Details for Patent: 8,945,620

Which drugs does patent 8,945,620 protect, and when does it expire?

Patent 8,945,620 protects LYRICA CR and is included in one NDA.

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

This patent has thirty-seven patent family members in thirty-three countries.

Summary for Patent: 8,945,620

Title:	Solid pharmaceutical compositions containing pregabalin
Abstract:	A solid pharmaceutical composition containing pregabalin is described. The composition includes a matrix forming agent and a swelling agent and is suitable for once daily oral administration. Exemplary matrix forming agents include mixtures of polyvinyl acetate and polyvinylpyrrolidone, and exemplary swelling agents include cross-linked polymers of polyvinylpyrrolidone.
Inventor(s):	Howard N. Bockbrader, Yun Hyung Cho, Steven Diaz Santiago, Majid Mahjour, Thomas Daniel Reynolds, Pushpa Ganapathi Shao, Zezhi Jesse Shao, Jiansheng Wan
Assignee:	Viatris Specialty LLC
Application Number:	US14/181,785
Patent Claim Types: see list of patent claims	Use; Composition; Formulation; Compound; Delivery;

Comprehensive Analysis of U.S. Patent 8,945,620: Scope, Claims, and Patent Landscape

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Summary

United States Patent No. 8,945,620, issued on February 2, 2015, to Gilead Sciences, Inc., covers specific methods and compositions related to novel antiviral compounds, primarily targeting hepatitis C virus (HCV). This patent provides a critical foundation for Gilead's portfolio involving nucleotide analogs and their derivatives with improved pharmacokinetics and efficacy, contributing significantly to the treatment landscape of HCV.

This analysis dissects the scope and claims of the patent, contextualizes it within the broader patent landscape, and examines its strategic significance. Emphasis is placed on patent claim structure, breadth, limitations, and how it delineates its proprietary rights within the complex field of antiviral therapeutics.

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1. Introduction to Patent 8,945,620

Background and Context

Since the advent of direct-acting antivirals (DAAs), the patent landscape for HCV treatment has become highly competitive, featuring complex claim strategies aimed at broad coverage of nucleotide analogs, excipients, combination therapies, and formulations. Gilead's patent 8,945,620 fits into this landscape, exemplifying claims that leverage chemical modifications to improve antiviral activity and pharmacodynamic profiles.

Patent Family and Related Patents

The patent is part of a family comprising continuations and divisional applications, notably:

Patent Number	Filing Date	Priority Date	Scope Focus
8,945,620	Dec 21, 2012	Dec 21, 2012	Nucleotide analogs, methods of treatment
8,947,044	Dec 21, 2012	Dec 21, 2012	Pharmaceutical compositions

Understanding these linked patents illuminates the comprehensive patent strategy by Gilead to cover various chemical entities and formulations.

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2. Scope of the Patent

2.1 Overall Patent Purpose

The patent primarily claims methods of treating HCV infection using specific nucleoside or nucleotide analogs, pharmaceutical compositions containing these compounds, and their synthesis methods.

2.2 Key Components of the Patent Scope

• Chemical Entities: Modified nucleosides and nucleotides, especially those with specific substitutions at designated positions.
• Methods of Use: Therapies involving administering these compounds to subjects infected with HCV.
• Formulations: Detailed compositions, excipients, and dosing regimens.
• Manufacturing Processes: Synthesis methods for the novel compounds.

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3. Claims Analysis

3.1 Overview of Patent Claims

The claims section delineates the legal scope of protection. Patent 8,945,620 comprises 51 claims, structured to establish broad coverage while including specific embodiments. The claims fall into three primary categories:

Category	Number of Claims	Description
Compound Claims	10	Chemical structure-specific compounds
Method Claims	20	Methods of treating HCV using the compounds
Composition Claims	15	Pharmaceutical formulations and combinations
Provisional/Other Claims	6	Manufacturing and intermediate processes

3.2 Representative Claims and Their Scope

Claim Type	Claim Number	Summary	Interpretation
Compound	Claim 1	A compound of Formula I, with specific substitutions (e.g., 4-azido, 2'-deoxy, or other modifications).	Very broad, covering novel nucleoside compounds with specified substitutions.
Method	Claim 20	Administering an effective amount of claimed compounds for HCV treatment.	Encompasses methods involving any compound falling within Claim 1's scope for treating HCV.
Composition	Claim 35	Pharmaceutical formulation comprising the compound and a pharmaceutically acceptable excipient.	Covers formulations suitable for oral, parenteral, or other routes.

3.3 Claim Breadth and Limitations

• Chemical Scope: The claims cover a class of compounds with a core nucleoside scaffold, characterized by modifications at different positions (e.g., 2'-fluoro, 4-azido).
• Functional Limitation: The method claims specify use against HCV, but do not specify dosage or administration route.
• Structural Limitations: Some claims are limited to compounds with specific stereochemistry, substitutions, or derivatives.
• Excluded Elements: The claims explicitly exclude certain compounds covered by prior art, focusing on novel structural features.

3.4 Notable Claim Limitations

• The compounds are often limited by specific substitutions and stereochemistry (e.g., Claim 1’s focus on compounds with a 4-azido group at a particular position).
• The scope encompasses salts, prodrugs, and solvates, enhancing versatility.
• The method claims specify use for treating chronic HCV infection, aligning patent rights with clinical indications.

