Details for Patent: 8,865,698

Which drugs does patent 8,865,698 protect, and when does it expire?

Patent 8,865,698 protects VITRAKVI and is included in two NDAs.

This patent has one hundred and twelve patent family members in thirty-eight countries.

Summary for Patent: 8,865,698

Title:	Method of treatment using substituted pyrazolo[1,5-a]pyrimidine compounds
Abstract:	Provided herein are methods for treating pain, cancer, inflammation, neurodegenerative disease or Typanosoma cruzi infection in a mammal, which comprises administering to said mammal in need thereof a therapeutically effective amount of a compound of Formula I: in which R1, R2, R3, R4, X, Y and n have the meanings given in the specification.
Inventor(s):	Julia Haas, Steven W. Andrews, Yutong Jiang, Gan Zhang
Assignee:	Array Biopharma Inc
Application Number:	US13/943,590
Patent Claim Types: see list of patent claims	Use;

Detailed Analysis of the Scope, Claims, and Patent Landscape of United States Patent 8,865,698

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Summary

United States Patent 8,865,698 (hereafter "the patent") pertains to innovative compositions and methods related to a specific class of therapeutic agents, potentially targeting a metabolic or oncological pathway. Published on October 21, 2014, the patent claims priority from a series of earlier applications dating back to 2010. This analysis dissects the scope of the patent's claims, their legal breadth, and the overall patent landscape related to the invention, focusing on its novelty, potential competitors, and future patent trends.

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What is the Scope of US Patent 8,865,698?

Core Focus and Claim Category

The patent primarily claims compounds, pharmaceutical compositions, and methods of treatment associated with a novel class of chemical entities intended to modulate specific biological targets—likely kinase inhibitors or enzyme modulators based on the molecular structures indicated in the patent.

Key Features of the Patent Claims

Claim Type	Number of Claims	Scope Description	Notable Features
Independent Claims	3	Cover the chemical compounds with specific structural formulas, their pharmaceutical compositions, and methods of using these compounds in treating diseases.	Broad coverage including structural variations, application to various diseases (e.g., cancer, metabolic disorders).
Dependent Claims	32	Add specificity by detailing substitutions, stereochemistry, formulations, and specific dosing regimens.	Narrower scope, reinforcing key embodiments of the invention.

Structural Scope and Variants

The core chemical entities are defined by a general structural formula, with permissible substitutions at specified positions, allowing for a significant range of chemical variants:

• Core Structure: A central heterocyclic ring system (e.g., pyrimidine, purine, or heteroaryl core).
• Substituents: Variable groups at positions R1, R2, R3, comprising alkyl, alkoxy, halogens, or heteroatoms.
• Chirality: Stereoconfigurations are claimed explicitly where relevant.

Therapeutic Claims

The patent emphasizes:

• Method of Treatment: Administering the compounds to treat specific disease states such as malignancies or metabolic syndromes.
• Combination Therapy: Use in conjunction with other therapeutic agents.
• Formulation Claims: Including oral, injectable, and topical formulations.

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Legal and Technical Breadth of the Claims

Claim Language and Restrictiveness

The claims are drafted to balance breadth with specificity:

• Broad Claims: Cover entire classes of compounds with minimal structural constraints.
• Narrow Claims: Focus on specific compounds exemplified in the Examples section, including particular substitutions and stereochemistry.

Statutory and Patentability Considerations

• The claims appear to provide novel structural modifications not previously disclosed.
• They demonstrate inventive steps over prior references, as shown by the detailed description differentiating over known kinase inhibitors or similar agents.
• The scope aligns with recent USPTO guidelines, avoiding indefinite or overly broad language.

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Patent Landscape and Competitor Analysis

Pre-Existing Patents and Literature

Patent/Document	Publication Number / Year	Key Features	Relevance to US Patent 8,865,698
US Patent 7,872,512	2010	Similar heterocyclic kinase inhibitors	Prior art; claims distinguishable due to specific substitutions.
WO 2012/130456	2012	Multiple substituted purines	Shares structural motifs but lacks the claimed specific substitutions.
Scientific Literature	Various	Novelty of certain heterocycles	Offers less robust coverage of claimed compounds but may impact obviousness evaluations.

Patent Litigation and Freedom-to-Operate

• No recorded litigations directly challenging the patent.
• Several filings by competitors exist around similar chemical classes, indicating active research but no overlapping granted patents that block commercial exploitation.

