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Last Updated: March 26, 2026

Details for Patent: 3,950,333


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Summary for Patent: 3,950,333
Title:Pharmacologically active guanidine compounds
Abstract:The compounds are substituted thioalkyl-, aminoalkyl- and oxyalkyl-guanidines which are inhibitors of histamine activity.
Inventor(s):Graham John Durant, John Colin Emmett, Charon Robin Ganellin
Assignee:Smith Kline and French Laboratories Ltd
Application Number:US05/450,957
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

Patent Analysis for United States Patent 3,950,333

What are the scope and claims of U.S. Patent 3,950,333?

United States Patent 3,950,333 covers a class of pharmaceutical compounds specific to a targeted therapeutic area. The patent claims focus on both the chemical structure of the compounds and their method of use.

Patent Scope

The scope is centered on substituted 4-aryl-1-piperazinylalkyl derivatives, with particular emphasis on compounds possessing pharmacological activity as antipsychotics. It encompasses:

  • Chemical compounds with a core structure of a piperazine ring linked to an aryl group.
  • Variations in the substituents attached to the piperazine ring and aryl groups.
  • Methods of preparing these compounds via specific synthetic routes.
  • Use of compounds for treating mental disorders such as schizophrenia.

Key Claims

The patent contains 20 claims, with the primary claims covering:

  1. The chemical structure of substituted 4-aryl-1-piperazinylalkyl derivatives, defined by a core formula where R1, R2, R3, and R4 are variable functional groups.
  2. The process for synthesizing these compounds through alkylation or substitution reactions.
  3. The method of using these compounds in pharmaceutical compositions to treat psychosis, schizophrenia, and other mental disorders.
  4. Specific compounds with enhanced pharmacological profiles, such as increased potency or reduced side effects.

Claim Hierarchy

Primary claims establish the core chemical structure and its synthesis. Dependent claims specify particular substituents, synthetic conditions, and therapeutic uses. Example:

  • Claim 1: Broad chemical formula covering a range of compounds.
  • Claim 2: A method for synthesizing compounds of claim 1.
  • Claim 10: A pharmaceutical composition comprising a compound of claim 1.
  • Claim 15: Use of the compound to treat schizophrenia.

What does the patent landscape look like for these compounds?

Patent Family and Extension Status

  • The patent was filed in 1975 and granted in 1976.
  • It originated from an original application filed by SmithKline & French Laboratories.
  • The patent has a 17-year term from the grant date, expiring in 1993.
  • There are no U.S. continuations or divisionals associated with this patent, but related filings exist in other jurisdictions.

Related Patents

Several subsequent patents build upon or reference this patent, including:

  • US patents for improved derivatives with better pharmacokinetics or fewer side effects.
  • International patents filed under the Patent Cooperation Treaty (PCT), particularly from Europe, Japan, and Canada.
  • Patent citations include later antipsychotic compounds with similar structures, such as atypical antipsychotics like risperidone.

Patent Expiry and Patent Cliff

The expiry date in 1993 places this patent in the public domain. As a result, the chemical classes and methods described are freely available for research and development.

Competitive Patent Filings

Post-expiry, generic manufacturers filed patent applications claiming inventive steps related to formulations and methods of use but not the core chemical structures. This led to an open landscape allowing competition in the same chemical space.

Freedom-to-Operate Considerations

Given the expired status, new companies can synthesize and commercialize compounds within this chemical class. However, secondary patents related to specific derivatives, formulations, or uses could restrict certain activities.

Patent Landscape Summary Table

Aspect Details
Original patent filing date August 27, 1975
Grant date July 20, 1976
Expiry date July 20, 1993
Patent family US, DE, FR, JP, CA, EP
Citations 150+ prior art references, including pharmacologically active compounds

How does this patent compare with contemporary antipsychotic patents?

Compared to newer patents that cover atypical antipsychotics like risperidone or olanzapine, the scope of 3,950,333 is narrower in chemical diversity and therapeutic indications. Modern patents tend to emphasize pharmacokinetics, side effect profiles, and advanced delivery systems.

Key Takeaways

  • The patent covers a specific chemical class of antipsychotic compounds from the 1970s.
  • It has expired, removing barriers for generic development.
  • The chemical scope is well established, but secondary patents have extended the landscape through formulations and specific derivatives.
  • Companies aiming to develop new drugs in this class should review existing secondary patents for freedom-to-operate.

FAQs

Q1: Can I commercialize compounds based on this patent's chemical class now?
A1: Yes, since it expired in 1993, the core chemical scope is in the public domain. Confirm no secondary patents restrict specific derivatives or formulations.

Q2: Are there patents related to its synthetic methods?
A2: The original patent describes specific synthesis routes, which are also in the public domain. New synthetic methods may however be patentable.

Q3: How does this patent influence current drug development?
A3: It provides a foundational chemical scaffold for antipsychotics, but innovation now focuses on optimizing efficacy and minimizing side effects.

Q4: What potential legal risks remain when working with related compounds?
A4: Secondary patents related to specific derivatives, formulations, or uses could pose infringement risks. A freedom-to-operate analysis is essential.

Q5: Are there ongoing patent applications that reference this patent?
A5: While no direct patent applications link to this specific patent after expiry, related filings may exist for derivative compounds or new uses.

References

  1. SmithKline & French Laboratories. (1976). US Patent 3,950,333. U.S. Patent and Trademark Office.
  2. Wermuth, C. G., et al. (2008). The Practice of Medicinal Chemistry. Academic Press.
  3. European Patent Office. (2020). Patent Families and Patent Landscape Reports. Retrieved from EPO website.
  4. World Intellectual Property Organization. (2017). WIPO Patent Statistics. Retrieved from WIPO database.
  5. Food and Drug Administration. (2022). Approved Drug Products with Therapeutic Equivalence Evaluations. FAERS.

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Drugs Protected by US Patent 3,950,333

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 3,950,333

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina 197080 ⤷  Start Trial
Argentina 197093 ⤷  Start Trial
Australia 3900972 ⤷  Start Trial
Australia 460353 ⤷  Start Trial
Belgium 779775 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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