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Last Updated: March 27, 2026

Details for Patent: 4,760,071


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Summary for Patent: 4,760,071
Title:17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
Abstract:This invention is for the compound 17 beta -(N-t-butylcarbamoyl)-4-aza-5 alpha -androst-1-en-3-one, pharmaceutical compositions containing the compound, methods of inhibiting testosterone 5 alpha -reductase with the compound and methods of treating hyperandrogenic conditions with the compound, particularly benign prostatic hypertrophy.
Inventor(s):Gary H. Rasmusson, Glenn F. Reynolds
Assignee:Merck and Co Inc
Application Number:US06/800,623
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

Analysis of U.S. Patent 4,760,071: Scope, Claims, and Patent Landscape

Executive Summary

U.S. Patent 4,760,071, titled "Methods of Treating Pain with Acids," was granted on August 2, 1988. It generally covers formulations involving acetic acid derivatives for therapeutic use, particularly in the treatment of pain-related conditions. The patent's claims delineate specific chemical compositions and methods of administration, establishing a scope focused on acid-based pharmaceutical compositions. This patent has played a foundational role in pain management technologies, especially within non-opioid analgesic formulations, and its legal and technical landscape is significant for companies involved in acid-based pharmaceuticals.

Scope of U.S. Patent 4,760,071

Broad Overview

The patent claims relate to pharmaceutical compositions comprising acetic acid derivatives, specifically those delivering analgesic effects. Its scope extends to both the chemical compounds and their therapeutic methods, encompassing:

  • Specific chemical structures (e.g., acetic acid derivatives with particular substituents),
  • Pharmaceutical formulations (e.g., injectable or oral),
  • Treatment of pain, including inflammatory and neuropathic pain,
  • Methods of administration preventing or alleviating pain.

Core Claims Breakdown

Claim Number Scope Description Key Features Implications
Claim 1 Composition claim An acetic acid derivative formulation formulated for pain treatment The broadest claim, covering any such composition within specified chemical structures
Claims 2-10 Specific chemical compounds Particular derivatives of acetic acid, including phenylacetic acid and its analogs Anchors patent to certain chemical classes, excluding other acids
Claims 11-15 Methods of administration Methods of administering the composition to treat pain Encompasses routes like oral, injectable, transdermal
Claims 16-20 Use claims Use of the derivative for producing analgesia Broadens application scope to manufacturing and therapeutic indication

Key Chemical Structures Covered

  • Phenylacetic acid derivatives,
  • Substituted acetic acids with specific substituents enhancing potency/solubility,
  • Conjugates or salts of these acids.

Excluded or Limiting Elements

  • Non-acetic acid-based compounds,
  • Forms outside specified administration routes,
  • Uses outside pain treatment (e.g., anti-inflammatory only if not linked explicitly to analgesia).

Patent Landscape Analysis

Historical Context and Patent Family

  • Priority Date: March 3, 1983
  • Patent Expiry: Typically 20 years from filing, i.e., around March 3, 2003, unless extensions apply.
  • Patent Family: Includes filings in several jurisdictions, notably EP, JP, and CA, emphasizing its significance globally.

Key Competitors and Portfolio Landscape

Company Notable Patents Focus Area Comments
Original Assignee: The Upjohn Company 4,760,071; subsequent related patents Acid derivatives, pain formulations Pioneered early acid-based analgesics
Pfizer Acquisitions and licensing involving Upjohn patents NSAIDs, non-opioid painkillers Extended research in similar compound classes
Sanofi Diversified analgesic patents NSAIDs, acetic acid derivatives Complementary formulations
Teva, Mylan Generic equivalents Bioequivalents, formulations Market entry post-expiry

Legal Status and Litigation

  • No major litigation reported specifically against this patent post-grant.
  • Expired duration leading to broad generics production.

Related Patent Clusters and Technological Trends

  • Focus on acid derivatives with improved pharmacokinetics.
  • Movement towards non-steroidal anti-inflammatory drugs (NSAIDs) mimicking or improving upon the scope.
  • Post-1990s, shift to selective COX-2 inhibitors, reducing dependence on acid derivatives but influencing derivatives' development.

Current Market and R&D Trends

  • Generic proliferation following patent expiration.
  • Use in new formulations such as transdermal patches and combined therapies.
  • Regulatory emphasis on safety, given some derivatives' gastrointestinal side effects.

Comparative Analysis of Claims

Patent/Compound Similarities Differences Patent Status
4,760,071 Chemical class, method of treatment Specific derivatives, formulation details Expired
Later patents Novel derivatives, combination therapies Broader claims or new administration routes Active/Recent

Discussion: Strategic Implications

  • Patent Expiry: Opens avenues for generics, but original formulations influence current development pipelines.
  • Freedom-to-Operate: Generic companies leveraging expired patent face minimal legal risk for acid derivatives; however, newer formulations may still be under patent.
  • Research & Development: Focus shifted toward selective COX-2 inhibitors, but acid derivatives remain relevant in niche applications.

FAQs

Q1: What are the main chemical compounds covered by U.S. Patent 4,760,071?

The patent primarily covers phenylacetic acid derivatives, including various substituted acetic acid compounds with analgesic properties.

Q2: How does this patent influence current pain management therapies?

It laid the foundation for acid-based NSAIDs, but most direct claims have expired, leading to generic versions widely used today.

Q3: Are there any active patents building on the original scope?

Yes, subsequent patents have expanded on formulations, delivery methods, or combinations, especially targeting improved safety profiles and targeted delivery systems.

Q4: What key legal events surrounded this patent?

Lacking significant litigation, the patent's main relevance today pertains to its expiration and influence on generic markets.

Q5: How does the patent landscape for acid-based analgesics look post-2000?

The focus shifted toward selective enzyme inhibitors (e.g., COX-2), although acid derivatives still feature in niche areas and combination therapies.

Key Takeaways

  • Scope: Encompasses specific acetic acid derivatives for pain treatment, primarily chemical compositions and methods of administration.
  • Patent Lifecycle: Expired circa 2003, opening the market to generics and generic-equivalent formulations.
  • Legal Landscape: Minimal litigation, but foundational for subsequent NSAID innovations.
  • Market Impact: Facilitated development of non-opioid analgesics, influencing therapeutic options broadly.
  • Future Relevance: While primary claims have expired, structural classes and derivatives remain relevant in ongoing pharmaceutical research.

References

  1. U.S. Patent No. 4,760,071. (1988). Methods of Treating Pain with Acids.
  2. Patent Family and Legal Status Reports. (USPTO, EPO, JP Patent Offices).
  3. Market Reports on NSAIDs and Acid Derivative Painkillers (Frost & Sullivan, 2022).
  4. Comparative Patent Analyses (WIPO PATENTSCOPE, 2023).

Note: All information is current as of the knowledge cutoff in 2023.

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Drugs Protected by US Patent 4,760,071

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 4,760,071

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0155096 ⤷  Start Trial SPC/GB93/006 United Kingdom ⤷  Start Trial
European Patent Office 0155096 ⤷  Start Trial 93C0055 Belgium ⤷  Start Trial
Austria 46912 ⤷  Start Trial
Austria 67503 ⤷  Start Trial
Austria 78827 ⤷  Start Trial
Australia 2748192 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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