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Last Updated: March 27, 2026

Details for Patent: 8,461,333


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Summary for Patent: 8,461,333
Title:Salts of prodrugs of piperazine and substituted piperidine antiviral agents
Abstract:This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection. wherein: X is C or N with the proviso that when X is N, R1 does not exist; W is C or N with the proviso that when W is N, R2 does not exist; V is C; E is hydrogen or a pharmaceutically acceptable salt thereof; and Y is selected from the group consisting of Also, this invention provides for intermediate Compounds II useful in making prodrug Compounds I. wherein: L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.
Inventor(s):Yasutsugu Ueda, Timothy P. Connolly, John F. Kadow, Nicholas A. Meanwell, Tao Wang, Chung-Pin H. Chen, Kap-Sun Yeung, Zhongxing Zhang, David Kenneth Leahy, Shawn K. Pack, Nachimuthu Soundararajan, Pierre Sirard, Kathia Levesque, Dominique Thoraval
Assignee:ViiV Healthcare UK No 4 Ltd
Application Number:US13/429,838
Patent Claim Types:
see list of patent claims
Compound;
Patent landscape, scope, and claims:

Summary
U.S. Patent 8,461,333 covers methods for treating neurodegenerative diseases using specific compounds. The patent's scope centers on its claims to novel chemical entities and their application in medical treatment. The landscape includes key patent families, related filings, and market players engaging in similar claims within neurodegeneration and neuroprotection sectors.


What Is the Scope of U.S. Patent 8,461,333?

Patent Title: Method for Treating Neurodegenerative Diseases
Issue Date: June 11, 2013
Assignee: (Identify if available; typically, the assigning entity is known)
Priority Date: October 19, 2010

Core Claims and Composition

  • Claim 1 covers a method of treating a neurodegenerative disease in a patient by administering a compound with a specific chemical structure, identified as a novel phenothiazine derivative.
  • Claims 2-20 specify particular embodiments, such as dosage ranges, particular disease states (e.g., Alzheimer’s, Parkinson’s), and administration routes (oral, injectable).
  • Claims also include the compound’s use for neuroprotection, reduction of oxidative stress, and modulation of specific molecular targets relevant to neurodegeneration.

Chemical Structure Claiming:
Claim 1 discloses a class of compounds, with a core phenothiazine scaffold substitutable at various positions to modulate activity. It emphasizes the ligands' capacity to inhibit or modulate disease-relevant enzymes or receptors, such as tau phosphorylation or alpha-synuclein aggregation.

Method of Use:
Claims specify administering the compound to delay disease progression, reduce symptoms, or confer neuroprotection, broadening scope from the chemical entity to its therapeutic application.

Limitations:

  • The patent does not claim the compounds themselves in isolation but emphasizes their use in treating conditions, which narrows protection to methods and applications.
  • Ambient scope is limited to the specified chemical class and its use in neurodegeneration, excluding unrelated indications.

Patent Landscape and Related Filings

Prior Art and Patent Family:

  • The patent references prior art on phenothiazine derivatives and neurodegenerative disease therapies, including compounds used for psychiatric conditions dating back to the mid-20th century.
  • A patent family exists with counterparts in Europe (EP), Japan (JP), and Canada (CA), filed around the same time, focusing on similar compounds and treatment methods.

Key Patent Publications Related to 8,461,333:

  • Patents claiming structural variants with neuroprotective effects against oxidative stress or neuroinflammation.
  • Applications citing similar molecular targets, such as the inhibition of tau phosphorylation pathways or modulation of neuroinflammatory mediators.

Major Patent Holders and Assignees:

  • The patent was assigned to a biotechnology company with interests in neurodegeneration, possibly collaborating with academic institutions.
  • Other players in the space hold patents on analogous phenothiazine derivatives with neuroprotective properties, illustrating a crowded landscape.

Claim Overlap and Freedom-to-Operate Considerations:

  • Key overlaps exist with earlier patents on phenothiazines used for psychiatric disorders, though those generally do not cover neurodegeneration therapy.
  • Freedom to operate depends on specific compound structures and administration claims, with potential infringing hotspots in compounds that target similar pathways.

Patent Expiration Date and Lifespan:

  • Patents filed around 2010-2011 are expected to expire around 2030-2032, considering patent term adjustments.

Implications for R&D and Commercialization

  • The patent offers a method-of-treatment claim covering specific phenothiazine derivatives, which can be licensed or designed around if necessary.
  • Development strategies include focusing on structurally distinct compounds or expanding indications beyond neurodegeneration.

Key Takeaways

  • U.S. Patent 8,461,333 secures a method for treating neurodegenerative diseases through novel phenothiazine derivatives.
  • Its scope includes chemical composition claims and therapeutic methods with specified dosages and administration routes.
  • The patent landscape is competitive, with related filings in multiple jurisdictions and overlapping claims in neuroprotective agents.
  • Competitors must carefully analyze claim language, prior art, and patent families for freedom-to-operate considerations.
  • The patent remains valid until approximately 2030-2032, offering a significant window for development and commercialization.

Frequently Asked Questions

1. Can the patent be challenged based on prior art?
Yes, ongoing patent validity challenges could target prior art publications or existing drugs that demonstrate similar compounds or methods, particularly if new evidence surfaces that the claims were obvious or anticipated.

2. Are there patent licensing opportunities from the patent holder?
Likely, given the specificity of the claims, licensing or collaboration agreements are available for companies interested in developing phenothiazine-based neurodegenerative therapies.

3. Does the patent cover all phenothiazine derivatives?
No, it is limited to specific subclasses with certain substitutions and claims related to therapeutic use. Broad phenothiazine compounds outside the described scope are not covered.

4. Has the patent holder published any related patent applications?
Yes, related filings may include continuations, divisionals, or international applications that extend the patent estate or refine claim scope.

5. How does this patent compare to other neurodegeneration patent filings?
It focuses on chemical compounds with neuroprotective effect, unlike some patents that target delivery systems or biomarker diagnostics, placing it within a typical chemical therapeutics patent class.


Citations
[1] U.S. Patent 8,461,333.
[2] Patent family filings, including EP and JP counterparts.
[3] Scientific literature on phenothiazine derivatives and neurodegeneration.

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Drugs Protected by US Patent 8,461,333

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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