Details for Patent: 9,493,470

Which drugs does patent 9,493,470 protect, and when does it expire?

Patent 9,493,470 protects ICLUSIG and is included in one NDA.

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

Summary for Patent: 9,493,470

Title:	Crystalline forms of 3-(imidazo[1,2-B] pyridazin-3-ylethynyl)-4-methyl-N-{4-[(4-methylpiperazin-1-yl) methyl]-3-(trifluoromethyl)phenyl}benzamide and its mono hydrochloride salt
Abstract:	Novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyljbenzamide free base and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methyl piperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, pharmaceutical compositions thereof and methods of their preparation and use are disclosed herein. The instant application is directed to novel crystalline forms of 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl}phenyl}benzamide and 3-(imidazo[1,2-b]pyridazin-3-ylethynyl)-4-methyi-N-{4-[(4-methylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl}benzamide mono hydrochloride, compositions comprising such crystalline forms, and to methods of their preparation and use.
Inventor(s):	Christopher K. Murray, Leonard W. Rozamus, John J. Chaber, Pradeep Sharma
Assignee:	Takeda Pharmaceuticals USA Inc
Application Number:	US14/651,577
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,493,470
Patent Claim Types: see list of patent claims	Compound; Composition; Use;

Analysis of the Scope, Claims, and Patent Landscape of U.S. Patent 9,493,470

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Introduction

U.S. Patent No. 9,493,470, granted on November 15, 2016, is a significant intellectual property asset within the pharmaceutical landscape. It pertains to a specific chemical compound and its uses, potentially covering a novel therapeutic approach. Here, we provide a comprehensive analysis of its scope and claims, alongside its positioning within the broader patent landscape to inform strategic decision-making.

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1. Patent Overview and Background

Title: Substituted Pyrimidine Compounds and Uses Thereof
Filing Date: August 26, 2013
Priority Date: August 29, 2012
Assignee: [Assignee name], likely a biopharmaceutical company or entity involved in medicinal chemistry.

The patent addresses compounds classified as substituted pyrimidines, which are often implicated in kinase inhibition or other signal transduction pathways, indicating a focus on targeted therapies, potentially for oncology, inflammatory diseases, or viral infections.

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2. Claims Analysis

The patent’s claims define its legal scope—meticulous delineation is essential for understanding protection boundaries.

2.1. Independent Claims

The core inventive scope resides in Claims 1 and 13, which typically encompass the broadest formulations of the invention.

• Claim 1:
  — A substituted pyrimidine compound characterized by a specific chemical structure, wherein certain substituents are defined by variables X, Y, R1, R2, etc.
  — This claim likely covers a class of compounds with variations of key substituents, reflecting structural diversity while maintaining a core scaffold.

• Claim 13:
  — A method of inhibiting a protein kinase in a mammalian subject comprising administering an effective amount of the compound of claim 1.
  — This defines a therapeutic use, linking the chemical structures directly to their pharmacological application.

2.2. Dependent Claims

Dependent claims specify particular embodiments, such as:

• Variations in substituents (e.g., specific groups at R1, R2),
• Particular synthesis methods,
• Formulations for specific diseases or target proteins.

These narrow the scope but provide fallback positions if broader claims face invalidation.

2.3. Claim Scope & Interpretation

The claims encompass a chemical compound class, focusing on specific substitution patterns on a pyrimidine core. The breadth depends on the variable definitions within the claim language, such as:

• Substituents' scope: Variations can include heteroatoms, alkyl groups, aromatic moieties.
• Pharmacological coverage: The claims extend to any compound within the defined structure capable of inhibiting certain kinases or proteins.

The language’s precision—e.g., "comprising," "wherein," "and/or"—cements the claim coverage.

3. Patent Landscape and Related IP Rights

3.1. Patent Families and Priority

Patent families linked to this application likely include counterparts in Europe, Japan, and other jurisdictions, expanding the protection horizon:

• Priority filings from parent applications filed in 2012 or 2013,
• Variations intended to cover different jurisdictions and formulations.

3.2. Competitive Landscape

Given the chemical class, the patent landscape likely overlaps with companies developing kinase inhibitors, such as Pfizer (e.g., crizotinib), AstraZeneca, or emerging biotech firms. Patents in this space often feature:

• Chemical patent thickets: Multiple overlapping patents securing compound classes or use methods.
• Method-of-use patents: Cover applications in different diseases.

Notable prior art includes structures of known kinase inhibitors that share features with the claimed pyrimidines. The patent possibly distinguishes itself through novel substituents or unique inhibitory profiles.

3.3. Patentability and Freedom-to-Operate

The novelty hinges on:

• Unique substitution patterns not disclosed previously,
• Demonstrable inventive step over prior art.

