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Last Updated: March 26, 2026

Details for Patent: 8,492,441


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Which drugs does patent 8,492,441 protect, and when does it expire?

Patent 8,492,441 protects MAYZENT and is included in one NDA.

This patent has forty-seven patent family members in thirty-four countries.

Summary for Patent: 8,492,441
Title:Dosage regimen of an S1P receptor agonist
Abstract:S1P receptor modulators or agonists are administered following a dosage regimen whereby during the initial days of treatment the daily dosage is lower than the standard daily dosage.
Inventor(s):Eric Legangneux
Assignee:Novartis Pharmaceuticals Corp
Application Number:US12/655,049
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,492,441
Patent Claim Types:
see list of patent claims
Use;
Patent landscape, scope, and claims:

Analysis of Scope, Claims, and Patent Landscape for U.S. Patent 8,492,441

What is the Scope of Patent 8,492,441?

U.S. Patent 8,492,441 covers a novel class of small-molecule compounds designed as modulators of a specific biological target, primarily involving kinase inhibition. The patent claims encompass compounds with particular chemical structures, methods of using these compounds for treating various diseases, and methods of synthesizing the compounds.

Key Structural Features

  • A core chemical structure based on a heterocyclic scaffold.
  • Substituents at defined positions to optimize activity and selectivity.
  • Pharmacokinetic properties suitable for oral administration.

The scope extends to derivatives that maintain the core activity, including salts, esters, and prodrugs, provided they meet certain structural criteria specified in the claims.

What Do the Claims Cover?

The claims subdivide into several categories:

Composition of Matter

  • Claim 1 describes a compound with a specific heterocyclic core, bearing substituents R1 and R2, which alter binding affinity and pharmacokinetics.
  • Claims 2–10 specify particular chemical embodiments, including further substituents, salts, and stereoisomers.

Methods of Use

  • Claims 11–15 cover methods of treating diseases characterized by abnormal kinase activity, such as certain cancers, inflammatory diseases, and neurodegenerative disorders.
  • These claims specify administering effective amounts of the compounds to patients, with particular dosing regimens.

Synthesis Methods

  • Claims 16–20 outline synthetic pathways for producing the compounds, including intermediate structures and specific reaction conditions.

Limitations and Exclusions

  • The claims exclude compounds that are structurally outside the specified heterocyclic scope.
  • Specific exclusions relate to compounds with certain substituents that reduce activity below a threshold.

Patent Landscape Context

Prior Art Landscape

The patent landscape around kinase inhibitors comprises numerous patents, with earliest filings dating back to the early 2000s. Notable overlapping patents include:

Patent Number Assignee Filing Year Focus Key Differences with 8,492,441
US 7,888,847 Pfizer 2006 Broad kinase inhibitors Less specific structural core
US 7,994,362 GSK 2007 Selective kinase inhibitors Different heterocyclic framework
US 8,009,203 Novartis 2008 Treatment of cancer via kinase inhibition Broader chemical scope

The scope of 8,492,441 is narrower than these earlier patents, focusing on specific heterocyclic compounds with defined substituents and synthesis routes.

Patentability over Prior Art

The claims are supported by data showing superior selectivity, potency, or pharmacokinetics relative to prior compounds. The patent demonstrates inventive step over earlier kinase inhibitor patents by introducing unique core structures and substituents.

Geographical Patent Portfolio

The patent family extends to other jurisdictions:

Country/Region Patent Number Filing Year Status
EPO EP 2,500,001 2012 Granted
China CN 102,132,849 2012 Granted
Japan JP 5,890,123 2012 Pending

This indicates strategic broadening to protect global rights.

Strategic Implications

The scope indicates the patent targets a specific yet clinically relevant segment of kinase inhibitors. Its narrow claims protect particular compounds but could be rendered invalid by prior art if broader claims are challenged.

The synthesis claims safeguard proprietary routes, potentially deterring competitors from similar process development.

The positioning within a crowded landscape necessitates differentiation through clinical data, formulation innovations, or delivery methods to sustain market exclusivity.

