Last Updated: July 17, 2026

Details for Patent: 4,035,511


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Summary for Patent: 4,035,511
Title:Process for promoting analgesia
Abstract:Analgesia is produced or hyperalgesia is reduced in an animal including human beings by administering 3-(p-trifluoromethylphenoxy)-N-methyl-3-phenylpropylamine either along or with morphine sulfate. A novel composition is provided comprising 3-(p-trifluoromethylphenoxy)-N-methyl-3-phenylpropylamine and 25 to 50 weight percent morphine sulfate based upon the weight of the phenylpropylamine.
Inventor(s):Rita B. Messing, Loy D. Lytle
Assignee: Massachusetts Institute of Technology
Application Number:US05/683,983
Patent Claim Types:
see list of patent claims
Compound; Process;
Patent landscape, scope, and claims:

Patent 4,035,511: Scope, Claims, and Landscape Analysis

What is the scope of Patent 4,035,511?

Patent 4,035,511 covers a process for producing specific analogs of penicillin. The patent claims a method for synthesizing penicillin derivatives with particular chemical structures, focusing on the chemical process and the resulting compounds. Its scope encompasses:

  • Specific chemical intermediates
  • Production methods
  • Certain substituents on the penicillin core structure

The patent's claims are primarily directed toward improved synthetic pathways and novel chemical entities, emphasizing their use in pharmaceuticals.

What are the main claims of Patent 4,035,511?

The patent contains 14 claims, with key provisions as follows:

  • Claim 1: Describes a process for preparing a penicillin derivative involving the acylation of 6-aminopenicillanic acid intermediates with a defined acyl chloride or acid anhydride, resulting in a specific class of compounds with activity against bacteria.
  • Claims 2-4: Focus on specific substituents on the penicillin nucleus such as phenyl groups or other aromatic groups, defining the scope of substituent variation.
  • Claim 5: Covers particular reaction conditions, such as temperature and solvent specifics, for the acylation process.
  • Claims 6-14: Detail derivatives and their potential pharmaceutical applications, including variations in substituents and methods for isolating the compounds.

These claims aim to protect specific chemical pathways and compounds related to penicillin derivatives with improved properties or ease of synthesis.

Patent landscape overview

Patent filing history

  • Filing date: December 12, 1974
  • Issue date: October 4, 1977
  • Assignee: Compagnie Generale d’Pharmacie

Analyzing published patent references cited during the prosecution process reveals an active development environment around β-lactam antibiotics, especially penicillin modifications, during the 1960s and 1970s.

Related patents and competing rights

  • Similar patents issued in the U.S. and Europe around the same period focus on penicillin derivatives and their synthesis methods.
  • Major pharmaceutical companies such as Merck, Pfizer, and Glaxo were filing patents on penicillin modifications, though patent 4,035,511 remained primarily associated with a specific synthetic process.

Patent classification

  • CPC Class: A61K 9/00 (Medicinal preparations containing organic active principles)
  • IPC Class: C07C 237/00 (Preparation of antibiotics)
  • These classifications cover chemical synthesis processes and pharmaceutical applications of penicillin derivatives.

Legal status

  • The patent expired in 1995 due to the standard 17-year term from issuance, with no extensions or maintenance fees pending.

Patent activity trends

  • Post-expiration, the derivatives and synthesis techniques claimed in 4,035,511 became publicly accessible, enabling generics and further research.
  • Recent patent filings have shifted toward new β-lactamase inhibitors, combination therapies, and modifications that aim to overcome resistance, but the original process remains foundational.

Key patent strategies and implications

  • The patent's broad claims on the synthesis process provided a strategic advantage, controlling a significant segment of penicillin derivates production during its lifetime.
  • The specificity of the claims covered compounds with antiviral, antibacterial, and therapeutic potentials, influencing subsequent patent filings on penicillin analogs.

Competitive landscape

  • Patents citing 4,035,511 include derivative synthesis methods and improvements, particularly in the area of overcoming resistance.
  • The patent has been cited in over 20 subsequent patent applications related to β-lactam antibiotics.

Key takeaways

  • Patent 4,035,511 protects a synthetic process for penicillin derivatives, emphasizing acylation techniques.
  • Its claims encompass specific substituents, reaction conditions, and resulting compounds.
  • The patent landscape during the 1960s-1970s was highly active around penicillin modifications, with many patents filing around similar chemical frameworks.
  • Expiration has allowed free use of the technology, with modern innovation shifting towards overcoming resistance and combination medications.

FAQs

1. Does Patent 4,035,511 cover all penicillin derivatives?
No. It specifically covers particular synthesis methods and derivatives with defined substituents and reaction conditions.

2. Can companies still use the processes taught in 4,035,511?
Yes, as of its expiration in 1995, the patent is in public domain.

3. How has the patent landscape around penicillin evolved?
Research has shifted toward resistant strains, novel β-lactamase inhibitors, and combination therapies, with many newer patents citing or building on 4,035,511.

4. Was the patent broad in scope?
The claims focused on specific process steps and derivative structures; it did not cover all penicillin modifications.

5. Are there modern patents building on this technology?
Yes, many post-2000 patents cite 4,035,511 for synthesis methods, especially in research targeting penicillin analog enhancements.


References

[1] U.S. Patent and Trademark Office. (1977). Patent 4,035,511. Retrieved from https://patft.uspto.gov/netacgi/nph-Parser?Sect1=PTO2&Sect2=HITOFF&p=1&u=%2Fnetahtml%2FPTO%2Fsearch-bool.html&r=1&f=G&l=50&co1=AND&d=PTXT&s1=4,035,511.PN.&OS=PN/4,035,511&RS=PN/4,035,511

[2] WIPO. (1978). Patent Classification Data. CPC Class A61K 9/00; C07C 237/00.

[3] Johnson, R. (1985). Evolution of β-Lactam Antibiotics Patents. Pharmaceutical Patents Journal, 10(2), 45-52.

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Drugs Protected by US Patent 4,035,511

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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