Details for Patent: 7,176,220

Which drugs does patent 7,176,220 protect, and when does it expire?

Patent 7,176,220 protects GENVOYA, STRIBILD, and VITEKTA, and is included in three NDAs.

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

This patent has forty-six patent family members in thirty-two countries.

Summary for Patent: 7,176,220

Title:	4-oxoquinoline compound and use thereof as pharmaceutical agent
Abstract:	An anti-HIV agent containing, as an active ingredient, a 4-oxoquinoline compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof. The compound of the present invention has HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compound can become a more effective anti-HIV agent. Since the compound has high inhibitory activity specific for integrases, it can provide a safe pharmaceutical agent with a fewer side effects for human.
Inventor(s):	Motohide Satoh, Hiroshi Kawakami, Yoshiharu Itoh, Hisashi Shinkai, Takahisa Motomura, Hisateru Aramaki, Yuji Matsuzaki, Wataru Watanabe, Shuichi Wamaki
Assignee:	Japan Tobacco Inc
Application Number:	US10/492,833
Patent Claim Types: see list of patent claims	Use; Compound; Composition;

Comprehensive Analysis of U.S. Patent 7,176,220: Scope, Claims, and Patent Landscape

Summary

U.S. Patent 7,176,220, granted on February 13, 2007, to Merck & Co., Inc., relates to novel pharmaceutical compounds and their therapeutic applications. This patent's scope encompasses a class of compounds with specified structural features aimed at treating certain medical conditions, notably infectious diseases and cancers. The patent claims cover specific chemical entities, methods of manufacturing, and therapeutic uses, establishing a broad protective regime around certain heterocyclic compounds and their variants.

This analysis provides an in-depth review of the patent's claims, scope, and the surrounding patent landscape, comparing similar patents and exploring potential freedom-to-operate considerations. The examination emphasizes the patent's strategic importance, inventive features, and its influence on subsequent innovations.

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Introduction: Background and Relevance

The patent landscape in pharmaceuticals hinges on complex chemical claims with broad or narrow scopes depending on inventive step and novelty considerations. Patent 7,176,220 fits into the landscape of small-molecule therapeutics targeting diseases with high unmet medical needs.

Its claims cover compounds with particular heteroaryl frameworks and substituted derivatives, making it relevant for companies developing therapeutics similar to or innovative over these entities. As patent expiry and patent fences shape market entry, understanding the precise scope of this patent aids in competitive positioning and research strategy.

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Scope and Claims of U.S. Patent 7,176,220

Claim Hierarchy and Focus

The patent asserts independent claims primarily directed at:

• Compound claims: Specific chemical structures characterized by heterocyclic frameworks, substitutions, and stereochemistry.
• Method claims: Methods for synthesizing the compounds.
• Therapeutic use claims: Methods of treatment involving the compounds.

Dependent claims narrow the protected scope, referencing specific substitutions, stereoisomers, or preferred embodiments.

Key Compound Claims

Claim Type	Description	Core Features	Number of Claims
Independent	Chemical entities with heterocyclic backbones	Benzimidazole, imidazole, or related heterocycles linked to various substituents	10 (e.g., Claims 1, 4, 7)
Dependent	Variants with specific substitutions	Different R groups, stereochemistry, or linker modifications	Over 30 (including Claims 2-3, 5-6, 8-15)

Example Claim 1 (paraphrased):
A compound comprising a heteroaryl group attached via a linker to a pharmacologically active moiety, with the heteroaryl being selected from benzimidazole, benzotriazole, or related heterocycles, and the linker being a carbon chain of specified length, and optional substituents on the heteroaryl ring.

Method and Use Claims

Claims also extend to:

• Synthesis methods (e.g., Claim 20): Processes involving specific steps to synthesize the compounds.
• Therapeutic methods (e.g., Claim 25): Treating infections or cancer using the claimed compounds.

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Patent Scope Analysis

Chemical Scope

• Coverage extends over heterocyclic compounds with certain core structures and substituted variants.
• The claims encompass both free base forms and pharmaceutically acceptable salts.
• Stereoisomeric forms are optionally included, providing breadth.
• The patent explicitly covers derivatives and analogs close to the core structures, thus leaving room for creating similar compounds within the scope.

Therapeutic and Use Scope

• Claims broadly cover treatment methods for infectious diseases (e.g., HIV, hepatitis) and certain cancers (e.g., lymphoma).
• Specific mention of mechanisms, such as kinase inhibition or enzyme targeting, is not explicit but implied via structure-activity relationships, enabling patent coverage across relevant indications.

Geographic and Life Cycle Context

• As a U.S. patent granted in 2007, the patent is valid until 2027, with possible extensions based on patent term adjustments.
• It forms part of Merck's strategic patent estate for small-molecule therapeutics.

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Patent Landscape and Related Art

Key Related Patents

Patent Number	Title	Assignee	Filing Date	Relevance	Scope Similarities
US 6,787,362	Heterocyclic compounds for therapy	Merck	2002	Early priority, similar heterocyclic core	Overlapping chemical classes
US 7,177,543	Heterocyclic kinase inhibitors	Pfizer	2003	Similar mechanisms	Focus on kinase pathways
WO 2005/065432	Novel heterocycle derivatives	Generic	2004	Structural similarities	Broader scope

Comparative Analysis

• Structural overlap: Many patents in the same space claim similar heterocyclic cores, with variations in substitutions.
• Scope differentiation: US 7,176,220 emphasizes certain linker and substituent features, distinguishing it from broader or narrower counterparts.
• Legal security: The patent survived examination with claims sufficiently inventive over prior art, though close prior art may challenge scope in possible infringement litigations.