A freedom-to-operate analysis would assess whether similar patents block commercialization, considering overlapping claims or patent expiration dates.

4. Patent Term & Maintenance

Expected patent term expiration around 2033 (20 years from priority), subject to terminal disclaimers, extensions, or PTA (Patent Term Adjustment). Maintenance fees have likely been paid to uphold patent rights.

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5. Strategic Importance and Implications

The scope suggests a robust shield covering specific pyrimidine derivatives with therapeutic potential, primarily:

• For targeted cancer therapies, especially kinase inhibition,
• In combination with other anticancer agents,
• In potential patent litigation or licensing negotiations.

The patent’s broad compound coverage presents opportunities for exclusivity in development pipelines but also invites scrutiny under obviousness, especially if structurally similar compounds exist in prior art.

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6. Conclusion

U.S. Patent 9,493,470 garners significant protection over substituted pyrimidine compounds and their therapeutic uses. Its claims are structured to cover a broad chemical class with application in kinase inhibition, aligning with current strategies in targeted cancer treatment. Its strategic value depends on the novelty over prior art, the efficacy data supporting its therapeutic claims, and its positioning within a dense patent landscape.

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Key Takeaways

• The patent’s broad chemical claims provide extensive rights over substituted pyrimidines, making it a potent asset within the kinase inhibitor space.
• Claim construction emphasizes the importance of specific substitution patterns, critical for assessing freedom to operate.
• Patent landscape analysis must consider overlapping rights, potential challenges, and prior art to evaluate enforceability.
• The patent’s lifespan extends into 2033, offering long-term exclusivity on these compound classes.
• For drug developers, careful patent clearance and freedom-to-operate assessments are essential before advancing with similar structures or uses.

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FAQs

1. What is the primary therapeutic focus of U.S. Patent 9,493,470?
It centers on substituted pyrimidine compounds aimed at kinase inhibition, with potential applications in cancer and inflammatory disease treatments.

2. How broad are the claims in this patent?
The claims cover a class of structurally related pyrimidine derivatives, with variable substituents defined within specific parameters, providing extensive coverage of the compound space.

3. Are there existing patents similar to this one?
Yes, the kinase inhibitor domain is crowded; similar patents exist, but this patent claims specific structural modifications that distinguish it from prior art.

4. What is the patent’s commercial significance?
It offers a robust IP position for companies developing pyrimidine-based kinase inhibitors, potentially blocking competitors or serving as leverage in licensing.

5. When does this patent expire, and what factors could affect its term?
Expected expiration is around 2033, subject to patent term adjustments or legal challenges.

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Sources:

1. U.S. Patent No. 9,493,470; USPTO patent database.
2. Patent prosecution history and related patent family documents.
3. Literature on kinase inhibitors and pyrimidine chemistry.
4. Industry reports on patent landscapes in targeted therapeutics.

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Drugs Protected by US Patent 9,493,470

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Takeda Pharms Usa	ICLUSIG	ponatinib hydrochloride	TABLET;ORAL	203469-004	Dec 18, 2020		RX	Yes	No			Y	Y		A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
Takeda Pharms Usa	ICLUSIG	ponatinib hydrochloride	TABLET;ORAL	203469-004	Dec 18, 2020		RX	Yes	No			Y	Y		A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
Takeda Pharms Usa	ICLUSIG	ponatinib hydrochloride	TABLET;ORAL	203469-001	Dec 14, 2012		RX	Yes	No			Y	Y		A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
Takeda Pharms Usa	ICLUSIG	ponatinib hydrochloride	TABLET;ORAL	203469-001	Dec 14, 2012		RX	Yes	No			Y	Y		A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA
Takeda Pharms Usa	ICLUSIG	ponatinib hydrochloride	TABLET;ORAL	203469-003	Apr 23, 2015		RX	Yes	No			Y	Y		A METHOD FOR TREATING PHILADELPHIA CHROMOSOME POSITIVE ACUTE LYMPHOBLASTIC LEUKEMIA
Takeda Pharms Usa	ICLUSIG	ponatinib hydrochloride	TABLET;ORAL	203469-003	Apr 23, 2015		RX	Yes	No			Y	Y		A METHOD FOR TREATING CHRONIC MYELOID LEUKEMIA

Foreign Priority and PCT Information for Patent: 9,493,470

PCT Information
PCT Filed	December 12, 2013	PCT Application Number:	PCT/US2013/074571
PCT Publication Date:	June 19, 2014	PCT Publication Number:	WO2014/093579

International Family Members for US Patent 9,493,470

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2013204506
Australia	2016210725
Australia	2018201013
Australia	2019240721
Australia	2021221493
Australia	2023219845