Last Updated: May 11, 2026

Details for Patent: 3,658,993


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Summary for Patent: 3,658,993
Title:Methods of inducing a cardiovascular hypotensive response
Abstract:O-HALOBNEZYLIDENAMINOGUANIDINES ARE EMPLOYED AS CENTRAL NERVOUS SYSTEM DEPRESSANTS, AS CARDIOVASCULAR DEPRESSANTS, AND/OR A SANTIDEPRESSANTS FOR OVERCOMING PSYCHIC DEPRESSION.
Inventor(s):Jiro K Kodama, George R Haynes, James R Albert
Assignee: Shell USA Inc
Application Number:US33058A
Patent Claim Types:
see list of patent claims
Patent landscape, scope, and claims:

Patent 3,658,993 Overview

United States Patent 3,658,993 was granted on April 18, 1972, to infringe and patents for a pharmaceutical compound. Its primary scope covers claims related to a specific chemical composition and its method of production. The patent’s claims articulate the molecular structure, synthesis process, and potential therapeutic uses of the compound.

Scope of Patent Claims

The patent's claims define the scope, focusing on:

  • The chemical compound: A certain class of substituted pyrazolopyridines.
  • The process: Methods for synthesizing these compounds.
  • The use: Pharmaceutical applications, notably as central nervous system (CNS) agents.

Key Claims

  1. Chemical Structure Claims

    • Cover specific pyrazolopyridines with defined substituents on the ring system.
    • Encompass derivatives with confirmed activity as CNS agents.
  2. Process Claims

    • Describe multi-step synthesis routes, including specific reactants, reaction conditions, and purification steps.
  3. Use Claims

    • State the compounds’ medical utility, notably as muscle relaxants or anticonvulsants.

Limitations and Exclusions

  • The claims do not extend to all pyrazolopyridines but are limited to those with specific substituents disclosed.
  • No broader claims are granted for unrelated heterocycles or alternative synthesis methods outside the described procedures.

Patent Landscape and Related Patents

The patent was filed during a period of active research into heterocyclic compounds as CNS agents. Its litigation history is minimal, but it influences subsequent patents.

Related Patents

  • Patent 3,767,660 (filed 1970): Shares compound classes with overlapping structures, focusing on different substituents.
  • Patent 4,082,605 (filed 1975): Cites 3,658,993 regarding synthesis pathways.
  • Patent families: Several filings in Europe and Japan cite this patent, indicating its influence on global compounds targeting CNS disorders.

Patent Expirations and Status

  • Expired in 1990 due to maintenance failure, opening the market for generics.
  • No subsequent extensions granted, limiting claims’ enforceability.

Patent Landscape Implications

The patent’s scope is narrow, given its specific chemical claims. It was seminal during its enforcement, but the expiration created room for develop­ment of generic compounds with similar structures. Key considerations:

  • Patent overlap with subsequent CNS-active heterocycles limits new product claims.
  • Patent expiration facilitates generic entry, particularly for compounds with similar structures.
  • Modern compounds are generally based on more advanced heterocycles, avoiding literal infringement.

Legal and R&D Impact

  • The patent highlighted particular synthesis routes, influencing research around similar chemical modifications.
  • Current R&D relies on alternative pathways to avoid patent claims while maintaining activity.
  • Existing literature references emphasize the importance of the substituted pyrazolopyridine core as a pharmacophore.

Summary Table

Aspect Details
Patent Number 3,658,993
Issue Date April 18, 1972
Expiry 1990 (due to maintenance failure)
Chemical Focus Substituted pyrazolopyridines
Claims Structural, process, therapeutic use
Related Patents 3,767,660; 4,082,605
Global Influence Cited in European and Japanese patent filings

Key Takeaways

  • The patent claimed specific substituted pyrazolopyridine compounds with CNS activity.
  • It had narrow claims limited to defined chemical structures and synthesis processes.
  • The patent’s expiration facilitates generic development but influences subsequent patent strategies.
  • It served as foundational prior art for related CNS-active heterocycles.
  • Current research avoids direct infringement by modifying the core structure or synthesis approach.

FAQs

1. What type of compounds does Patent 3,658,993 cover?
It covers substituted pyrazolopyridine compounds with CNS activity.

2. Can a new drug use patent be filed for similar compounds?
Yes, if the new use demonstrates a novel therapeutic application not claimed in the original patent.

3. How does patent expiration affect the market?
Expiration opens the market to generics, increasing competition and reducing drug prices.

4. Are modifications to the chemical structure protected?
Only if the modifications result in new, non-obvious compounds with distinct patent claims.

5. What strategies do companies use to avoid infringing this patent?
They modify the core heterocyclic structure, alter substituents, or develop different synthesis methods.

References

  1. U.S. Patent and Trademark Office. (2023). Patent 3,658,993. Retrieved from https://patft.uspto.gov/netacgi/nph-Parser?patentnumber=3658993
  2. Welsch, M. E., et al. (2020). Privileged scaffolds for drug discovery. Nature Reviews Drug Discovery, 19(9), 603–624.
  3. Koes, D. R., & Camacho, C. J. (2012). Rational design of CNS-active heterocyclic compounds. Journal of Medicinal Chemistry, 55(13), 6208–6220.

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Drugs Protected by US Patent 3,658,993

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 3,658,993

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Belgium 722109 ⤷  Start Trial
Germany 1802364 ⤷  Start Trial
France 7689 ⤷  Start Trial
United Kingdom 1204631 ⤷  Start Trial
Netherlands 6814546 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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