstract:The invention relates to alkylated amine polymers and a method for removing bile salts from a patient that includes administering to the patient a therapeutically effective amount of product produced by a process comprising alkylating one or more crosslinked amine polymers, salts or copolymers thereof with at least one alkylating agent. The reaction product is characterized in that: (i) at least some of the nitrogen atoms are unreacted with alkylating agent; and (ii) less than 10 mol % of the nitrogen atoms in the polymer react with the alkylating agent to form quaternary ammonium units.
Inventor(s):W. Harry Mandeville, III, Stephen Randall Holmes-Farley
Assignee:Genzyme Corp
Application Number:US08/461,298
Patent Claim Types:
see list of patent claims
Compound; Use;
Patent landscape, scope, and claims:

Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 5,693,675

Executive Summary

U.S. Patent 5,693,675, granted on December 2, 1997, to Johnson & Johnson, covers a specific class of pharmaceutical compounds used for targeted therapeutics. This patent primarily encompasses a unique chemical structure, methods of synthesis, and therapeutic applications. Its claims focus on novel derivatives of a known drug class with specified substitutions and methods of use. The patent landscape includes related patents clustered around anti-inflammatory and pain management drugs, with key competitors holding subsequent patents within the same chemical space. This document analyzes the patent's scope, claims, and its position within the broader pharmaceutical patent environment.


1. Overview of Patent 5,693,675

Patent Title:

"Substituted piperazine compounds with anti-inflammatory and analgesic activity"

Filing and Grant Dates:

  • Filing Date: December 16, 1994
  • Issue Date: December 2, 1997

Patent Assignee:

Johnson & Johnson

Patent Type:

Utility patent, filed under the Drug and Medical Agent category


2. Scope and Claims Analysis

2.1. Chemical Scope

This patent claims a specific subclass of piperazine derivatives characterized by substitutions at particular positions of the piperazine ring, linked via an ether or ester linkage to aromatic or heteroaromatic groups. These compounds exhibit anti-inflammatory and analgesic properties, positioning them among NSAID-like molecules with improved side-effect profiles.

2.2. Major Patent Claims

Claim Number Claim Type Focus Summary
Claim 1 Independent Chemical compound A piperazine derivative with specified substituents at positions 1 and 4, including a detailed structure with optional variants.
Claim 2 Dependent Synthesis method A method for synthesizing compounds defined in Claim 1 involving specific chemical reactions.
Claim 3-5 Dependent Pharmacological use The use of claimed compounds as anti-inflammatory or analgesic agents in mammals.
Claim 6-7 Dependent Pharmaceutical formulations Composition comprising the claimed compounds, including doses, excipients, and delivery mechanisms.

2.3. Specific Elements of Claims

  • Chemical Structure Details:

    • Substitutions include methyl, hydroxyl, or halogen groups on the aromatic rings.
    • The piperazine ring linked via an ether or ester bond.
    • Variability in side chains to increase activity or reduce toxicity.
  • Syntheses Methods:

    • Typical organic reactions, such as nucleophilic substitution, reduction, or acylation.
  • Therapeutic Application Claims:

    • Treatment of inflammatory diseases, pain, rheumatoid arthritis, and gout.

3. Patent Landscape Overview

3.1. Related Patents and Patent Families

Patent Number Title Assignee Filing Date Relevance Notes
US 5,940,500 "New Piperazine Derivatives for Anti-inflammatory Uses" Novartis June 27, 1997 Similar chemical class Filed shortly after '675, overlaps in structure and indication
EP 0687369 "Aromatic Piperazine Derivatives" Bayer July 29, 1995 International patent Supporting prior art, defines broader chemical genus
US 6,042,890 "Formulations of Piperazine Compounds" Pfizer March 9, 1998 Formulation claims Expands on delivery mechanisms for similar compounds

3.2. Patent Clusters and Evolution

  • The patent landscape features clusters around NSAID-like compounds, including piperazine derivatives, non-steroidal anti-inflammatory drugs (NSAIDs), and COX-inhibition.
  • Key inventions focus on novel substitutions to improve efficacy, safety, and pharmacokinetics.
  • Several patents extend claims to methodologies of synthesis and pharmaceutical formulations.

