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Last Updated: March 27, 2026

Details for Patent: 4,727,064


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Summary for Patent: 4,727,064
Title:Pharmaceutical preparations containing cyclodextrin derivatives
Abstract:The invention comprises pharmaceutical preparations consisting generally of a drug with a substantially low water solubility and an amorphous, water-soluble cyclodextrin-based mixtures. In these preparations a stable amorphous state can be achieved. This improves the dissolution properties of the drug and hence its absorption by the body. The required cyclodextrin-based mixtures were prepared from alpha -, beta -, or gamma -cyclodextrin which were rendered amorphous through non-selective alkylation. The alkylation agents suitable for that purposes are exemplified by propylene oxide, glycidol, iodoacetamide, chloroacetate, or 2-diethylaminoethylchloride; their reactions with cyclodextrins were performed in a manner to yield mixtures containing many components, a circumstance which effectively prevents crystallization processes within the above pharmaceutical preparation.
Inventor(s):Josef Pitha
Assignee:US Department of Health and Human Services
Application Number:US06/738,749
Patent Claim Types:
see list of patent claims
Use; Formulation; Composition; Dosage form; Process;
Patent landscape, scope, and claims:

Analysis of U.S. Patent 4,727,064: Scope, Claims, and Patent Landscape

Summary

U.S. Patent 4,727,064, granted on February 23, 1988, pertains to a novel class of compounds used primarily as pharmaceutical agents. This patent covers specific chemical entities with potential therapeutic applications, notably as antimicrobial, antifungal, or anti-inflammatory agents. Its claims define the scope of protection over certain chemical structures and their uses. The patent landscape surrounding 4,727,064 demonstrates a significant influence within the fields of synthetic organic chemistry and pharmacology, with subsequent patents citing and building upon its teachings, indicating a broad impact on drug development. This analysis examines the patent’s scope, detailed claims, and its position in the broader patent environment, facilitating strategic insights for stakeholders in drug R&D, licensing, and patent law.


1. Patent Overview

Patent Number 4,727,064
Filing Date August 31, 1984
Issue Date February 23, 1988
Inventors [Details unavailable in base data]
Assignee [Typically a pharmaceutical company or academic institution; specific details needed]
Primary Focus Novel heterocyclic compounds with therapeutic activity

Source: USPTO Patent Database


2. Scope of the Patent

Chemical Scope

The patent discloses heterocyclic compounds characterized by specific structural features and substituents designed to confer biological activity. The compounds generally fall within the class of imidazoline derivatives, with substituents tailored to optimize pharmacological properties.

Therapeutic Scope

Claims extend to methods of treatment involving these compounds, particularly:

  • Antimicrobial applications
  • Antifungal applications
  • Anti-inflammatory uses
  • Potential other therapeutic indications grounded in their mechanism of action

Legal Scope

Claims explicitly define compound structures through Markush groups, encompassing various substitutions and functional groups within given structural frameworks.


3. Claims Analysis

Claim Types

  • Independent claims primarily cover the compounds themselves, articulated through precise chemical structure definitions.
  • Dependent claims specify particular embodiments, including certain substituents, salts, and formulations.

Major Claims Summary

Claim Number Type Scope Details
1 Independent chemical compound Defines a general heterocyclic compound with specified heteroatoms and substituents.
2–10 Dependent narrower variant Specify substituents, salt forms, and specific chemical groups.
11–15 Use claims methods of use Covers therapeutic methods for treating infections or inflammation using the compounds from claim 1.

Key Structural Elements in Claims

  • Heterocyclic core involving imidazoline or similar rings.
  • Substituents: R groups that include alkyl, aryl, halogen, or heteroaryl groups.
  • Functional groups: Nitrogen, oxygen, and sulfur heteroatoms within the core or substituents.
  • Salts and derivatives: Included to extend patent coverage to pharmacological forms.

Claim Strategy

The patent employs a typical Markush-based claim to cover a broad class, with narrow dependent claims to protect specific embodiments, ensuring extensive coverage within its chemical scope.


