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Last Updated: January 7, 2025

Details for Patent: 5,545,644


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Summary for Patent: 5,545,644
Title: Indole derivatives
Abstract:Compounds of the formula ##STR1## wherein n is 0, 1, or 2; X is hydrogen, chlorine, bromine or iodine; R.sub.1 is hydrogen; R.sub.3 is selected from hydrogen and C.sub.1 to C.sub.6 linear or branched alkyl; and R.sub.2 is as defined in the specification and the pharmaceutically acceptable salts thereof are useful psychotherapeutics and are potent serotonin (5-HT.sub.1) agonists and may be used in the treatment of depression, anxiety, eating disorders, obesity, drug abuse, cluster headache, migraine, pain, chronic paroxysmal hemicrania and headache associated with vascular disorders, and other disorders arising from deficient serotonergic neurotransmission. The compounds can also be used as centrally acting antihypertensives and vasodilators. A process for forming indoles by transition metal catalyzed cyclization of a dihalogenated intermediate is also disclosed.
Inventor(s): Macor; John E. (New York, NY), Wythes; Martin J. (New York, NY)
Assignee: Pfizer Inc. (New York, NY)
Application Number:08/466,644
Patent Claim Types:
see list of patent claims
Compound; Use; Composition;
Patent landscape, scope, and claims:

United States Patent 5,545,644: A Detailed Analysis of Scope and Claims

Introduction

United States Patent 5,545,644, titled "Indole derivatives," is a significant patent that covers a range of indole compounds, their preparation, and their medicinal uses. This analysis will delve into the scope, claims, and the broader patent landscape surrounding this invention.

Background

The patent, issued to the assignees of the invention, pertains to indole derivatives, which are compounds of interest in pharmaceutical research due to their potential therapeutic applications. The patent was granted on August 13, 1996, and has since expired, but its impact on the field of pharmaceuticals remains relevant.

Scope of the Patent

Indole Derivatives

The patent focuses on indole derivatives, specifically those that are useful in treating various disorders such as migraine and other cephalic pain conditions. The compounds described are characterized by their chemical structures, which include substitutions at specific positions of the indole ring[4].

Medicinal Use

The active compounds of the invention are highlighted for their therapeutic potential, particularly in the treatment of migraine and other related disorders. This includes 5HT1-receptor agonist and vasoconstrictor activities, which are crucial for the targeted therapeutic effects[4].

Chemical Structure and Variants

The patent details various chemical structures of the indole derivatives, including optical isomers (R and S enantiomers) and their racemic mixtures. The preferred compounds are specified with particular substitutions at the indole ring, such as R1, R2, and R3, which define the pharmacologically active forms of the compounds[4].

Claims of the Patent

Claim Structure

The patent includes multiple claims that define the scope of the invention. These claims are structured to cover the specific chemical compounds, their preparation methods, pharmaceutical compositions containing these compounds, and their medicinal uses.

Key Claims

  • Compound Claims: These claims specify the chemical structures of the indole derivatives, including the preferred compounds and their optical isomers.
  • Method Claims: These claims cover the processes and intermediates for preparing the indole derivatives.
  • Composition Claims: These claims pertain to pharmaceutical compositions containing the indole derivatives.
  • Use Claims: These claims detail the medicinal uses of the compounds, particularly in treating migraine and other disorders[4].

Patent Landscape

Prior Art

The patent references several prior art documents, including U.S. Pat. Nos. 4,839,377 and 4,855,314, and European Patent Application Publication Numbers 313397 and 303506. These prior art documents discuss related indole compounds and their therapeutic applications, highlighting the evolutionary nature of the current invention[4].

International Patent Offices

The patent landscape for indole derivatives is not limited to the United States. Similar patents and applications exist in other jurisdictions, such as the European Patent Office (EPO) and the Japan Patent Office (JPO). These international patents often cover similar compounds and uses, reflecting a global interest in these therapeutic agents[1].

Patent Analytics and Claim Coverage

To fully understand the patent landscape, companies often use patent analytics tools. These tools help in categorizing patents by claims and scope concepts, making it easier to identify gaps or opportunities in the intellectual property portfolio. For example, a Claim Coverage Matrix can show which patents and claims are actively protecting the intellectual property related to indole derivatives[3].

Impact and Relevance

Therapeutic Applications

The indole derivatives covered by this patent have significant therapeutic potential, particularly in the treatment of migraine and other cephalic pain conditions. The 5HT1-receptor agonist and vasoconstrictor activities of these compounds make them valuable in clinical settings.

Pharmaceutical Industry

The patent has influenced the development of pharmaceuticals in the field of pain management. Companies have built upon this research to develop new drugs and therapies, contributing to the advancement of medical science.

Expiration and Public Domain

The patent has expired, which means that the inventions described are now in the public domain. This allows other researchers and companies to use the disclosed information without infringing on the original patent rights. However, any new developments or improvements on these compounds could still be patented.

Conclusion

United States Patent 5,545,644 is a pivotal document in the field of pharmaceutical research, particularly concerning indole derivatives. Understanding its scope, claims, and the broader patent landscape is crucial for researchers and companies involved in drug development.

Key Takeaways

  • Indole Derivatives: The patent covers specific indole compounds useful in treating migraine and other disorders.
  • Chemical Structure: The patent details the chemical structures and preferred compounds, including optical isomers.
  • Claims: The patent includes claims for the compounds, preparation methods, pharmaceutical compositions, and medicinal uses.
  • Prior Art: The patent references several prior art documents, indicating an evolutionary development in the field.
  • International Landscape: Similar patents exist in other jurisdictions, reflecting global interest in these therapeutic agents.
  • Public Domain: The patent has expired, making the disclosed information available for public use.

FAQs

What are the primary therapeutic applications of the indole derivatives covered by US Patent 5,545,644?

The primary therapeutic applications are in the treatment of migraine and other cephalic pain conditions due to their 5HT1-receptor agonist and vasoconstrictor activities.

How do the claims of the patent structure the scope of the invention?

The claims are structured to cover the specific chemical compounds, their preparation methods, pharmaceutical compositions containing these compounds, and their medicinal uses.

What is the significance of the patent's expiration?

The expiration of the patent means that the inventions described are now in the public domain, allowing other researchers and companies to use the disclosed information without infringing on the original patent rights.

How can patent analytics tools help in understanding the patent landscape for indole derivatives?

Patent analytics tools help in categorizing patents by claims and scope concepts, making it easier to identify gaps or opportunities in the intellectual property portfolio related to indole derivatives.

Are there international patents similar to US Patent 5,545,644?

Yes, similar patents and applications exist in other jurisdictions such as the European Patent Office (EPO) and the Japan Patent Office (JPO), reflecting a global interest in these therapeutic agents.

Sources

  1. USPTO: Search for patents - USPTO
  2. Google Patents: US7288662B2
  3. SLWIP: Patent Analytics | Intellectual Property Law
  4. Google Patents: US5545644A - Indole derivatives
  5. PubChem: Process for preparing eletriptan hydrobromide having α-form ...

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Drugs Protected by US Patent 5,545,644

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 5,545,644

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 0592438 ⤷  Subscribe C00592438/01 Switzerland ⤷  Subscribe
European Patent Office 0592438 ⤷  Subscribe SPC/GB01/023 United Kingdom ⤷  Subscribe
European Patent Office 0592438 ⤷  Subscribe 02C0013 France ⤷  Subscribe
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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