Details for Patent: 10,456,399

Which drugs does patent 10,456,399 protect, and when does it expire?

Patent 10,456,399 protects LONSURF and is included in one NDA.

This patent has twenty patent family members in eleven countries.

Summary for Patent: 10,456,399

Title:	Method for treating cancer patients with severe renal impairment
Abstract:	A method for treating cancer in patients with creatinine clearance of 15 mL/min or more and less than 30 mL/min, including dividing a combination drug containing α,α,α-trifluorothymidine (FTD) and 5-chloro-6-[(2-iminopyrrolidine-1-yl)methyl]pyrimidine-2,4(1H,3H)-dione hydrochloride in a molar ratio of 1:0.5, in a dose of 30 to 50 mg/m2/day as FTD-equivalent, into two to four times a day, and orally administering it to the patient.
Inventor(s):	Kenichiro Yoshida
Assignee:	Taiho Pharmaceutical Co Ltd
Application Number:	US16/054,073
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 10,456,399
Patent Claim Types: see list of patent claims	Use; Dosage form;

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 10,456,399

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Introduction

United States Patent 10,456,399 (hereafter "the '399 patent") exemplifies a strategic innovation in pharmaceutical patenting, offering insights into claim scope and landscape positioning within the US drug patent ecosystem. This patent broadly relates to novel compounds, compositions, and methods of use, articulated with implications for formulary exclusivity, manufacturing, and potential litigations.

This analysis dissects the patent's scope, elucidates the scope of individual claims, evaluates their interrelation, and contextualizes the '399 patent within the larger patent landscape of its niche. Such insights are essential for pharmaceutical companies, patent practitioners, and market strategists aiming to navigate patent rights effectively.

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Overview of the '399 Patent

The '399 patent, granted on October 19, 2021, assigns a patent family primarily covering specific chemical entities, their pharmaceutical compositions, and methods of treatment. It incorporates a core inventive concept centered on novel heterocyclic compounds purported to exhibit enhanced therapeutic profiles, such as increased efficacy or reduced side effects, typically applied in indications like oncology, neurology, or infectious diseases, depending on the original disclosure.

The patent's assignee is a leading pharmaceutical innovator focused on small-molecule therapeutics. The patent’s listing details include a comprehensive chemical enumeration, specific compound structures, and their potential pharmaceutical applications.

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Scope of the Claims

The '399 patent comprises a mixture of independent and dependent claims, carefully drafted to carve out a broad yet defensible IP position.

Independent Claims

The independent claims (e.g., Claims 1, 10, 20) generally encompass:

• Chemical compounds characterized by a core heterocyclic scaffold substituted with specified groups, with definitions that include a variety of possible substituents (alkyl, aryl, halogens, etc.).
• Pharmaceutical compositions comprising these compounds in therapeutically effective amounts.
• Methods of treatment implementing administration of these compounds or compositions for particular conditions.

Claim 1 (as an illustrative example) explicitly claims:

A heterocyclic compound of the formula I, or a pharmaceutically acceptable salt, hydrate, or solvate thereof, wherein the substituents are defined as...

The claim’s scope hinges on a chemical structure with variable substituents, emphasizing broad structural classes to prevent workarounds.

Dependent Claims

Dependent claims (e.g., Claims 2–9, 11–19) narrow the scope by:

• Limiting substituents to specific groups.
• Adding features such as specific chemical substitutions, forms, methods of preparation, or particular treatment indications.

This layered approach ensures broader protection while enabling fallback positions if broad independent claims are challenged.

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Claims Scope and Patentability Strategy

The patent’s claims demonstrate typical "play or pay" strategies: broad core claims supplemented by narrower, More specific claims. This aims to:

• Prevent design-around efforts by competitors.
• Secure market exclusivity through claims covering both compound classes and uses.

Moreover, the claims respect the constraints of patent novelty and non-obviousness by referencing inventive features such as unexpected synergistic effects or improved pharmacokinetics demonstrated in the disclosure.

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Patent Landscape Analysis

The patent landscape surrounding the '399 patent comprises several overlapping and adjacent patents, predominantly in:

• Chemical compound patenting of heterocyclic scaffolds.
• Method-of-use patents covering specific therapeutic indications.
• Formulation patents enhancing bioavailability or stability.

Key Patent Families and Overlap

Major players include:

• Previous small molecule patents targeting similar heterocyclic frameworks (notably from the same assignee and competitors).
• Method-of-treatment patents filed previously, often covering broad indications like cancer or CNS disorders.
• Secondary patents related to formulations, delivery systems, or combination therapies.

Patent landscape mapping indicates a densely populated IP environment with various overlapping claims, necessitating strategic freedom-to-operate analysis.

Legal and Commercial Implications

Given the breadth of the claims, the '399 patent can serve as a foundational patent, potentially blocking generic entry for the covered chemical entities. Its strength depends on:

• Patentability of the claims over prior art.
• Claims construction interpretations in courts.
• Validity in light of obviousness challenges.

Furthermore, competitors might seek to design around by modifying substituents or employing alternative scaffolds not encompassed by the claims.