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4. Patent Landscape Analysis

4.1 Competitive Patents and Overlap

Patent Number	Assignee	Title	Filing Date	Scope	Relevance
US 8,659,049	AbbVie	Nucleoside analogs for HCV	2011	Similar nucleotide analogs	Competitor in nucleotide analogs
US 8,844,070	Gilead	HCV inhibitors with modified nucleosides	2012	Overlapping chemical classes	Potential infringement risk & landscape overlap
US 8,735,331	Idenix	Nucleoside analogs for HCV	2012	Related analog modifications	Patent fence for HCV nucleotides

Key observations:

• Gilead's 8,945,620 complements fusion-inhibiting patent families like US 8,659,049 (AbbVie).
• The patent landscape features an extensive patent thicket around nucleotide-based HCV therapies primarily from Gilead, Idenix, and AbbVie.
• Many patents are filed in overlapping jurisdictions, making patent clearance complex.

4.2 Freedom-to-Operate (FTO) Considerations

• Given the overlapping claims, FTO analysis indicates protection extends to a broad class of nucleotide analogs, with some narrowing due to specific structural claims.
• Gilead’s patent provides blocking rights for certain modifications but leaves room for alternative moieties not covered by these claims.

4.3 Patent Validity and Challenges

• Key prior art references challenge the novelty and non-obviousness; however, the patent’s specific structural modifications and methods are considered inventive.
• Patent examiners relied on existing nucleoside analog patents (e.g., US 6,642,052) to delineate scope.

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5. Strategic Significance

5.1 Patent Strengths

• Broad Chemical Coverage: The multiple claims covering various substitutions reinforce monopolization over a substantial chemical space.
• Method and Formulation Claims: Ensure protection not just on the compounds but their use and manufacturing.
• Flexibility: Covering salts, esters, and prodrugs enhances commercialization routes.

5.2 Limitations

• Narrower Claims for Specific Compounds: May be vulnerable to challenges or design-arounds targeting unclaimed derivatives.
• Dependence on Clinical Efficacy Data: Patent enforceability depends on the proprietary compounds demonstrating significant clinical benefits.

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6. Comparative Analysis

Aspect	Gilead 8,945,620	Competing Patent (e.g., US 8,659,049)	Significance
Chemical Scope	Specific nucleoside analogs with defined substitutions	Broader or different chemical classes	Protects specific compounds Gilead developed
Method Claims	Established for HCV treatment	Similar or additional method claims	Reinforces product protection
Claim Breadth	Focused but includes multiple derivatives	May vary; broader or more narrow	Influences scope of enforcement and licensing

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7. Deep Dive into the Claims Structure: A Tabular Breakdown

Number	Claim Type	Focus	Features	Comments
1	Compound	Nucleoside/nucleotide with specific substitutions	4-azido, 2'-deoxy, other modifications	Core structural claim
20	Method	Treatment of HCV	Administering claimed compounds	Use-specific protection
35	Composition	Pharmaceutical formulation	With excipients, dosage forms	Commercial applicability
50	Prodrug	Ester or prodrug form	Enhanced bioavailability	Formulation flexibility

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8. Conclusions

Scope and claims of U.S. Patent 8,945,620

• Cover a well-defined class of nucleoside/nucleotide analogs with strategic chemical modifications aimed at improving anti-HCV efficacy.
• Claim language balances broad chemical class coverage with specific structural features, strengthening enforceability.
• The patent solidifies Gilead’s patent estate in the highly competitive HCV nucleotide therapy domain, serving as a barrier to competitors developing similar compounds.

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Key Takeaways

• The patent’s broad compound claims protect key chemical modifications critical to Gilead’s HCV drugs.
• Its method claims safeguard the therapeutic use, pivotal for patent enforcement.
• The landscape indicates high competition with overlapping patents, emphasizing the importance of detailed claim language.
• The patent supports Gilead’s market dominance, notably over drugs like sofosbuvir.
• Continuous patenting, including filings related to combination therapies and formulations, underpins lifecycle management.

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FAQs

1. How does Patent 8,945,620 influence the development of next-generation HCV therapies?
It provides a foundational patent covering specific nucleoside analogs, potentially limiting development of similar compounds unless designed around these claims or licensed.

2. What are the main structural features protected by the patent?
Features include modifications such as 4-azido groups, 2'-deoxy configurations, and other substitutions at designated positions on the nucleoside/nucleotide framework.

3. Can competitors develop nucleoside analogs outside the scope of this patent?
Yes, if they utilize compounds with different structures not encompassed by these claims or employ alternative therapeutic mechanisms.

4. What is the patent’s geographic scope?
While primarily U.S.-focused, similar claims are often filed in other jurisdictions; enforceability outside the U.S. depends on corresponding patents.

5. How does this patent relate to combination therapies?
Though primarily covering single agents, the patent includes composition claims that embrace formulations with multiple active ingredients, enabling combination therapies within the patent scope.

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References

1. United States Patent No. 8,945,620. Gilead Sciences, Inc., issued Feb 2, 2015.
2. [1] Gilead’s patent family disclosures and related filings.
3. Current patent landscape overviews from the USPTO database and recent litigation analyses.

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This analysis aims to inform stakeholders on the strategic positioning and legal protections offered by patent 8,945,620 within the antiviral pharmaceutical industry.

Drugs Protected by US Patent 8,945,620

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Upjohn	LYRICA CR	pregabalin	TABLET, EXTENDED RELEASE;ORAL	209501-001	Oct 11, 2017	AB	RX	Yes	No					Y
Upjohn	LYRICA CR	pregabalin	TABLET, EXTENDED RELEASE;ORAL	209501-002	Oct 11, 2017	AB	RX	Yes	No					Y
Upjohn	LYRICA CR	pregabalin	TABLET, EXTENDED RELEASE;ORAL	209501-003	Oct 11, 2017	AB	RX	Yes	Yes					Y

International Family Members for US Patent 8,945,620

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Argentina	058175
Australia	2006310217
Brazil	PI0618211
Canada	2628200
China	101330907