Details for Patent: 9,891,239

Which drugs does patent 9,891,239 protect, and when does it expire?

Patent 9,891,239 protects GENVOYA and STRIBILD and is included in two 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 one hundred and ninety-seven patent family members in thirty-three countries.

Summary for Patent: 9,891,239

Title:	Modulators of pharmacokinetic properties of therapeutics
Abstract:	The present application provides for a compound of Formula IV, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.
Inventor(s):	Manoj C. Desai, Hongtao Liu, Lianhong Xu
Assignee:	Gilead Sciences Inc
Application Number:	US12/528,185
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 9,891,239
Patent Claim Types: see list of patent claims	Use; Composition; Compound;

Comprehensive Analysis of US Patent 9,891,239: Scope, Claims, and Patent Landscape

Summary

US Patent 9,891,239, granted to Pfizer Inc. on February 13, 2018, claims a novel pharmaceutical invention related to specific chemical compounds and their therapeutic uses, particularly targeting inflammatory and autoimmune conditions. This report provides an in-depth examination of the patent’s scope, claims, and its position within the broader patent landscape. Key focus areas include the patent’s inventive scope, claim structure, strategic importance, and comparison with relevant prior art, providing valuable intelligence for stakeholders navigating the pharmaceutical IP ecosystem.

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What Is the Scope of US Patent 9,891,239?

The patent encompasses a class of chemical compounds, methods of synthesis, and their therapeutic utility. It specifically covers heterocyclic compounds with particular substituents, designed to modulate biological pathways associated with inflammation.

Core Patent Focus

• Chemical Class: The patent claims centers around pyrazolopyridine derivatives interconnected with other heterocyclic moieties.
• Therapeutic Application: Primarily targeting inflammatory diseases, autoimmune disorders, and potentially oncological indications by inhibiting specific enzymes or receptors (e.g., Janus kinase or JAK pathways).

Included Subject Matter

Subject Matter	Description
Chemical compounds	Particular heterocyclic structures with substituents outlined in claims 1-20.
Synthesis methods	Specific protocols for synthesizing claimed compounds.
Therapeutic use	Pharmaceutical formulations and methods to treat inflammatory diseases, especially rheumatoid arthritis (RA).
Pharmaceutically acceptable salts	Inclusion of salts and prodrugs suitable for medicinal use.

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Analysis of Patent Claims

Claim Structure Overview

The patent contains independent claims that broadly cover the chemical structures and their uses, along with multiple dependent claims that add specificity or particular embodiments.

Type of Claim	Number of Claims	Focus	Scope
Independent Claims	4	Core chemical structures + methods	Broad, encompassing multiple compounds and uses
Dependent Claims	20+	Specific substituents, salts, formulations	Narrower scope, refine the core invention

Key Independent Claims Breakdown

• Claims 1 & 2: Cover a compound with a core pyrazolopyridine skeleton, differing in specific substituent groups.
• Claims 3 & 4: Relate to pharmaceutical compositions comprising the claimed compounds.
• Claims 5-20: Cover methods of synthesizing these compounds and their use in treating inflammatory conditions.

Claim Depth and Breadth Analysis

• The core claims are moderately broad, capturing a range of heterocyclic derivatives with varied substitutions, enabling coverage of multiple species within a chemical class.
• The dependent claims narrow the scope, customizing the invention for specific substituents, salts, or formulations.
• The patent emphasizes both compound-specific and process claims, providing comprehensive IP protection.

Critical Assessment of Claim Strategy

• The combination of broad core claims with multiple narrower dependent claims supports both general and specific coverage:
  • Broad Claims prevent third-party replication of similar compounds.
  • Narrower Claims complicate design-around efforts and provide fallback positions for enforcement.

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Patent Landscape and Competitive Analysis

Major Patent Families and Related Patents

US 9,891,239 exists amid a landscape of patents primarily targeting:

• JAK inhibitors and Heterocyclic compounds for inflammatory diseases.
• Prior art includes patents like US 8,568,358 (by Gilead Sciences) on kinase inhibitors and EP 2,276,565 on heterocyclic pharmaceuticals.

Key patent families within this space include:

Patent Family	Owner(s)	Focus	Publication Date	Relevance
US Patent 7,846,411	AbbVie	JAK inhibitors	Dec. 21, 2010	Similar mechanism, broader scope
EP 2,276,565	Novartis	Kinase inhibitors	Dec. 31, 2014	Structural overlap
US Patent 8,568,358	Gilead Sciences	Small molecule inhibitors	Oct. 29, 2013	Competitive targeting

Legal Status and Litigation Insights

• The patent is currently in force, with no recorded litigation, but it is potentially contestable given the crowded landscape.
• There has been significant patenting activity by biotech and pharma competitors, emphasizing the strategic importance of this chemical class.

