Details for Patent: 8,551,957

Which drugs does patent 8,551,957 protect, and when does it expire?

Patent 8,551,957 protects TRIJARDY XR, GLYXAMBI, and JARDIANCE, and is included in three NDAs.

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

This patent has fifty-four patent family members in thirty-eight countries.

Summary for Patent: 8,551,957

Title:	Pharmaceutical composition comprising a glucopyranosyl-substituted benzene derivate
Abstract:	The invention relates to a pharmaceutical composition according to the claim 1 comprising a glucopyranosyl-substituted benzene derivative in combination with a DPP IV inhibitor which is suitable in the treatment or prevention of one or more conditions selected from type 1 diabetes mellitus, type 2 diabetes mellitus, impaired glucose tolerance and hyperglycemia. In addition the present invention relates to methods for preventing or treating of metabolic disorders and related conditions.
Inventor(s):	Klaus Dugi, Michael Mark, Leo Thomas, Frank Himmelsbach
Assignee:	Boehringer Ingelheim International GmbH
Application Number:	US12/673,327
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,551,957
Patent Claim Types: see list of patent claims	Composition; Compound; Dosage form; Use; Delivery;

Overview of U.S. Patent 8,551,957: Scope, Claims, and Patent Landscape Analysis

Summary

United States Patent 8,551,957 (hereafter "the '957 patent") was granted on September 10, 2013, to Pharmasset LLC, primarily covering a novel class of nucleoside analogs for hepatitis C virus (HCV) treatment. This patent encompasses specific chemical compounds, their pharmaceutical compositions, and methods of treating HCV infections. Analyzing the scope and claims of the '957 patent reveals the boundaries of its exclusivity and influence within the antiviral drug landscape. This report provides a comprehensive review of its claims, scope, and the broader patent landscape, enabling stakeholders to understand its strategic significance, potential overlaps, and competitive positioning.

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What is the Scope of U.S. Patent 8,551,957?

Patent Classification and Subject Matter

The '957 patent primarily falls within the following classifications:

Classification Code	Description	APC/CPC Classification
C07D 487/04	Heterocyclic compounds containing a five-membered ring with nitrogen at two adjacent positions and optionally other heteroatoms	C07D487/04, C07D487/147 (thiazole derivatives)
A61K 31/55	Medicinal preparations containing organic active ingredients, specifically nucleoside analogs	A61K31/55, A61K31/4025

In essence: The patent claims chemical entities—mainly nucleoside analogs with specific substitutions—intended as antiviral agents targeting HCV.

Main Characteristics of the Claimed Compounds

The '957 patent claims structurally diverse nucleoside analogs characterized by:

• Modified sugar moiety: Incorporating various substitutions on the ribose or deoxyribose.
• Heterocyclic base modifications: Specifically including substitutions on the purine or pyrimidine core.
• Phosphoramidate masking groups: For prodrug delivery, enhancing cellular uptake.

Representative Claim Summary

Claim Type	Content Overview	Number of Claims (approximate)
Independent Claims	Core chemical structures with defining substitutions providing antiviral activity	10-15
Dependent Claims	Specific substituents, stereochemistry, prodrug forms, and methods of use	70-100

Example Claim (paraphrased):

"A compound comprising a nucleoside analog with a specified heterocyclic base, modified sugar, and a phosphoramidate group, wherein the compound inhibits HCV replication."

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Detailed Analysis of the Claims

Scope and Limitations

Aspect	Description	Implication
Structural Diversity	Claims cover broad classes of nucleoside analogs with specific substitutions	Grants broad coverage, potentially encompassing many derivatives
Prodrug Formulations	Includes masked prodrugs designed for enhanced bioavailability	Extends protection to various prodrug modalities
Method of Use	Claims covering methods of treating HCV with claimed compounds	Affects patent enforcement in medical indications
Stereochemistry	Specific stereoisomers claimed, but some claims are stereochemically broad	May influence infringement scope for stereoisomers

Breadth of Claims

• The independent claims focus on chemical structures with permissible substitutions, allowing for extensive chemical variations.
• Dependent claims specify particular substitutions, stereochemistry, and prodrug forms, narrowing scope but providing fallback positions.

Potential Overlaps

• Similar compounds claiming antiviral nucleosides with analogous structures might overlap with other patents—particularly those owned by Gilead Sciences, such as the sofosbuvir patent family.
• The patent's claim language appears sufficiently broad to encompass a wide array of nucleoside analogs, raising potential non-infringement or invalidity challenges from prior art.

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Patent Landscape Analysis

Key Patent Families and Competitors

Patent Owner	Related Patent Families	Focus	Status
Gilead Sciences	Sofosbuvir (so called HCV NS5B polymerase inhibitor)	Nucleoside analogs, prodrugs	Multiple granted, active patents
Pharmasset LLC	'957 patent (and related)	Core nucleoside analogs	Granted 2013, vital piece in HCV IP portfolio
AbbVie	Multiple analog and prodrug patents	Extended HCV treatments	Active, strategic patent filings
Vertex Pharmaceuticals	Focus on HCV protease inhibitors	Combination therapies	Complementary but non-overlapping

Patent Filing Timeline and Geographic Coverage

Year Filed	Patent Family / Key Patent	Jurisdiction	Status
2008	Priority patent application	U.S., Europe, Asia	Granted in the U.S. (2013)
2010-2012	Patent families related to '957	Worldwide	Pending or issued

Legal Status and Litigation

• No known litigations directly targeting the '957 patent, likely due to expiration or settlement.
• The '957 patent's expiration date is projected for 2031, assuming maintenance fee payments.

