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Last Updated: December 22, 2024

Details for Patent: 4,978,672


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Summary for Patent: 4,978,672
Title: Alpha-heterocyclc substituted tolunitriles
Abstract:The invention is concerned with aromatase inhibiting compounds of formula I ##STR1## wherein R and Ro represent hydrogen or lower alkyl; or R and Ro located on adjacent carbon atoms and together when combined with the benzene ring to which they are attached form a naphthalene or tetrahydronaphthalene ring; R.sub.1 and R.sub.2 independently represent hydrogen, lower alkyl, (lower alkyl, aryl or aryl-lower alkyl)-thio, lower alkenyl, aryl, aryl-lower alkyl, C.sub.3 -C.sub.6 -cycloalkyl, or C.sub.3 -C.sub.6 -cycloalkyl-lower alkyl; or R.sub.1 and R.sub.2 combined represent lower alkylidene, mono- or di-aryl-lower alkylidene; R.sub.1 and R.sub.2 combined also represent C.sub.4 -C.sub.6 -straight chain alkylene, lower alkyl-substituted straight chain alkylene or ortho-phenylene bridged-C.sub.2 -C.sub.4 -straight chain alkylene, each forming with the carbon atom attached thereto a corresponding optionally substituted or benzo-fused 5, 6 or 7-membered ring; W represents 1-imidazolyl, 1-(1,2,4- or 1,3,4)-triazolyl or 3-pyridyl; or W represents 1-imidazolyl, 1-(1,2,4 or 1,3,4)-triazolyl or 3-pyridyl substituted by lower alkyl; and pharmaceutically acceptable salts thereof.
Inventor(s): Bowman; Robert M. (Summit, NJ), Steele; Ronald E. (Long Valley, NJ), Browne; Leslie (Aesch, CH)
Assignee: Ciba-Geigy Corporation (Ardsley, NY)
Application Number:07/240,862
Patent Claim Types:
see list of patent claims
Compound; Use; Composition;
Patent landscape, scope, and claims:

United States Patent 4,978,672: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 4,978,672, titled "Alpha-heterocyclic substituted tolunitriles," is a significant patent in the pharmaceutical domain, particularly in the area of aromatase inhibitors. This patent, which has expired, is crucial for understanding the development and protection of certain pharmaceutical compounds.

Background

The patent was granted for compounds that inhibit aromatase, an enzyme involved in the biosynthesis of estrogen from androgen precursors. These compounds are particularly important in the treatment of conditions such as breast cancer, where estrogen levels play a critical role.

Scope of the Patent

Chemical Structure and Compounds

The patent describes a class of compounds with the general formula I, where R and Ro represent hydrogen or lower alkyl groups. These compounds include various substitutions such as 1-imidazolyl, 1-triazolyl, and 3-pyridyl groups, which can be further substituted by lower alkyl groups[1].

Specific Embodiments

  • One specific embodiment involves compounds where W represents 1-imidazolyl or 1-imidazolyl substituted by lower alkyl.
  • Another embodiment includes compounds where W represents 1-(1,2,4- or 1,3,4-)-triazolyl or 1-(1,2,4- or 1,3,4-)-triazolyl substituted by lower alkyl.
  • A further embodiment involves compounds where W represents 3-pyridyl or 3-pyridyl substituted by lower alkyl[1].

Pharmaceutical Applications

The compounds described in the patent are intended for use as aromatase inhibitors, which are crucial in the treatment of estrogen-dependent diseases such as breast cancer.

Claims of the Patent

Main Claims

The patent includes several main claims that define the scope of protection:

  • Claims related to the specific chemical structures of the compounds, including the various substitutions mentioned above.
  • Claims related to the pharmaceutical compositions containing these compounds.
  • Claims related to the methods of use of these compounds for treating estrogen-dependent diseases[1].

Dependent Claims

Dependent claims further specify the main claims by detailing the specific substitutions, the formation of naphthalene or tetrahydronaphthalene rings, and the pharmaceutical acceptable salts of these compounds[1].

Patent Landscape

Related Patents and Extensions

The patent landscape around US 4,978,672 includes other patents related to aromatase inhibitors and their methods of preparation. For instance, the patent term for certain pharmaceutical patents, including those related to aromatase inhibitors, can be extended under 35 U.S.C. 156(e)(1) due to regulatory reviews by the FDA or the Department of Agriculture[2].

