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Last Updated: December 22, 2024

Details for Patent: 4,335,125


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Summary for Patent: 4,335,125
Title: 1-(1,3-Dioxolan-2-ylmethyl)-1H-imidazoles
Abstract:Novel 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles useful as antifungal and antibacterial agents.
Inventor(s): Heeres; Jan (Vosselaar, BE), Backx; Leo J. J. (Arendonk, BE), Mostmans; Joseph H. (Antwerp, BE)
Assignee: Janssen Pharmaceutica, N.V. (Beerse, BE)
Application Number:06/001,613
Patent Claim Types:
see list of patent claims
Compound; Composition;
Patent landscape, scope, and claims:

Detailed Analysis of the Scope and Claims of United States Patent 4,335,125

Introduction

United States Patent 4,335,125, titled "1-(1,3-Dioxolan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles useful as antifungal and antibacterial agents," is a seminal patent in the field of pharmaceuticals, particularly in the development of antifungal and antibacterial compounds. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Background of the Invention

The patent, filed by Heeres et al. and assigned to Janssen Pharmaceutica, describes novel compounds belonging to the classes of 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles. These compounds are designed to exhibit antifungal and antibacterial properties, addressing a significant need in the treatment of fungal and bacterial infections[4].

Scope of the Invention

The scope of the invention is broad and encompasses several key aspects:

Chemical Compounds

The patent details the synthesis and properties of various 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles. These compounds are characterized by their specific chemical structures, which include phenyl groups, alkyl groups, and other functional groups that contribute to their antifungal and antibacterial activities[4].

Antifungal and Antibacterial Activity

The compounds described in the patent are specifically designed to target fungal and bacterial pathogens. The antifungal activity is particularly noteworthy, as it includes the ability to inhibit the growth of various fungi species, making these compounds valuable in the treatment of fungal infections[4].

Pharmaceutical Applications

The patent outlines the potential pharmaceutical applications of these compounds, including their use in topical and systemic treatments. This includes formulations such as creams, ointments, and other dermatological preparations[4].

Claims of the Patent

The claims of the patent are crucial in defining the intellectual property rights associated with the invention. Here are some key claims:

Independent Claims

  • Claim 1 describes the general structure of the 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles, including the specific chemical groups and their arrangements.
  • Claim 2 specifies the methods for preparing these compounds, including the reactants and reaction conditions.
  • Claim 3 outlines the pharmaceutical compositions containing these compounds, including the formulation and dosage forms[4].

Dependent Claims

  • Dependent claims further detail the specific embodiments of the compounds, such as the substitution patterns on the phenyl ring and the types of alkyl groups.
  • These claims also cover various aspects of the pharmaceutical formulations, including the use of excipients and the methods of administration[4].

Patent Landscape

Understanding the patent landscape surrounding US 4,335,125 involves analyzing related patents, prior art, and subsequent developments.

Prior Art

The patent references several prior art documents, including earlier patents related to antifungal and antibacterial agents. For example, it cites patents related to the synthesis of similar compounds and their pharmaceutical applications[4].

Related Patents

Other patents, such as US 5,854,246, build upon the discoveries made in US 4,335,125. This later patent describes topical ketoconazole emulsions, which are related to the antifungal compounds disclosed in the earlier patent[2].

Patent Analytics

To fully understand the patent landscape, patent analytics tools can be employed. These tools help in categorizing patents by claims and scope concepts, identifying gaps in coverage, and highlighting future design opportunities. For instance, a Claim Coverage Matrix can show which patents and claims are actively protecting the intellectual property related to these antifungal and antibacterial compounds[3].

Impact and Applications

The impact of US 4,335,125 is significant in the pharmaceutical industry:

Clinical Use

Compounds like ketoconazole, which is a specific example of the 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles, have been widely used in clinical settings for treating fungal infections. Ketoconazole shampoos, for instance, are used to treat dandruff and other scalp conditions caused by fungal infections[1].

Research and Development

The patent has also spurred further research into the development of new antifungal and antibacterial agents. The understanding of the chemical structures and their biological activities has led to the synthesis of new compounds with improved efficacy and safety profiles.

Key Takeaways

  • Chemical Compounds: The patent describes novel 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles with antifungal and antibacterial properties.
  • Pharmaceutical Applications: These compounds are used in various pharmaceutical formulations, including topical and systemic treatments.
  • Claims: The patent includes claims that define the chemical structures, methods of preparation, and pharmaceutical compositions.
  • Patent Landscape: The patent is part of a broader landscape that includes related patents and subsequent developments in antifungal and antibacterial agents.
  • Impact: The patent has had a significant impact on the treatment of fungal and bacterial infections and has driven further research in this area.

FAQs

Q: What are the main compounds described in US 4,335,125? A: The main compounds are 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles and 1H-1,2,4-triazoles.

Q: What is the primary use of these compounds? A: These compounds are primarily used as antifungal and antibacterial agents.

Q: How do these compounds differ from other antifungal agents? A: They have specific chemical structures that include phenyl groups, alkyl groups, and other functional groups that contribute to their antifungal and antibacterial activities.

Q: What is the significance of ketoconazole in this context? A: Ketoconazole is a specific example of the 1-(1,3-dioxolan-2-ylmethyl)-1H-imidazoles and is widely used in clinical settings for treating fungal infections.

Q: How can patent analytics tools help in understanding the patent landscape? A: Patent analytics tools can help in categorizing patents by claims and scope concepts, identifying gaps in coverage, and highlighting future design opportunities.

Sources

  1. Justia Patents: Ketoconazole shampoo containing butylated hydroxytoluene or butylated hydroxyanisole.
  2. Google Patents: United States Patent (19) - TOPICAL KETOCONAZOLE EMULSIONS.
  3. SLWIP: Patent Analytics | Intellectual Property Law.
  4. Google Patents: US4335125A - 1-(1,3-Dioxolan-2-ylmethyl)-1H-imidazoles.
  5. Law360: U.S. Patent Number 4,335,125 : Articles :: Law360.

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Drugs Protected by US Patent 4,335,125

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

International Family Members for US Patent 4,335,125

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Austria 366683 ⤷  Subscribe
Austria A63678 ⤷  Subscribe
Australia 3285078 ⤷  Subscribe
Australia 521329 ⤷  Subscribe
Belgium 863382 ⤷  Subscribe
Canada 1094559 ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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