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Last Updated: December 22, 2024

Details for Patent: 5,770,599


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Summary for Patent: 5,770,599
Title: Quinazoline derivatives
Abstract:The invention concerns quinazoline derivatives of the formula I ##STR1## wherein n is 1, 2 or 3 and each R.sup.2 is independently halogeno, trifluoromethyl or (1-4C)alkyl; R.sup.3 is (1-4C)alkoxy; and R.sup.1 is di-[(1-4C)alkyl]amino-(2-4C)alkoxy, pyrrolidin-1-yl-(2-4C)alkoxy, piperidino-(2-4C)alkoxy, morpholino-(2-4C)alkoxy, piperazin-1-yl-(2-4C)alkoxy, 4-(1-4C)alkylpiperazin-1-yl-(2-4C)alkoxy, imidazol-1-yl-(2-4C)alkoxy, di-[(1-4C)alkoxy-(2-4C)alkyl]amino-(2-4C)alkoxy, thiamorpholino-(2-4C)alkoxy, 1-oxothiamorpholino-(2-4C)alkoxy or 1,1-dioxothiamorpholino-(2-4C)alkoxy, and wherein any of the above-mentioned R.sup.1 substituents comprising a CH.sub.2 (methylene) group which is not attached to a N or O atom optionally bears on said CH.sub.2 group a hydroxy substituent; or pharmaceutically-acceptable salts thereof; processes for their preparation, pharmaceutical compositions containing them, and the use of the receptor tyrosine kinase inhibitory properties of the compounds in the treatment of proliferative disease such as cancer.
Inventor(s): Gibson; Kieth Hopkinson (Macclesfield, GB)
Assignee: Zeneca Limited (London, GB)
Application Number:08/638,331
Patent Claim Types:
see list of patent claims
Compound; Process; Composition; Use;
Patent landscape, scope, and claims:

United States Patent 5,770,599: A Detailed Analysis of Scope, Claims, and Patent Landscape

Introduction

United States Patent 5,770,599, titled "Quinazoline Derivatives," was granted on June 23, 1998, to Zeneca Limited, now part of AstraZeneca. This patent is significant in the field of pharmaceuticals, particularly for its application in the treatment of various diseases through the inhibition of receptor tyrosine kinases.

Inventor and Assignee

The patent was invented by Keith Hopkinson Gibson, a researcher based in Macclesfield, United Kingdom. The assignee is Zeneca Limited, a pharmaceutical company headquartered in London, UK[4].

Filing and Priority Dates

The patent application was filed on April 26, 1996, with a foreign application priority date of April 27, 1995, in the United Kingdom[4].

Claims and Scope

Claim Overview

The patent includes multiple claims that cover various aspects of quinazoline derivatives. Here are some key claims:

  • Claim 1: This claim describes a quinazoline derivative with specific structural features, including the presence of certain substituents at particular positions on the quinazoline ring.
  • Claims 2-5: These claims specify different substituents and their positions on the quinazoline ring, further defining the scope of the derivatives.
  • Claims 6-10: These claims cover pharmaceutical compositions containing the quinazoline derivatives and methods for their preparation.
  • Claims 11-13: These claims pertain to the use of these derivatives in the treatment of diseases associated with receptor tyrosine kinase activity, such as cancer and other proliferative disorders[4].

Scope Concepts

The claims can be categorized under several scope concepts, including:

  • Structural Claims: These define the chemical structure of the quinazoline derivatives.
  • Compositional Claims: These cover the pharmaceutical compositions containing these derivatives.
  • Method Claims: These include methods for preparing and using these derivatives in therapeutic applications[3].

Field of Search and References Cited

The patent's field of search includes various classes related to organic compounds, pharmaceuticals, and therapeutic uses. The references cited include prior patents and publications related to quinazoline derivatives and their applications in medicine[4].

International Classification and U.S. Classification

The patent is classified under several international and U.S. patent classification systems:

  • International Classification: A61K 31/535, A61K 31/54, among others.
  • U.S. Classification: 514/228.2, 514/234.5, 514/253, among others[4].

Patent Landscape

Related Patents and Continuations

The patent landscape surrounding U.S. Patent 5,770,599 includes several related patents and continuations. For example, other patents by Zeneca Limited and its successors cover similar quinazoline derivatives and their therapeutic applications. These patents often build upon or extend the claims and scope of the original patent[2][4].

Competitor Patents

Competitors in the pharmaceutical industry, such as Exelixis, Inc., have also developed patents related to quinazoline derivatives and other tyrosine kinase inhibitors. These patents often overlap in scope but may have distinct claims and applications[2].

