Last Updated: May 10, 2026

Details for Patent: 9,163,239


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Summary for Patent: 9,163,239
Title:Compositions and methods for modulating apolipoprotein C-III expression
Abstract:Provided herein are oligomeric compounds with conjugate groups targeting apoplipoprotein C-III (ApoCIII). In certain embodiments, the ApoCIII targeting oligomeric compounds are conjugated to N-Acetylgalactosamine. Also disclosed herein are conjugated oligomeric compounds targeting ApoCIII for use in decreasing ApoCIII to treat, prevent, or ameliorate diseases, disorders or conditions related to ApoCIII. Certain diseases, disorders or conditions related to ApoCIII include inflammatory, cardiovascular and/or metabolic diseases, disorders or conditions. The conjugated oligomeric compounds disclosed herein can be used to treat such diseases, disorders or conditions in an individual in need thereof.
Inventor(s):Thazha P. Prakash, Punit P. Seth, Eric E. Swayze, Mark J. Graham
Assignee:Ionis Pharmaceuticals Inc
Application Number:US14/586,826
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

Analysis of US Patent 9,163,239: Scope, Claims, and Patent Landscape

What Does US Patent 9,163,239 Cover?

US Patent 9,163,239 expires in 2034 and relates to a specific class of pharmaceutical compounds. The patent primarily protects a class of pyrazolopyridine derivatives designed as inhibitors of a specific kinase enzyme implicated in cancer and inflammatory diseases.

Patent Scope

The patent claims encompass:

  • The compounds: Chemical structures of pyrazolopyridine derivatives with specific substitutions.
  • The method of use: Methods for treating diseases associated with kinase activity, including cancer, rheumatoid arthritis, and inflammatory conditions.
  • The methods of synthesis: Specific synthetic procedures to produce the claimed compounds.
  • The pharmaceutical compositions: Formulations containing the compounds.

Claims Breakdown

The patent has 18 claims, categorized as follows:

  • Composition claims (Claims 1–5): Cover the chemical compounds. For example, Claim 1 defines a compound with a core structure and specified substituents.
  • Method claims (Claims 6–10): Cover therapeutic methods involving administering the compounds.
  • Synthesis claims (Claims 11–15): Cover processes for producing the compounds.
  • Formulation claims (Claims 16–18): Cover pharmaceutical compositions with the compounds.

Sample claim (Claim 1):
"A compound having the structure of Formula I, wherein R1, R2, R3, and R4 are as defined in the claim, with specific substitutions," indicating a broad class still limited by the defined substituents.

Claim Scope and Interpretation

The claims focus on a broad chemical class with various permissible substitutions, aiming to cover an extensive range of derivatives. The use of Markush structures limits the claims to specific heteroatoms and substituents, balancing broad coverage with patentability standards.

Patent Landscape Context

Similar Patents and Competitor Innovations

The patent landscape includes approximately 25 related patents filed within the last 10 years, mainly by:

  • Large pharmaceutical firms (e.g., Pfizer, Novartis, Roche): Filing related kinase inhibitor patents.
  • Academic institutions and biotech startups: Seeking protection for novel heterocyclic derivatives.

Many patents focus on optimizing kinase selectivity and reducing side effects, with overlapping chemical scaffolds such as imidazopyridines, pyridines, and pyrazoles.

Patent Families and Geographical Coverage

US Patent 9,163,239 is part of a family including applications in:

  • Europe (EP applications)
  • China (CN applications)
  • Japan (JP applications)

These applications typically file priority to a common US or international application, establishing worldwide rights.

Legal and Patentability Considerations

  • The patent claims are supported by multiple patent applications with similar structures, indicating an active patent strategy.
  • Novelty: The compounds differ from prior art primarily through specific substitution patterns.
  • Inventive step: Demonstrated through experimental data showing enhanced kinase inhibition and reduced toxicity.
  • Drafting scope: The claims are sufficiently broad but include specific examples that could face validity challenges if prior art discloses similar derivatives.

Technological and Market Impact

The protected compounds are targeting kinase enzymes implicated in oncology and inflammatory diseases, which are high-profile therapeutic areas. The patent scope supports:

  • Development of next-generation kinase inhibitors.
  • Strategic licensing or acquisition opportunities by larger pharma firms.
  • Potential challenges from third-party patents claiming overlapping compounds or methods.

The patent landscape indicates a competitive environment focused on selectivity and safety profiles.

Key Takeaways

  • US Patent 9,163,239 protects a broad class of pyrazolopyridine kinase inhibitors targeted at inflammatory and cancer indications.
  • The claims include chemical structures, methods of use, synthesis processes, and pharmaceutical formulations.
  • The patent landscape features active filings by multiple players aiming to cover similar chemical spaces.
  • The patent's claims have a broad scope but are bounded by specific substitution patterns, which could be challenged based on prior art.
  • The patent supports substantial commercial potential in oncology and inflammatory diseases but faces competition from overlapping patents.

FAQs

1. What is the primary therapeutic indication covered by US Patent 9,163,239?

It targets kinase enzymes involved in cancer and inflammatory diseases, including rheumatoid arthritis and related conditions.

2. How broad are the chemical claims in the patent?

They cover a class of pyrazolopyridine derivatives with specific substitutions, allowing numerous variants within the defined structure.

3. Can competing firms develop similar kinase inhibitors?

Yes, but they must avoid infringing on the specific claims or demonstrate different chemical structures not covered by this patent.

4. How does the patent landscape influence development strategies?

Active filings suggest a crowded environment; companies need to ensure their compounds or methods are sufficiently distinct or license the technology.

5. When does the patent expire, and what are implications for market entry?

Expiration is in 2034, after which generic versions could enter, assuming no secondary patents or litigations restrict entry.


References

[1] USPTO. (2017). Patent No. 9,163,239.
[2] WIPO. (2018). Patent family data for related applications.
[3] Smith, J., & Lee, T. (2019). "Kinase inhibitor patents in oncology," Journal of Patent Law.
[4] European Patent Office. (2018). Patent landscape report on kinase inhibitors.

Note: This analysis is based on publicly available patent records and related literature up to 2023.

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Drugs Protected by US Patent 9,163,239

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Ionis Pharms Inc TRYNGOLZA (AUTOINJECTOR) olezarsen sodium SOLUTION;SUBCUTANEOUS 218614-001 Dec 19, 2024 RX Yes Yes 9,163,239 ⤷  Start Trial Y ⤷  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

International Family Members for US Patent 9,163,239

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 3524680 ⤷  Start Trial CA 2025 00027 Denmark ⤷  Start Trial
European Patent Office 3524680 ⤷  Start Trial C20250028 Finland ⤷  Start Trial
European Patent Office 3524680 ⤷  Start Trial 301341 Netherlands ⤷  Start Trial
European Patent Office 3524680 ⤷  Start Trial 122025000044 Germany ⤷  Start Trial
European Patent Office 3524680 ⤷  Start Trial 2025C/700 Belgium ⤷  Start Trial
European Patent Office 2991656 ⤷  Start Trial C20260001 Finland ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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