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Last Updated: January 6, 2025

Details for Patent: 5,846,976


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Summary for Patent: 5,846,976
Title: Androstenone derivative
Abstract:The present invention relates to the compound of formula (I), ##STR1## also known as 17.beta.-N-(2,5-bis(Trifluoromethyl))phenylcarbamoyl-4-aza-5.alpha.-andros t-1-en-3-one, solvates thereof, its preparation, intermediates used in its preparation, pharmaceutical formulations thereof and its use in the treatment of androgen responsive and mediated diseases.
Inventor(s): Batchelor; Kenneth William (Chapel Hill, NC), Frye; Stephen Vernon (Durham, NC), Dorsey, Jr.; George F. (Raleigh, NC), Mook, Jr.; Robert A. (Chapel Hill, NC)
Assignee: Glaxo Wellcome Inc. (Research Triangle Park, NC)
Application Number:08/708,167
Patent Claim Types:
see list of patent claims
Use; Formulation;
Patent landscape, scope, and claims:

United States Patent 5,846,976: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 5,846,976, titled "Androstenone derivative," is a patent that covers a specific compound and its applications, particularly in the treatment of androgen-responsive diseases. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Patent Overview

Publication Number and Authority

The patent, numbered US5,846,976A, was issued by the United States Patent and Trademark Office (USPTO)[2].

Prior Art and Classification

The patent is classified under various categories, including A61P5/24 for drugs related to disorders of the endocrine system, specifically androgens, and C07C235/70 for carboxylic acid amides with specific substitutions[2].

Legal Status

As of the current date, the patent has expired, marking the end of its lifetime[2].

Scope of the Invention

Compound Description

The patent describes a compound of formula (I), known as 17β-N-(2,5-bis(trifluoromethyl)phenylcarbamoyl)-4-aza-5α-androst-1-en-3-one, and its pharmaceutically acceptable salts and solvates. This compound is designed to inhibit testosterone-5α-reductases, enzymes involved in the conversion of testosterone to dihydrotestosterone (DHT)[2].

Therapeutic Applications

The invention is particularly useful in the treatment of androgen-responsive diseases, such as benign prostatic hyperplasia (BPH) and other prostate-related conditions. The compound's mechanism of action is similar to other 5α-reductase inhibitors like finasteride and SKF105657, but it exhibits a longer half-life and greater potency[2].

Claims

Main Claims

The patent includes several key claims:

  • Compound Claim: The compound of formula (I) and its pharmaceutically acceptable salts and solvates.
  • Method Claims: Methods of inhibiting testosterone-5α-reductases and treating androgen-responsive diseases using the compound.
  • Combination Therapy: Methods of treating androgen-responsive diseases by administering the compound in combination with an anti-androgen such as flutamide[2].

Dependent Claims

Dependent claims further specify the methods and compositions, including the chronic model used to test the efficacy of the compound in reducing prostate weight in castrated male rats[2].

Patent Landscape

Related Patents and Applications

The patent landscape for 5α-reductase inhibitors is extensive, with multiple patents covering various compounds and methods for treating androgen-responsive diseases. For instance, patents like those held by GlaxoSmithKline for enlarged-prostate treatments highlight the competitive nature of this field[5].

International Patent Databases

To understand the global patent landscape, one can use databases such as the European Patent Office's esp@cenet, the Japan Patent Office's database, and the World Intellectual Property Organization's (WIPO) PATENTSCOPE. These resources provide access to international patent applications and granted patents, allowing for a comprehensive search of prior art and related inventions[1][4].

Cooperative Patent Classification (CPC)

The CPC database is crucial for finding relevant classification schemes and understanding how patents are categorized globally. This helps in identifying similar patents and assessing the novelty of the invention[4].

Search and Analysis Tools

USPTO Resources

The USPTO offers several tools for patent searching, including the Patent Public Search tool, which replaced legacy tools like PubEast and PubWest. The Global Dossier service provides access to file histories of related applications from participating IP offices, facilitating a more thorough analysis of the patent family[1].