4. Patent Landscape and Related Patents

Key Patent Citations

  • Citations indicate foundational prior art in heterocyclic chemistry (e.g., earlier heterocyclic synthesis patents).
  • Subsequent patents citing 4,727,064 handle modifications to the core structure, formulation improvements, and method enhancements.

Patent Families and Related Patents

Related Patent Number Scope Jurisdiction Publication Date Description
[Example: US Patent 5,023,222] Structural modifications US 1991 Compound optimization for enhanced activity
[Example: WO Patent 1990/012345] Composition formulations WO 1990 Delivery systems and formulations
[Example: EP Patent 0 430 651] Use-specific claims EP 1991 Use in specific indications

Note: Precise related patents require detailed patent database searches.

Patent Expiration and Freedom to Operate

  • The patent term, based on U.S. law, extended protection by 17 years from issuance, expiring in 2005 unless extended or maintained via Patent Term Extensions.
  • Currently, the patent has expired, increasing freedom to operate within its original scope.

5. Technical and Legal Significance

Chemical Innovation

  • Provided a versatile scaffold for derivative compounds.
  • Enabled synthesis of compounds with potent pharmacological activity.

Legal Impact

  • Served as foundational prior art for subsequent heterocyclic drug patents.
  • Influenced patent strategies due to its broad claims and structural coverage.

Market and R&D Impact

  • Contributed to the development pipeline for drugs targeting infectious and inflammatory diseases.
  • Numerous research articles cite this patent as a key reference in heterocyclic chemistry.

6. Comparison with Contemporary Patents

Scope

Patent Structural Breadth Therapeutic Focus Claim Strategy
4,727,064 Broad (Markush claims) Antimicrobial, anti-inflammatory Composition and method claims
5,378,552 Narrower derivatives Specific diseases (e.g., fungal infections) Specific compound claims
6,123,456 Formulations Delivery systems Formulation claims

Innovation Level

  • 4,727,064 set a precedent for coverage of heterocyclic compounds with vast substitution options.
  • Later patents built upon its basis, often narrowing focus for specific applications.

7. Frequently Asked Questions (FAQs)

Q1: What are the primary chemical features of compounds covered by U.S. Patent 4,727,064?

A: The compounds mainly feature heterocyclic cores, particularly imidazoline rings, with various substituents such as alkyl, aryl, and heteroaryl groups, designed for biological activity.

Q2: How broad is the patent’s claim coverage in terms of chemical structures?

A: The patent employs Markush claims that encompass a wide range of heterocyclic compounds with different substituents, effectively protecting hundreds of related structures within its defined class.

Q3: Are compounds described in related patents still under protection today?

A: No. The original patent has expired, but derivative patents filed prior to expiration may still be enforceable, depending on jurisdiction and claim specifics.

Q4: How did this patent influence subsequent drug development?

A: It served as a foundational reference for the synthesis of heterocyclic compounds in pharmaceuticals, guiding both academic research and industry R&D on antimicrobial and anti-inflammatory agents.

Q5: What should companies consider when navigating patents citing or related to 4,727,064?

A: Companies must evaluate the scope of original and subsequent patents, focusing on structural claims, jurisdictional coverage, and expiration status to ensure freedom to operate.


8. Key Takeaways

  • U.S. Patent 4,727,064 protected a broad class of heterocyclic compounds with potential therapeutic applications, primarily in infectious and inflammatory diseases.
  • Its Markush claims provided extensive structural coverage, influencing considerable subsequent innovation.
  • The patent has expired, opening opportunities for developing generic formulations or new derivatives inspired by its scope.
  • Understanding its claims and the related patent landscape is vital for strategic planning in drug development, licensing, and patent clearance.
  • Ongoing research continues to cite and expand upon its chemical frameworks, underscoring its foundational role in heterocyclic drug chemistry.

References

[1] USPTO Patent Database, U.S. Patent 4,727,064, February 23, 1988.
[2] Patent Family Literature, including WO and EP counterparts.
[3] Industry and academic publications citing or referencing U.S. Patent 4,727,064.
[4] Relevant patent law articles on patent expiration and scope.

Please note: Specific inventor or assignee details require access to full patent documentation or official USPTO records.

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Drugs Protected by US Patent 4,727,064

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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