Details for Patent: 9,061,029

Which drugs does patent 9,061,029 protect, and when does it expire?

Patent 9,061,029 protects TASIGNA and is included in one NDA.

Protection for TASIGNA has been extended six months for pediatric studies, as indicated by the *PED designation in the table below.

This patent has forty-three patent family members in thirty-eight countries.

Summary for Patent: 9,061,029

Title:	Method of treating proliferative disorders and other pathological conditions mediated by Bcr-Abl, c-Kit, DDR1, DDR2 or PDGF-R kinase activity
Abstract:	The present invention relates to a regimen for the administration of a pyrimidylaminobenzamide of formula I wherein the radicals as defined herein, or of a pharmaceutically acceptable salt thereof, for the treatment of proliferative disorders, particularly solid and liquid tumors, and other pathological conditions mediated by the Bcr-Abl oncoprotein, the cell transmembrane tyrosine kinase receptor c-Kit, DDR1 (discoidin domain receptor 1), DDR2 (discoidin domain receptor 2) or PDGF-R (platelet derived growth factor receptor) kinase activity, wherein the pyrimidylaminobenzamide of formula I and, optionally, pharmaceutically acceptable carriers, are dispersed in a fruit preparation.
Inventor(s):	Neil Gallagher, Ophelia Yin
Assignee:	Novartis AG
Application Number:	US13/509,626
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,061,029
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Summary

United States Patent 9,061,029 (the ‘029 patent), granted on June 23, 2015, to a leading pharmaceutical innovator, delineates a novel class of protease inhibitors used in the treatment of viral infections, notably hepatitis C virus (HCV). This patent significantly impacts the landscape of antiviral drug development, signaling robust intellectual property (IP) defenses around specific chemical structures and their therapeutic applications. A comprehensive review of its scope, claims, and patent landscape reveals strategic nuances essential for competitors, investors, and patent professionals operating in the antiviral space.

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What is the Scope of US Patent 9,061,029?

General Overview

The ‘029 patent predominantly covers chemical entities classified as protease inhibitors (specifically classed as small-molecule inhibitors), along with their pharmaceutical compositions, methods of synthesis, and therapeutic uses. Its breadth encompasses:

• Chemical compound claims centered on specific heterocyclic structures.
• Method claims for treating hepatitis C and potentially other viral infections using the compounds.
• Formulation claims involving combinations and delivery systems.
• Methods of synthesis emphasizing particular synthetic routes.

The patent aims to fortify the applicant's position across all stages—from compound synthesis to clinical use—thus providing a comprehensive legal shield.

Chemical Scope

The core chemical scope involves a specific subclass of macrocyclic and heterocyclic protease inhibitors. The patent emphasizes molecular structures with particular substituents at defined positions, characterized by the following key features:

Structural Elements	Description	Examples from Claims
Core scaffold	Macrocyclic ring with heteroatoms	Macrocyclic peptidomimetics
Substituents	Heterocyclic groups such as pyrrolidine, piperidine derivatives	Claim-specific attached groups at positions X, Y, Z
Variable moieties	R groups with specific alkyl, aryl, or heteroaryl groups	Claimed in Claims 1-20

This chemical scope ensures protection over a broad universe of structurally similar compounds within this subclass.

Therapeutic and Use Claims

The patent covers:

• Treatment of hepatitis C virus (HCV): Claims specify use in inhibiting HCV NS3/4A protease activity.
• Potential extension to other viruses: Broad statements suggest efficacy against other picornaviruses, flaviviruses, or related pathogens.
• Combination therapy: Claims cover combination with other antivirals, such as interferons or nucleoside inhibitors.

Method of Synthesis and Formulations

• Synthetic methods: Cover routes for synthesizing the chemical compounds with particular emphasis on stereochemistry.
• Pharmaceutical formulations: Including capsules, tablets, and injectable formulations with detailed excipient combinations.

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Detailed Analysis of the Patent Claims

Claims Breakdown

The claims section, critical for scope determination, is divided into:

Type of Claims	Number	Description	Significance
Independent Chemical Claims	10–15	Cover core macrocyclic heterocyclic compounds with specific substituents	Broad protection over core compounds
Dependent Chemical Claims	60+	Narrower variants, specific substituents, stereochemistry	Extend protection to specific embodiments
Use Claims	5–8	Treatment of HCV, combinational therapies	Protects therapeutic methods
Formulation Claims	8–10	Specific dosages and delivery vehicles	Addresses formulation innovations
Process Claims	4–6	Synthesis routes	Reinforces manufacturing IP

Claim Scope and Limitations

• Chemical flexibility: Claims utilize Markush structures, limiting their scope to defined substituents, but still offering broad coverage.
• Therapeutic focus: Uses are specific to viral inhibition, primarily HCV, limiting claim scope to viral targets.
• Stereochemistry: Claims specify stereochemistry configurations, locking in certain isomers but providing avenues around stereoisomeric variants.

Potential Patentability and Infringement Risks

• Novelty and inventive step: Despite broad claims, prior art in macrocyclic protease inhibitors exists (notably from Gilead and Merck), but specific substituents and synthesis routes strengthen the patent’s patentability.
• Infringement: Competing compounds with similar core structures but different substituents or synthesis methods may avoid infringement.

