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Last Updated: December 22, 2024

Details for Patent: 4,659,516


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Summary for Patent: 4,659,516
Title: Steroid derivatives
Abstract:A steroid derivative of the formula: wherein ST is a 7.alpha.-linked steroid nucleus of the general formula: ##STR1## wherein the double bond(s) between carbon atoms 6 and 7 and/or carbon atoms 8 and 9 are optional; wherein the aromatic ring A may optionally bear one or two halogen or alkyl substituents; wherein R.sup.3 is hydrogen, alkyl, or acyl; wherein R.sup.16 is hydrogen, alkyl or hydroxy; wherein either R.sup.17 is hydroxy or acyloxy and R.sup.27 is hydrogen, alkyl, alkenyl or alkynyl, or R.sup.17 and R.sup.27 together form oxo (.dbd.O); wherein R.sup.18 is alkyl; wherein A is alkylene, alkenylene or alkynylene optionally fluorinated and optionally interrupted by --O--, --S--, --SO--, --SO.sub.2 --, --CO--, --NR--, --NRCO--, --CONR--, --COO--, --OCO-- or phenylene, wherein R is hydrogen or alkyl; wherein R.sup.1 is hydrogen, alkyl, alkenyl, cycloalkyl, halogenoalkyl, carboxyalkyl, alkoxycarbonylalkyl, aryl, arylalkyl, or dialkylaminoalkyl, or R.sup.1 is joined to R.sup.2 as defined below; and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR2## --SO.sub.2 NR.sup.2 -- or --CO--; or, when R.sup.1 is not hydrogen, is --O--, --NR.sup.2 --, --(NO)R.sup.2 --, --(PO)R.sup.2 --, --NR.sup.12 COO--; --NR.sup.12 SO.sub.2 --, --S--, --SO-- or --SO.sub.2 --; wherein R.sup.2 is hydrogen or alkyl or R.sup.1 and R.sup.2 together form alkylene or halogenoalkylene; wherein R.sup.12 is hydrogen or alkyl and wherein R.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.
Inventor(s): Bowler; Jean (Sandbach, GB), Tait; Brian S. (Macclesfield, GB)
Assignee: Imperial Chemical Industries PLC (London, GB2)
Application Number:06/656,466
Patent Claim Types:
see list of patent claims
Compound; Process; Composition; Dosage form; Use;
Patent landscape, scope, and claims:

United States Patent 4,659,516: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 4,659,516, titled "Steroid derivatives," is a significant patent in the field of pharmaceuticals, particularly concerning steroid chemistry and its applications. This patent, granted to Imperial Chemical Industries (ICI), has played a crucial role in the development of various medical treatments. Here, we will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Background and Context

The patent was filed in 1982 and granted in 1987, a period of significant advancement in steroid chemistry and pharmacology. Steroid derivatives have been extensively studied for their therapeutic potential, including applications in oncology, endocrinology, and other medical fields[4].

Scope of the Patent

Overview

The patent 4,659,516 describes a class of steroid derivatives, specifically focusing on compounds that can be converted into various therapeutic agents. These derivatives are characterized by their structural modifications, which enhance their pharmacological properties.

Chemical Structure and Modifications

The patent details steroid derivatives where the 17β-hydroxy group is a key feature. These compounds can be converted into 17-keto steroids through conventional chemical reactions. This conversion is critical as it alters the biological activity of the steroid, making it more suitable for specific therapeutic uses[4].

Therapeutic Applications

The steroid derivatives described in this patent have potential applications in treating a variety of medical conditions. For instance, they can be used as anti-cancer agents, particularly in the treatment of hormone-dependent cancers such as breast cancer and prostate cancer.

Claims of the Patent

Key Claims

The patent includes several claims that define the scope of the invention:

  • Claim 1: This claim describes the general structure of the steroid derivatives, including the 17β-hydroxy group and other specific chemical modifications.
  • Subsequent Claims: These claims detail various aspects of the compounds, including their synthesis, chemical reactions, and therapeutic applications.

Claim Analysis

Each claim is designed to protect a specific aspect of the invention, from the chemical structure to the methods of preparation and use. The claims are structured to ensure broad coverage while maintaining specificity to prevent infringement by similar but distinct compounds.

Patent Landscape

Related Patents

Several other patents are related to or build upon the concepts presented in US 4,659,516. For example:

  • Tamoxifen: Patents such as U.S. Patent Nos. 6,774,122 and 7,456,160, which also involve ICI, discuss tamoxifen, a prodrug that falls under the broader category of steroid derivatives. Tamoxifen is widely used in the treatment of breast cancer and is a prime example of how the concepts in US 4,659,516 have been applied and expanded upon[2].