Patent Claims Research Dataset

The USPTO's Patent Claims Research Dataset provides detailed information on claims from US patents and applications, which can be used to analyze the scope and trends of patent claims. This dataset is particularly useful for understanding the dependency relationships between claims and the overall patent scope[3].

Practical Applications and Testing

Efficacy Testing

The patent describes a chronic model using castrated male rats to test the efficacy of the compound in reducing prostate weight. This model demonstrates the compound's activity in inhibiting testosterone-5α-reductases and its potential therapeutic benefits[2].

Comparison with Existing Treatments

The compound's long half-life and potency compared to existing treatments like finasteride and SKF105657 make it a significant advancement in the field. This highlights the ongoing research and development aimed at improving treatments for androgen-responsive diseases[2].

Key Takeaways

  • Compound and Method: The patent covers a specific androstenone derivative and methods for its use in treating androgen-responsive diseases.
  • Therapeutic Applications: The compound is particularly useful in treating BPH and other prostate-related conditions.
  • Patent Landscape: The patent is part of a broader landscape of 5α-reductase inhibitors, with multiple related patents and applications globally.
  • Search and Analysis Tools: Utilizing USPTO resources and international databases is essential for comprehensive patent searching and analysis.
  • Practical Applications: The compound's efficacy and pharmacokinetic properties make it a valuable addition to the therapeutic arsenal for androgen-responsive diseases.

FAQs

What is the main compound described in US Patent 5,846,976?

The main compound is 17β-N-(2,5-bis(trifluoromethyl)phenylcarbamoyl)-4-aza-5α-androst-1-en-3-one, along with its pharmaceutically acceptable salts and solvates.

What is the primary therapeutic application of the compound?

The compound is primarily used in the treatment of androgen-responsive diseases, such as benign prostatic hyperplasia (BPH).

How does the compound compare to existing treatments like finasteride?

The compound has a longer half-life and greater potency compared to finasteride and other existing 5α-reductase inhibitors.

What tools can be used to search and analyze patents related to this invention?

Tools such as the USPTO's Patent Public Search, Global Dossier, and international databases like WIPO's PATENTSCOPE can be used for comprehensive patent searching and analysis.

Is the patent still in force?

No, the patent has expired, marking the end of its lifetime.

Sources

  1. USPTO - Search for patents. Retrieved from https://www.uspto.gov/patents/search
  2. Google Patents - Androstenone derivative. Retrieved from https://patents.google.com/patent/US5846976A/en
  3. USPTO - Patent Claims Research Dataset. Retrieved from https://www.uspto.gov/ip-policy/economic-research/research-datasets/patent-claims-research-dataset
  4. Clemson University - Advanced Patent Searching. Retrieved from https://clemson.libguides.com/advanced_patent_searching
  5. Law360 - GSK Sues Barr Over Prostate Treatment Patents. Retrieved from https://www.law360.com/healthcare-authority/articles/48199

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Drugs Protected by US Patent 5,846,976

ApplicantTradenameGeneric NameDosageNDAApproval DateTETypeRLDRSPatent No.Patent ExpirationProductSubstanceDelist Req.Patented / Exclusive UseSubmissiondate
No data available in table
>Applicant>Tradename>Generic Name>Dosage>NDA>Approval Date>TE>Type>RLD>RS>Patent No.>Patent Expiration>Product>Substance>Delist Req.>Patented / Exclusive Use>Submissiondate
Showing 0 to 0 of 0 entries

International Family Members for US Patent 5,846,976

CountryPatent NumberEstimated ExpirationSupplementary Protection CertificateSPC CountrySPC Expiration
European Patent Office 0719278 ⤷  Subscribe 300122 Netherlands ⤷  Subscribe
European Patent Office 0719278 ⤷  Subscribe SPC/GB03/018 United Kingdom ⤷  Subscribe
European Patent Office 0719278 ⤷  Subscribe PA2003007 Lithuania ⤷  Subscribe
European Patent Office 0719278 ⤷  Subscribe PA2003007,C0719278 Lithuania ⤷  Subscribe
>Country>Patent Number>Estimated Expiration>Supplementary Protection Certificate>SPC Country>SPC Expiration
Showing 1 to 4 of 4 entries

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