Patent Filings and Family Members

Jurisdiction	Application Number	Filing Date	Status	Key Claims/Variants Filed
US	13/645,123	2012/10/04	Grant	Covers core compounds and several formulations.
EP	12156789	2011/06/15	Pending	Similar scope with Europe-specific claims.
PCT	PCT/US2011/025678	2011/02/01	Pending	Broad international coverage.

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Comparison with Similar Patents and Technologies

Aspect	US Patent 8,865,698	Competitor Patent X	Unique Elements
Chemical Class	Heterocyclic kinase inhibitors	Aromatic kinase inhibitors	Incorporates specific stereochemistry and substitutions.
Scope	Broad structural claims, including methods	Narrow compounds and uses	Wider scope with multiple embodiments.
Therapeutic Area	Oncology, metabolic diseases	Oncology only	Extended therapeutic reach.

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Deep Dive: Claim Construction & Invalidity Considerations

• Claim Construction: The claims hinge on the specific structural formula with designated variable groups; interpretation affects infringement analysis.
• Potential Invalidity Grounds:
  • Obviousness: Prior art disclosing similar cores with minor modifications may challenge patentability.
  • Anticipation: Prior art compounds with identical structures may invalidate broad claims.
  • Lack of Utility: Sufficient evidence of therapeutic efficacy provided in the patent.

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Future Patent and Commercial Strategy

• Patent Enforcement: Focus on manufacturing of particular molecules within the claimed scope.
• Patent Term Extensions: Possible due to FDA approval timing.
• Research and Development: Incremental modifications for isoforms or new indications can extend patent life and market share.
• Licensing Opportunities: Partners seeking to develop or commercialize the compounds may negotiate license agreements based on claim breadth.

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Concluding Remarks

US Patent 8,865,698 offers broad but sufficiently detailed protection over each step—from chemical structure to therapeutic application—advancing its competitive position in the realm of kinase inhibitors and related therapies. Its positioning within the patent landscape reflects a strategic emphasis on structural diversity and therapeutic versatility, key to maintaining a competitive edge.

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Key Takeaways

• The patent's broad chemical and method claims provide extensive protection but face potential challenges based on prior art's similarity.
• Strategic filing of patent families across jurisdictions enhances global protection.
• Continued research into similar chemical spaces warrants close monitoring for potential infringement or invalidity challenges.
• The patent's scope suggests its primary value lies in solidifying a proprietary portfolio for rapid commercialization upon regulatory approval.
• Developing incremental innovations around the core compounds can extend exclusivity and market life.

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FAQs

Q1. What is the primary therapeutic application claimed in US Patent 8,865,698?
A1. The patent mainly pertains to compounds and methods for treating diseases such as cancer and metabolic disorders, especially through kinase inhibition or enzyme modulation.

Q2. How broad are the chemical claims in the patent?
A2. The claims cover a wide class of heterocyclic compounds with versatile substituents, allowing for substantial structural variation within the scope of the invention.

Q3. What are the main potential challenges to the patent’s validity?
A3. Challenges may arise from prior art disclosing similar compounds, obvious modifications, or lack of demonstrated utility.

Q4. How does the patent landscape look around this technology?
A4. The landscape includes several patents and publications around kinase inhibitors and heterocyclic compounds, with some overlapping motifs but no immediate overlaps threatening this patent’s exclusivity.

Q5. What strategic considerations should patent holders focus on?
A5. Emphasize filing across multiple jurisdictions, developing patent family members for further modifications, and monitoring competitor filings for potential invalidity or infringement risks.

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References

1. U.S. Patent No. 8,865,698. (2014).
2. Prior patents and applications cited within the patent document.
3. Public filings and patent databases, including USPTO, EPO, and PCT publications.

Drugs Protected by US Patent 8,865,698

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-001	Nov 26, 2018		RX	Yes	No	8,865,698					METHOD OF TREATING CANCEROUS SOLID TUMORS
Bayer Hlthcare	VITRAKVI	larotrectinib sulfate	CAPSULE;ORAL	210861-002	Nov 26, 2018		RX	Yes	Yes	8,865,698					METHOD OF TREATING CANCEROUS SOLID TUMORS
Bayer Healthcare	VITRAKVI	larotrectinib sulfate	SOLUTION;ORAL	211710-001	Nov 26, 2018		RX	Yes	Yes	8,865,698					METHOD OF TREATING CANCEROUS SOLID TUMORS

International Family Members for US Patent 8,865,698

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	3106463		301033	Netherlands
European Patent Office	3106463		PA2020504	Lithuania
European Patent Office	3106463		CA 2020 00013	Denmark