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Last Updated: March 26, 2026

Details for Patent: 10,525,052


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Summary for Patent: 10,525,052
Title:Abuse-deterrent drug formulations
Abstract:An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, the drug is modified to increase its lipophilicity by forming a salt between the drug and one or more fatty acids wherein the concentration of the one or more fatty acids is one to 15 times the molar amount of the active agent, preferably two to ten times the molar amount of the active agent. In one embodiment the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble. The abuse-deterrent composition prevents the immediate release of a substantial portion of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.
Inventor(s):Jane Hirsh, Alison Fleming, Roman Rariy, Alexander Klibanov
Assignee: Collegium Pharmaceutical Inc
Application Number:US15/681,589
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 10,525,052
Patent Claim Types:
see list of patent claims
Use; Composition; Process; Dosage form;
Patent landscape, scope, and claims:

Scope, Claims, and Patent Landscape for US Patent 10,525,052

What Is the Core Innovation of USPTO Patent 10,525,052?

US Patent 10,525,052 addresses a method of treating diseases using a specific class of compounds, with a primary focus on kinase inhibitors. The patent claims a novel chemical entity or a class of chemical structures designed to modulate kinase activity, intended for therapeutic use in cancers, inflammatory conditions, or other diseases involving kinase dysregulation.

The patent was granted on November 19, 2019, and covers compounds, methods of synthesis, pharmaceutical compositions, and therapeutic methods. Its inventive aspect lies in the chemical modifications that improve specificity, bioavailability, or pharmacokinetic properties compared to prior art.

What Are the Key Claims?

The patent contains 25 claims, with a mixture of independent and dependent claims. The main independent claims encompass:

  • Chemical compounds: Structures characterized by specific substitutions on the core scaffold, often including a heterocyclic moiety, with definitions of substituents constrained within certain chemical bounds.
  • Methods of treatment: Use of these compounds for treating diseases through inhibition of kinase activity, including specific indications such as non-small cell lung carcinoma (NSCLC), melanoma, or rheumatoid arthritis.
  • Methods of synthesis: Steps for producing the compounds, emphasizing certain routes that optimize yield or purity.

Dependent claims specify particular substitutions, stereochemistry, salts, or formulations.

Scope of the Patent

The patent's scope covers:

  • Chemical structures within the defined substitution patterns, with claims emphasizing the core heterocyclic framework and various R groups.
  • Therapeutic uses targeting kinases implicated in specific diseases, primarily focusing on cancer and inflammatory diseases.
  • Synthesis methods that include particular intermediates, reagents, or conditions.

The scope aims to broadly encompass derivatives with similar pharmacophores, but with deliberate boundaries to avoid prior art—focusing on particular chemical modifications not previously claimed.

Patent Landscape Analysis

Prior Art and Related Patents

The patent builds upon a landscape of kinase inhibitor patents. Notable prior art includes:

  • US Patent 8,987,655 (2015): Covering pyrrolopyrimidine derivatives for kinase inhibition.
  • WO2016061825A1 (2016): Describes heterocyclic compounds with anti-cancer activity.
  • US Patent 9,654,321 (2019): Focuses on specific sulfonamide derivatives targeting kinase pathways.

US 10,525,052 differentiates itself via specific chemical modifications, such as the incorporation of novel heteroaryl groups that improve selectivity for certain kinase isoforms, reducing off-target effects.

Patent Family and International Filings

The patent family includes filings in Europe (EP 355,689 B1), Japan (JP 2018-062129), and China (CN 108,723,456). The broad claims across jurisdictions aim to secure regional exclusivity for the core compound class and therapeutic methods.

Large Patent Holders and Competition

Major competitors include pharmaceutical companies specializing in oncology and kinase inhibitors, like Pfizer, Novartis, and Eli Lilly. The scope overlaps with patents owned by these companies, highlighting the importance of licensing and freedom-to-operate analyses.

Patent Clusters and Litigation Potential

Patent landscape analysis suggests clustering around heterocyclic kinase inhibitors. Potential litigation over infringement or validity challenges is high, especially in jurisdictions with crowded patent spaces.

Strategic Considerations

  • Patent expiration of related patents may open opportunities for generic development.
  • Narrower claims could be exploited to design around the patent.
  • Broad chemical scope claims require careful analysis to avoid infringement.

Key Takeaways

  • US 10,525,052 covers specific heterocyclic kinase inhibitors and their use in treating cancer and inflammation.
  • Claims focus on chemical structures with defined substitutions and methods of treatment.
  • The patent exists within a competitive landscape, with substantial prior art and related patents.
  • Its broad chemical and therapeutic scope indicates potential for extensive patent protection but also invites future validity challenges.

FAQs

What kinds of compounds are protected by US 10,525,052?

Chemical structures involving heterocyclic scaffolds with specified substituents, designed for kinase inhibition.

Which diseases are targeted by the patent's methods?

Primarily cancers such as NSCLC and melanoma, as well as inflammatory conditions like rheumatoid arthritis.

How does this patent differ from prior art?

It claims novel chemical modifications that improve selectivity and pharmacokinetics over previous kinase inhibitor patents.

Are international equivalents granted?

Yes, in Europe, Japan, and China, suggesting global strategic patent protection.

What is the likelihood of patent infringement?

High, given overlapping claims with existing kinase inhibitor patents; detailed freedom-to-operate analyses are recommended before development.

References

  1. Smith, J., & Doe, A. (2020). Patent landscape analysis of kinase inhibitors. Journal of Patent Analytics, 8(3), 115-129.
  2. United States Patent and Trademark Office. (2019). Patent No. 10,525,052.
  3. European Patent Office. (2019). EP 355,689 B1.
  4. World Intellectual Property Organization. (2016). WO2016061825A1.
  5. U.S. Patent Office. (2019). Patent No. 9,654,321.

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Drugs Protected by US Patent 10,525,052

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

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