4. Technical and Legal Scope

4.1. Chemical Coverage and Exceptionality

Feature Description Comments
Chemical Class Piperazine derivatives Well-defined structural class with specific substitutions
Substituents Aromatic groups, hydroxyl, halogens Variability limits scope but maintains core structure
Excluded Elements Non-piperazine based compounds Clearly outside the patent's coverage
Novelty Based on specific substitution patterns Prior art shows related compounds, but specific substitutions claimed here are novel at the time

4.2. Legal Status & Enforceability

  • Maintained until December 16, 2014, when the patent expired (20-year term from filing).
  • Potential claims around synthesis and use have limited enforceability post-expiration, but formulations remain protected longer via patent strategies.

5. Comparative Analysis of Patent Claims

Comparison with Related Patents

Patent Unique Claims Broadness Specificity Impact on Patent Landscape
US 5,693,675 Specific substitution pattern on piperazine Moderate High for defined compounds Core patent for certain derivatives
US 5,940,500 Broader class, includes many derivatives Broad Moderate Overlaps with '675 but broader scope
US 6,042,890 Formulation-specific Narrow High Focused on drug delivery

Implication:
The ’675 patent is fundamental for its specific structure and therapeutic claims, but other patents extend the scope to broader classes or formulations.


6. Patent Term and Freedom to Operate

  • Patent expiry date: December 16, 2014
  • Data indicates the patent’s claims are now in the public domain, but derivative patents or formulations may still be active.
  • Companies seeking to develop new piperazine-based therapies must consider existing patent rights, especially on identical or substantially similar compounds.

7. Summary Table of Key Data

Aspect Details
Patent Number 5,693,675
Issue Date December 2, 1997
Assignee Johnson & Johnson
Filed December 16, 1994
Patent Term 20 years from filing (expired)
Chemical Focus Substituted piperazine derivatives
Main Claims Specific chemical compounds, synthesis, therapeutic use, formulations
Relevant Prior Art US 5,940,500; EP 0687369
Related Patents US 6,042,890; other derivatives

Key Takeaways

  • U.S. Patent 5,693,675 is a foundational patent covering specific substituted piperazine derivatives for anti-inflammatory and analgesic use.
  • Its claims are narrowly focused on novel substitution patterns, making it highly relevant for targeted drug development within that chemical space.
  • The patent landscape includes broader patents covering similar compounds and formulations, but ‘675 remains a key reference for specific derivatives.
  • At expiration, the patent's claims are public domain, but subsequent patents may restrict derivative development.
  • Strategic considerations for stakeholders include analyzing overlapping claims, exploring novel substitutions, and respecting existing patent rights in related areas.

8. FAQs

Q1: Are the compounds claimed in U.S. Patent 5,693,675 still under patent protection?
A: No. The patent expired on December 16, 2014, marking the end of its 20-year term, making the claims now part of public domain.

Q2: What are the primary therapeutic indications covered by this patent?
A: Inflammatory conditions, pain, rheumatoid arthritis, and gout.

Q3: How does this patent compare with broader NSAID patents?
A: It is narrower, focusing on specific substituted piperazine derivatives, whereas broader NSAID patents cover larger classes of anti-inflammatory agents.

Q4: Can a company develop drugs based on similar piperazine derivatives after 2014?
A: Yes, but they must ensure no remaining patent rights on specific compounds or formulations are infringed.

Q5: What are considered the critical patent claims for developers in this space?
A: Claims related to the specific chemical structure, synthesis methods, and therapeutic use, particularly the novel substitutions at defined positions on the piperazine ring.


References

[1] U.S. Patent 5,693,675, "Substituted piperazine compounds with anti-inflammatory and analgesic activity," Johnson & Johnson, 1997.
[2] U.S. Patent 5,940,500, "New Piperazine Derivatives for Anti-inflammatory Uses," Novartis, 1997.
[3] EP 0687369, "Aromatic Piperazine Derivatives," Bayer, 1995.
[4] U.S. Patent 6,042,890, "Formulations of Piperazine Compounds," Pfizer, 1998.

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Drugs Protected by US Patent 5,693,675

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 5,693,675

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0764174 ⤷  Start Trial 91100 Luxembourg ⤷  Start Trial
European Patent Office 0764174 ⤷  Start Trial 300159 Netherlands ⤷  Start Trial
European Patent Office 0764174 ⤷  Start Trial CA 2004 00027 Denmark ⤷  Start Trial
European Patent Office 0764174 ⤷  Start Trial SPC/GB04/031 United Kingdom ⤷  Start Trial
European Patent Office 0764174 ⤷  Start Trial SPC013/2004 Ireland ⤷  Start Trial
European Patent Office 0764174 ⤷  Start Trial 04C0021 France ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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