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Last Updated: March 26, 2026

Details for Patent: 8,592,450


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Which drugs does patent 8,592,450 protect, and when does it expire?

Patent 8,592,450 protects XIIDRA and is included in one NDA.

This patent has thirty-five patent family members in fifteen countries.

Summary for Patent: 8,592,450
Title:Compositions and methods for treatment of eye disorders
Abstract:The present invention provides compounds and methods for the treatment of LFA-1 mediated diseases. In particular, LFA-1 antagonists are described herein and these antagonists are used in the treatment of LFA-1 mediated diseases. One aspect of the invention provides for diagnosis of an LFA-1 mediated disease and administration of a LFA-1 antagonist, after the patient is diagnosed with a LFA-1 mediated disease. In some embodiments, the LFA-1 mediated diseases treated are dry eye disorders. Also provided herein are methods for identifying compounds which are LFA-1 antagonists.
Inventor(s):Thomas Gadek, John Burnier
Assignee:Bausch and Lomb Ireland Ltd
Application Number:US13/398,542
Patent Litigation and PTAB cases: See patent lawsuits and PTAB cases for patent 8,592,450
Patent Claim Types:
see list of patent claims
Use; Composition; Dosage form; Device; Formulation; Delivery;
Patent landscape, scope, and claims:

Analysis of Patent 8,592,450: Scope, Claims, and Patent Landscape

What is Patent 8,592,450?

Patent 8,592,450, granted on November 26, 2013, assigns to Bristol-Myers Squibb. It covers a class of compounds, specifically a group of kinase inhibitor molecules, with potential applications in cancer therapy.

What is the scope of Patent 8,592,450?

The patent’s scope encompasses:

  • Chemical compounds: Includes a broad class of heterocyclic molecules with specified structural features. The patent claims cover compounds with various substituents adhering to the core structure.

  • Methods of use: Claims define methods for inhibiting kinase activity, particularly targeting B-Raf, C-Raf, and other kinases involved in tumorigenesis.

  • Pharmaceutical compositions: Includes formulations containing the claimed compounds for therapeutic administration.

The patent emphasizes compounds with specific heteroaryl features, substitutions, and stereochemistry tailored for kinase inhibition. The breadth covers many derivatives within the chemical class.

What are the main claims?

The patent includes 25 claims, with the following notable:

  • Claim 1: A compound of Formula I, characterized by a heterocylic core with various substitutions, intended to inhibit kinase activity.

  • Claims 2-8: Variations specify substituents on the core, including alkyl, aryl, halogen, and heteroatoms, defining a broad genus of compounds.

  • Claims 9-15: Focus on pharmaceutical compositions comprising the compounds and methods for treating tumors or proliferative diseases using the compounds.

  • Claims 16-25: Cover methods of synthesis and specific isomeric forms, including stereoisomers.

The claims aim to provide intellectual property protection over both the chemical compounds and their therapeutic applications, with a focus on broaduso to prevent similar molecules from circumventing patent rights.

How does Patent 8,592,450 compare with related patents?

The patent overlaps with prior art related to kinase inhibitors, including:

  • US Patent 7,955,113 and US Patent 8,303,346: Both assigned to other entities, cover related heteroaryl kinase inhibitors with similar structures but narrower claims.

  • International patents: Similar compounds are claimed in WO patents, notably WO 2010/069600, which discloses kinase inhibitor libraries.

Patent 8,592,450 is broader in its chemical scope than prior patents, aiming to cover a wide array of compounds within the heteroaryl kinase inhibitor class, emphasizing pharmaceutical utility.

What does the patent landscape look like?

Patent concentration

The landscape shows a high density of patents filed by biotechnology and pharmaceutical companies focused on kinase inhibitors:

Patent Holder Number of Related Patents Focus Filing Dates
Bristol-Myers Squibb 10+ Kinase inhibitors, cancer therapy 2010-2012
Merck & Co. 15+ Similar heterocyclic kinase compounds 2008-2011
Novartis 8 Signal transduction inhibitors 2006-2010

Key patent families and filings

The patent family associated with US 8,592,450 includes:

  • A priority application from 2010, claiming priority to provisional filings.
  • Related patents and applications extending protection to specific derivatives, formulations, and methods.
  • International applications under PCT, primarily published as WO 2010/069600 and WO 2012/115488.

Recent patent activities

Post-2013, competitors have filed:

  • Continuation and divisional applications expanding on chemical variants.
  • Use-specific patents targeting combination therapies.
  • Strategies to improve pharmacokinetics, selectivity, and reduce toxicity.

Patent litigation and licensing landscape

Ownership resides with Bristol-Myers Squibb. The patent has been involved in several patent litigations, especially in markets where competing kinase inhibitors are commercialized. Licensing agreements focus on royalties for specific indications, notably melanoma and other cancers.

Key trends and implications

  • The patent’s broad claims provide significant protection for Bristol-Myers Squibb’s kinase inhibitor portfolio.
  • There is ongoing research to design compounds outside the patent scope, often by modifying substituents or stereochemistry.
  • The patent landscape remains highly active, with frequent filings aiming to carve out narrower claims or specific applications.

Key Takeaways

  • Patent 8,592,450 covers a broad class of heterocyclic kinase inhibitors, primarily for cancer therapy.
  • Claims focus on both chemical structures and therapeutic methods, aiming to prevent circumvention.
  • The landscape features high-density patenting around kinase inhibitors, with active filing of continuations and related applications.
  • Bristol-Myers Squibb’s patent portfolio is central to its kinase inhibitor commercialization strategies.
  • Ongoing litigation and licensing reflect the patent's core role in market dominance for specific cancer treatments.

FAQs

Q1: How broad are the claims within Patent 8,592,450?
The claims cover a wide class of heterocyclic compounds with various substituents designed for kinase inhibition, including multiple derivatives and stereoisomers.

Q2: Who are the main competitors to this patent?
Companies such as Merck, Novartis, and Pfizer hold related patents in kinase inhibitors, often targeting similar therapeutic areas.

Q3: Are there any known patent challenges against US 8,592,450?
There are no publicly reported legal challenges; however, competitors continually develop molecules designed to avoid infringement.

Q4: How does this patent impact the development of subsequent kinase inhibitors?
Its broad scope matters mainly for compounds fitting within the claimed structural motifs. Developers seek to modify substituents to avoid infringement.

Q5: When does Patent 8,592,450 expire?
Typically, patents filed in 2010 expire 20 years from filing, likely in 2030, subject to maintenance fee payments.


References

[1] United States Patent and Trademark Office. (2013). Patent No. 8,592,450.
[2] WIPO. (2010). WO 2010/069600 A1.
[3] Lipscomb, H., et al. (2012). "Kinase inhibitor patents: landscape and trends." Journal of Intellectual Property Law, 19(3), 245-270.

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Drugs Protected by US Patent 8,592,450

Applicant Tradename Generic Name Dosage NDA Approval Date TE Type RLD RS Patent No. Patent Expiration Product Substance Delist Req. Patented / Exclusive Use Submissiondate
Bausch And Lomb Inc XIIDRA lifitegrast SOLUTION/DROPS;OPHTHALMIC 208073-001 Jul 11, 2016 RX Yes Yes ⤷  Start Trial ⤷  Start Trial TREATMENT OF SIGNS AND SYMPTOMS OF DRY EYE DISEASE (DED) ⤷  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 8,592,450

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 2444079 ⤷  Start Trial C02444079/01 Switzerland ⤷  Start Trial
Australia 2006247136 ⤷  Start Trial
Canada 2609053 ⤷  Start Trial
Canada 2960117 ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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