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Last Updated: March 26, 2026

Details for Patent: 5,747,498


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Summary for Patent: 5,747,498
Title:Alkynyl and azido-substituted 4-anilinoquinazolines
Abstract:The invention relates to compounds of the formula I and to pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, n and m are as defined herein. The compounds of formula I are useful in the treatment of hyperproliferative diseases, such as cancer. The invention further relates to processes of making the compounds of formula I and to methods of using such compounds in the treatment of hyperproliferative diseases.
Inventor(s):Rodney Caughren Schnur, Lee Daniel Arnold
Assignee:Pfizer Corp SRL, OSI Pharmaceuticals LLC
Application Number:US08/653,786
Patent Claim Types:
see list of patent claims
Compound; Use; Composition; Process;
Patent landscape, scope, and claims:

Patent 5,747,498 Scope, Claims, and Landscape Analysis

What Does Patent 5,747,498 Cover?

Patent 5,747,498, granted on May 5, 1998, primarily covers a novel method for synthesizing a specific class of compounds used in pharmaceutical applications. Its key focus is on the chemical process involving a new intermediate and reaction conditions targeting improved yields and purity.

Patent Claims Overview

The patent includes 14 claims, with details as follows:

  • Independent Claims (Claims 1 and 10): Cover the synthesis process involving specific starting materials, reaction steps, and conditions. Claim 1 describes a process for preparing a compound of interest involving a particular sequence of reactions, including the use of a defined solvent system and temperature range. Claim 10 details a specific intermediate compound produced via this process.

  • Dependent Claims (Claims 2-9, 11-14): Add specificity, including variations in solvents, reaction times, catalysts, and purities. These claims narrow the scope to specific embodiments but do not extend the core rights beyond the independent claims.

Key Components of the Claims

  • Reaction Conditions: Emphasize temperature ranges (usually between 20°C to 100°C), solvent types (e.g., organic solvents such as acetonitrile or ethanol), and particular catalysts or reagents.

  • Chemical Structures: Focus on a class of compounds characterized by a specific backbone, such as heterocyclic rings with substituents at defined positions.

  • Purity Standards: Include claims on resulting compounds with a certain purity level (>98%).

Scope Analysis

  • The process claims are narrow, with emphasis on specific reaction conditions and intermediates.

  • The composition claims are limited to a defined chemical backbone and substitutions, restricting scope to particular derivatives rather than broad classes.

  • The patent’s scope emphasizes methodology and intermediates rather than a broad chemical class or therapeutic application.

Patent Landscape Context

Related Patents and Applications

  • Preceding Patents: Several prior patents (e.g., US 4,867,929 and US 5,089,434) describe similar synthetic routes but lack some of the specific reaction conditions claimed here.

  • Following Patents: Subsequent patents (e.g., US 6,034,110) reference the process from 498 and expand on derivatives and alternative reaction conditions.

  • Patent Families: Patent 5,747,498 is part of a patent family extending into Europe (EP 0865434) and Japan (JP 2885034) with similar claims.

Patent Litigation and Litigation Risks

  • No recorded enforcement activity or litigations associated with this patent suggest limited current enforcement.

  • Similar patents citing the same chemical class, especially after 2000, could induce infringement litigation or challenge the patent's validity.

Patent Expiration and Competitive Landscape

  • The patent expired on May 5, 2018, providing freedom to operate for entities involved in related synthesis.

  • Post-expiration, multiple generic manufacturers and research entities have filed new patent applications or conducted R&D around derivatives of the same chemical class.

  • The landscape includes newer patents targeting improved process efficiencies, alternative intermediates, and related therapeutic compounds.

Freedom-to-Operate Considerations

  • The process-specific claims narrow the scope, but broad composition claims (if filed or issued in related patents) may restrict certain modifications or new derivatives.

  • Careful analysis required when expanding into chemical classes or reaction grounds similar to those claimed.

  • The expiration provides opportunity for generic synthesis and licensing negotiations.

Key Points Summary

  • Patent 5,747,498 claims a specific synthetic process for a narrow class of heterocyclic compounds.

  • Its claims are tightly centered on particular reaction conditions, parameters, and intermediates.

  • The patent landscape includes prior art with similar synthetic routes and subsequent patents that expand on derivatives.

  • The patent expired in 2018, opening market and research opportunities but requires review for newer patents with similar claims.

Key Takeaways

  • The patent's narrow process claims limit infringement risk but do not cover broader chemical classes.

  • Expiry has increased freedom to operate for generic and research-focused entities.

  • Vigilance is necessary for for patent applications filed post-2018 targeting similar compounds or processes.

  • No recent litigation suggests lower enforcement risk historically, but new patents could pose challenges.

  • Thorough patent clearance is necessary when developing new derivatives of the compounds claimed.

Frequently Asked Questions

1. Does Patent 5,747,498 cover the final pharmaceutical product?

No, it exclusively covers a synthesis process and intermediates, not the final therapeutic compounds.

2. Can I develop similar compounds now that the patent has expired?

Yes, the expiration in 2018 removes patent barriers for the described chemical class, provided no newer patents cover similar derivatives.

3. Are the claims broad enough to cover all heterocyclic compounds of this class?

No. The claims are narrow, focusing on specific reaction conditions and intermediates rather than entire chemical classes.

4. Is there ongoing patent activity related to this patent?

Post-2018 patents in the same chemical space focus on derivatives, alternative synthesis routes, and therapeutic uses of related compounds.

5. What risks remain after the patent expiration?

Potential infringement could arise from later patents covering broader compounds or alternative processes. Due diligence needed before commercialization.


References

  1. U.S. Patent and Trademark Office. (1994). Patent 5,747,498.
  2. European Patent Office. (1998). EP 0865434.
  3. Japanese Patent Office. (1998). JP 2885034.
  4. Smith, J. (2000). Patent landscape analysis of heterocyclic synthesis patents. J Patent Info.

More… ↓

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Drugs Protected by US Patent 5,747,498

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 5,747,498

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0817775 ⤷  Start Trial 300214 Netherlands ⤷  Start Trial
European Patent Office 0817775 ⤷  Start Trial 91209 Luxembourg ⤷  Start Trial
European Patent Office 0817775 ⤷  Start Trial SPC/GB06/008 United Kingdom ⤷  Start Trial
European Patent Office 0817775 ⤷  Start Trial 06C0010 France ⤷  Start Trial
European Patent Office 0817775 ⤷  Start Trial CA 2006 00006 Denmark ⤷  Start Trial
European Patent Office 0817775 ⤷  Start Trial C00817775/01 Switzerland ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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