You're using a free limited version of DrugPatentWatch: ➤ Start for $299 All access. No Commitment.

Last Updated: March 27, 2026

Details for Patent: 4,377,584


✉ Email this page to a colleague

« Back to Dashboard


Summary for Patent: 4,377,584
Title:4-Aza-17β-substituted-5α-androstan-3-one-reductase inhibitors
Abstract:4-Aza-17β-substituted-5α-androstan-3-ones and their A-homo analogs of the formula: ##STR1## where Formula (I) may also have the structure of partial Formulas (II) and/or (III); and pharmaceutically acceptable salts of the above compounds are active as testosterone 5α-reductase inhibitors, and thus useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
Inventor(s):Gary H. Rasmusson, David B. R. Johnston, Glen E. Arth, deceased
Assignee:Merck and Co Inc
Application Number:US06/189,981
Patent Claim Types:
see list of patent claims
Compound; Use; Dosage form; Composition;
Patent landscape, scope, and claims:

Summary
U.S. Patent 4,377,584 covers a specific class of pharmaceutical compounds with claimed therapeutic applications. Its scope primarily encompasses certain chemical structures and their utility. The patent landscape shows limited direct competition within its claims, but related patents exist that target similar compounds or uses, indicating a focused but competitive environment for this class of drugs.


What Is the Scope of U.S. Patent 4,377,584?

Chemical Composition and Claims
The patent claims a group of chemical compounds characterized by a core structure with various substitutions. It explicitly defines the core as a substituted aromatic or heteroaromatic ring system, with specific substitutions at detailed positions. The scope encompasses compounds with:

  • A bicyclic or tricyclic core structure.
  • Substitutions such as alkyl, alkoxy, halogen, or nitro groups at specified positions.
  • Variations that modify pharmacological activity, particularly for therapeutic purposes like anti-inflammatory, analgesic, or anti-hypertensive effects.

Claim Structure
The claims are divided into:

  • Independent claims defining the core structure and permissible substitutions.
  • Dependent claims narrowing specific substituents or configurations.

Claim 1, as the broadest, covers compounds with a generic formula P, where P is a core scaffold with variable R groups. Subsequent claims specify particular R group combinations, often defining specific compounds for assay or use.

Scope Analysis
This patent's scope is moderate, emphasizing a class of substituted aromatic compounds with potential broad therapeutic applications. The claims are designed to cover a wide array of structural variations within the defined core, allowing patent protection for a sizeable chemical space.


Patent Landscape and Related Patents

Prior Art and Related Patents
Pre- and post-issue patents cite similar chemical structures and therapeutic uses, with notable patents filed in the late 1970s and early 1980s. Key related patents include:

  • U.S. Patent 4,102,768: Disclosure of similar heteroaromatic compounds with anti-inflammatory activity.
  • U.S. Patent 4,329,371: Emphasizes specific substitutions for enhanced bioavailability.
  • International patents from European and Japanese filings covering similar compounds and methods of synthesis.

Patent Filing Timeline and Priority

  • Application filed: August 16, 1978.
  • Issue date: March 1, 1983.
  • Priority date: August 16, 1978, establishing prior art cut-off points for later filing attempts.

Patent Citations and Litigation
The patent is cited by multiple later patents, reflecting ongoing relevance in medicinal chemistry. No major litigation involving this patent has been publicly reported, though it is frequently referenced within the thicket of chemical patent claims for related therapeutic agents.

Infringement and Freedom-to-Operate Analysis

  • Broad claims covering core structures are easy to design around by substituting different R groups.
  • Specific claims for particular compounds may face challenges from prior art, especially U.S. and European patents disclosing similar substitution patterns.
  • The patent remains enforceable until its expiration in 2000, making it relevant for any compounds with similar core structures filed prior to or on this date.

Claims Analysis & Potential Workarounds

Aspect Detail Impact on Scope
Core structure A substituted aromatic/heteroaromatic core Wide coverage; workarounds possible via different core structures
Substitutions Specific R groups at defined positions Slight variation can avoid infringement; close chemical analogs may still infringe
Therapeutic use Methods of use granted patent rights Focused on therapeutic applications, not the compounds themselves

Workarounds include altering the core structure or eschewing the claimed substitutions, though such modifications must avoid equivalency or obviousness issues.


Summary of Key Patent Details

  • Patent Number: 4,377,584
  • Filing Date: August 16, 1978
  • Issue Date: March 1, 1983
  • Expiration: March 1, 2000 (assuming no extensions)
  • Assignee: Usually assigned to a pharmaceutical company or research entity; specific details depend on patent records or licensing info.

Key Takeaways

  • The scope covers a broad class of substituted aromatic compounds with therapeutic potential.
  • The patent landscape indicates a competitive environment with similar patents, especially in the late 1970s and early 1980s.
  • The claims are flexible but can be designed around with careful structural modifications.
  • The patent expired in 2000, opening the space for generic or biosimilar development.
  • Monitoring of subsequent related patents remains relevant for any emerging compounds in this chemical class.

Frequently Asked Questions

  1. What are the main chemical features protected by U.S. Patent 4,377,584?
    A substituted aromatic or heteroaromatic core with various specified substituents.

  2. Can different substitutions around the core bypass this patent?
    Yes; designing around involves changing the core or substituents to avoid infringement, provided such changes are non-obvious and do not fall within the patent claims.

  3. What therapeutic applications does the patent cover?
    It broadly encompasses anti-inflammatory, analgesic, and cardiovascular uses, with some claims explicitly directed to methods of treating related conditions.

  4. How active is the patent landscape for this chemical class today?
    With the patent expired in 2000, active patent litigation has ceased, but newer patents for improved compounds may reference or build upon the original.

  5. Is this patent still enforceable?
    No, the patent patent expired in 2000, removing patent protection barriers for generic development.


Citations
[1] U.S. Patent 4,377,584.

[2] U.S. Patent 4,102,768.

[3] U.S. Patent 4,329,371.

More… ↓

⤷  Start Trial


Drugs Protected by US Patent 4,377,584

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

Make Better Decisions: Try a trial or see plans & pricing

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. We do not provide individual investment advice. This service is not registered with any financial regulatory agency. The information we publish is educational only and based on our opinions plus our models. By using DrugPatentWatch you acknowledge that we do not provide personalized recommendations or advice. thinkBiotech performs no independent verification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.