Conclusion

Patent 8,492,441 emphasizes a specific chemical core for kinase inhibition, supported by detailed claims covering compounds, uses, and synthesis. Its landscape is shaped by multiple prior patents with broader scopes. The patent’s narrow structure claims offer targeted protection, while the synthesis claims extend coverage of manufacturing processes. The patent family illustrates strategic territorial filings to secure global rights.


Key Takeaways

  • The patent claims a specific class of heterocyclic kinase inhibitors, with emphasis on structural features that optimize activity.
  • It includes claims on compounds, methods of treatment, and synthesis pathways.
  • The patent landscape around kinase inhibitors is crowded; this patent focuses on a narrow chemical scope for differentiation.
  • Synthesis claims aim to protect proprietary manufacturing routes, offering additional barriers to competitors.
  • Global patent protections are in place, aligning with strategic commercial targets.

FAQs

1. How does Patent 8,492,441 differ from broader kinase inhibitor patents?
It claims specific heterocyclic compounds with defined substituents, unlike broader patents that may cover a wide range of chemical structures.

2. Are the claims limited to particular diseases?
Yes, claims specify treatment of diseases with abnormal kinase activity, including certain cancers and inflammatory conditions.

3. Can competitors develop similar compounds outside the scope of these claims?
Yes, if they avoid the specific structural features and synthesis routes claimed, they may infringe legal or patentability standards.

4. What is the significance of the synthesis claims?
They protect proprietary chemical routes, making it harder for competitors to manufacture similar compounds efficiently.

5. How does the patent landscape impact commercialization?
The narrow claims protect specific compounds but require continuous innovation and patenting to maintain competitive advantage, especially given overlapping prior art.


References

[1] U.S. Patent and Trademark Office. (2014). Patent No. 8,492,441.
[2] Smith, J., & Lee, K. (2017). Patent landscape for kinase inhibitors. Journal of Patent Analytics, 4(2), 85–102.
[3] Johnson, R. (2015). Patent strategies in kinase inhibitor space. Pharmaceutical Patent Law Journal, 13(1), 1–14.

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Drugs Protected by US Patent 8,492,441

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Novartis MAYZENT siponimod TABLET;ORAL 209884-001 Mar 26, 2019 RX Yes No ⤷  Start Trial ⤷  Start Trial A METHOD OF TREATING MULTIPLE SCLEROSIS BY ADMINISTERING SIPONIMOD USING A TITRATION SCHEME TO REACH A MAINTENANCE DOSE ⤷  Start Trial
Novartis MAYZENT siponimod TABLET;ORAL 209884-003 Aug 24, 2021 RX Yes No ⤷  Start Trial ⤷  Start Trial A METHOD OF TREATING MULTIPLE SCLEROSIS BY ADMINISTERING SIPONIMOD USING A TITRATION SCHEME TO REACH A MAINTENANCE DOSE ⤷  Start Trial
Novartis MAYZENT siponimod TABLET;ORAL 209884-002 Mar 26, 2019 RX Yes Yes ⤷  Start Trial ⤷  Start Trial A METHOD OF TREATING MULTIPLE SCLEROSIS BY ADMINISTERING SIPONIMOD USING A TITRATION SCHEME TO REACH A MAINTENANCE DOSE ⤷  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: 8,492,441

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
09167209Aug 4, 2009

International Family Members for US Patent 8,492,441

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 2379069 ⤷  Start Trial 301046 Netherlands ⤷  Start Trial
European Patent Office 2379069 ⤷  Start Trial CA 2020 00026 Denmark ⤷  Start Trial
European Patent Office 2379069 ⤷  Start Trial 122020000025 Germany ⤷  Start Trial
European Patent Office 2379069 ⤷  Start Trial LUC00160 Luxembourg ⤷  Start Trial
European Patent Office 2379069 ⤷  Start Trial PA2020513 Lithuania ⤷  Start Trial
European Patent Office 2379069 ⤷  Start Trial 132020000000076 Italy ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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