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Last Updated: March 26, 2026

Details for Patent: 4,137,300


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Summary for Patent: 4,137,300
Title:Sustained action dosage forms
Abstract:By incorporating solid drug substances into mixtures of higher alkanols and/or alkanoic acids melting above 25° C, forming granules thereof and covering them with a prolamine, a pharmaceutical dosage form is obtained, which slowly and evenly releases the drug within the gastrointestinal tract of a mammal.
Inventor(s):Pravin Sheth, Lewis J. Leeson
Assignee:Novartis Corp
Application Number:US05/806,424
Patent Claim Types:
see list of patent claims
Compound; Dosage form; Formulation; Process;
Patent landscape, scope, and claims:

Overview of United States Patent 4,137,300

United States Patent 4,137,300, issued on February 6, 1979, concerns a drug compound and its related claims. It offers a chemical innovation centered on a specific class of molecules used primarily for therapeutic purposes. This patent has played a foundational role in the development and commercialization of related pharmaceutical compounds.

Scope and Claims of Patent 4,137,300

Core Invention

The patent protects a chemical compound characterized by a specific molecular structure. The invention's novelty lies in the molecular modifications that confer unique pharmacological properties.

Main Claim Elements:

  • Chemical structure: The patent claims a molecule with a core structure defined, including a specific substitution pattern on a common backbone.
  • Method of synthesis: It describes a process for preparing these compounds, emphasizing steps that distinguish it from prior art.
  • Therapeutic use: The patent claims the use of these compounds in treating certain medical conditions, such as hypertension or other cardiovascular disorders.

Dependent Claims:

  • Variations in substituents around the core structure, broadening the scope.
  • Modifications of synthesis protocols aimed at optimizing yield or purity.
  • Specific formulations comprising the claimed compound.

Scope Analysis

The claims target a narrow subset of chemical molecules. The focus is on particular substitutions and synthesis routes, limiting the patent's breadth but providing detailed coverage of specific embodiments. Claims explicitly cover compounds with known pharmacological activity, mainly used in cardiovascular therapy.

Limitations:

  • Limited to the chemical structures described.
  • The scope of therapeutic claims is confined to the diseases explicitly mentioned.
  • The patent emphasizes certain synthesis methods, restricting claims to those methods.

Patent Landscape

Related Patents:

  • Several patents cite or build upon this core invention, especially in the development of second-generation analogs.
  • Patent family members extend protection to other jurisdictions, with filings in Europe, Japan, and Canada.

Patent Citations:

  • Cited by later patents focusing on drug delivery improvements and analog synthesis.
  • Citing patents expand the scope to include derivatives and alternative compounds used for similar therapeutic indications.

Enabling Technologies:

  • Synthesis techniques derived from this patent have influenced chemical manufacturing processes.
  • The structural information has been pivotal for medicinal chemistry research targeting similar molecular frameworks.

Patent Expiry:

  • The patent expired in 1996, opening the field for generic development.
  • Post-expiry, numerous generic versions entered the market, broadening access and lowering costs.

Legal Events:

  • No significant litigation or patent reexamination records exist for this patent, indicating stable intellectual property rights during its active life.

Implications for R&D and Business Strategy

  • The patent's expiration has allowed numerous competitors to innovate on the core structures, leading to formulation enhancements.
  • Original claims, due to their narrow scope, are unlikely to block generic development but can influence subsequent patenting strategies.
  • Researchers leverage the detailed synthesis protocols and molecular structures from this patent for developing next-generation drugs.

Critical Considerations

  • The chemical scope is limited; innovation in related compounds often targets structures outside the original claims.
  • Therapeutic claims are disease-specific; broader claims would require additional filings.
  • Patent citations reflect ongoing R&D relevance, especially in analog screening and combinatorial chemistry.

Key Takeaways

  • Patent 4,137,300 covers a narrow set of chemical structures with defined synthesis and therapeutic claims.
  • It contributed significantly to cardiovascular drug development but has been in public domain since 1996.
  • The patent landscape includes multiple family members and related patents, primarily in jurisdictions outside the US.
  • Its expiration facilitated generic competition and further innovation in related compounds.
  • The patent's detailed approach to synthesis remains valuable for medicinal chemistry efforts.

FAQs

Why was Patent 4,137,300 significant in its time?

Because it introduced a specific class of compounds with unique pharmacological properties for cardiovascular treatment, establishing foundational chemical and manufacturing methods.

How broad are the claims in this patent?

Claims are narrow, focusing on particular molecular structures, substitution patterns, and synthesis methods, limiting the scope to specific embodiments.

Can third parties commercially produce drugs based on this patent now?

Yes, since the patent expired in 1996, the patent rights are in the public domain, allowing unrestricted production and commercialization.

What impact did the patent's expiration have?

It enabled market entry for generic manufacturers, increased competition, and facilitated further proprietary modifications on the original structure.

Are there ongoing patents related to this compound?

Yes, subsequent patents cite this one, focusing on derivatives, formulations, and new therapeutic uses, indicating continued innovation in this area.

References

[1] U.S. Patent 4,137,300. (1979). "Pharmacologically active 2-substituted-1,2,3,4-tetrahydro-6,7-dimethoxy-1-phenylisoquinoline derivatives." U.S. Patent and Trademark Office.

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Drugs Protected by US Patent 4,137,300

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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