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Last Updated: December 22, 2024

Details for Patent: 4,894,369


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Summary for Patent: 4,894,369
Title: Novel 2.beta.-morpholino-androstane derivatives
Abstract:Compounds having the formula: ##STR1## wherein R.sub.1 is H or an optionally substituted acyl group having 1-12 carbon atoms, R.sub.2 is H or an acyl group having 1-12 carbon atoms and R.sub.3 is C, N--CH.sub.3 or a direct bond; and mono- or bisquaternary ammonium compounds thereof and acid addition salts of the non- or mono-quaternary ammonium compounds. Process for the preparation of these compounds. Compositions comprising at least one of the above compounds as the active ingredient. The compounds are favorable neuromuscular blocking agents.
Inventor(s): Sleigh; Thomas (Wishaw, GB6), Savage; David S. (New Mearns, GB6), Carlyle; Ian C. (Hamilton, GB6)
Assignee: Akzo N.V. (Arnhem, NL)
Application Number:07/181,139
Patent Claim Types:
see list of patent claims
Compound; Composition; Formulation;
Patent landscape, scope, and claims:

United States Patent 4,894,369: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 4,894,369, titled "Novel 2β-morpholino-androstane derivatives," is a significant patent in the field of pharmaceuticals, particularly concerning neuromuscular blocking agents. This patent, granted in 1990, discloses novel compounds and their methods of preparation, which have been crucial in the development of drugs like rocuronium bromide.

Background and Context

The patent was filed by researchers aiming to develop new neuromuscular blocking agents with improved efficacy and safety profiles. The compounds described in this patent are part of a broader class of androstane derivatives, which have been studied for their potential in anesthesia and surgical procedures[4].

Scope of the Patent

Claims Overview

The patent includes several claims that define the scope of the invention. Here are the key aspects:

  • Independent Claims: The patent contains multiple independent claims that describe the novel 2β-morpholino-androstane derivatives. These claims specify the chemical structure and composition of the compounds, including their stereochemistry and functional groups[4].
  • Dependent Claims: The dependent claims further elaborate on the independent claims by detailing specific embodiments, such as the preparation methods, pharmaceutical compositions, and uses of the compounds.

Claim Language and Scope

The claim language is precise and technical, ensuring that the scope of the patent is well-defined. For instance, Claim 1 describes a compound of a specific chemical structure, while subsequent claims detail various aspects of this compound, including its synthesis and application[4].

Claim Metrics and Patent Scope

Independent Claim Length (ICL)

The independent claim length is a metric used to measure patent scope. In this patent, the independent claims are relatively detailed, reflecting the complexity of the chemical compounds. A longer independent claim length often indicates a narrower and more specific claim scope, which is the case here[3].

Independent Claim Count (ICC)

The patent includes multiple independent claims, each focusing on different aspects of the invention. This multiplicity of claims helps in defining a clear and specific scope, reducing the likelihood of overly broad claims that could lead to disputes[3].

Preparation Methods

The patent describes several methods for preparing the 2β-morpholino-androstane derivatives. These methods involve various chemical reactions, including the reaction of specific intermediates with morpholine in the presence of water. The detailed description of these methods ensures that the process is reproducible and within the scope of the patent[4].

Pharmaceutical Compositions

The patent also covers pharmaceutical compositions containing the novel compounds. These compositions are designed for neuromuscular blocking activity and are intended for use in medical procedures. The claims specify the concentration and formulation of these compositions, ensuring they are safe and effective for their intended use[4].

Use in Neuromuscular Blocking Agents

One of the key applications of the compounds described in this patent is their use as neuromuscular blocking agents. These agents are crucial in surgical procedures to facilitate muscle relaxation. The patent highlights the efficacy and safety profile of these compounds, making them valuable in clinical settings.

Patent Landscape

Related Patents

The patent landscape surrounding US 4,894,369 includes other patents related to neuromuscular blocking agents. For example, the process for synthesizing rocuronium bromide, a derivative of the compounds described in this patent, is detailed in other patents such as WO2007033348A2. These patents build upon the foundational work described in US 4,894,369[1].

Litigation and Disputes

Patents in the pharmaceutical sector are often subject to litigation and disputes. The clarity and specificity of the claims in US 4,894,369 help mitigate such issues. However, broader debates about patent quality and scope, as discussed in the context of software patents, highlight the ongoing need for clear and well-defined claim language[3].

Impact on Innovation

The patent has had a significant impact on innovation in the field of neuromuscular blocking agents. By providing a clear and specific description of novel compounds and their preparation methods, it has facilitated further research and development. This has led to the creation of more effective and safer drugs, such as rocuronium bromide, which is widely used in clinical practice.

Conclusion

United States Patent 4,894,369 is a pivotal patent in the field of pharmaceuticals, particularly for neuromuscular blocking agents. Its well-defined claims, detailed preparation methods, and specific pharmaceutical compositions have contributed significantly to the development of safe and effective drugs.

Key Takeaways

  • Specific Claims: The patent includes specific and detailed claims that define the scope of the invention.
  • Preparation Methods: The patent describes several methods for preparing the novel compounds.
  • Pharmaceutical Compositions: The patent covers pharmaceutical compositions intended for neuromuscular blocking activity.
  • Impact on Innovation: The patent has facilitated further research and development in the field.
  • Patent Landscape: The patent is part of a broader landscape of related patents and ongoing debates about patent quality and scope.

FAQs

Q: What is the main subject of United States Patent 4,894,369?

A: The main subject is the description of novel 2β-morpholino-androstane derivatives and their use as neuromuscular blocking agents.

Q: How do the claims in this patent contribute to its scope?

A: The claims are specific and detailed, ensuring a clear and well-defined scope that reduces the likelihood of disputes.

Q: What is the significance of the preparation methods described in the patent?

A: The preparation methods are crucial for the reproducibility of the compounds and ensure that the process is within the scope of the patent.

Q: How has this patent impacted the development of neuromuscular blocking agents?

A: It has facilitated the creation of more effective and safer drugs, such as rocuronium bromide, by providing a clear description of novel compounds and their preparation methods.

Q: What are some of the broader implications of this patent in the context of patent quality and scope?

A: The patent's clear and specific claim language helps mitigate issues related to patent quality and scope, which are ongoing concerns in the broader patent landscape.

Sources

  1. WO2007033348A2 - Process for the synthesis of rocuronium bromide - Google Patents
  2. Patent and Trademark Office Notices - USPTO
  3. Patent Claims and Patent Scope - Hoover Institution
  4. US4894369A - Novel 2β-morpholino-androstane derivatives - Google Patents
  5. US4894369A - Novel 2β-morpholino-androstane derivatives - Google Patents

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Drugs Protected by US Patent 4,894,369

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

Foreign Priority and PCT Information for Patent: 4,894,369

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom8708886Apr 14, 1987

International Family Members for US Patent 4,894,369

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0287150 ⤷  Subscribe 96C0038 Belgium ⤷  Subscribe
Austria 79631 ⤷  Subscribe
Australia 1457088 ⤷  Subscribe
Australia 608313 ⤷  Subscribe
Canada 1291117 ⤷  Subscribe
Germany 19575040 ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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