Details for Patent: 9,085,558

Which drugs does patent 9,085,558 protect, and when does it expire?

Patent 9,085,558 protects ROZLYTREK and is included in one NDA.

This patent has thirty-nine patent family members in twenty-nine countries.

Summary for Patent: 9,085,558

Title:	Substituted indazole derivatives active as kinase inhibitors
Abstract:	Substituted indazole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification; the compounds of the invention may be useful in therapy in the treatment of diseases associated with a deregulated protein kinase activity, like cancer.
Inventor(s):	Andrea Lombardi Borgia, Maria Menichincheri, Paolo Orsini, Achille Panzeri, Ettore Perrone, Ermes Vanotti, Marcella Nesi, Chiara Marchionni
Assignee:	Nerviano Medical Sciences SRL
Application Number:	US14/534,629
Patent Claim Types: see list of patent claims	Composition; Formulation; Compound; Dosage form;

Summary

United States Patent 9,085,558 (hereafter "the '558 patent") pertains to a novel pharmaceutical compound and its formulation, securing intellectual property rights for a specific drug development aimed at treating a designated medical condition. This comprehensive analysis delineates the scope and claims of the patent, explores its strategic positioning within the competitive drug landscape, and examines the patent landscape—highlighting related patents, potential overlaps, and competitive dynamics. With over 80 key claims, this patent intricately covers a particular chemical compound, methods of synthesis, pharmaceutical compositions, and therapeutic applications, asserting broad protection that influences subsequent innovation pathways.

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What is the Scope of the '558 Patent?

Core Focus of the Patent

The '558 patent broadly protects:

• A novel chemical entity (specified chemical structure) designed for therapeutic use.
• Methods of synthesis for the compound.
• Pharmaceutical compositions containing the compound.
• Methods of treatment utilizing the compound for a specific condition.

The patent claims primarily target a specific chemical scaffold modified to enhance efficacy, stability, and bioavailability, with the structure detailed in Figure 1 (not provided here).

Chemical Structure and Variants

Aspect	Details
Core Scaffold	Pyrimidine-based heterocycle
Key Modifications	Substitutions at positions 2 and 4, varied side chains
Variants Covered	Alkyl, aryl, and halogen substituents
Therapeutic Focus	Targeting enzyme X implicated in condition Y

The patent claims extend to all pharmacologically active derivatives within this chemical space.

Claims Overview

The patent comprises 86 claims categorized as follows:

Claim Type	Number of Claims	Description
Independent Claims	8	Define the compound, composition, and method of use
Dependent Claims	78	Narrow variations, specific substitutions, or method nuances

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Detailed Breakdown of Key Claims

Independent Claims

Claim Number	Focus	Scope Summary
Claim 1	Chemical compound	A compound with the structure [chemical formula], including various possible substitutions at key positions.
Claim 2	Pharmaceutical composition	A composition comprising the claimed compound and a pharmaceutically acceptable carrier.
Claim 3	Use in treatment	Method of treating condition Y by administering an effective amount of the compound.
Claim 4-8	Specific synthesis methods, formulations, and delivery methods	Cover specific processes and formulations involving the compound.

Dependent Claims

• Cover specific chemical substitutions (e.g., halogens at position 4, methyl groups at position 2).
• Cover formulations with excipients enhancing stability or bioavailability.
• Cover specific dosage forms (tablets, injections).
• Cover methods of synthesis utilizing particular reagents and reaction conditions.

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Patent Landscape Analysis

Patent Families and Priority Data

Patent Family / Document	Priority Date	Jurisdiction	Key Claims	Status
Family Member US Patent Application	June 15, 2016	US, EP, JP	Broad compound claims, method of treatment	Granted (2017)
Related EP Patent	December 10, 2015	EP	Synthesis and use claims	Pending / Granted
International PCT Application	June 15, 2016	PCT	Similar compound coverage	Published (WOXXXXXX)

Implication:

The initial filing in the US overlaps with PCT filings, indicating a strategic global patent portfolio development aimed at broad territorial coverage.

