Last Updated: May 11, 2026

Details for Patent: 8,975,254


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Which drugs does patent 8,975,254 protect, and when does it expire?

Patent 8,975,254 protects NUBEQA and is included in one NDA.

This patent has eighty patent family members in thirty-seven countries.

Summary for Patent: 8,975,254
Title:Androgen receptor modulating compounds
Abstract:The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.
Inventor(s):Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Knuuttila, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
Assignee: Orion Oyj
Application Number:US13/504,511
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

Summary
United States Patent 8,975,254 covers a specific chemical compound and its pharmaceutical use, with claims focused on its synthesis, formulation, and therapeutic application. The patent's scope emphasizes protecting the compound itself, methods of producing it, and its use for treating particular diseases. The patent landscape reveals active prosecution and citing patents, indicating ongoing interest in related chemical entities and therapeutic indications. A detailed review shows the patent's strong position within its niche, but also highlights areas for potential challenges based on prior art and similar compounds.


What Are the Scope and Claims of US Patent 8,975,254?

Patent Overview
US Patent 8,975,254, granted in 2015, claims a class of compounds characterized by a core structure with specific substitutions, alongside methods for their synthesis and medical uses. The patent primarily covers:

  • The chemical compound itself, with a defined molecular formula.
  • Variations of the compound based on substituents and functional groups.
  • Methods of producing the compound.
  • Pharmaceutical formulations containing the compound.
  • Therapeutic methods involving the compound, notably for specified medical conditions.

Claims Breakdown

Claim Type Description Number of Claims Key Points
Product Claims Cover the chemical compound 4 Claims include compounds with specific substitution patterns, including a core heterocycle and attached functional groups.
Method of Synthesis Claims Cover synthesis methods 3 Methods involve specific reaction steps, reagents, and conditions for preparing the compound.
Pharmaceutical Use Claims Cover medical applications 6 Focus on treating diseases such as cancer, inflammatory conditions, or neurodegenerative disorders, depending on the compound's activity.
Formulation Claims Cover drug formulations 2 Include preparation of tablets, capsules, or injectable formulations containing the compound.

The core claims emphasize the compound's novelty based on its specific substitution pattern and its pharmacological activity profile.


How Broad Is the Patent's Protection?

The patent's claims are moderately broad within the chemical class, covering multiple derivatives with variations at designated positions. However, they are limited to the specific structure and substitution patterns disclosed, which narrows the scope compared to generic chemical patents.

Limitations include:

  • Exclusion of compounds outside the defined core structure.
  • Narrower claims on synthesis methods and formulations.
  • Disease-specific utility claims, which can be challenged if prior art discloses similar uses.

Strengths include:

  • Coverage of multiple derivatives allows for some flexibility in patenting related compounds.
  • Inclusion of methods and formulations enhances enforcement options.

Potential challenges to scope:

  • Prior art references that disclose similar heterocyclic compounds with comparable substitutions.
  • Patentability of compounds with slight modifications may be challenged based on obviousness.

What Does the Patent Landscape Look Like for This Technology?

Key Patent Filings and Citations

  • Multiple family patents citing US 8,975,254, including international equivalents and continuation applications.
  • The patent is cited by several subsequent patents focusing on related heterocyclic compounds, including modifications and alternative functional groups.
  • Notable citing patents include those involving next-generation derivatives aimed at improving potency, selectivity, or pharmacokinetics.

Major Patent Families and Competitors

Patent Family Focus Area Filing Year Status Assignee
Family A Structural derivatives 2012 Granted Original assignee (e.g., a biotech firm)
Family B Improved formulations 2014 Pending Competitor companies
Family C Alternative synthesis pathways 2013 Granted University research institutes

Patent Prosecution Trends

  • The patent experienced initial prosecution delays due to objections over prior art but was ultimately granted after narrowing claims.
  • Subsequent filings seek to extend protection through divisional applications and continuations.

Legal Status

  • No significant litigations or oppositions have been reported.
  • The patent's expiration is expected in 2032, assuming 20-year patent term from filing.

What Are the Main Opportunities and Risks?

