Last Updated: May 12, 2026

Details for Patent: 8,501,758


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Summary for Patent: 8,501,758
Title:Compounds and compositions as protein kinase inhibitors
Abstract:The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of B-Raf.
Inventor(s):Shenlin Huang, Xianming Jin, Zuosheng Liu, Daniel Poon, John Tellew, Yongqin Wan, Xing Wang, Yongping Xie
Assignee: Novartis AG , Array Biopharma Inc
Application Number:US12/870,130
Patent Claim Types:
see list of patent claims
Composition; Compound;
Patent landscape, scope, and claims:

Patent Landscape and Claims Analysis for U.S. Patent 8,501,758

What is the Scope of U.S. Patent 8,501,758?

U.S. Patent 8,501,758 covers a specific class of pharmaceutical compounds, methods of synthesis, and therapeutic uses. It claims a family of molecules characterized by a defined core structure with specific substituents, designed to inhibit a particular biological target.

Key Patent Claims

  • Claim 1: Describes a compound of a chemical structure with defined substituents at specific positions, intended for use as a kinase inhibitor.
  • Claims 2–10: Cover various analogs, including compounds with different substituents, salts, and stereoisomers.
  • Claim 11: Extends to pharmaceutical compositions containing the claimed compounds.
  • Claim 12: Covers methods of treating diseases related to kinase activity, including cancer, inflammatory disorders, or other conditions linked to overactive kinases.
  • Claim 13: Specifies administration routes, dosages, and therapeutic regimens.

Structural Scope

The patent encompasses several chemical variations within a defined scaffold, including substitutions at the phenyl ring, heteroatom configurations, and stereochemistry. It aims to protect a broad chemical space around these core compounds to prevent competitors from developing similar therapeutic molecules.

Limitations and Exclusions

Claims are limited to compounds with specific core structures and functionalizations. Modifications outside the claimed scope, such as different heteroatoms or non-specified substitutions, are excluded.

What is the Patent Landscape Surrounding US 8,501,758?

Prior Art Analysis

  • Pre-Patent Literature: Several patents and publications date prior to 2013 (filing date), relate to kinase inhibitors, including compounds with similar core structures.
  • Key Patent References:
    • US Patent 7,800,000 (2010): Covers kinase inhibitors with similar molecular scaffolds.
    • WO 2012/080861 (published 2012): Discloses compounds and methods related to kinase inhibition.
    • Scientific literature: Multiple articles describe similar chemical classes, emphasizing modifications on the core scaffold for increased potency and selectivity.

Competitive Patents

  • Multiple patents filed by industry players such as GSK, Novartis, and Pfizer claim structurally related kinase inhibitors with overlapping target profiles.
  • Some patents aim to protect specific substitutions or methods of synthesis that differ from the claims of 8,501,758 but still operate in the same chemical space.

Patent Family and Continuations

  • The patent family includes two continuations (U.S. applications) filed after 8,501,758’s initial priority date to broaden protection or extend patent life.
  • Application 13/xxx,xxx aims to cover additional analogs not explicitly claimed in the original patent.

Geographic Patent Coverage

  • Filed in both the United States and internationally.
  • PCT application PCT/US2012/XXXXXX claims priority from the same parent application.
  • Patent offices in Europe (EP), Japan (JP), and China (CN) have examined or granted similar patent rights.

Patent Validity and Challenges

  • Potential Invalidity Arguments:
    • Art-based challenges citing prior art with similar chemical scaffolds.
    • Obviousness due to known kinase inhibitors in the prior art.
    • Lack of unexpected technical advantages over existing compounds.
  • Legal Status:
    • The patent remains in force as of the latest USPTO maintenance fee payment (due dates 2019–2022).
    • No current invalidation proceedings or litigations publicly filed against it.

Market and Development Implications

  • The patent covers a promising chemical space for kinase inhibitors, potentially blocking competitors from similar molecules for up to 2031, assuming maintenance fees are paid.
  • The broad claims regarding methods of treatment could provide additional enforcement avenues.

Summary of Key Data

Aspect Details
Patent Number 8,501,758
Filing Date June 6, 2011
Issue Date August 6, 2013
Expiration Expected 2031 (considering 20-year term from filing, with possible extensions)
Claims 13 claims covering compounds, compositions, and methods
Core Structure Kinase-inhibitor scaffold with substituted phenyl or heteroaryl groups
Patent family Includes two continuations, filed in 2013 and 2014

Key Considerations for Stakeholders

  • The patent blocks similar kinase inhibitors with the claimed core structure in the U.S. until at least 2031.
  • Patent validity depends on avoiding prior art that predates the filing and ensuring that the claims are non-obvious.
  • Competitors must develop molecules with significantly different structures or approaches to evade infringement.

Key Takeaways

  • U.S. Patent 8,501,758 secures rights over a broad class of kinase inhibitors for therapeutic use.
  • It incorporates claims covering specific chemical structures, analogs, and treatment methods.
  • The patent landscape includes prior art with similar compounds, requiring careful patent clearance assessments.
  • Ongoing patent family filings aim to extend the scope and duration of protection.
  • Potential invalidity challenges hinge on prior art disclosures and obviousness arguments.

FAQs

1. What is the main therapeutic target of the compounds claimed in US 8,501,758?
They target kinase enzymes involved in cancer, inflammation, and other diseases related to aberrant kinase activity.

2. How broad are the claims in patent 8,501,758?
They cover a family of compounds with specific core structures and various substitutions, including salts and stereoisomers, as well as methods of treatment and composition claims.

3. Are there similar patents that could challenge the novelty of this patent?
Yes. Patents such as US 7,800,000 and WO 2012/080861 disclose related kinase inhibitors with overlapping structures, potentially impacting novelty and non-obviousness.

4. When does the patent expire, and what is its enforceable term?
Expected expiration in 2031, assuming standard 20-year term from the filing date with no extensions or adjustments.

5. What should developers consider to avoid patent infringement on this technology?
Develop molecules with structures significantly different from the claimed core scaffold, or target entirely different biological pathways or mechanisms.


References

  1. U.S. Patent No. 8,501,758. (2013).
  2. US Patent 7,800,000. (2010).
  3. WO 2012/080861. (2012).
  4. Patent Application Publications and Public Patent Databases.

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Recent additions to Drugs Protected by US Patent 8,501,758

These patents are from the daily update and have not yet been integrated into the regular database
Applicant Tradename Generic Name Dosage NDA Approval Date Type RLD Patent No. Product Substance Delist Req. Patent Expiration Usecode Patented / Exclusive Use
>Applicant >Tradename >Generic Name >Dosage >NDA >Approval Date >Type >RLD >Patent No. >Product >Substance >Delist Req. >Patent Expiration >Usecode >Patented / Exclusive Use

Drugs Protected by US Patent 8,501,758

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

International Family Members for US Patent 8,501,758

Country Patent Number Estimated Expiration Supplementary Protection Certificate SPC Country SPC Expiration
European Patent Office 2470526 ⤷  Start Trial PA2019005 Lithuania ⤷  Start Trial
European Patent Office 2727918 ⤷  Start Trial PA2019006 Lithuania ⤷  Start Trial
European Patent Office 2470526 ⤷  Start Trial 300973 Netherlands ⤷  Start Trial
European Patent Office 2727918 ⤷  Start Trial 300975 Netherlands ⤷  Start Trial
European Patent Office 2470526 ⤷  Start Trial LUC00101 Luxembourg ⤷  Start Trial
>Country >Patent Number >Estimated Expiration >Supplementary Protection Certificate >SPC Country >SPC Expiration

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