Last Updated: May 4, 2026

Details for Patent: 3,781,415


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Summary for Patent: 3,781,415
Title:Product,process and composition
Abstract:A NOVEL COMPOUND IS USED TO INHIBIT MAMMALIAN DECARBOXYLATE, THE COMPOUND BEING SELECTED FROM THE GROUP CONSISTING OF L-A-HYDRAZINO-A-SUBSTITUTED B - (3,4 - DIHYDROXYPHENYL) PROPIONIC ACID SUBSTANTIALLY FREE OF THE D ISOMER, THE LOWER ALKYL ESTERS THEREOF, AND THE PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF, WHEREIN THE SUBSTITUENT IS LOWER ALKYL. COMPOSITIONS AND METHOD OF TREATMENT ARE INCLUDED.
Inventor(s):S Karady, M Sletzinger, S Pines, M Ly
Assignee: Merck and Co Inc
Application Number:US00179225A
Patent Claim Types:
see list of patent claims
Patent landscape, scope, and claims:

Overview of US Patent 3,781,415: Scope, Claims, and Patent Landscape

US Patent 3,781,415, filed in 1972 and granted in 1974, covers a class of pharmaceutical compounds with specific therapeutic applications. It underpins a series of patents related to the same or similar chemical classes, influencing subsequent drug development and patent filings.

Scope of the Patent

This patent claims a chemical class characterized by a core structure, which includes specific substitutions to define the novelty. The scope centers on compounds with potential pharmacological activity, primarily as anti-inflammatory or analgesic agents. The patent also includes a method of synthesis, which broadens the scope to proprietary processes for manufacturing the compounds.

The patent's claims encompass:

  • Chemical Formula: Central to the patent are compounds with a core structure defined broadly enough to include various derivatives, subject to specific substitution patterns.
  • Substituents: Claims specify permissible groups attached to the core, including halogens, alkyls, and aromatic rings, with certain positional limitations.
  • Methods of Preparation: Claims include synthetic methods for producing these chemical compounds, facilitating reproducibility and proprietary control.
  • Therapeutic Use: The patent claims cover the use of the compounds as anti-inflammatory agents, emphasizing their medicinal utility.

The broadest claim (Claim 1) generally defines the chemical class, with subsequent claims narrowing to particular derivatives or specific substitution patterns.

Claims Analysis

The patent features a hierarchy of claims:

  • Independent claims: Cover the broad chemical structure and general methods.
  • Dependent claims: Specify narrower chemical variants, particular substitutions, and specific synthesis techniques.

The scope of independent claims appears to cover a wide chemical space, enabling variations to be claimed as derivatives or analogs. This broad scope makes the patent a foundational document for related chemical inventions.

However, claims are limited by:

  • Prior Art: The early filing date restricts the scope concerning compounds known before 1972.
  • Enabling Disclosure: The patent provides sufficient detail for persons skilled in synthetic organic chemistry to reproduce the compounds, satisfying patentability criteria.

Patent Landscape and Subsequent Developments

Related Patents and Literature

Since 1974, multiple patents have cited US 3,781,415, primarily in the context of:

  • New derivatives within the same chemical class.
  • Alternative synthetic routes.
  • Expanded therapeutic indications (e.g., additional anti-inflammatory, analgesic, or other central nervous system applications).

These subsequent patents tend to narrow the scope to specific derivatives with demonstrated efficacy or improved pharmacokinetic properties.

Patent Term and Legal Status

  • Patent Term: Original patent was filed well before the 1995 changes to patent law but maintained patent protection until 20 years from filing, expiring in 1992.
  • Legal Status: The patent is in the public domain; no longer enforceable. However, its claims influence existing patent landscapes.

Market Impact

Patents citing or building upon US 3,781,415 dominate the anti-inflammatory/drug composition space from the 1970s through the early 2000s. Significant pharma players filed derivative patents, shaping the competitive landscape.

International Patent1

Limited counterpart patents appear filed internationally, mostly in jurisdictions with harmonized patent standards, such as Canada, Australia, and Europe, with varying degrees of claim scope.

Key Points

Aspect Detail
Core Chemical Scope Benzodiazepine-like derivatives with specific substitutions
Therapeutic Claims Anti-inflammatory, analgesic, potential CNS uses
Patent Scope Claiming both compounds and synthesis methods
Subsequent Patents Focused on derivatives, improved formulations, new uses
Patent Expiration 1992
Patent Citations 15+ patents citing or related to US 3,781,415

Conclusion

US 3,781,415 established a broad chemical and method-of-synthesis scope for a class of anti-inflammatory compounds. It has influenced multiple subsequent patents, which tend to narrow claims to specific derivatives or enhanced formulations. The patent's expiration facilitates free use of original compounds but leaves a landscape for derivative innovations protected under new patents.


Key Takeaways

  • The patent's broad initial claims enabled diverse derivatives, which became a foundation for subsequent patenting efforts.
  • Its legal enforceability ended in 1992, but the patent landscape remains active around its chemical class.
  • Most derivative patents focus on improved pharmacokinetics or expanded therapeutic uses.
  • The patent's original scope covers both compounds and synthesis methods, giving it a strategic foothold in pharmaceutical development.
  • It continues to influence patent strategies, especially in generic and biosimilar markets.

FAQs

Q1: What is the core chemical structure covered by US Patent 3,781,415?
It covers benzodiazepine-like derivatives with specific substitution patterns designed for anti-inflammatory activity.

Q2: Are compounds described in the patent still protected by patent law?
No, the patent expired in 1992, leaving the compounds in the public domain.

Q3: How has the patent landscape evolved around this patent?
Subsequent patents focused on derivatives, improved synthesis methods, and expanded uses, citing US 3,781,415 extensively.

Q4: Can new drugs be developed based on compounds from this patent?
Yes, but newer patents filed before the expiration or patent filings for derivatives may provide protection.

Q5: What is the significance of this patent for current pharmaceutical research?
It provides a broad chemical scaffold that remains relevant for drug design within the anti-inflammatory class.


References

  1. [1] United States Patent and Trademark Office. (2023). Patent full-text and image database. U.S. Patent 3,781,415.

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Drugs Protected by US Patent 3,781,415

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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