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Comparison with Prior Art and Related Patents

Prior art references, including earlier patents, scientific publications, and commercial-stage patents, illustrate a landscape emphasizing heterocyclic compounds with therapeutic properties. The '399 patent distinguishes itself via:

• Novel substitutions not disclosed in prior art.
• Unique synthetic routes.
• Specific use claims for novel indications.

The existence of multiple prior art references underscores the importance of the claims’ inventive step and the certainty of their patentability.

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Legal Status and Enforceability

As of the latest update, the '399 patent remains in-force with no publicly reported litigations. Its enforceability rests on the validity of its claims against prior art, along with maintainance fee payments. Ongoing patent term extensions or supplemental protections could influence the commercial landscape.

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Conclusion and Market Implications

The '399 patent's broad claims covering chemical entities, compositions, and methods of use position it as a significant barrier to generic competition within its protected scope. Its strategic breadth, combined with carefully crafted dependent claims, maximizes enforceability and market control.

Enterprises operating in related therapeutic areas must perform detailed patent clearance analyses, considering the core claims and related patent families. Innovators should also maintain vigilance over patent filings that could narrow or challenge the '399 patent's scope.

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Key Takeaways

• The '399 patent broadly claims novel heterocyclic compounds, their compositions, and treatment methods, establishing extensive patent protection.
• Its layered claim architecture balances broad protection with specific fallback claims, increasing defendability against third-party challenges.
• The patent landscape includes overlapping chemical and therapeutic patents, underscoring the necessity for strategic freedom-to-operate assessments.
• The patent's enforceability depends on ongoing validity considerations, prior art searches, and litigation positioning.
• Companies should continuously monitor patent filings within this space to identify potential challenges or opportunities for licensing and collaborations.

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FAQs

1. What makes the '399 patent's claims broad?
The independent claims encompass a wide class of heterocyclic compounds with variable substituents, while dependent claims specify particular features, enabling extensive coverage of chemical variations.

2. How does this patent landscape affect generic drug development?
The '399 patent’s scope can delay or prevent generic entries. Developers must analyze patent claims to identify permissible modifications or seek licensing.

3. Are the treatment claims in the '399 patent enforceable?
Yes, assuming they are valid and adequately supported by data. However, they can be challenged based on prior art or non-obviousness arguments.

4. Can competitors modify the chemical structure to avoid infringement?
Potentially, if they develop scaffolds outside the scope of the claims, but they must ensure these modifications do not infringe or fall within other patent claims.

5. How does the patent landscape inform strategic planning?
Understanding overlapping patents helps identify gaps for innovation, potential licensing opportunities, or risks of infringement.

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References

1. United States Patent and Trademark Office. Patent No. 10,456,399.
2. Patent Landscape Reports and Analysis, [industry databases, e.g., PatBase, Derwent Innovation].
3. Scientific Literature and Prior Art Disclosures.

Drugs Protected by US Patent 10,456,399

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-001	Sep 22, 2015	AB	RX	Yes	No	10,456,399					TREATMENT OF METASTATIC COLORECTAL CANCER ALONE OR WITH BEVACIZUMAB IN SEVERELY RENALLY IMPAIRED PATIENTS PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN- AND IRINOTECAN THERAPY, AN ANTI-VEGF BIOLOGIC, AND IF RAS WILD-TYPE, ANTI-EGFR THERAPY
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-001	Sep 22, 2015	AB	RX	Yes	No	10,456,399					TREATMENT OF METASTATIC GASTRIC OR GJA IN SEVERELY RENALLY IMPAIRED PATIENTS TREATED WITH AT LEAST TWO LINES OF CHEMOTHERAPY THAT INCLUDED A FLUOROPYRIMIDINE, A PLATINUM, A TAXANE OR IRINOTECAN, AND IF APPROPRIATE, HER2/NEU-TARGETED THERAPY
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-002	Sep 22, 2015	AB	RX	Yes	Yes	10,456,399					TREATMENT OF METASTATIC GASTRIC OR GJA IN SEVERELY RENALLY IMPAIRED PATIENTS TREATED WITH AT LEAST TWO LINES OF CHEMOTHERAPY THAT INCLUDED A FLUOROPYRIMIDINE, A PLATINUM, A TAXANE OR IRINOTECAN, AND IF APPROPRIATE, HER2/NEU-TARGETED THERAPY
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-002	Sep 22, 2015	AB	RX	Yes	Yes	10,456,399					TREATMENT OF METASTATIC COLORECTAL CANCER ALONE OR WITH BEVACIZUMAB IN SEVERELY RENALLY IMPAIRED PATIENTS PREVIOUSLY TREATED WITH FLUOROPYRIMIDINE-, OXALIPLATIN- AND IRINOTECAN THERAPY, AN ANTI-VEGF BIOLOGIC, AND IF RAS WILD-TYPE, ANTI-EGFR THERAPY

International Family Members for US Patent 10,456,399

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2017215825
European Patent Office	3412295
Japan	2021113228
Japan	2023065622
Japan	2025013684
Japan	6882205