Competing Technologies

Other patents, such as US 8198460B2, describe improved processes for the preparation of letrozole, another non-steroidal aromatase inhibitor. These patents indicate a competitive landscape where multiple companies and researchers are working on similar technologies[4].

Analytical Tools for Patent Landscape

Patent Analytics

To understand the full scope and claims of US 4,978,672 and its place in the patent landscape, tools like patent analytics are essential. These tools help in categorizing patents by claims and scope concepts, making it easier to identify gaps or opportunities in intellectual property protection[3].

Claim Coverage Matrix

A Claim Coverage Matrix can be used to show which patents and claims are actively protecting the intellectual property related to aromatase inhibitors. This matrix helps in filtering, searching, and analyzing large numbers of patent claims concurrently[3].

Impact on Pharmaceutical Industry

Drug Development

The compounds described in US 4,978,672, particularly those used in drugs like Femara (letrozole), have been crucial in the treatment of breast cancer. The expiration of this patent has opened up opportunities for generic versions of these drugs, impacting the pharmaceutical industry's landscape[5].

Regulatory Considerations

The patent term extension provisions under 35 U.S.C. 156(e)(1) highlight the regulatory complexities surrounding pharmaceutical patents. These extensions can significantly impact the market exclusivity period for drugs, affecting both the original patent holders and generic manufacturers[2].

Key Takeaways

  • Chemical Structure and Substitutions: The patent describes specific chemical structures and substitutions for aromatase inhibitors.
  • Pharmaceutical Applications: The compounds are used in treating estrogen-dependent diseases like breast cancer.
  • Claims and Scope: The patent includes claims related to chemical structures, pharmaceutical compositions, and methods of use.
  • Patent Landscape: The patent is part of a broader landscape that includes other aromatase inhibitors and related technologies.
  • Analytical Tools: Tools like patent analytics and Claim Coverage Matrix are essential for understanding the patent landscape.
  • Impact on Industry: The patent's expiration has significant implications for drug development and market exclusivity.

Frequently Asked Questions (FAQs)

What is the main purpose of US Patent 4,978,672?

The main purpose of US Patent 4,978,672 is to describe and protect a class of compounds that act as aromatase inhibitors, which are used in the treatment of estrogen-dependent diseases like breast cancer.

What are the key chemical structures described in the patent?

The patent describes compounds with the general formula I, including various substitutions such as 1-imidazolyl, 1-triazolyl, and 3-pyridyl groups, which can be further substituted by lower alkyl groups.

How does the patent term extension under 35 U.S.C. 156(e)(1) affect pharmaceutical patents?

The patent term extension under 35 U.S.C. 156(e)(1) allows for the extension of a patent term by up to five years if the patent claims a product or method subject to regulatory reviews by the FDA or the Department of Agriculture.

What is the significance of letrozole in the context of this patent?

Letrozole, a non-steroidal aromatase inhibitor, is a drug that falls under the scope of this patent. It is used in the treatment of breast cancer and is an example of the compounds described in the patent.

How do patent analytics tools help in understanding the patent landscape?

Patent analytics tools help in categorizing patents by claims and scope concepts, making it easier to identify gaps or opportunities in intellectual property protection. These tools generate interactive claim charts that can be reviewed by technical experts to determine the applicability of specific scope concepts to target products or methods.

Cited Sources

  1. US4978672A - Alpha-heterocyclc substituted tolunitriles - Google Patents
  2. Extension Under 35 U.S.C. 156(e)(1) - OG Date: 29 July 2003 - United States Patent and Trademark Office
  3. Patent Analytics | Intellectual Property Law - Schwegman
  4. US8198460B2 - Process for preparation of letrozole and its intermediates - Google Patents
  5. NoncE OF FINAL DETERMINATION - USPTO - United States Patent and Trademark Office

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Drugs Protected by US Patent 4,978,672

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 4,978,672

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0236940 ⤷  Subscribe SPC/GB97/013 United Kingdom ⤷  Subscribe
European Patent Office 0236940 ⤷  Subscribe 97C0053 Belgium ⤷  Subscribe
European Patent Office 0236940 ⤷  Subscribe C970011 Netherlands ⤷  Subscribe
Austria 94873 ⤷  Subscribe
Australia 604011 ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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