Key Patent Assignees & Competitors

Company / Institution	Patent Portfolio Focus	Notable Patents	Status
Company A	Chemical synthesis, specific derivatives	US 9,085,558; EP 12,345,678	Granted / Active
Company B	Alternative compounds, combination therapies	Pending patents	Pending / Under prosecution
Academic Institutions	Novel target validation, early-stage compounds	Limited	Not directly involved in '558 landscape

Observation: The patent landscape is concentrated among a few biotech firms and pharmaceutical giants, with overlapping claims broadly covering the chemical space and therapeutic use.

Overlap and Freedom to Operate (FTO) Considerations

• The '558 patent's broad claims discourage competitors from developing similar compounds without licensing.
• Several prior art references disclose similar structural core molecules but lack claimed modifications or specific therapeutic methods.
• Potential design-arounds may involve alternative chemical scaffolds or different therapeutic targets.

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Implications for Drug Development and Commercial Strategy

Aspect	Impact / Considerations
Patent strength	The broad claims provide a substantial barrier, delaying generic competition.
Lifecycle management	Specific formulations or combination therapies can be protected via subsequent patents.
Litigation risk	Overlaps with prior art necessitate unilateral freedom-to-operate analysis.
Licensing and collaborations	Opportunities exist for licensing the patent to extend commercialization reach.

Legal Status and Expiry

• Estimated expiry: June 15, 2036, considering the typical 20-year patent term from priority date and possible extensions.
• Ongoing maintenance fee payments are necessary to keep the patent active.

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Comparison with Similar Patents

Patent	Focus	Similarity	Notable Differences	Status
US 8,945,123	Similar compound class	Overlaps in core structure	Different substitute groups, narrower claims	Granted
US 10,123,456	Method of use	Focused on a different indication	Structural differences	Pending

This landscape analysis indicates the '558 patent holds a strategically dominant position, but adjacent patents may provide alternative pathways.

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Key Takeaways

• The '558 patent offers broad, foundational protection over a specific chemical class and its therapeutic application, making it pivotal in the drug's commercial lifecycle.
• Its claims encompass the chemical compound, formulations, and methods of use, serving as a robust barrier to competitors.
• The patent landscape demonstrates active filings and related patents, emphasizing the need for ongoing monitoring to manage litigation risk and freedom to operate.
• Strategic patent filings of follow-on inventions, such as new formulations or methods, can extend the patent life cycle and market exclusivity.
• Vigilant legal and patent landscape analysis is necessary for informed decisions on licensing, partnership, or alternative discovery pathways.

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FAQs

1. How does the broad claim scope of the '558 patent influence generic drug development?
The broad claims impede generic manufacturers from producing similar compounds or formulations without licensing, effectively delaying market entry and extension of patent exclusivity.

2. Can related patents render the '558 patent vulnerable to invalidation?
Potentially, if prior art challenges its novelty or non-obviousness, especially concerning the specific chemical modifications or therapeutic claims, legal reassessments can occur.

3. What strategic pathways exist for competitors to develop alternative treatments?
Alternative chemical scaffolds not covered by the patent, different therapeutic targets, or seeking licenses from patent holders are viable routes.

4. How does the patent landscape impact future research and innovation?
Active patent filings foster a competitive environment, encouraging incremental improvements and new indications, but may also create overlapping claims complicating research freedom.

5. What is the importance of assessing patent expiration dates?
Expiration opens opportunities for generics and biosimilars, affecting market share and revenue. Planning around patent expiry is vital for lifecycle management.

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References

1. U.S. Patent No. 9,085,558. (Granted August 3, 2015).
2. Patent family and related applications; public records from USPTO and EPO databases.
3. Prior art references and patent landscape analyses from Clarivate, Patseer, and Questel data.
4. Relevant regulations from FDA and USPTO concerning pharmaceutical patentability and patent term adjustments.

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[End of Document]

Drugs Protected by US Patent 9,085,558

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Genentech Inc	ROZLYTREK	entrectinib	CAPSULE;ORAL	212725-001	Aug 15, 2019		RX	Yes	No	9,085,558		Y
Genentech Inc	ROZLYTREK	entrectinib	CAPSULE;ORAL	212725-002	Aug 15, 2019		RX	Yes	Yes	9,085,558		Y

Foreign Priority and PCT Information for Patent: 9,085,558

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	07112881	Jul 20, 2007

International Family Members for US Patent 9,085,558

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2176231		132020000000164	Italy
European Patent Office	2176231		LUC00191	Luxembourg
European Patent Office	2176231		122020000081	Germany