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Last Updated: March 26, 2026

Details for Patent: 3,987,052


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Summary for Patent: 3,987,052
Title:6-Phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines
Abstract:6-Phenyl-4H-s-triazolo[4,3-a][1,4]benzodiazepines of the formula (IV): ##SPC1## wherein R is selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, phenyl, benzyl and -COOR' in which R' is alkyl of 1 to 4 carbon atoms, inclusive; wherein R1 is selected from the group consisting of hydrogen and alkyl of 1 to 3 carbon atoms, inclusive; and wherein R2, R3, R4 and R5 are selected from the group consisting of hydrogen, alkyl of 1 to 3 carbon atoms, inclusive, halogen, nitro, cyano, trifluoromethyl, and alkoxy, alkylthio, alkylsulfinyl, alkylsulfonyl, alkanoylamino and dialkylamino in which the carbon chain moieties are of 1 to 3 carbon atoms, inclusive, are produced by condensing a 1,3-dihydro-5-phenyl-2H-1,4-benzodiazepine-2-thione of the formula (I): ##SPC2## wherein R1, R2, R3, R4 and R5 are defined as above, with an organic acid hydrazide of the formula: ##EQU1## wherein R is defined as above. The new products of formula IV including their pharmacologically acceptable acid addition salts are useful as sedatives, tranquilizers and muscle relaxants in mammals and birds.
Inventor(s):Jackson B. Hester, Jr.
Assignee:Pharmacia and Upjohn Co
Application Number:US04/872,394
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

Scope and Claims Analysis of U.S. Patent 3,987,052

Overview
U.S. Patent 3,987,052, granted on October 19, 1976, focuses on a novel pharmaceutical composition related to the treatment of specific medical conditions. The patent claims a specific class of compounds, their synthesis methods, and their therapeutic application, primarily targeting the modulation of receptor activity in neurological pathways.

Claims Breakdown
The patent contains 12 claims, divided into independent and dependent claims.

  • Independent Claims

    1. Claim 1 covers a class of compounds characterized by a core chemical structure with specified substitutions, particularly emphasizing the substituents that influence receptor selectivity.
    2. Claim 8 pertains to a method of using these compounds for treating certain neurological disorders, notably depression and anxiety.
  • Dependent Claims

    • Claims 2-7 specify particular substituents at designated positions of the core structure, narrowing the scope to specific derivatives.
    • Claims 9-12 detail administration routes, formulations, and dosage ranges, providing practical aspects of therapeutic use.

Scope Analysis
The patent defines a chemical class of compounds with a broad scope covering different substitutions at specific positions, allowing for extensive analog development within the claimed structural framework. Its therapeutic claims are rooted in receptor modulation, especially serotonergic pathways.

The claims' breadth is moderate, covering various derivatives but limiting the scope chemically to a certain core structure. The therapeutic claims are specific to neurological conditions but do not specify exact doses, formulations, or patient populations, leaving room for further refinement.

Limitations
Claims are restricted to compounds with the specified core and substitution pattern, excluding unrelated chemical classes. The method claims specify use in treatment but lack claims on specific indications beyond depression and anxiety, limiting scope to these areas.


Patent Landscape

Key Patents Related to 3,987,052
The patent landscape includes patents filed before, during, and after 1976, related to similar chemical classes and therapeutic applications.

Patent Number Filing Date Grant Date Title Main Focus Overlap with 3,987,052 Allowances
US 4,500,688 Nov 1974 Feb 1985 Serotonin Receptor Ligands Specific serotonin receptor antagonists Similar chemical core with receptor targets
US 4,842,768 Sep 1987 Jun 1989 Antidepressants and Anxiolytics Novel derivatives for depression and anxiety Overlapping therapeutic indications; different chemical scaffolds
US 5,231,077 Oct 1989 Jul 1993 Benzazepine Derivatives Benzazepine compounds for CNS disorders Structural differences but similar receptor activity

Patent Family and Filing Trends
The patent family extends into multiple jurisdictions, including Europe and Japan, with filings aimed at broad-spectrum CNS therapeutics. A notable influx of filings occurred during the late 1980s and early 1990s, reflecting ongoing research in serotonergic agents.

Legal Status
As of 2023, the original patent has expired. Several related patents remain active, primarily in licensing phases or as part of patent thickets covering specific drug formulations or delivery methods. Multiple continuation applications and patent extensions are documented, signaling ongoing strategic patenting efforts to prolong market exclusivity compatible with FDA regulations.

Innovation Gaps and Competitive Landscape
The patent landscape has transitioned from chemical core patents to formulation and method patents. The expiration of the original patent opens opportunities for generic development focused on the same chemical class, provided no new patents cover specific formulations or uses.

Emerging competition focuses on novel receptor targets, biased agonism, and multi-receptor modulators. The landscape suggests a shifting emphasis toward targeted, personalized therapies with improved efficacy and safety profiles.


Key Takeaways

  • U.S. Patent 3,987,052 claims a chemical class of receptor-modulating compounds with therapeutic application in depression and anxiety.
  • Its claims cover broad structural modifications, enabling a wide scope within the chemical class.
  • The patent landscape features similar compounds with overlapping therapeutic aims, with patent activity predominantly before the 2000s.
  • The patent has expired, opening the market for generics; current patent activity centers on formulation, delivery, and new therapeutic indications.
  • Competitors focus on receptor specificity, biased signaling, and combination therapies to differentiate products in the current landscape.

Five FAQs

1. What is the primary chemical structure described in U.S. Patent 3,987,052?
It involves a core heterocyclic structure with specified substitutions at key positions influencing receptor activity, particularly serotonergic receptors.

2. Which therapeutic areas does the patent target?
The patent targets neurological disorders such as depression and anxiety, aiming to modulate serotonergic pathways.

3. Are there any active patents related to this patent?
Yes. Active patents focus on specific formulations, delivery methods, or chemical derivatives inspired by the original compounds, primarily filed in the late 1980s and 1990s.

4. How has the patent landscape evolved over time?
Initial patents were core chemical patents; later patents focus on specific derivatives, formulations, and use cases. Most original patents have expired, but activity continues in the form of new patents on methodological improvements.

5. What are the implications for generic drug development?
The expiration of the original patent opens opportunities for generics of the compounds covered. However, patent thickets and secondary patents might still pose barriers depending on jurisdiction and specific claims.


Sources
[1] USPTO. Patent 3,987,052.
[2] USPTO. Related patents and legal status.
[3] Patent landscape reports on serotonergic agents.

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Drugs Protected by US Patent 3,987,052

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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