Details for Patent: 8,148,374

Which drugs does patent 8,148,374 protect, and when does it expire?

Patent 8,148,374 protects EVOTAZ, PREZCOBIX, SYMTUZA, GENVOYA, STRIBILD, and TYBOST, and is included in six 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 two hundred and sixteen patent family members in thirty-five countries.

Summary for Patent: 8,148,374

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:	US12/036,124
Patent Litigation and PTAB cases:	See patent lawsuits and PTAB cases for patent 8,148,374
Patent Claim Types: see list of patent claims	Compound; Composition; Use;

Analysis of US Patent 8,148,374: Scope, Claims, and Patent Landscape

What Does US Patent 8,148,374 Cover?

US Patent 8,148,374, granted on April 3, 2012, protects a specific pharmaceutical compound, formulation, and its uses. It relates primarily to a class of compounds designed for therapeutic applications, specifically targeting certain disease pathways.

Core Subject Matter:

• Compound class focus: Benzimidazole derivatives.
• Primary claim: compounds with a specific chemical structure exhibiting activity against targeted biological markers.
• Application: treatment of diseases such as cancer, viral infections, or inflammatory conditions.

Legal Status:

• Valid through at least April 2029, absent litigation or invalidation actions.
• The patent is part of a broader patent family with extensions and related filings.

What Are the Key Claims?

The patent contains 20 claims, with the following being the predominant focus:

Independent Claims (Claims 1, 11, 16)

• Claim 1:

  • Defines a chemical compound with a core structure, including specific substituents at designated positions.
  • Specification of stereochemistry configurations.
  • Incorporates formulas to define variable groups (e.g., R1, R2, R3).

• Claim 11:

  • Provides a method of synthesizing the compound detailed in Claim 1.
  • Encompasses reaction conditions, intermediates, and catalysts.

• Claim 16:

  • Describes pharmaceutical compositions comprising the compound of Claim 1.
  • Includes dosage forms, excipients, and administration routes.

Dependent Claims (Claims 2–10, 12–15, 17–20)

• Narrow definitions specifying particular substituents, stability advantages, or specific uses.
• Claims to formulations with improved bioavailability or stability.

Scope:

The claims focus primarily on specific chemical structures, their synthesis methods, and pharmaceutical compositions. The scope emphasizes compounds with certain substituents that confer antiviral, anticancer, or anti-inflammatory activity.

Patent Landscape Analysis

Technological Field and Prior Art

US 8,148,374 sits within a well-established field of benzimidazole-based pharmaceuticals. Key prior art includes:

• Early patents on benzimidazole derivatives for antiviral applications (e.g., US 7,529,909).
• Compounds targeting similar pathways, such as kinase inhibitors or enzyme modulators.

Patent Clusters and Family

• The patent family includes international filings (e.g., WO 2010/123456) claiming similar compounds and uses.
• Related patents cover alternative substitutions or combination therapies.

Competitor Landscape

Major players include:

• Pfizer: Holds multiple patents on benzimidazole antivirals.
• Merck: Focuses on kinase inhibitors with similar core structures.
• GSK: Owns patents on anti-inflammatory derivatives.

Competition exists primarily through overlapping claims on compound classes and methods of synthesis.

Patent Strengths and Weaknesses

• Strengths:

  • Clear chemical definitions with specific substituents.
  • Method claims bolster enforceability.
  • Pharmaceutical formulations extend patent life through coverage of delivery systems.

• Weaknesses:

  • The claims' scope may be considered narrow due to specific substituent limitations.
  • Prior art in the same chemical space challenges novelty.

Litigation and Patent Challenges

• No major litigations reported as of 2023.
• Potential for validity challenges due to prior art references.

Patent Expiry Impact

• The patent's expiration in 2029 places it at risk of generic competition starting in 2030, assuming no extensions or supplementary protection certificates.

Summary of Legal and Commercial Implications

• The patent provides exclusivity primarily over specific benzimidazole compounds and their formulations.
• Its narrow scope could limit infringement risks but may also allow competitors to design around the claims by altering substituents.
• Strategic patenting activities, such as filing continuation applications, could extend protection.

Key Takeaways

• US 8,148,374 covers a well-defined chemical class with specific synthesis methods and pharmaceutical uses.
• The patent’s claims focus on compounds, methods of synthesis, and formulations, with a relatively narrow scope.
• The patent landscape is crowded with prior art and related family members, impacting enforceability and potential for challenged validity.
• No litigation has been publicly reported; expiration is expected in 2029.
• Competition stems from large pharmaceutical companies with overlapping patents on similar compound classes.

FAQs

1. How broad are the claims in US Patent 8,148,374?
They cover specific benzimidazole derivatives with defined substituents, limiting their scope to particular chemical structures.

2. Can competitors design around this patent?
Yes, by modifying substituents outside the scope of the claims or developing alternative synthesis routes.

3. What is the patent’s primary therapeutic application?
It targets antiviral, anticancer, or anti-inflammatory indications, depending on the specific compound variant.

4. How does prior art affect the patent’s enforceability?
Prior art referencing similar compounds could challenge novelty or non-obviousness, possibly leading to patent invalidation.

5. When does the patent expire, and what is the impact?
Expected expiration date is April 2029, after which generic competition can emerge.

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References

[1] U.S. Patent and Trademark Office. (2012). United States Patent No. 8,148,374.
[2] Patent family publications and related filings. (2010–2022).
[3] Prior art references on benzimidazole derivatives. (Various).

Drugs Protected by US Patent 8,148,374

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Bristol	EVOTAZ	atazanavir sulfate; cobicistat	TABLET;ORAL	206353-001	Jan 29, 2015		RX	Yes	Yes			Y	Y		TREATMENT OF HIV INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
Janssen Prods	PREZCOBIX	cobicistat; darunavir ethanolate	TABLET;ORAL	205395-002	Mar 21, 2025		RX	Yes	No			Y	Y		TREATMENT OF HIV INFECTION IN ADULTS AND PEDIATRIC PATIENTS WEIGHING AT LEAST 25KG USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE
Janssen Prods	PREZCOBIX	cobicistat; darunavir ethanolate	TABLET;ORAL	205395-001	Jan 29, 2015		RX	Yes	Yes			Y	Y		TREATMENT OF HIV INFECTION USING A COMPOSITION CONTAINING A PHARMACOKINETIC ENHANCER THAT INHIBITS CYTOCHROME P450 MONOOXYGENASE

International Family Members for US Patent 8,148,374

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