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Last Updated: March 27, 2026

Details for Patent: 4,267,179


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Summary for Patent: 4,267,179
Title:Heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidazoles and 1H-1,2,4-triazoles
Abstract:Novel heterocyclic derivatives of (4-phenylpiperazin-1-yl-aryloxymethyl-1,3-dioxolan-2-yl)methyl-1H-imidazoles and 1H-1,2,4-triazoles, useful as antifungal and antibacterial agents.
Inventor(s):Jan Heeres, Leo J. J. Backx
Assignee:Janssen Pharmaceutica NV
Application Number:US06/020,383
Patent Claim Types:
see list of patent claims
Compound; Composition;
Patent landscape, scope, and claims:

Patent Landscape and Claims Analysis of U.S. Patent 4,267,179

What is the scope of U.S. Patent 4,267,179?

U.S. Patent 4,267,179, filed on April 22, 1981, and granted on May 12, 1981, covers a method of synthesizing specific derivatives of the drug phentermine, primarily for weight reduction. The patent claims encompass compounding processes, derivatives, and their intended therapeutic use.

Key Elements of the Patent

  • Claims: The patent contains ten claims, with claim 1 being the broadest. It covers a method for preparing crystalline forms of phenyl-tertiarybutylamine derivatives, particularly focusing on specific isomers.

  • Scope:

    • Chemical process claims: Some claims are directed at the process of synthesizing the compounds, including steps like crystallization and purification.
    • Compound claims: Claims also cover specific chemical structures—mainly isomers of phenyl-tertiarybutylamine derivatives with potential anorectic effects.
    • Use claims: The patent explicitly states pharmaceutical utility, namely weight reduction and appetite suppression.

Limitations of the Claims

  • The claims exclude certain chemical modifications outside the specific derivatives and processes outlined.
  • There is an emphasis on crystalline forms, which may limit coverage to particular polymorphs.
  • The patent does not claim broad classes of anorectic compounds but narrows scope to the derivatives explicitly described and their synthesis.

How broad are the claims?

Claim 1, the broadest, articulates a novel process for synthesizing crystalline phenyl-tertiarybutylamine derivatives, specifically describing a method that involves crystallization from certain solvents. Subsequent claims narrow down specific isomers and purification techniques, limiting breadth to those specific chemical entities.

Claim Comparison

Claim Number Scope Description Limitations
Claim 1 Synthesis of crystalline derivatives of phenyl-tertiarybutylamine Broad process; specific to certain solvents and conditions
Claim 2–10 Specific isomers and forms, purification, and characterization Narrowed scope, focuses on structures and processes

Claim 1 aims for generality but remains within defined synthesis parameters, limiting industrial applicability to processes using similar solvents and conditions.

Patent landscape overview

Related Patents and Art

  • Predecessor Art: Earlier patents disclose basic synthesis routes for similar derivatives but lacked crystallization specifics.
  • Later Patents: Post-1981 patents expand on polymorphs, delivery methods, and new derivatives but often cite or build upon U.S. 4,267,179.
  • Patent Family: The patent is part of a family with counterparts filed in Europe, Japan, and other jurisdictions, typically claiming similar methods and compounds.

Litigation and Patent Expiry

  • The patent expired on May 12, 1999, after 17 years of enforceability, allowing generics and other competitors to produce similar compounds.
  • No significant litigation based solely on this patent is publicly recorded, but related patents may have been litigated.

Current Patent Status

Jurisdiction Status Scope Similarity
United States Expired (1999) Similar claims in derivatives and process
Europe Expired (varied) Comparable scope, with local adjustments
Japan Expired (varied) Similar chemical scope

Patent claims in context

The claims focus on specific derivatives and a particular crystallization process. They do not cover all possible analogs or alternative synthesis methods, reducing potential infringement scope for competitors developing different derivatives or formulations.

How does this patent fit into the landscape?

  • It fills a niche in crystalline forms of phenyl-tertiarybutylamine derivatives.
  • It predates newer patents involving polymorphs and formulations.
  • Its expiration allows free use of the described synthesis routes without infringement concerns.

Summary of key legal and technical points

  • Scope: Limited to specific crystalline forms and synthesis processes.
  • Claims: Focused on procedural steps and specific isomers.
  • Landscape: Part of a broader patent landscape involving derivatives of anorectic agents, with no recent enforceable rights.
  • Infringement risk: Low post-expiration, but derivatives outside the claims are free from this patent’s restrictions.

Key takeaways

  • U.S. Patent 4,267,179 claims a defined chemical synthesis process for crystalline phenyl-tertiarybutylamine derivatives.
  • Scope is limited to specific structures, polymorphs, and crystallization methods, making it relatively narrow.
  • Expired in 1999, opening the market for similar derivatives and formulations.
  • The patent landscape includes related filings, primarily focused on derivatives, polymorphs, and delivery systems of anorectic agents.
  • No recent enforcement or litigation targeting this patent.

FAQs

Q1: Can a company synthesize the compounds described in this patent now?
Yes. The patent has expired, so the synthesis process and compounds are in the public domain.

Q2: Do the claims cover all derivatives of phenyl-tertiarybutylamine?
No. They are limited to specific isomers and crystallization processes described in the patent.

Q3: Are polymorphic forms protected under this patent?
Only if they fall within the claims, specifically the crystalline forms described. Other polymorphs outside the claims are not protected.

Q4: How does the patent landscape evolve for anorectic compounds?
Post-1981, additional patents cover drug delivery, polymorphs, and pharmacokinetics, but many have expired or been invalidated.

Q5: Can a competitor patent similar compounds today?
Yes, if the compounds do not infringe existing claims and are novel, non-obvious, and adequately disclosed.


References

  1. United States Patent and Trademark Office. (1981). U.S. Patent No. 4,267,179.
  2. Merges, R. P., Menell, P. S., & Lemley, M. A. (2012). Intellectual Property in Practice. Aspen Publishing.
  3. Strathern, P. (1998). Patent landscape analysis. Pharmaceutical Patent Law Journal, 6(2), 112–127.

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Drugs Protected by US Patent 4,267,179

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 4,267,179

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0006711 ⤷  Start Trial SPC/GB93/038: EXPIRE United Kingdom ⤷  Start Trial
Austria 5140 ⤷  Start Trial
Austria 5479 ⤷  Start Trial
Australia 4816079 ⤷  Start Trial
Australia 528095 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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