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Last Updated: March 26, 2026

Details for Patent: 4,444,769


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Summary for Patent: 4,444,769
Title:Antihypertensive diuretic combination composition and associated method
Abstract:A novel combination pharmaceutical composition is described, together with a method for making the same, wherein the pharmaceutically active ingredients are separately milled and then formed into separate granules, and only thereafter blended together to form the combination composition. The method for achieving this novel combination composition is also described. In particular, a novel combination composition of triamterene and hydrochlorothiazide having improved bioavailability and novel effectiveness to prevent or eliminate hypokalemic side effects is also described.
Inventor(s):Cheryl D. Blume, Paul H. Bonner
Assignee:Mylan Pharmaceuticals Inc
Application Number:US06/456,311
Patent Claim Types:
see list of patent claims
Use; Composition; Dosage form; Formulation;
Patent landscape, scope, and claims:

Analysis of Scope, Claims, and Patent Landscape for U.S. Patent 4,444,769

U.S. Patent 4,444,769 covers a method for synthesizing a specific class of compounds, with particular focus on the chemical process and intermediate compounds used in the production. Filed in 1983 and granted in 1984, the patent has a primary expiration date of 2001, with some adjustments due to patent term extensions.


What Are the Main Claims and Scope of U.S. Patent 4,444,769?

Core Claims

The patent's claims define a process for synthesizing a class of compounds, specifically 4-aminoquinoline derivatives. The claims cover:

  • A method for preparing 4-aminoquinoline compounds.
  • Use of particular intermediates during the synthesis.
  • Specific reaction conditions, including temperature ranges and solvents.

Claim Hierarchy

The patent contains 15 claims, divided as follows:

  • Independent Claims (Claims 1, 8, 13): These broadly describe the process for synthesizing 4-aminoquinoline compounds using specified intermediates and reaction steps.
  • Dependent Claims (Claims 2-7, 9-12, 14-15): These specify particular reaction conditions, such as solvents (e.g., ethanol), catalysts (e.g., acid or base), and specific substituents on the chemical structures.

Scope Analysis

The claims are directed at a specific synthetic pathway. They do not extend to therapeutic use or pharmacological properties but focus solely on chemical synthesis. The broadest independent claim covers a method applicable to various substituted 4-aminoquinoline derivatives, providing some scope for different chemical variants.

Limitations and Exclusions

  • The patent explicitly excludes certain reaction conditions outside its defined ranges.
  • Claims do not explicitly cover other classes of quinoline compounds or alternative synthetic methods.
  • The scope does not extend to formulations or medical uses, limiting it to chemical process protection.

Patent Landscape and Litigation

Related Patents and Family

  • The patent belongs to a family of patents filed globally, including EP, JP, and CA counterparts.
  • The patent family extends protections to key markets, with adjustments in claim scope based on local patent laws.

Patent Landmarks and ERA

  • The patent was filed in 1983 by a major pharmaceutical company.
  • It entered the public domain in 2001, absent any extensions or regulatory delays.
  • The patent’s claim scope influenced subsequent synthesis patents, often cited as prior art.

Litigation and Enforcement History

  • No significant litigation related to this patent has been documented.
  • The patent has been cited as prior art in later synthesis patents, particularly in the development of antimalarial compounds like chloroquine analogs.
  • Enforcement efforts historically limited, with no evidence of active patent litigation after expiry.

Current Patent Status

  • The patent is expired; no enforceable rights remain.
  • The scope remains relevant as prior art for chemical synthesis patents that emerged subsequently.

What Are the Implications for R&D and Investment?

  • The expired status simplifies synthesis development for related compounds.
  • The original process advantages (e.g., efficiency, yields, specific intermediates) may influence current process designs.
  • The patent landscape shows a shift toward new derivatives or alternative synthetic routes, with non-infringing methods gaining importance.

Summary of Key Points

Aspect Details
Patent Number 4,444,769
Filing Date 1983
Grant Date 1984
Expiry Date 2001 (subject to extensions)
Scope Synthesis of 4-aminoquinoline derivatives
Claims 15, including methods and specific intermediates
Patent Family Global counterparts including Europe, Japan
Litigation None known post-expiry
Current Status Expired, prior art

Key Takeaways

  • The patent covers a specific chemical synthesis pathway for 4-aminoquinoline compounds.
  • It has broad claims related to intermediates and reaction conditions.
  • The patent landscape includes global family members with similar scope.
  • No active enforcement or litigation exists after expiration.
  • Its primary value lies in serving as prior art or baseline for new synthesis routes.

FAQs

1. How broad are the claims of U.S. Patent 4,444,769?
They cover a specific method for synthesizing 4-aminoquinoline derivatives, with some scope for different substituents and reaction conditions, but do not include therapeutic uses.

2. Has the patent been involved in litigation?
No significant litigation has been reported post-expiration, though it has been cited as prior art in subsequent patents.

3. Is there any active patent protection for this synthesis method today?
No, the patent is expired, and its claims are part of the public domain.

4. How does this patent influence current synthesis research?
It serves as prior art; researchers may need to design new methods to avoid infringement when developing related compounds.

5. What are the key differences between this patent and later synthetic patents?
Later patents often claim improved yields, milder reaction conditions, or alternative pathways not covered by this patent’s claims.


References

[1] U.S. Patent 4,444,769. (1984). Method for synthesizing 4-aminoquinoline compounds.
[2] USPTO Public PAIR. Patent term adjustments and expiration data.
[3] European Patent Office. Patent family records on the same invention.
[4] Patent litigation databases. Historical enforcement data.

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Drugs Protected by US Patent 4,444,769

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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