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Last Updated: December 22, 2024

Details for Patent: 4,386,085


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Summary for Patent: 4,386,085
Title: Novel steroids
Abstract:Novel 19-nor steroids and 19-nor-D-homo-steroids of the formula ##STR1## wherein R.sub.1 is an organic radical of 1 to 18 carbon atoms containing at least one atom selected from the group consisting of nitrogen, phosphorous and silicon with the atom immediately adjacent to the 11-carbon atom being carbon, R.sub.2 is a hydrocarbon of 1 to 8 carbon atoms, X is selected from the group consisting of a pentagonal ring and a hexagonal ring optionally substituted and optionally containing a double bond, B and C together form a double bond or an epoxy group, the C.dbd.A group at position 3 is selected from the group consisting of C.dbd.O, ketal, ##STR2## --C.dbd.NOH, --C.dbd.NOAlK.sub.3 and .dbd.CH.sub.2, AlK.sub.1, AlK.sub.2 and AlK.sub.3 are selected from the group consisting of alkyl of 1 to 8 carbon atoms and aralkyl of 7 to 15 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having anti-glucocorticoid activity and a process for their preparation.
Inventor(s): Teutsch; Jean G. (Pantin, FR), Costerousse; Germain (Saint-Maurice, FR), Philibert; Daniel (La Varenne Saint Hilaire, FR), Deraedt; Roger (Pavillons sous Bois, FR)
Assignee: Roussell Uclaf (Paris, FR)
Application Number:06/338,077
Patent Claim Types:
see list of patent claims
Compound; Process; Composition; Use;
Patent landscape, scope, and claims:

United States Patent 4,386,085: A Detailed Analysis of Scope and Claims

Introduction

United States Patent 4,386,085, titled "Novel Steroids," is a significant patent that outlines the synthesis, properties, and applications of novel steroid derivatives. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Background and State of the Art

The patent builds upon earlier work described in U.S. Pat. No. 4,233,296, which details steroids substituted in the 11-position with various substituents. The current patent expands on this by introducing new steroid derivatives and their preparation methods[2].

Scope of the Invention

The patent covers a wide range of novel steroid compounds, particularly those with substitutions at the 11-position and modifications at other positions. Here are the key aspects of the scope:

Novel Steroid Compounds

The patent describes the synthesis of steroid derivatives with specific substitutions, including those with ketal, thioketal, oxime, or methyloxime groups. These compounds are designed to have particular pharmacological properties, such as antiglucocorticoid activity[2].

Preparation Methods

The invention includes several novel processes for preparing these steroid compounds. These methods involve reactions with dehydration agents, ketalization agents, reducing agents, and etherification agents. For example, the use of sulfonic acid resins, inorganic acids, and peracids is detailed for freeing ketone groups and introducing specific substituents[1].

Specific Compounds and Their Synthesis

The patent provides detailed examples of the synthesis of specific compounds, such as the preparation of 3,3-[1,2-ethanediyl-bisoxy]-17α-(prop-1-ynyl)-5α,10α-epoxy-9(11)-estrene-17α-ol. These compounds are synthesized through a series of reactions involving epoxidation, ketalization, and reduction steps[1].

Claims of the Patent

The patent includes 46 claims that cover various aspects of the invention:

Compound Claims

Claims are made for the novel steroid compounds themselves, including their structures and the specific substituents at various positions. These claims are crucial for defining the intellectual property protected by the patent[2].

Process Claims

The patent claims cover the methods for preparing these compounds, including the use of specific reagents and reaction conditions. These process claims are essential for protecting the innovative synthesis methods described in the patent[1].

Use Claims

Claims are also made for the use of these compounds in pharmaceutical applications, particularly as antiglucocorticoids. This includes the composition of these compounds with inert pharmaceutical carriers or excipients[1].

Patent Landscape

Understanding the broader patent landscape is crucial for assessing the significance and impact of this patent.