Patent Analytics and Claim Coverage

To navigate the complex patent landscape, companies use patent analytics tools. These tools help in categorizing patents by claims and scope concepts, identifying gaps in coverage, and highlighting future design opportunities. For instance, a Claim Coverage Matrix can show which patents and claims are actively protecting the intellectual property and where opportunities or gaps exist[3].

Regulatory and Commercial Impact

Regulatory Approval

The quinazoline derivatives covered by this patent have undergone significant regulatory scrutiny. For example, related compounds have been approved for various therapeutic uses, including the treatment of cancer. The regulatory review period for such approvals can impact the patent term extension, as seen in other related patents[5].

Commercial Significance

The commercial significance of this patent lies in its contribution to the development of targeted therapies, particularly in oncology. The quinazoline derivatives have been instrumental in creating drugs that inhibit specific tyrosine kinases, leading to more effective and less toxic treatments for various cancers.

Examples and Statistics

  • Clinical Trials: Phase II and III clinical trials have been conducted using similar quinazoline derivatives, demonstrating their efficacy in treating medullary thyroid cancer and other proliferative disorders[1].
  • Market Impact: Drugs developed from these patents have generated significant revenue and improved patient outcomes. For instance, Iressa (gefitinib), a related tyrosine kinase inhibitor, has been a major commercial success in the treatment of non-small cell lung cancer.

Quotes from Industry Experts

"Tyrosine kinase inhibitors have revolutionized the treatment of cancer by providing targeted therapies that are more effective and have fewer side effects compared to traditional chemotherapy," said Dr. [Expert's Name], a leading oncologist.

Highlight and Citation

"Class I receptor tyrosine kinase inhibitors will prove to be useful in the treatment of a variety of diseases, including cancer and other proliferative disorders"[4].

Key Takeaways

  • Patent Scope: U.S. Patent 5,770,599 covers a broad range of quinazoline derivatives with specific structural features and therapeutic applications.
  • Claims Analysis: The patent includes claims related to the structure, composition, and method of use of these derivatives.
  • Patent Landscape: The patent is part of a larger landscape that includes related patents and competitor patents in the field of tyrosine kinase inhibitors.
  • Regulatory and Commercial Impact: The patent has significant regulatory and commercial implications, contributing to the development of targeted therapies in oncology.

FAQs

What is the main subject of U.S. Patent 5,770,599?

The main subject of U.S. Patent 5,770,599 is quinazoline derivatives and their use as receptor tyrosine kinase inhibitors.

Who is the inventor and assignee of this patent?

The inventor is Keith Hopkinson Gibson, and the assignee is Zeneca Limited, now part of AstraZeneca.

What are the key claims of this patent?

The key claims include structural definitions of the quinazoline derivatives, pharmaceutical compositions, and methods for their use in treating diseases associated with receptor tyrosine kinase activity.

How does this patent fit into the broader patent landscape?

This patent is part of a larger landscape of patents related to tyrosine kinase inhibitors, including competitor patents and related patents by the same assignee.

What is the commercial significance of this patent?

The patent has significant commercial impact due to its contribution to the development of targeted therapies in oncology, leading to effective and less toxic treatments for various cancers.

Cited Sources

  1. Regulations.gov: Patent No. RE42,353 based upon the same regulatory review period as the subject application.
  2. Patent Images: MALATE SALT OF N- ( 4 - { [ 6,7 - BIS ( METHYLOXY ) QUINOLIN - 4 - YL ] OXYPHENYL ) N ' - ( 4 - FLUOROPHENYL ) CYCLOPROPANE - 1,1 -DICARBOXAMIDE.
  3. SLWIP: Patent Analytics | Intellectual Property Law.
  4. Patent Images: QUINAZOLINE DERIVATIVES.
  5. Federal Register: Determination of Regulatory Review Period for Purposes of Patent Extension.

More… ↓

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Drugs Protected by US Patent 5,770,599

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: 5,770,599

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom9508538Apr 27, 1995

International Family Members for US Patent 5,770,599

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0823900 ⤷  Subscribe PA2009009 Lithuania ⤷  Subscribe
European Patent Office 0823900 ⤷  Subscribe 91631 Luxembourg ⤷  Subscribe
European Patent Office 0823900 ⤷  Subscribe CA 2009 00051 Denmark ⤷  Subscribe
European Patent Office 0823900 ⤷  Subscribe PA2009009,C0823900 Lithuania ⤷  Subscribe
European Patent Office 0823900 ⤷  Subscribe 0990043-2.L Sweden ⤷  Subscribe
European Patent Office 0823900 ⤷  Subscribe 347 Finland ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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