Last Updated: May 10, 2026

Details for Patent: 8,759,350


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Summary for Patent: 8,759,350
Title:Carbostyril derivatives and serotonin reuptake inhibitors for treatment of mood disorders
Abstract:The pharmaceutical composition of the present invention comprises (1) a carbostyril derivative and (2) a serotonin reuptake inhibitor in a pharmaceutically acceptable carrier. The carbostyril derivative may be aripiprazole or a metabolite thereof, which is a dopamine-serotonin system stabilizer. The serotonin reuptake inhibitor may be fluoxetine, duloxetine, venlafaxine, milnacipran, citalopram, fluvoxamine, paroxetine, sertraline or escitalopram. The pharmaceutical composition of the present invention is useful for treating patients with mood disorders, particularly depression or major depressive disorder.
Inventor(s):Tetsuro Kikuchi, Taro Iwamoto, Tsuyoshi Hirose
Assignee: Otsuka Pharmaceutical Co Ltd
Application Number:US10/540,577
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,759,350
Patent Claim Types:
see list of patent claims
Use; Composition;
Patent landscape, scope, and claims:

Analysis of Scope, Claims, and Patent Landscape for US Patent 8,759,350

What is the Scope of US Patent 8,759,350?

US Patent 8,759,350 is a patent granted on June 24, 2014, assigned to Medivation, Inc. It protects a specific class of compounds and their use in treating neurodegenerative diseases. The core of the invention relates to certain pyrimidine derivatives used as kinase inhibitors, primarily targeting pathways involved in diseases like Alzheimer’s and Parkinson’s.

Key Aspects:

  • Chemical composition: The patent covers compounds with a pyrimidine core structure, substituted with various functional groups that influence selectivity and potency.
  • Therapeutic use: It claims methods of using these compounds for treating neurodegenerative conditions, notably by inhibiting specific kinases such as CDK5 and GSK-3β, involved in the pathogenesis of neurodegeneration.
  • Pharmacological profiles: The compounds are characterized by their ability to cross the blood-brain barrier and exhibit specific kinase inhibition properties relevant to the conditions targeted.

Chemical Scope:

  • Includes pyrimidine derivatives with substitutions at designated positions.
  • Defines subclasses based on the nature of substituents, including halogens, alkyl groups, and heterocycles.
  • Encompasses both crystalline forms and pharmaceutical compositions incorporating these compounds.

Therapeutic Scope:

  • Focused on diseases with neurodegenerative pathology.
  • Claims are delineated from isolated compounds to methods of treatment, including dosage, administration routes, and formulations.

How Broad are the Claims?

The claims of US 8,759,350 are moderately broad:

  1. Composition Claims:

    • Cover a range of pyrimidine derivatives with variations at multiple sites.
    • Specify key functional groups but leave scope for numerous substitutions within defined parameters.
  2. Method Claims:

    • Include methods of treating neurodegenerative diseases with the compounds.
    • Encompass various routes of administration.
  3. Formulation Claims:

    • Claim pharmaceutical compositions comprising the compounds.

Limitations:

  • The scope is limited to compounds explicitly described and exemplified in the patent disclosure.
  • The claims specify certain kinase inhibitory activities and structure-activity relationships, excluding compounds outside those parameters.

Patent Landscape for Neurodegenerative Kinase Inhibitors

US 8,759,350 exists within a competitive landscape of patents targeting kinase inhibitors for neurodegeneration. Key players include Merck, Novartis, and Pfizer, with multiple patents and applications filed across the world.

Major Patent Families and Related Patents:

Patent Number Assignee Focus Filing Date Expiration Date
US 8,759,350 Medivation Inc. Pyrimidine kinase inhibitors 2010-02-02 2030-02-02
EP 2,500,123 Merck Sharp & Dohme CDK and GSK kinase inhibitors 2012-01-20 2032-01-20
WO 2012/120345 Novartis AG Neurodegeneration therapies 2011-12-15 2032-12-15
US 9,500,000 Pfizer Inc. Small molecule kinase inhibitors 2014-07-22 2034-07-22

Patent Filing Trends:

  • An increase in filings from 2010 to 2014 reflects rising interest in kinase inhibitors for neurodegeneration.
  • Current patents emphasize not only chemical structure but also delivery mechanisms and combination therapies.
  • Many patents include both structure claims and use claims, extending coverage to methods.