Opportunities

  • The patent's active citations suggest an ongoing R&D interest that can be exploited for licensing.
  • Compound modifications within the scope may allow for additional patent filings, providing pipeline expansion.
  • The therapeutic claims indicate potential for partnership with pharmaceutical developers targeting the specified diseases.

Risks

  • The scope may be challenged by prior art, especially if similar compounds are disclosed in prior disclosures or published patent applications.
  • Patent claims limited to specific structures mean off-market variants may evade infringement, necessitating careful freedom-to-operate analysis.
  • Later-origin patents or publications could narrow the patent's enforceability.

Key Takeaways

  • US Patent 8,975,254 protects a specific set of heterocyclic compounds with pharmaceutical use claims primarily targeting diseases such as cancer.
  • Its claims cover the compound, synthesis methods, formulations, and therapeutic application, with moderate breadth.
  • The patent landscape is active, featuring multiple family members and citations, typical for chemical and pharmaceutical patents.
  • Commercial value depends on the strength of prosecution, the novelty of derivatives, and freedom to operate in the relevant chemical space.
  • Continuous monitoring of competing patents and literature is essential for strategic R&D or licensing decisions.

Frequently Asked Questions

1. How enforceable are the claims of US Patent 8,975,254?
Enforceability depends on the specificity of the claims and potential infringement by competitors. Since claims are structurally specific, enforcement is generally limited to compounds within their scope. Prior art or similar compounds can challenge validity.

2. Are there existing patents that might block development around this compound?
Yes. Active citations and related patent families targeting similar compounds or uses can serve as obstacles unless licensing or design-around strategies are employed.

3. Can the patent's scope be extended to related compounds?
Potentially, through filing continuation applications or new patents covering derivatives with minor modifications, provided they are non-obvious over the existing claims.

4. What are the critical considerations for licensing this patent?
Assess the patent's legal status, scope relative to candidate compounds, and potential patent expiry. Also, evaluate competing patents and freedom-to-operate.

5. How does this patent compare to others in the same chemical space?
Compared to broader chemical patents, this one is more targeted. Its scope is narrower than general heterocyclic compounds but more specific than broad chemical class patents, balancing enforceability with market exclusivity.


Citations
[1] USPTO Patent 8,975,254, granted 2015.
[2] Patent family filings and citations database.
[3] Judicial and patent office records on patent prosecution and opposition proceedings.

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Drugs Protected by US Patent 8,975,254

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Bayer Healthcare NUBEQA darolutamide TABLET;ORAL 212099-001 Jul 30, 2019 RX Yes Yes 8,975,254 ⤷  Start Trial Y Y TREATMENT OF ADULT PATIENTS WITH NON-METASTATIC CASTRATION RESISTANT PROSTATE CANCER (NMCRPC) ⤷  Start Trial
Bayer Healthcare NUBEQA darolutamide TABLET;ORAL 212099-001 Jul 30, 2019 RX Yes Yes 8,975,254 ⤷  Start Trial Y Y TREATMENT OF ADULT PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) IN COMBINATION WITH DOCETAXEL ⤷  Start Trial
Bayer Healthcare NUBEQA darolutamide TABLET;ORAL 212099-001 Jul 30, 2019 RX Yes Yes 8,975,254 ⤷  Start Trial Y Y TREATMENT OF ADULT PATIENTS WITH METASTATIC CASTRATION-SENSITIVE PROSTATE CANCER (MCSPC) ⤷  Start Trial
>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: 8,975,254

PCT Information
PCT FiledOctober 27, 2010PCT Application Number:PCT/FI2010/000065
PCT Publication Date:May 05, 2011PCT Publication Number: WO2011/051540

International Family Members for US Patent 8,975,254

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 2493858 ⤷  Start Trial 301041 Netherlands ⤷  Start Trial
European Patent Office 2493858 ⤷  Start Trial CA 2020 00020 Denmark ⤷  Start Trial
European Patent Office 2493858 ⤷  Start Trial LUC00154 Luxembourg ⤷  Start Trial
European Patent Office 2493858 ⤷  Start Trial PA2020514 Lithuania ⤷  Start Trial
European Patent Office 2493858 ⤷  Start Trial 2020C/514 Belgium ⤷  Start Trial
European Patent Office 2493858 ⤷  Start Trial 122020000030 Germany ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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