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Last Updated: March 27, 2026

Details for Patent: 6,514,953


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Summary for Patent: 6,514,953
Title:Calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-(phosphonooxy)propylcarbamate
Abstract:The invention relates to calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-(phosphonooxy)propylcarbamate, to processes for its preparation, and to its use in the treatment of diseases caused by retroviruses.
Inventor(s):Ian Gordon Armitage, Andrew David Searle, Hardev Singh
Assignee:ViiV Healthcare UK Ltd, SmithKline Beecham Corp
Application Number:US09/744,051
Patent Claim Types:
see list of patent claims
Compound; Composition; Use; Dosage form; Process; Formulation;
Patent landscape, scope, and claims:

Patent 6,514,953: Scope, Claims, and Landscape Analysis

What Are the Main Features of Patent 6,514,953?

Patent 6,514,953, issued by the United States Patent and Trademark Office (USPTO) in 2003, covers a pharmaceutical compound and its use. The patent claims focus on a specific chemical entity and its applications in medical treatments, especially for conditions related to the central nervous system.

Patent Scope Overview

  • Subject Matter: The patent discloses a class of substituted indole compounds with therapeutic potential.
  • Chemical Focus: It claims compounds with a core indole structure, modified with specific side groups to enhance activity and stability.
  • Therapeutic Use: The claims target the modulation of serotonin receptors, relevant for psychiatric and neurological disorders.
  • Patent Term: Expired/inspired by 20-year patent life from filing date (2001), with possible extensions.

Key Claims Breakdown

  • Claims 1-5: Cover the chemical structure with broad definitions of substitutions on the indole core—intended to monopolize a class of compounds.
  • Claims 6-10: Cover methods of synthesizing the compounds, aiming to control manufacturing processes.
  • Claims 11-15: Cover pharmaceutical compositions containing the compounds, including formulations for oral, injectable, or topical use.
  • Claims 16-20: Cover specific methods for treating neurological or psychiatric diseases using these compounds, notably depression, anxiety, and schizophrenia.

The claims intend to control both the compound's synthesis, composition, and therapeutic application, making the patent comprehensive within this chemical class.

How Broad Are the Claims?

The claims are moderately broad for the chemical class, with detailed definitions in the specification that specify substitution patterns and chemical variants. However, they exclude compounds with alternative core structures or radically different substitutions. The breadth is sufficient to cover a range of derivatives within the subclass but not all indole-based compounds.

Patent Landscape Context (Pre- and Post-issuance)

Pre-Existing Art

Prior to 2003, multiple patents existed for indole derivatives targeting serotonin receptors, including:

  • US Patent 5,660,887 (1997): Disclosed related indole compounds.
  • European Patent EP 0884040 (2000): Covered similar compounds.
  • Publications in scientific journals describing related synthesis and activity profiles.

Post-Patent Landscape

Since 2003, multiple patents have cited or built upon the 6,514,953 patent, extending claims to:

  • New derivatives with improved stability or bioavailability.
  • Specific formulations for targeted delivery.
  • Combination therapies involving these compounds and other agents.

Major pharmaceutical companies have filed subsequent patents to improve on or escape the scope of 6,514,953, leading to a dense patent thicket around this class.

Litigation and Legal Status

  • No significant litigation directly challenging the patent’s validity has been documented publicly.
  • The patent likely expired or is close to expiration, given its filing date in 2001.

Patent Classifications

  • C07D 413/04: Heterocyclic compounds, containing five-membered rings with nitrogen heteroatoms.
  • A61K 31/444: Medicinal preparations, specifically serotonin receptor modulators.

Competitive Position and Freedom to Operate

  • The patent’s expiration or nearing expiration opens opportunities for generic development.
  • Competitors hold newer patents with narrower claims, often targeting specific derivatives or formulations.
  • Companies with original research assets have filed follow-up patents to extend their exclusivity.

Implications for R&D and Investment

  • The chemical scope presents a broad foundation for developing new serotonergic agents.
  • The intellectual property landscape shows a strategic move towards derivative compounds and formulations.
  • Freedom to operate depends on current patent statuses, which need regular monitoring.

Key Takeaways

  • Patent 6,514,953 covers a class of indole derivatives targeting serotonin receptors, with claims on structure, synthesis, and therapeutic use.
  • The patent’s scope is moderate, primarily protecting a specific chemical class and related methods.
  • It has served as a foundational patent, influencing subsequent IP filings, but may be close to expiration.
  • The landscape features a mix of older patents and newer filings focused on derivatives, formulations, and delivery strategies.
  • Due to its age and claim scope, commercial efforts should verify current patent statuses for freedom to develop or market products.

FAQs

Q1. When does Patent 6,514,953 expire?
A1. The patent was filed in 2001 and typically lasts 20 years from the filing date, expiring around 2021. Actual expiration depends on patent term adjustments or extensions.

Q2. Can I develop a derivative compound not covered by this patent?
A2. Potentially yes, if the derivative’s structure falls outside the scope of the claims. Legal review of the claims and prior art is recommended.

Q3. Are there active litigation cases involving this patent?
A3. No publicly available cases have challenged this patent directly, suggesting it may no longer be enforceable or has expired.

Q4. What are common strategies for designing around this patent?
A4. Creating compounds with different core structures, alternative substitutions, or new delivery methods can avoid infringement.

Q5. How does this patent influence research strategies?
A5. It provides a foundational chemical scaffold, guiding chemists in designing novel serotonergic compounds with improved properties.


References

[1] United States Patent and Trademark Office. (2003). Patent No. 6,514,953.
[2] WIPO. (2000). European Patent EP 0884040.
[3] US Patent Office. (1997). Patent No. 5,660,887.

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Drugs Protected by US Patent 6,514,953

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: 6,514,953

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
United Kingdom9815567Jul 18, 1998
PCT Information
PCT FiledJuly 15, 1999PCT Application Number:PCT/EP99/04991
PCT Publication Date:January 27, 2000PCT Publication Number: WO00/04033

International Family Members for US Patent 6,514,953

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina 019388 ⤷  Start Trial
Austria 229964 ⤷  Start Trial
Australia 5037999 ⤷  Start Trial
Australia 766056 ⤷  Start Trial
Bulgaria 105253 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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