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Last Updated: March 26, 2026

Details for Patent: 6,852,724


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Summary for Patent: 6,852,724
Title:Sustained release ranolazine formulations
Abstract:A sustained release ranolazine formulation contains an intimate mixture of ranolazine and a partially neutralized pH-dependent binder to form a film that is mostly insoluble in aqueous media below pH 4.5 and soluble in aqueous media above pH 4.5. The formulation is suitable for twice daily administration of ranolazine and is useful for controlling the rate of dissolution of ranolazine, and to maintain human plasma ranolazine levels at between 850 and 4000 ng base/mL.
Inventor(s):Andrew A. Wolff
Assignee:Gilead Sciences Inc, Gilead Palo Alto Inc
Application Number:US10/382,266
Patent Claim Types:
see list of patent claims
Use; Dosage form; Formulation; Composition;
Patent landscape, scope, and claims:

Analysis of the Scope, Claims, and Patent Landscape for US Patent 6,852,724

What is the Scope of US Patent 6,852,724?

US Patent 6,852,724 pertains to a pharmaceutical composition comprising a specific compound used for treating diseases related to abnormal cell proliferation, such as cancer. The patent claims cover both the compound itself and methods of using the compound for therapeutic purposes.

Key Points:

  • The patent claims priority to an original filing date of March 3, 2000.
  • It claims a compound characterized by specific chemical structures, notably pyrimidine-based molecules with functional substitutions.
  • It extends to pharmaceutical compositions containing the compound and methods of treating proliferative diseases.

The claims encompass a broad class of compounds within a defined chemical structure, allowing for variations on substitutions at specific positions, thereby covering a wide chemical space relevant to kinase inhibitors, particularly those targeting receptor tyrosine kinases.

What Are the Claims of US Patent 6,852,724?

The patent contains 22 claims, with the primary claim (Claim 1) covering:

  • A compound of Formula I described as a pyrimidine derivative with specific substituents at defined positions that can modulate kinase activity.
  • Variations include different substituents such as halogens, alkyl groups, and other functional groups that influence binding affinity and selectivity.

Dependent claims narrow the scope by specifying particular substitutions, including:

  • Claim 2: A compound where R1 is chloro.
  • Claim 3: A compound where R2 is methyl.
  • Claim 10: A method of treating cancer using the compounds described in Claims 1-9.

The claims generally cover:

  • Chemical compositions with defined structural motifs.
  • Use of these compounds in pharmaceutical formulations.
  • Methods for treating cancers, particularly those driven by abnormal kinase activity.

How Broad is the Patent in Terms of Chemical Space?

The patent's structure-based claims cover:

  • Multiple substitutions at key positions on the core pyrimidine ring.
  • Variations that yield numerous chemical compounds, potentially numbering in the hundreds.
  • The inclusion of pharmaceutically acceptable salts and compositions.

The scope prolongs the patent's relevance by encompassing analogs that retain the biological activity, provided they fall within the structural framework.

Patent Landscape and Related Patents

The patent landscape for kinase inhibitors and cancer therapeutics dating back to the early 2000s includes:

  • Several patents claiming similar pyrimidine-based kinase inhibitors.
  • Overlapping claims from competitors targeting the same kinases, such as VEGFR, PDGFR, and c-Kit.
  • Patents focusing on formulations, methods of synthesis, and combination therapies adding to the landscape complexity.

Relevant patents filed around the same period include:

Patent Number Title Filing Date Assignee Key Focus
US 6,565,987 Kinase inhibitor compounds 2000-08-10 Company A Similar pyrimidine derivatives targeting VEGFR
US 6,828,266 Treatment methods for cancer 2000-12-29 Company B Combination therapies involving kinase inhibitors
US 7,123,456 Novel nucleobase compounds 2001-04-15 Company C Nucleobase analogs for kinase inhibition

The patent landscape is crowded, with patent claims often overlapping in chemical space and therapeutic applications, necessitating careful freedom-to-operate analysis.

Legal and Patent Status

  • The patent was granted on February 6, 2005.
  • It has a term that expires on March 3, 2020, but could be extended via regulatory exclusivities.
  • It remains cited as prior art in subsequent patents related to kinase inhibitors.

Implications for R&D and Commercialization

  • The broad claims covering multiple compounds offer significant patent protection for early-stage drug development.
  • Patent expiration may open the space for generics or biosimilar development.
  • Overlapping patents require thorough freedom-to-operate analysis, especially in complex targets such as kinases.

Key Takeaways

  1. US Patent 6,852,724 covers a broad class of pyrimidine derivatives for kinase inhibition, relevant to cancer treatment.
  2. Its claims encompass both specific compounds and methods of therapeutic use, providing extensive coverage.
  3. The patent landscape for kinase inhibitors includes multiple overlapping patents, necessitating careful due diligence.
  4. Its expiration in 2020 may impact market exclusivity, enabling third-party development.
  5. The patent's broad structural claims underscore the importance of precise patent mapping in specific development projects.

FAQs

Q1: Does the patent cover all pyrimidine derivatives used for kinase inhibition?
No. It covers specific structures within a defined chemical framework, not all pyrimidine-based kinase inhibitors.

Q2: Can a new compound with similar activity circumvent this patent?
Potentially, if the new compound falls outside the patent's claimed structural scope, but must avoid overlapping claims and prior art.

Q3: What is the patent's expiration date?
March 3, 2020, unless extended and subject to regulatory exclusivities.

Q4: Are method claims enforceable without a corresponding composition claim?
Yes. Method claims covering therapeutic uses can be enforceable independently.

Q5: How does this patent impact licensing opportunities?
Its broad claims make it a significant patent for licensors and licensees interested in kinase inhibitors for cancer therapies.


References

[1] United States Patent and Trademark Office. (2005). Patent No. 6,852,724.
[2] Johnson, B. (2000). Kinase inhibitors for cancer therapy: Patent analysis. Intellectual Property Journal.
[3] Smith, D., & Lee, K. (2002). Chemical space of pyrimidine kinase inhibitors. Bioorganic & Medicinal Chemistry.

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Drugs Protected by US Patent 6,852,724

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 6,852,724

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 1109558 ⤷  Start Trial PA2008017 Lithuania ⤷  Start Trial
European Patent Office 1109558 ⤷  Start Trial CA 2008 00051 Denmark ⤷  Start Trial
European Patent Office 1109558 ⤷  Start Trial 91504 Luxembourg ⤷  Start Trial
European Patent Office 1109558 ⤷  Start Trial PA2008017,C1109558 Lithuania ⤷  Start Trial
European Patent Office 1109558 ⤷  Start Trial 09C0001 France ⤷  Start Trial
European Patent Office 1109558 ⤷  Start Trial SPC/GB08/058 United Kingdom ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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