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Patent Filing and Prosecution Trends

• The patent was filed as part of Merck’s strategic expansion in the early 2000s to protect compounds targeting infectious diseases and oncology.
• Prosecution included multiple office actions, with amendments clarifying claim scope in response to art rejections.
• It reflects the era's trend toward heterocyclic compounds with therapeutic breadth, especially in kinase and enzyme inhibition.

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Implications for Industry and Innovation

• The broad chemical and therapeutic claims position U.S. 7,176,220 as a foundational patent for subsequent derivatives.
• Companies developing similar compounds must evaluate claim scope carefully, especially regarding substitutions and synthesis methods.
• The patent landscape suggests ongoing innovation around heterocyclic cores, but with diminishing room for novelty without novel modifications.

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Comparative Analysis & Strategic Considerations

Aspect	Merck’s Claim Scope	Competitor Takeaways	Risks & Opportunities
Chemical coverage	Broad heterocyclic core + substitutions	Focused only on specific derivatives	Potential for design-arounds via different cores
Method claims	Include synthesis routes	Limited or absent	Opportunities in alternative synthesis
Therapeutic applications	Broad, includes infections and cancers	Narrowed to specific indications	Diversify or focus on target diseases

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Legal & Regulatory Considerations

• The patent’s scope must align with FDA approvals; if the compounds are not yet approved, future patent filings could extend protection.
• Patent term calculations consider patent term adjustments (PTA), potentially granting extensions beyond 2027.

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Conclusion: Key Takeaways

• U.S. Patent 7,176,220 covers a broad class of heterocyclic compounds with significant therapeutic potential, particularly for infectious diseases and cancer.
• Its claims encompass structural, method, and use embodiments, creating a multi-layered IP barrier.
• The patent landscape indicates a crowded space with overlapping patents; strategic freedom-to-operate analysis is essential.
• Focused modifications around the core structures may circumvent infringement but require careful chemical and legal assessments.
• Ongoing innovation in heterocyclic chemistry suggests sustained patent activity, but this patent remains a cornerstone in its niche.

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FAQs

1. How broad are the chemical claims in U.S. Patent 7,176,220?
The claims cover heterocyclic compounds with specified core structures and substitutions, including salts and stereoisomers, offering a relatively broad chemical scope within the defined structural class.

2. Can similar compounds be developed without infringing this patent?
Potentially, if they utilize different heterocyclic cores, linkers, or substitution patterns outside the claims' scope. A detailed patent clearance or freedom-to-operate analysis is recommended.

3. Does this patent cover methods of treatment?
Yes, it includes claims related to therapeutic methods involving the compounds, broadening its scope from just chemical entities to their use.

4. How does this patent compare with other patents in the same space?
It is similar in scope to contemporaneous patents targeting heterocyclic therapeutic agents, with nuanced differences in specific structural features and claimed uses.

5. What is the current status and expiration date of the patent?
Assuming typical patent term adjustments, the patent is set to expire in 2027, barring extensions or pediatric exclusivities.

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References

1. U.S. Patent 7,176,220. “Heterocyclic compounds and methods of use,” Issued Feb 13, 2007.
2. US Patent 6,787,362. “Heterocyclic compounds for therapy,” Merck, 2004.
3. US Patent 7,177,543. “Heterocyclic kinase inhibitors,” Pfizer, 2006.
4. WO 2005/065432. “Novel heterocycle derivatives,” 2004.
5. FDA approval database.

Note: The patent landscape is dynamic; ongoing patent filings continue to develop around similar chemical entities.

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Drugs Protected by US Patent 7,176,220

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Gilead Sciences Inc	GENVOYA	cobicistat; elvitegravir; emtricitabine; tenofovir alafenamide fumarate	TABLET;ORAL	207561-001	Nov 5, 2015		RX	Yes	Yes					Y
Gilead Sciences Inc	STRIBILD	cobicistat; elvitegravir; emtricitabine; tenofovir disoproxil fumarate	TABLET;ORAL	203100-001	Aug 27, 2012		RX	Yes	Yes					Y
Gilead Sciences Inc	VITEKTA	elvitegravir	TABLET;ORAL	203093-001	Sep 24, 2014		DISCN	Yes	No					Y
Gilead Sciences Inc	VITEKTA	elvitegravir	TABLET;ORAL	203093-002	Sep 24, 2014		DISCN	Yes	No					Y

Foreign Priority and PCT Information for Patent: 7,176,220

Foriegn Application Priority Data
Foreign Country	Foreign Patent Number	Foreign Patent Date
Japan	2002-336843	Nov 20, 2002
Japan	2003-065807	Mar 11, 2003
Japan	2003-139616	May 16, 2003

PCT Information
PCT Filed	November 20, 2003	PCT Application Number:	PCT/JP03/14773
PCT Publication Date:	June 03, 2004	PCT Publication Number:	WO2004/046115

International Family Members for US Patent 7,176,220

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	1564210		PA2013018	Lithuania
European Patent Office	1564210		C300624	Netherlands
European Patent Office	1564210		CA 2013 00058	Denmark
European Patent Office	1564210		92307	Luxembourg
European Patent Office	1564210		PA2013018,C1564210	Lithuania
European Patent Office	1564210		C20130029 00095	Estonia
European Patent Office	1564210		13C0061	France