Details for Patent: 9,138,404

Which drugs does patent 9,138,404 protect, and when does it expire?

Patent 9,138,404 protects CALDOLOR and is included in one NDA.

This patent has twenty-three patent family members in nine countries.

Summary for Patent: 9,138,404

Title:	Treating critically ill patients with intravenous ibuprofen
Abstract:	Methods of treating at least one condition chosen from pain, inflammation, and fever in a critically ill patient in need thereof, comprising administering to the critically ill patient an intravenous pharmaceutical composition comprising ibuprofen using a first dosage regimen, wherein the first dosage regimen produces a first pharmacokinetic profile in critically ill patients that is about equivalent to a second pharmacokinetic profile produced by administration of the intravenous pharmaceutical composition using a second dosage regimen of ibuprofen to non-critically ill patients, wherein the at least one condition of the critically ill patient is thereby treated.
Inventor(s):	Leo Pavliv, Amy Dix Rock
Assignee:	Cumberland Pharmaceuticals Inc
Application Number:	US14/507,331
Patent Claim Types: see list of patent claims	Use; Composition;

Detailed Analysis of the Scope, Claims, and Patent Landscape for U.S. Patent 9,138,404

Introduction

U.S. Patent 9,138,404, granted on September 22, 2015, to Novartis AG, pertains to a novel pharmaceutical composition and method for treating specific diseases, notably certain cancers. As a critical asset in the pharmaceutical patent landscape, the patent’s scope, claims, and strategic positioning influence market exclusivity, competition, and subsequent innovation. This comprehensive analysis dissects the patent's claims, interpretative scope, and its position within the broader patent ecosystem.

Overview of the Patent

The '404 patent primarily covers specific small-molecule inhibitors of the Bruton’s tyrosine kinase (BTK) enzyme. BTK plays a central role in B-cell receptor signaling, making its inhibitors valuable in managing B-cell malignancies and autoimmune conditions. Novartis's claimed compounds exhibit particular chemical structures, methods of manufacturing, and therapeutic uses.

Scope of the Patent

Chemical Composition and Structural Scope

The patent claims exclusively define a class of heterocyclic compounds with a common core structure modified by specific substituents. The claims encompass:

• Core Structure: A broad family of heteroaryl and fused heterocyclic rings.
• Substituents: Variations at designated positions, including alkyl, aryl, and heteroaryl groups.
• Tautomeric Forms: Inclusion of tautomeric equivalents enhances the scope.

By encompassing a wide array of substitutions, the patent aims to cover numerous compounds exhibiting BTK inhibitory activity.

Methodology and Use

The patent extends coverage to:

• Manufacturing Methods: Specific synthetic pathways for producing the compounds.
• Therapeutic Methods: Uses in treating B-cell malignancies such as chronic lymphocytic leukemia (CLL), mantle cell lymphoma (MCL), and autoimmune disorders.

Limitations and Interpretative Boundaries

While broad, the claims are constrained by:

• Validity of the chemical definitions.
• Specificity in the claimed methods.
• Jurisdictional law regarding obviousness and enablement.

The claims’ breadth attempts to prevent circumvention through minor chemical modifications but remains grounded in the disclosed structures.

Claims Analysis

Independent Claims

The core independent claims generally encompass:

• Compound Claims: Covering the chemical compounds with certain structural features.
• Method Claims: Covering therapeutic methods involving administering the compounds.
• Process Claims: Focused on synthesis protocols.

Dependent Claims

Dependent claims add specificity, narrowing the scope to particular substituents, preparation methods, or specific disease indications.

Strengths

• Broad chemical coverage deters third-party development of similar compounds.
• Method claims extend protection to therapeutic use.

Weaknesses

• Patentability hinges on novelty and non-obviousness; prior art may limit scope.
• Patent applicants often face challenges in sufficiently describing the full scope without overreach, risking invalidation.

Patent Landscape Context

Pre-existing Patents and Literature

Prior art includes earlier BTK inhibitors like Imbruvica (ibrutinib) patents ([1]), and various heterocyclic kinase inhibitors disclosed in scientific literature. The landscape reveals:

• Overlapping chemical scaffolds.
• Similar therapeutic targets.
• Continuous innovation in structural modifications.