Related Patents

Other patents, such as U.S. Pat. No. 4,233,296, provide context and background information on steroid chemistry. French patent No. 2,423,486 is also referenced for specific epoxidation methods used in the synthesis of these compounds[1].

Competitive Landscape

The development and commercialization of these steroid derivatives have been influenced by various factors, including regulatory approvals and market demand. For example, the approval and commercialization of mifepristone, a related steroid derivative, have been subject to significant regulatory and societal scrutiny[4].

Patent Analytics and Claim Coverage

To fully understand the protection and value of this patent, patent analytics tools can be employed:

Claim Coverage Matrix

A Claim Coverage Matrix can help identify which patents and claims are actively protecting the intellectual property related to these steroid derivatives. This tool categorizes patents by claims and scope concepts, making it easier to analyze large numbers of patent claims concurrently[3].

Scope Concepts

The scope concepts of the patent claims relate directly to their value. High-value claims are those that are currently crucial to the company, while medium-value claims indicate potential future directions. Low-value claims may not be worth maintaining. Interactive claim charts generated by tools like ClaimScape® can help in this analysis[3].

Applications and Impact

The novel steroid compounds and their preparation methods described in this patent have significant pharmaceutical applications:

Antiglucocorticoid Activity

These compounds are designed to have antiglucocorticoid activity, making them useful in various medical treatments. The specific pharmacological properties of these compounds are a key focus of the patent[1].

Market and Regulatory Environment

The approval and use of these compounds are subject to regulatory oversight. For instance, the approval process for mifepristone, a related compound, involved extensive clinical trials and regulatory hurdles[4].

Key Takeaways

  • Novel Compounds: The patent introduces new steroid derivatives with specific substitutions and modifications.
  • Preparation Methods: Detailed processes for synthesizing these compounds are provided, including the use of various reagents and reaction conditions.
  • Claims: The patent includes claims for the compounds, their preparation methods, and their pharmaceutical uses.
  • Patent Landscape: The patent is part of a broader landscape of steroid chemistry patents and is influenced by regulatory and market factors.
  • Patent Analytics: Tools like Claim Coverage Matrix and scope concepts help in analyzing the value and protection of the patent claims.

FAQs

What is the main focus of United States Patent 4,386,085?

The main focus of this patent is the synthesis, properties, and applications of novel steroid derivatives, particularly those with antiglucocorticoid activity.

What are the key preparation methods described in the patent?

The patent describes methods involving dehydration agents, ketalization agents, reducing agents, and etherification agents to synthesize the steroid compounds.

How does this patent fit into the broader patent landscape?

This patent builds upon earlier work in steroid chemistry and is part of a larger landscape that includes related patents and regulatory approvals.

What is the significance of the claims in this patent?

The claims cover the novel compounds, their preparation methods, and their pharmaceutical uses, providing broad protection for the intellectual property.

How can patent analytics tools help in understanding this patent?

Patent analytics tools, such as Claim Coverage Matrix and scope concepts, help in categorizing and analyzing the claims to determine their value and coverage.

What are some of the pharmaceutical applications of the compounds described in this patent?

The compounds are designed to have antiglucocorticoid activity, making them useful in various medical treatments.

Sources

  1. US4634695A - Steroid derivatives - Google Patents
  2. United States Patent (19) - googleapis.com
  3. Patent Analytics | Intellectual Property Law
  4. Mifepristone - Wikipedia

More… ↓

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Drugs Protected by US Patent 4,386,085

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: 4,386,085

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
France81 00272Jan 09, 1981

International Family Members for US Patent 4,386,085

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0057115 ⤷  Subscribe SPC/GB93/030 United Kingdom ⤷  Subscribe
Austria 12239 ⤷  Subscribe
Austria 23167 ⤷  Subscribe
Austria 23344 ⤷  Subscribe
Austria 396787 ⤷  Subscribe
Austria 46702 ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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