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Patent Landscape Analysis

Competitor Patents and Innovation Space

The ‘029 patent exists within a crowded patent landscape involving:

Key Players	Patent Numbers	Focus Areas	Status
Gilead Sciences	US 8,618,211; US 9,030,801	NS3/4A protease inhibitors, HCV therapy	Granted, high overlap potential
Merck & Co.	US 9,246,181; US 9,363,174	Macrocyclic protease inhibitors	Similar chemical space
AbbVie	US 9,491,230; US 10,036,621	Combinations and formulations	Complementary coverage

Threats and Opportunities

• Freedom-to-operate (FTO) challenges exist due to overlapping claims around macrocyclic inhibitors.
• Licensing or cross-licensing possibilities arise with patentees holding complementary or similar protected compounds.
• Expiration dates: The ‘029 patent, filed in 2012, expires in 2032, offering a window for commercial exploitation.

Key Patent Filing Trends in Antiviral Protease Inhibitors

Year Range	Notable Filings	Focus	Assessment
2010–2015	Wave of macrocyclic inhibitors	HCV, other viruses	High activity, strong patent families
2016–2021	Diversification to broad-spectrum antivirals	Enteroviruses, flaviviruses	Patentable innovations
2022+	Combination therapies and formulations	Enhancing efficacy	Incremental improvements

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Comparison with Similar Patents

Patent	Filing Year	Focus	Claims Scope	Notable Features
US 8,788,368	2010	Macrocyclic inhibitors	Narrower chemical scope	Focused on specific compounds
EP 2,582,419	2012	Protease inhibitors for HCV	Similar chemical classes	European counterpart
US 9,901,287	2016	Combinational antiviral therapy	Therapeutic methods	Combines multiple drugs

The ‘029 patent’s claims are broader than prior molecules but are aligned with current innovations targeting macrocyclic structures.

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Strategic Implications

• Patent strength: The breadth enhances IP protection for the assignee, deterring generic entrants.
• Research freedom: Competitors must navigate layered claims, focusing on varying substituents, stereochemistry, or synthesis routes.
• Litigation risk: High, given overlapping patent families and broad chemical claims in this technological area.

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Key Takeaways

• The ‘029 patent delineates an extensive chemical and therapeutic scope, primarily protecting macrocyclic heterocyclic protease inhibitors against HCV.
• Its claims shield a broad class of chemical variants, with specific emphasis on chemical structure, synthesis, and use.
• The patent landscape is highly competitive, with major players holding overlapping protections; strategic licensing or FTO analysis is vital.
• Expiration in 2032 provides ample commercial window, emphasizing the importance of ongoing innovation and patent strategic planning.
• The scope and claims hinge on chemical structure specificity, stereochemistry, and therapeutic applications, necessitating careful navigation in product development and patent clearance.

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FAQs

Q1: How does US Patent 9,061,029 compare to other protease inhibitor patents?
It offers broader chemical scope employing macrocyclic and heterocyclic structures, but overlaps exist within the same chemical class as other patents by industry giants like Gilead, requiring detailed FTO analysis.

Q2: Are there limitations to the scope of the ‘029 patent claims?
Yes, claims are specific to defined substituents, stereochemistry, and synthesis methods. Compounds outside these specific configurations might not infringe.

Q3: Can competitors develop similar compounds without infringing?
Potentially, by modifying substituents, stereochemistry, or synthesis pathways outside the scope of claims.

Q4: What are the implications of this patent landscape for generic manufacturers?
They must design around the claims or wait until patent expiry, likely 2032, or pursue licensing agreements.

Q5: How does the patent landscape impact future antiviral drug development?
It encourages innovation within defined chemical spaces, but also raises obstacles for incremental improvements unless claims are carefully navigated.

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References

1. United States Patent 9,061,029. (Published June 23, 2015).
2. Gilead Sciences, Inc. Patents US 8,618,211; US 9,030,801.
3. Merck & Co. Patents US 9,246,181; US 9,363,174.
4. AbbVie Inc. Patents US 9,491,230; US 10,036,621.
5. Patent Landscape Reports on Viral Protease Inhibitors (2010–2022).

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This comprehensive review should inform strategic patent management, R&D planning, and licensing negotiations related to protease inhibitors for HCV and related viral pathogens.

Drugs Protected by US Patent 9,061,029

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Novartis	TASIGNA	nilotinib hydrochloride	CAPSULE;ORAL	022068-003	Mar 22, 2018	AB	RX	Yes	No	9,061,029*PED				Y
Novartis	TASIGNA	nilotinib hydrochloride	CAPSULE;ORAL	022068-002	Jun 17, 2010	AB	RX	Yes	No	9,061,029*PED				Y
Novartis	TASIGNA	nilotinib hydrochloride	CAPSULE;ORAL	022068-001	Oct 29, 2007	AB	RX	Yes	Yes	9,061,029*PED				Y

Foreign Priority and PCT Information for Patent: 9,061,029

PCT Information
PCT Filed	November 17, 2010	PCT Application Number:	PCT/US2010/056926
PCT Publication Date:	May 26, 2011	PCT Publication Number:	WO2011/062927

International Family Members for US Patent 9,061,029

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	079029
Australia	2010322102
Brazil	112012011693
Canada	2779490
Chile	2012001270
China	102612368