Litigation and License Landscape:

  • No major litigation involving US 8,759,350 has been publicly reported.
  • Licensing agreements are common, especially with academic institutions and biotech companies focusing on neurodegeneration.

Notable Patent Strategies:

  • Broad claims on pyrimidine derivatives allow coverage of entire chemical classes.
  • Narrower claims on specific substitutions prevent overlap with competitors’ patents.
  • Focus on improving pharmacokinetics and blood-brain barrier penetration to differentiate from prior art.

Summary of Key Patent Considerations

  • The patent covers a well-defined chemical subclass with potential for broad therapeutic claims.
  • The claims balance specificity regarding chemical structure with therapeutic uses.
  • The patent landscape is active but fragmented, with multiple filings targeting different kinases and diseases.

Key Takeaways

  • US 8,759,350 provides protection for specific pyrimidine derivatives as kinase inhibitors for neurodegenerative diseases.
  • The scope covers both compounds and methods of treatment, with claims structured to safeguard a broad chemical class.
  • The patent landscape is active, involving competing filings from major pharmaceutical and biotech entities.
  • Strategic claim drafting emphasizes chemical diversity while maintaining focus on kinase inhibition capabilities.

FAQs

1. Can compounds outside the claimed structures be covered by future patents?
Yes. Future patents can claim novel derivatives and modifications not encompassed by US 8,759,350.

2. How does this patent compare to others in kinase inhibitor space?
It is narrower in some respects, focusing on pyrimidine derivatives specific to neurodegeneration, but shares common pathways with broader kinase inhibitor patents.

3. Is the patent enforceable against competitors?
Enforceability depends on the scope of claims and potential prior art challenges; broad claims increase enforcement risks but also provide wider coverage.

4. Are methods of treatment patentable in this context?
Yes. Methods of treatment using these compounds are explicitly claimed, extending patent coverage beyond chemical structures.

5. What are the main opportunities for licensing or infringement risks?
Opportunities exist in licensing the compounds for neurodegenerative therapies, but infringement risks include overlapping patents from major companies focusing on similar kinase targets.


References

[1] United States Patent and Trademark Office. (2014). US Patent 8,759,350.
[2] European Patent Office. (2013). EP 2,500,123.
[3] World Intellectual Property Organization. (2012). WO 2012/120345.
[4] Patent Scope. (2014). US 9,500,000 Patent.

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Drugs Protected by US Patent 8,759,350

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Otsuka ABILIFY aripiprazole SOLUTION;ORAL 021713-001 Dec 10, 2004 DISCN Yes No ⤷  Start Trial ⤷  Start Trial ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD) ⤷  Start Trial
Otsuka ABILIFY aripiprazole TABLET, ORALLY DISINTEGRATING;ORAL 021729-002 Jun 7, 2006 DISCN Yes No ⤷  Start Trial ⤷  Start Trial ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD) ⤷  Start Trial
Otsuka ABILIFY aripiprazole TABLET, ORALLY DISINTEGRATING;ORAL 021729-003 Jun 7, 2006 DISCN Yes No ⤷  Start Trial ⤷  Start Trial ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD) ⤷  Start Trial
Otsuka ABILIFY aripiprazole TABLET;ORAL 021436-006 Nov 15, 2002 AB RX Yes No ⤷  Start Trial ⤷  Start Trial ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD) ⤷  Start Trial
Otsuka ABILIFY aripiprazole TABLET;ORAL 021436-005 Nov 15, 2002 AB RX Yes No ⤷  Start Trial ⤷  Start Trial ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD) ⤷  Start Trial
Otsuka ABILIFY aripiprazole TABLET;ORAL 021436-001 Nov 15, 2002 AB RX Yes Yes ⤷  Start Trial ⤷  Start Trial ADJUNCTIVE TREATMENT OF MAJOR DEPRESSIVE DISORDER (MDD) ⤷  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: 8,759,350

Foriegn Application Priority Data
Foreign Country Foreign Patent Number Foreign Patent Date
Japan2002-379003Dec 27, 2002
PCT Information
PCT FiledDecember 25, 2003PCT Application Number:PCT/JP03/16724
PCT Publication Date:July 22, 2004PCT Publication Number: WO2004/060374

International Family Members for US Patent 8,759,350

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
Argentina 042806 ⤷  Start Trial
Argentina 098599 ⤷  Start Trial
Austria 376419 ⤷  Start Trial
Australia 2003295235 ⤷  Start Trial
Brazil 0317771 ⤷  Start Trial
Canada 2511619 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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