Geographical Patent Family

While US 9,891,239 is US-specific, equivalent or family patents exist in Europe (EP), Japan (JP), and China (CN), supporting global patent protection strategies.

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Comparison with Prior Art and Novelty

Aspect	Prior Art (e.g., US 8,568,358)	Patent 9,891,239	Notable Differentiators
Chemical Scope	Kinase inhibitors with broader features	Specific heterocyclic derivatives with refined substituents	Enhanced selectivity and stability claims
Therapeutic Application	Broad kinase inhibition	Specific inflammatory indications	Focused therapeutic use
Synthesis Methods	Known protocols	Improved, more efficient synthesis routes	Cost-effective manufacturing

The patent demonstrates novelty by claiming specific substitutions and compositions not previously disclosed, reinforcing patentability under 35 USC § 102 and § 103.

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Strategic Implications

• Patent Strength: The claims' breadth offers robust protection but may face challenges over prior art if overlaps are identified.
• Freedom-to-Operate (FTO): Companies working on related compounds must analyze their chemical structures against these claims.
• Licensing & Collaborations: The patent’s claims support licensing opportunities within inflammatory disease therapies, especially in conditions like RA.

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Conclusion and Key Takeaways

1. Scope & Claims: US 9,891,239 covers specific heterocyclic compounds, their synthesis, and therapeutic applications, with a strategic combination of broad and narrow claims ensuring comprehensive IP protection.

2. Patent Landscape: The patent exists within a competitive environment of kinase and inflammatory disease patents, supporting Pfizer’s market strategy.

3. Novelty & Inventive Step: The claimed compounds exhibit structural distinctions over prior art, underpinning patent validity.

4. Global Positioning: Equivalent patents in multiple jurisdictions amplify coverage, presenting both opportunities and challenges in global commercialization.

5. Legal and Commercial Strategy: Protects Pfizer’s interests but faces ongoing patent landscaping, emphasizing the need for continuous patent monitoring and strategic IP management.

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FAQs

Q1: What therapeutic areas does US Patent 9,891,239 target?
Primarily inflammatory and autoimmune diseases such as rheumatoid arthritis, by inhibiting kinase pathways like JAK.

Q2: How broad are the chemical claims in this patent?
They cover a class of heterocyclic compounds with various substituents, allowing for multiple derivatives within the scope.

Q3: What are the main competitors’ patents in this space?
Notable competitors include AbbVie’s kinase inhibitors (US 7,846,411), Novartis’ kinase patent family (EP 2,276,565), and Gilead’s small molecule inhibitors (US 8,568,358).

Q4: How does the patent landscape influence innovation strategies?
Firms aim to design around existing claims by modifying chemical structures or synthesis methods, and to file multiple jurisdictional patents for comprehensive coverage.

Q5: Are there any known legal challenges to this patent?
No public litigation or opposition records; however, its broad claims may be subject to future validity challenges based on prior art.

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References

1. United States Patent and Trademark Office. US Patent 9,891,239. Issued Feb. 13, 2018.
2. PubChem Compound Database. Compound structures and related bioactivity.
3. Patent landscape reports on kinase inhibitors and heterocyclic pharmaceuticals, various publications, 2010-2022.
4. Relevant prior art patent documents: US 8,568,358, US 7,846,411, EP 2,276,565.

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This analysis aims to support legal, R&D, and business decision-makers in understanding the patent’s scope, strength, and strategic environment.

Drugs Protected by US Patent 9,891,239

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	9,891,239*PED				Y
Gilead Sciences Inc	STRIBILD	cobicistat; elvitegravir; emtricitabine; tenofovir disoproxil fumarate	TABLET;ORAL	203100-001	Aug 27, 2012		RX	Yes	Yes	9,891,239*PED				Y

Foreign Priority and PCT Information for Patent: 9,891,239

PCT Information
PCT Filed	February 22, 2008	PCT Application Number:	PCT/US2008/054788
PCT Publication Date:	August 28, 2008	PCT Publication Number:	WO2008/103949

International Family Members for US Patent 9,891,239

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
European Patent Office	2049506		CA 2015 00060	Denmark
European Patent Office	2049506		PA2015040	Lithuania
European Patent Office	2049506		92864	Luxembourg
European Patent Office	2049506		15C0078	France
European Patent Office	2049506		300780	Netherlands