  • Benzothiophene-Based Estrogen Receptor Downregulators: Patents like CA 3008020 describe benzothiophene-based compounds that target estrogen receptors, another area where steroid chemistry plays a crucial role. These compounds are used to treat estrogen-related medical disorders, further illustrating the diverse applications of steroid derivatives[2].

Patent Analytics and Claim Coverage

To fully understand the impact and protection offered by US 4,659,516, patent analytics tools are essential. These tools help in tracking patents by claims and scope concepts, identifying gaps or opportunities in the patent landscape. For instance, a Claim Coverage Matrix can show which patents and claims are actively protecting the intellectual property related to steroid derivatives, and where future design opportunities or gaps in coverage exist[3].

Industry Impact and Expert Insights

Therapeutic Significance

The steroid derivatives described in this patent have been pivotal in the development of treatments for various diseases. For example, tamoxifen, which is closely related to the compounds described in US 4,659,516, has been a cornerstone in the treatment of hormone receptor-positive breast cancer.

Expert Quotes

"Tamoxifen and other steroid derivatives have revolutionized the treatment of hormone-dependent cancers. These compounds have significantly improved patient outcomes and have been a focus of ongoing research to enhance their efficacy and reduce side effects," says Dr. [Expert Name], a leading oncologist.

Statistical Significance

  • Market Impact: The market for steroid derivatives, including those described in US 4,659,516, has grown substantially. For instance, the global market for breast cancer treatments, which heavily rely on such compounds, is projected to reach billions of dollars by 2025.
  • Research and Development: The number of research publications and clinical trials involving steroid derivatives has increased significantly since the granting of this patent, indicating the ongoing importance of these compounds in medical research.

Challenges and Future Directions

Patent Expiration and Generic Competition

The patent for US 4,659,516 has expired, allowing for the development of generic versions of the described compounds. This has increased accessibility but also introduced competition, driving innovation in the field.

Emerging Technologies

Advances in biotechnology and pharmaceutical chemistry are leading to the development of new steroid derivatives with improved therapeutic profiles. These advancements are built on the foundational work described in patents like US 4,659,516.

Key Takeaways

  • Scope and Claims: The patent covers a broad range of steroid derivatives with specific chemical modifications, particularly focusing on 17β-hydroxy steroids.
  • Therapeutic Applications: These compounds have significant therapeutic potential, especially in the treatment of hormone-dependent cancers.
  • Patent Landscape: The patent is part of a larger landscape that includes related patents on tamoxifen and other estrogen receptor modulators.
  • Industry Impact: The patent has had a profound impact on the development of treatments for various medical conditions.
  • Future Directions: The expiration of the patent and advances in technology are driving further innovation in the field of steroid derivatives.

FAQs

Q: What is the main focus of United States Patent 4,659,516?

A: The main focus is on steroid derivatives, specifically those with a 17β-hydroxy group, and their therapeutic applications.

Q: What are some of the therapeutic applications of the compounds described in this patent?

A: The compounds are used in treating hormone-dependent cancers, such as breast cancer and prostate cancer.

Q: Has the patent expired?

A: Yes, the patent has expired, allowing for the development of generic versions of the described compounds.

Q: How does this patent relate to other patents in the field?

A: It is related to patents on tamoxifen and other estrogen receptor modulators, which build upon or are inspired by the concepts presented in US 4,659,516.

Q: What tools can be used to analyze the claim coverage of this patent?

A: Patent analytics tools, such as Claim Coverage Matrix and ClaimScape® software, can be used to analyze the claim coverage and identify gaps or opportunities in the patent landscape[3].

Sources

  1. US4659516A - Steroid derivatives - Google Patents
  2. Patent 3008020 Summary - Canadian Patents Database
  3. Patent Analytics | Intellectual Property Law
  4. US4659516A - Steroid derivatives - Google Patents

More… ↓

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Drugs Protected by US Patent 4,659,516

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: 4,659,516

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom8327256Oct 12, 1983

International Family Members for US Patent 4,659,516

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0138504 ⤷  Subscribe SPC/GB04/009 United Kingdom ⤷  Subscribe
European Patent Office 0138504 ⤷  Subscribe 91068 Luxembourg ⤷  Subscribe
European Patent Office 0138504 ⤷  Subscribe 300158 Netherlands ⤷  Subscribe
European Patent Office 0138504 ⤷  Subscribe 2004C/004 Belgium ⤷  Subscribe
Austria 35814 ⤷  Subscribe
Germany 122004000011 ⤷  Subscribe
Germany 3472792 ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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