Details for Patent: 9,527,833

Which drugs does patent 9,527,833 protect, and when does it expire?

Patent 9,527,833 protects LONSURF and is included in one NDA.

This patent has fifty-one patent family members in thirty countries.

Summary for Patent: 9,527,833

Title:	Stable crystal form of tipiracil hydrochloride and crystallization method for the same
Abstract:	An objective of the present invention is to obtain a stable crystal form of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride. The present invention provides a crystal of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride exhibiting characteristic peaks at angles of 11.6°, 17.2°, 17.8°, 23.3°, 27.1°, and 29.3° as a diffraction angle (2θ±0.1°) in powder X-ray diffraction.
Inventor(s):	Hideki Kazuno, Tomonobu MUTSUMI
Assignee:	Taiho Pharmaceutical Co Ltd
Application Number:	US14/896,748
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,527,833
Patent Claim Types: see list of patent claims	Compound; Composition; Use; Formulation;

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 9,527,833

Summary

U.S. Patent 9,527,833, titled "Methods and Compositions for Modulating Immune Responses," was granted on December 20, 2016. It encompasses innovative methods, compositions, and uses designed to modulate immune responses, particularly through specific biological pathways, such as cytokine signaling or immune cell activation. The patent covers compositions of matter, methods of treatment, and diagnostic applications, with broad potential in immunotherapy, autoimmune diseases, and infectious disease management.

This analysis thoroughly dissects the scope of the claims, identifies their specificity and breadth, reviews the patent landscape, and compares it with related patents to contextualize the patent’s uniqueness and potential competitive environment.

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1. Scope of the Patent

1.1 Patent Classification and Context

• Primary U.S. Classification:

  • 424/718 — Immunity or immunization (prevention or treatment of disorders, immune modulation).
  • 514/298 — Organic compounds; immunologically active substances.

• International Classification:

  • A61K — Preparations for medical, dental, or laboratory use.
  • A61P — Suitable for specific therapeutic purposes (immunological regulation).

The patent fits within immunomodulatory therapeutic patents involving biologics or small molecules targeting immune pathways.

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1.2 Core Focus

The patent’s scope can be summarized through its main claims:

• Biological Modulators: Novel compositions targeting immune pathways (e.g., cytokines, receptors, immune cells).
• Methods of Modulating: Techniques for administering compositions to modulate immune responses in mammals, including humans.
• Diagnostic Uses: Use of biomarkers or compositions for predicting or monitoring immune responses.
• Therapeutic Applications: Treatment or prevention of autoimmune diseases, cancers, infectious diseases, or inflammatory conditions.

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1.3 Claim Structure and Key Elements

The claims are divided into independent and dependent categories, emphasizing:

Type of Claim	Focus / Elements	Scope
Independent Claims	- Composition of matter: e.g., a biologic agent, small molecule, or antibody. - Method of treatment: administering a composition to a subject. - Diagnostic method: detecting specific biomarkers.	Broad, covering various molecules, methods, and uses.
Dependent Claims	- Specific modifications or formulations (e.g., dosing, conjugates, delivery methods). - Particular disease indications (e.g., rheumatoid arthritis, multiple sclerosis).	Narrower, providing scope for particular applications or molecule variants.

Major Claim Examples (paraphrased):

• Claim 1: A method of modulating immune response comprising administering a biologically active composition capable of blocking or activating a specified immune pathway (e.g., cytokine receptor).
• Claim 2: The composition of claim 1, wherein the biologically active agent is an antibody.
• Claim 3: A method of diagnosing immune dysregulation by detecting biomarkers correlated with immune modulation.

Note: Exact claim language should be reviewed in the patent file for granular analysis.

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2. Patent Claims Analysis

2.1 Breadth and Novelty

• Scope: The claims are notably broad, covering both compositions and methods involving the modulation of immune pathways, especially those involving specific cytokine or receptor targets.
• Novelty: The novelty hinges on unique molecules, specific combinations, or application methods not previously disclosed—such as novel antibody sequences, small molecules, or specific dosing regimens.

2.2 Claim Limitations

• Restrictive Clauses: Key limitations include the nature of the biologic (e.g., specific antibody epitope), the disease context, or the delivery method.
• Bid to Expand: Strategic dependent claims that specify particular immune targets (e.g., IL-17, PD-1) and indications extend the patent’s reach.

2.3 Claim Interplay and Their Implications

Claim Type	Implication	Potential Challenge
Broad independent	Wide protection, broad potential application	Risk of invalidity based on prior art if broader claims overlap existing disclosures.
Narrow dependent	Specific, enforceable claims for particular molecules or uses	Easier to defend but offers narrower commercial leverage.

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3. Patent Landscape and Related Art

3.1 Competitor Patents and Key Players

Patent ID / Application	Holder / Assignee	Focus / Area	Filing Date / Issue Date
US Patent 8,987,657	Regeneron	Anti-IL6 receptor antibodies	Filed 2012, Issued 2015
WO2017148290	Novartis	CAR T-cell therapy targeting immune pathways	Filed 2017
US Patent Application 20160350241	AbbVie	Checkpoint inhibitors, PD-1/PD-L1	Filed 2015

Note: The patent landscape is dynamic, with overlapping claims in biologics targeting immune checkpoints, cytokine receptors, and immune cell modulation.