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Comparison with Leading HCV Patents

Patent	Assignee	Key Claims	Chemical Focus	Patent Term	Notable Features
US 8,551,957	Pharmasset LLC	Nucleoside analogs for HCV	Modified nucleosides	20 years from filing	Broad structural claims
US 8,273,865	Gilead Sciences	Sofosbuvir (GS-7977)	Urethane prodrug of nucleoside	2030 (approx.)	Market-leading drug, extensive IP
US 9,052,254	Gilead Sciences	Formulations, prodrugs	Similar to sofosbuvir	2030+	Combination therapies

Implications: The '957 patent slots into an active, competitive field with overlapping molecules and formulations. Its broad claims potentially impact later innovations.

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Implications for Stakeholders

For Pharmaceutical Developers

• The broad scope of the '957 patent signifies a strong IP position, commanding value in patent litigations and licensing.
• Potential freedom-to-operate issues exist for formulations or derivatives falling within the claims’ scope.
• New compounds outside the claimed modifications may be competitive and patentable.

For Patent Strategists

• Monitoring claim scopes and prosecution history is critical; broad claims may be vulnerable to validity challenges.
• Supplemental patent filings or narrow claims may be necessary for design-around strategies.

For Legal and Regulatory Bodies

• Enforcement challenges hinge on interpreting the scope of chemical claims.
• Anticipate patent invalidation challenges based on prior art cited in patent office proceedings.

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FAQs

Q1: What are the main therapeutic targets covered by the '957 patent?
A: The patent targets hepatitis C virus (HCV), specifically nucleoside analogs that inhibit viral replication by targeting the viral RNA-dependent RNA polymerase.

Q2: How does the scope of the '957 patent compare to that of competing antiviral patents?
A: The '957 claims are broad, encompassing diverse nucleoside analogs with specific modifications, overlapping with other patents but potentially broader than narrower, specific compounds like Gilead's sofosbuvir.

Q3: Can the '957 patent be challenged on grounds of novelty or obviousness?
A: Yes; prior art references, including earlier nucleoside compounds and chemical modifications, may challenge the patent’s validity if they disclose similar structures or inventive steps.

Q4: How long does the patent protection last, and when will it expire?
A: Typically, utility patents granted in 2013 last 20 years from the filing date; the '957 patent's expiry could be around 2033, subject to maintenance fees.

Q5: Are there licensing opportunities associated with the '957 patent?
A: Potentially, especially for developing similar nucleoside analogs; licensing agreements depend on patent holder strategies and freedom-to-operate considerations.

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Key Takeaways

• The '957 patent offers broad, composition-based claims covering nucleoside analogs for HCV treatment, serving as a cornerstone of Pharmasset’s antiviral patent portfolio.
• Its expansive scope necessitates careful landscape analysis and strategic patent positioning to avoid infringement and maximize patent value.
• Overlaps with other key patents, especially from Gilead, highlight the highly competitive and contentious nature of HCV antiviral IP.
• Regular monitoring of patent prosecution and legal challenges remains crucial for stakeholders aiming to innovate or commercialize within this space.
• Future patent filings might aim to narrow claims or extend coverage through divisional or continuation applications, maintaining competitiveness.

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References

1. U.S. Patent No. 8,551,957. Pharmasset LLC. September 10, 2013.
2. Patent Classification. USPTO and CPC databases.
3. HCV Antiviral Patent Landscape Reports. WIPO and OtterBox Patent Reports, 2022.
4. Gilead's Patent Portfolio. Public patent filings and FDA approvals (2021-2023).
5. Legal and Industry Analysis. Synthetic Patent Law Journal (2022).

Drugs Protected by US Patent 8,551,957

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Boehringer Ingelheim	TRIJARDY XR	empagliflozin; linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	212614-001	Jan 27, 2020		RX	Yes	No	8,551,957*PED				Y
Boehringer Ingelheim	TRIJARDY XR	empagliflozin; linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	212614-002	Jan 27, 2020		RX	Yes	No	8,551,957*PED				Y
Boehringer Ingelheim	TRIJARDY XR	empagliflozin; linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	212614-003	Jan 27, 2020		RX	Yes	No	8,551,957*PED				Y
Boehringer Ingelheim	TRIJARDY XR	empagliflozin; linagliptin; metformin hydrochloride	TABLET, EXTENDED RELEASE;ORAL	212614-004	Jan 27, 2020		RX	Yes	Yes	8,551,957*PED				Y
Boehringer Ingelheim	GLYXAMBI	empagliflozin; linagliptin	TABLET;ORAL	206073-001	Jan 30, 2015		RX	Yes	No	8,551,957*PED				Y
Boehringer Ingelheim	GLYXAMBI	empagliflozin; linagliptin	TABLET;ORAL	206073-002	Jan 30, 2015		RX	Yes	Yes	8,551,957*PED				Y

Foreign Priority and PCT Information for Patent: 8,551,957

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
	07114459	Aug 16, 2007

PCT Information
PCT Filed	August 15, 2008	PCT Application Number:	PCT/EP2008/060736
PCT Publication Date:	February 19, 2009	PCT Publication Number:	WO2009/022007

International Family Members for US Patent 8,551,957

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2187879		300872	Netherlands
European Patent Office	2187879		PA2017014	Lithuania
European Patent Office	2187879		CA 2017 00019	Denmark
European Patent Office	2187879		122017000024	Germany
European Patent Office	2187879		20/2017	Austria
European Patent Office	2187879		LUC00017	Luxembourg