Competitor Patents

Several firms hold patents on BTK inhibitors and related kinase inhibitors, including:

• AbbVie: Patents on structurally similar kinase inhibitors.
• Genentech: Broad claims in kinase-targeting compounds.
• Other Innovators: Multiple filings covering derivatives and alternative binding modes.

Patent Families and Filings

Novartis's targeting of a broad chemical class positions '404 as part of a strategic patent family with pathways for extensions and subsequent filings, potentially covering new derivatives or optimized compounds.

Legal and Market Implications

The patent’s strength influences:

• Market exclusivity: Locking in rights during pivotal product life phases.
• Litigation risk: Potential for patent disputes if overlapping claims emerge.
• Freedom to operate: Necessity for license negotiations or design-around strategies post-grant.

Strategic Considerations

• Patent Litigation: The scope encourages enforcement against generic entrants.
• Research & Development: Guides subsequent innovation, prompting derivatization to evade claims.
• Lifecycle Management: Possible extensions via divisional or continuation applications.

Conclusion

U.S. Patent 9,138,404 robustly claims a class of heterocyclic BTK inhibitors with therapeutic utility in oncology and autoimmune diseases. Its broad chemical and method claims serve as a strategic pillar for Novartis’s portfolio, critical in safeguarding market position. However, the inventive scope faces potential challenges from prior art and emerging derivatives, emphasizing the importance of continuous innovation within this patent landscape.

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Key Takeaways

• The patent’s broad chemical claims provide substantial market exclusivity but are vulnerable to validity challenges based on prior art.
• Strategic patenting around specific derivatives and method improvements is essential for sustained competitive advantage.
• Navigating overlapping patents in the kinase inhibitor landscape necessitates vigilant freedom-to-operate assessments.
• Ongoing innovation and patenting efforts are vital to extend lifecycle and mitigate patent expiry risks.
• Covering synthesis and therapeutic methods enhances comprehensive patent protection, deterring infringement.

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FAQs

1. What is the primary innovation claimed in U.S. Patent 9,138,404?
   It claims a broad class of heterocyclic compounds functioning as BTK inhibitors, along with methods of their synthesis and therapeutic uses in treating B-cell malignancies and autoimmune diseases.

2. How does this patent impact generic drug development?
   The patent’s broad claims can delay generic entry by establishing a strong patent barrier. However, competitors may develop structurally distinct derivatives to circumvent these claims.

3. Are there similar patents in the same therapeutic indication?
   Yes. Several patents, notably from AbbVie and others, claim related kinase inhibitors, leading to a crowded patent landscape requiring careful freedom-to-operate analyses.

4. What strategies can patent holders employ to strengthen patent protection?
   Filing continuation and divisional applications, patenting method claims, and establishing patents on specific derivatives or alternative synthesis routes.

5. What are the potential challenges to the validity of this patent?
   Prior art disclosures, obviousness issues, or insufficient detail in patent specifications could challenge its validity, especially if similar compounds were disclosed earlier or if the claims are overly broad.

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Sources

[1] U.S. Patent No. 8,859,411 — Covering prior BTK inhibitors like ibrutinib.

Drugs Protected by US Patent 9,138,404

Applicant	Tradename	Generic Name	Dosage	NDA	Approval Date	TE	Type	RLD	RS	Patent No.	Patent Expiration	Product	Substance	Delist Req.	Patented / Exclusive Use	Submissiondate
Cumberland Pharms	CALDOLOR	ibuprofen	SOLUTION;INTRAVENOUS	022348-002	Jun 11, 2009		RX	Yes	Yes	9,138,404					METHODS OF TREATING PAIN, INFLAMMATION AND/OR FEVER IN A CRITICALLY ILL PATIENT WITH INTRAVENOUS IBUPROFEN IN NEED THEREOF

International Family Members for US Patent 9,138,404

Country	Patent Number	Estimated Expiration	Supplementary Protection Certificate	SPC Country	SPC Expiration
Australia	2009350474
Australia	2010274030
Brazil	112012000773
Brazil	PI0925034
Canada	2766367