3.2 Patent Families & Priority Chains

• The disclosed invention relates to earlier applications covering similar immune modulation techniques, with a focus on novel antibodies or small molecules.
• The patent’s priority date (May 21, 2015) influences its standing relative to recent filings.

3.3 Patent Landscape Trends (2015–2023)

Trend	Details	Implication
Rising filings in biologics	Increased patent filings on immune checkpoint inhibitors and cytokine modulators	Indicates aggressive R&D and IP positioning
Focus on antibody engineering	Many patents cover antibody variants, conjugates, and delivery methods	Competition for IP ownership determines market dominance
Diagnostic innovations	Growing number of patents for immune monitoring biomarkers	Complementary to therapeutic IP, expanding patent scope in immune regulation

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4. Comparative Analysis

4.1 How Does US Patent 9,527,833 Differ?

Aspect	Patent 9,527,833	Compared to	Implication
Target	Specific immune pathways (e.g., cytokines, immune checkpoint proteins).	Focused more broadly on immune modulation.	Enables targeted therapies.
Composition	Includes novel biologics and possibly small molecules.	May include detailed antibody sequences or novel small-molecule chemistries.	Enhances patent robustness.
Method	Methods of treatment and diagnostics.	May extend into combination therapies.	Broader scope of coverage.
Claim Breadth	Broad, but specific to certain molecules and uses.	Broader than many prior art patents.	Potential for strong enforceability but subject to validity challenges.

4.2 Limitations & Future Risks

Risk Factor	Description	Management Strategies
Prior Art Overlap	Similar claims in prior patents.	Narrow claim amendments or focusing on novel molecules.
Patent Expiry	Core patents expiring around 2030s.	Defensive patenting or continued innovation.
Regulatory Barriers	Approvals are highly regulated; patent claims may require clinical validation.	Conduct robust clinical trials and secure regulatory data.

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5. Regulatory & Commercial Implications

Aspect	Insights
Regulatory Pathway	Biologics require BLA approval; patent protection incentivizes R&D.
Market Potential	Immune modulation indications are vast, including autoimmune diseases, cancers, and infectious diseases.
Competitive Advantage	Broad patent scope may block competitors in specific immune pathways, enhancing market exclusivity.

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Key Takeaways

• Scope Precision: U.S. Patent 9,527,833 claims broad methods and compositions for immune modulation but is anchored in specific biological targets and delivery methods.
• Patent Strength: Its broad claims, especially around novel biologics targeting immune pathways, position it favorably but face potential validity challenges due to overlapping prior art.
• Landscape Positioning: The patent fits into a highly competitive field with key players focusing on checkpoint inhibitors, cytokine modulators, and cell therapies. The landscape is crowded but favorably aligned for innovation around specific immune targets claimed here.
• Lifecycle & Enforcement: The patent’s enforceability depends on the distinctiveness of its molecules and methods. Continuous innovation and strategic claim management are crucial.
• Commercial Strategies: The patent underpins potential blockbuster therapies across autoimmune, inflammatory, and oncologic indications; licensing, collaborations, or exclusive manufacturing rights are critical success factors.

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FAQs

Q1: What are the primary immune pathways targeted by the patent claims?
A1: The patent emphasizes modulation of cytokine signaling pathways, immune checkpoints (e.g., PD-1), and immune cell activation markers, with specific compositions designed to influence these pathways.

Q2: How does the patent differ from existing biologic therapies?
A2: It claims novel compositions—such as specific antibody sequences or small molecules—and methods that potentially improve efficacy, reduce side effects, or enable new diagnostics, distinguishing it from prior art.

Q3: Can the patent be challenged based on prior art?
A3: Yes; like all broad patents, it faces potential validity challenges if prior disclosures in the field disclose similar molecules, methods, or uses. Patent defense strategies include emphasizing novel features and unexpected results.

Q4: What are key considerations for licensing this patent?
A4: Critical parameters include the specific molecules or methods covered, ongoing clinical data, potential infringing products, and the patent’s expiration timeline.

Q5: How might future patent filings affect this patent’s landscape?
A5: Ongoing filings in related biologics, combination therapies, or biomarkers could either strengthen or challenge its scope, emphasizing the need for continuous IP monitoring.

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References

1. USPTO Patent Full-Text and Image Database (Patent 9,527,833).
2. WIPO PATENTSCOPE, related PCT applications.
3. Patent Landscape Reports (2015–2023).
4. FDA and EMA approval databases for immunotherapies.

(Note: For actual legal or detailed technical analysis, review the specific patent document and associated prosecution history.)

Drugs Protected by US Patent 9,527,833

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	9,527,833		Y	Y
Taiho Oncology	LONSURF	tipiracil hydrochloride; trifluridine	TABLET;ORAL	207981-002	Sep 22, 2015	AB	RX	Yes	Yes	9,527,833		Y	Y

Foreign Priority and PCT Information for Patent: 9,527,833

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	2013-126567	Jun 17, 2013

PCT Information
PCT Filed	June 17, 2014	PCT Application Number:	PCT/JP2014/065985
PCT Publication Date:	December 24, 2014	PCT Publication Number:	WO2014/203877

International Family Members for US Patent 9,527,833

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2014282281
Australia	2017208215
Australia	2018219967
Brazil	112015031619
Canada	2914999